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| ID | PMID | YEAR | Sequence | Name | Length | N-ter MOD | C-ter MOD | Linear/Cyclic | Chirality | Chem-MOD | Origin | Nature | Incubation Time | Concentration | Half Life | Units Half Life | Protease | Assay | Test Sample | Vivo/Vitro | Reference | Patent No. | Activity |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role in clotting | N.A. | 25 IU/kg | 31 | HemA mice plasma protease | Chromogenic activity assays | HemA mice plasma | In Vivo | PDB id : 5K8D | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role in clotting | N.A. | 50 IU/kg | 30 | HemA mice plasma protease | Chromogenic activity assays | HemA mice plasma | In Vivo | PDB id : 5K8D | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role in clotting | N.A. | 100 IU/kg | 25 | HemA mice plasma protease | Chromogenic activity assays | HemA mice plasma | In Vivo | PDB id : 5K8D | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role in clotting | N.A. | 100 IU/kg | 32.7 | Cynomolgus monkeys plasma protease | Chromogenic activity assays | Cynomolgus monkeys plasma | In Vivo | PDB id : 5K8D | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role in clotting | N.A. | 300 IU/kg | 33.6 | Cynomolgus monkeys plasma protease | Chromogenic activity assays | Cynomolgus monkeys plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role In Clotting | N.A. | 100 IU/kg | 29.3 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role In Clotting | N.A. | 300 IU/kg | 34 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 31.8 | HemA mice plasma protease | chromogenic activity assays | HemA mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 29.9 | VWF Het mice plasma protease | chromogenic activity assays | VWF Het mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc-VWF-XTEN (construct 4) (BIVV001) | 3,611 | Free | Free | Linear | L | Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 26.9 | DKO mice plasma protease | chromogenic activity assays | DKO mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc | 865 | Free | IgG1 Fc | Linear | L | None | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 16.4 | HemA mice plasma protease | chromogenic activity assays | HemA mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc | 865 | Free | IgG1 Fc | Linear | L | None | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 13.2 | VWF Het mice plasma protease | chromogenic activity assays | VWF Het mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIIIFc | 865 | Free | IgG1 Fc | Linear | L | None | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 1.85 | DKO mice plasma protease | chromogenic activity assays | DKO mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIII | 654 | Free | Free | Linear | L | None | Synthetic | Role In Clotting | N.A. | 125 IU/kg | 7.63 | HemA mice plasma protease | chromogenic activity assays | HemA mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIII | 654 | Free | Free | Linear | L | None | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 5.43 | VWF Het mice plasma protease | chromogenic activity assays | VWF Het mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIII | 654 | Free | Free | Linear | L | None | Synthetic | Role In Clotting | N.A. | 150 IU/kg | 0.23 | DKO mice plasma protease | chromogenic activity assays | DKO mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 33374407 | 2020 | Tα1-PAS | 28 | Free | PAS#1(600) | Linear | L | None | Synthetic | Antiviral, Anticancer | Blood samples (100 µL) were taken from 5 animals each at various time points | 3.4 mg/kg | 15.7 ± 0.8 (Τ1/2a) | Rats plasma protease | sandwich ELISA | Rats plasma | In Vivo | UniprotKb ID: P06454 | None | N.A. | |||
| 33374407 | 2020 | Tα1-PAS | 28 | Free | PAS#1(600) | Linear | L | None | Synthetic | Antiviral, Anticancer | Blood samples (100 µL) were taken from 5 animals each at various time points | 3.4 mg/kg | 15.9 ± 0.9 (Τ1/2b ) | Rats plasma protease | sandwich ELISA | Rats plasma | In Vivo | UniprotKb ID: P06454 | None | N.A. | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 50 nmol/kg | 53.19 ± 1.42 | SD rats serum protease | LC-MS/MS | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 100 nmol/kg | 58.37 ± 4.51 | SD rats serum protease | LC-MS/MS | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 200 nmol/kg | 73.68 ± 6.52 | SD rats serum protease | LC-MS/MS | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 50 nmol/kg | 56.40 ± 2.71 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 100 nmol/kg | 63.15 ± 4.93 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 200 nmol/kg | 114.91 ±7.32 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33310780 | 2020 | NYBSP-4 | 34 | Acetylation | Amidation | Linear | L | 2-(7-octenyl)alanine-2-(4-pentenyl)alanine modifications | Derived from ACE2 | Antiviral | 0, 10, 30, 60, and 120 min | 1mM | >289 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 1.97 ± 0.14 μM in HT1080/ACE2 cells | |||
| 33310780 | 2020 | NYBSP-C | 30 | Acetylation | Amidation | Linear | L | None | Derived from ACE2 | Antiviral | 0, 10, 30, 60, and 120 min | 1 mM | >289 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | IC50 >27.7 μM in HT1080/ACE2 cells | |||
| 33284103 | 2020 | Mouse ucOCN | 46 | Free | Free | Cyclic (C19-C25 Disulfide bond) | L | Uncarboxylation at all glutamic acid | Osteoblast Derived hormone | Antidiabetes | 0 to 5 hr at 37°C | 100 ng/mL | ~120 | Mouse plasma protease | ELISA | Mouse plasma | In Vitro | None | None | N.A. | |||
| 33284103 | 2020 | Mouse O-glycosylated ucOCN | 46 | Free | Free | Cyclic (C19-C25 Disulfide bond) | L | O-glycosylation likely at Ser8 in SVPSPDP, Uncarboxylation at all glutamic acid | Osteoblast Derived hormone | Antidiabetes | 0 to 5 hr at 37°C | 100 ng/mL | >5 | Mouse plasma protease | ELISA | Mouse plasma | In Vitro | None | None | N.A. | |||
| 33284103 | 2020 | Mouse O-glycosylated ucOCN | 46 | Free | Free | Cyclic (C19-C25 Disulfide bond) | L | O-glycosylation likely at Ser8 in SVPSPDP, Uncarboxylation at all glutamic acid | Osteoblast Derived hormone | Antidiabetes | 2 hours at 37°C | 40 ng/g | ~182 | Mice serum protease | OCN ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 33284103 | 2020 | Mouse ucOCN | 46 | Free | Free | Cyclic (C19-C25 Disulfide bond) | L | Uncarboxylation at all glutamic acid | Osteoblast Derived hormone | Antidiabetes | 2 hours at 37°C | 40 ng/g | ~108 | Mice serum protease | OCN ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 33203916 | 2020 | Native TRAIL | 168 | Free | Free | Linear | L | None | Synthetic | Anticancer | Blood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h | 0.01 mg/mL | 3.4 ± 1.1 | BALB/c wild type mice plasma protease | Western blotting | BALB/c wild type mice plasma | In Vivo | PDB id: 1D0G | None | KD (M) = (6.02 ± 1.99) × 10–8 (Binding kinetics of TRAIL-ATNC and TRAIL against TRAIL receptor DR5.) | |||
| 33203916 | 2020 | TRAIL-ATNC | 168 | Free | TRAIL joined with ATNC using flexible linkers consisting of small amino acids (GSGGGSG) that could form a bridge between the C-terminal of TRAIL and the triple helix | Linear | L | None | Synthetic | Anticancer | Blood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h | 1 mg/mL | 56.1 ± 5.8 | BALB/c wild type mice plasma protease | Western blotting | BALB/c wild type mice plasma | In Vivo | PDB id: 1D0G | None | KD (M) = (2.56 ± 2.58) × 10–10 (Binding kinetics of TRAIL-ATNC and TRAIL against TRAIL receptor DR5.) | |||
| 33203916 | 2020 | TRAIL-ATNCIL4rP | 168 | Free | TRAIL joined with ATNC using flexible linkers consisting of small amino acids (GSGGGSG) that could form a bridge between the C-terminal of TRAIL and the triple helix followed by (MMP2) cleavage site (GPLGLAG) then IL4rP (CRKRLDRNC) | Linear | L | None | Synthetic | Anticancer | Blood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h | 1 mg/mL | 53.6 ± 5.8 | BALB/c wild type mice plasma protease | Western blotting | BALB/c wild type mice plasma | In Vivo | PDB id: 1D0G | None | IC50 value of 0.48 nM for TRAIL-ATNCIL4rP | |||
| 33125843 | 2020 | 5a | 45 | Free | Either or nonsulfated gastrin-6 were coupled to the C-terminus of 2d and 2k through two OEG spacers, affording 5a−5d | Linear | L | Aib substiuition at position 2, Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 1.7 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.040 ± 0.011 (Effects of 5a on GLP-1R) | |||
| 33125843 | 2020 | 5b | 45 | Free | Either or nonsulfated gastrin-6 were coupled to the C-terminus of 2d and 2k through two OEG spacers, affording 5a−5d | Linear | L | Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 1.9 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.048 ± 0.018 (Effects of 5b on GLP-1R) | |||
| 33125843 | 2020 | 6a | 45 | Free | 4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d | Linear | L | C1 = structure given in paper, Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 4.6 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.022 ± 0.008 (Effects of 6a on GLP-1R) | |||
| 33125843 | 2020 | 6b | 45 | Free | 4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d | Linear | L | C1 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 5 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R) | |||
| 33125843 | 2020 | 7a | 45 | Free | 4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d | Linear | L | Modification of 6a and 6b with the introduction of C2 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 2.9 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R) | |||
| 33125843 | 2020 | 7b | 45 | Free | 4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d | Linear | L | Modification of 6a and 6b with the introduction of C2 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 3.1 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R) | |||
| 33057063 | 2020 | NRG1-MFc | 268 | Free | fusion of the C-terminus of NRG1 to the N-terminus of the Fc fragment | Linear | L | None | Synthetic | Her4-Selective Agonism | Overnight at 4 °C | 10 μg/mL | 1.4 | Mouse serum protease | ELISA | Mouse serum | In Vitro | PDB ID: 3U7U | None | HER4 binding KD = 640 nM | |||
| 33057063 | 2020 | 1F7-MFc | 268 | Free | C-terminus of 1F7 is directly fused to the Fc fragment | Linear | L | Small set of mutations, including His2, Lys24, and P29 | Synthetic | Her4-Selective Agonism | Overnight at 4 °C | 10 μg/mL | 6.6 | Mouse serum protease | ELISA | Mouse serum | In Vitro | PDB ID: 3U7U | None | EC50 (nM) = 0.4 for 1F7 in HER2/HER4 Luc | |||
| 33057063 | 2020 | ALM6 | 75 | Free | Free | Linear | L | None | Synthetic | Her4-Selective Agonism | Overnight at 4 °C | 10 μg/mL | 1.4 | Mouse serum protease | ELISA | Mouse serum | In Vitro | None | None | HER4 binding KD = 440 nM | |||
| 33057063 | 2020 | ALM6-1F7 | 130 | Free | C-terminus of ALM6 is directly fused to 1F7 | Linear | L | Small set of mutations, including His2, Lys24, and P29 | Synthetic | Her4-Selective Agonism | Overnight at 4 °C | 10 μg/mL | 6.6 | Mouse serum protease | ELISA | Mouse serum | In Vitro | None | None | EC50 (nM) = 0.4 for 1F7 in HER2/HER4 Luc | |||
| 33008433 | 2020 | Hypoxic-Ischemic Brain Damage Associated Peptide (HIBDAP) | 17 | Free | Free | Linear | L | None | derives from the 210st to 226st amino acids of HSP90AA1 | Involved In The Nod-Like Receptor (Nlr) Signaling Pathway | N.A. | N.A. | 3.5 | Mammalian reticulocytes protease | N.A. | Mammalian reticulocytes with OGD ( oxygen and glucose deprivation (OGD)) | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Lau-PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 2.96 | Simulated intestinal fluid protease | HPLC | Simulated intestinal fluid | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Lau- PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.3 | Simulated intestinal fluid protease | HPLC | Simulated intestinal fluid | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | N.A. | Simulated intestinal fluid protease | HPLC | Simulated intestinal fluid | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 4.52 | Simulated intestinal fluid protease | HPLC | Simulated intestinal fluid | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Lau-PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.6 | 50% W/V liver homogenate protease | HPLC | 50% w/v liver homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Lau- PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.95 | 50% W/V liver homogenate protease | HPLC | 50% w/v liver homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 18.5 | 50% W/V liver homogenate protease | HPLC | 50% w/v liver homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 1.36 | 50% W/V liver homogenate protease | HPLC | 50% w/v liver homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Lau-PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.15 | 50% V/V mouse plasma protease | HPLC | 50% v/v mouse plasma | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Lau- PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 5.86 | 50% V/V mouse plasma protease | HPLC | 50% v/v mouse plasma | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.11 | 50% V/V Mouse Plasma Protease | HPLC | 50% v/v Mouse plasma | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.87 | 50% V/V Mouse Plasma Protease | HPLC | 50% v/v Mouse plasma | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Lau-PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.36 | 50% W/V Brain Homogenate Protease | HPLC | 50% w/v Brain Homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Lau- PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.2 | 50% W/V Brain Homogenate Protease | HPLC | 50% w/v Brain Homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.16 | 50% W/V Brain Homogenate Protease | HPLC | 50% w/v Brain Homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.25 | 50% W/V Brain Homogenate Protease | HPLC | 50% w/v Brain Homogenate | In Vitro | None | None | N.A. | |||
| 32858124 | 2020 | Cmpd# 3 | 16 | Acetylation | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.1 mg/kg | 0.362 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 1.95 ± 1.16 | |||
| 32858124 | 2020 | Cmpd# 6 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.1 mg/kg | 2.31 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 2.31 ± 0.57 | |||
| 32858124 | 2020 | Cmpd# 10 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C13 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.1 mg/kg | 3.4 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 6.22 ± 1.6 | |||
| 32858124 | 2020 | Cmpd# 12 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C15 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.1 mg/kg | 1.84 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.39 ± 0.73 | |||
| 32858124 | 2020 | Cmpd# 14 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C17 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.1 mg/kg | 2.18 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE =7.42 ± 0.9 | |||
| 32858124 | 2020 | Cmpd# 17 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 diacid | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.1 mg/kg | 2.32 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.10 ± 0.62 | |||
| 32858124 | 2020 | Cmpd# 23 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C18-diacid | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.1 mg/kg | 19.7 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 117 ± 23.3 | |||
| 32858124 | 2020 | Cmpd# 6 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 2.6 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 2.31 ± 0.57 | |||
| 32858124 | 2020 | Cmpd# 10 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C13 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 10.2 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 6.22 ± 1.6 | |||
| 32858124 | 2020 | Cmpd# 12 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C15 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 6.3 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.39 ± 0.73 | |||
| 32858124 | 2020 | Cmpd# 14 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C17 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 10.3 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE =7.42 ± 0.9 | |||
| 32858124 | 2020 | Cmpd# 17 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 diacid | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 4.1 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.10 ± 0.62 | |||
| 32858124 | 2020 | Cmpd# 23 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C18-diacid | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | > 24 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 117 ± 23.3 | |||
| 32847850 | 2020 | PPP2R5A | 407 | Free | Free | Linear | L | Blue fluorescent protein (BFP) labeling | encoded by the PPP2R5A gene in humans | Antiviral | 48 hours | 250 ng | ~2 | 293T Cell Line Lysate Protease | flow cytometry | 293T cell line lysate with Vif | In Vivo | PDB id = 2IAE | None | N.A. | |||
| 32844654 | 2020 | Peptide 4 | 34 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | L | Cysteine substiution at 10, 17 | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | N.A. | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 2.3 ± 0.3 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 8 | 34 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | L | Cysteine substiution at 23, 30 | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | N.A. | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 1.2 ± 0.1 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 11 | 34 | Free | Amidation | Linear | L | None | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | 1.2 | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 0.29 ± 0.03 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 13 | 34 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | L | Cysteine substiution at 10, 17 | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | N.A. | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 0.62 ± 0.09 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 18 | 34 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | L | Cysteine substiution at 23, 30 | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | 4.5 | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 0.91 ± 0.08 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 11 | 34 | Free | Amidation | Linear | L | None | PYY analog | Antiobesity | Blood samples were collected between 0.25 and 48 h | 0.1 mg/kg | 1.21 | Rats plasma protease | UPLC-MS/MS | Rats plasma | In Vivo | None | None | EC50 (nM) = 0.29 ± 0.03 for hNPY2R (cAMP) | |||
| 32841660 | 2020 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1R agonist | Attenuates renal fibrosis | N.A. | 90 nmol/kg | 64.74 ± 3.06 | SD rats serum protease | N.A. | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.11 (In vitro receptor activation profiles of GLP-1 peptides for GLP-1R) | |||
| 32841660 | 2020 | XFL6 | 43 | Free | Free | Linear | L | Modifcation of lysine site at position at 16 with C16 fatty acid | GLP-1/GIP/Gcg receptor triagonist | Antidiabetes, Antiobesity | N.A. | 10 nmol/kg | 41.35 ± 1.42 | SD rats serum protease | N.A. | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R) | |||
| 32841660 | 2020 | XFL6 | 43 | Free | Free | Linear | L | Modifcation of lysine site at position at 16 with C16 fatty acid | GLP-1/GIP/Gcg receptor triagonist | Antidiabetes, Antiobesity | N.A. | 30 nmol/kg | 58.23 ± 2.17 | SD rats serum protease | N.A. | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R) | |||
| 32841660 | 2020 | XFL6 | 43 | Free | Free | Linear | L | Modifcation of lysine site at position at 16 with C16 fatty acid | GLP-1/GIP/Gcg receptor triagonist | Antidiabetes, Antiobesity | N.A. | 90 nmol/kg | 75.81 ± 3.58 | SD rats serum protease | N.A. | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R) | |||
| 32812282 | 2020 | α-MSH | 14 | Free | Free | Linear | L | None | Deriving from the pro-opimelanocortin (POMC) | Stimulates The Production And Release Of Melanin By Melanocytes | 4 ◦C for 15 min | 40 μM | 7.4 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | N.A. | |||
| 32812282 | 2020 | ACTH | 39 | Free | Free | Linear | L | None | Deriving from the pro-opimelanocortin (POMC) | Stimulates The Adrenal Cortex To Produce And Secrete Cortisol | 4 ◦C for 15 min | 40 μM | 250 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | N.A. | |||
| 32808659 | 2020 | Fc-ELA-21 | 266 | Fc joined with ELA-21 by linker (GGGS)3 | Free | Linear | L | None | Derived from ELA | Anti-Heart Failure Activity | About 10 μl of blood was collected at each time point of 0, 1, 2, 4, 8, 24, 32, 48, 56, and 72 h after administration | 5 mg/kg | ∼44 | Mice plasma protease | Western blotting | Mice plasma | In Vivo | https://sci-hub.se/10.1016/j.ijcard.2019.04.089 | None | EC50 =1.58 nM (cAMP supression) | |||
| 32808659 | 2020 | ELA-21 | 21 | Free | Free | Linear | L | None | produced endogenously in the body | Anti-Heart Failure Activity | Blood was collected at time points of 0, 3, 10, 30 and 90 mins, and 4.5, 12 and 24 h | 100 mg/kg | ∼13 | Mice plasma protease | Western blotting | Mice plasma | In Vivo | https://sci-hub.se/10.1016/j.ijcard.2019.04.089 | None | EC50 = 0.6 nM (cAMP supression) | |||
| 32803073 | 2020 | Pal-Rb | 169 | Free | Free | Linear | L | Conjugation of palmitic acid at AzF, biotinylated labelling, , (AzF) was incorporated into the position 126 on the repebody followed by lipid conjugation | Synthetic | Antitumor | Blood was collected in predetermined time points postinjection (n = 5; 0.05, 0.5, 1, 2, 4, 6, 12 and 24 h | 10 mg/kg | 10.7 (Elimination Half-Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB ID: 4J4L | None | The tumor size remained around 200 mm3 until 27 days when Pal-Rb was administered (p < 0.01), whereas tumor continued to grow over 600 mm3 when WT-Rb and PBS were injected. | |||
| 32803073 | 2020 | WT-Rb | 168 | Free | Free | Linear | L | Biotinylation | Synthetic | Antitumor | Blood was collected in predetermined time points postinjection (n = 5; 0.05, 0.5, 1, 2, 4, 6, 12 and 24 h | 10 mg/kg | 20 (Initial Half-Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB ID: 4J4L | None | The tumor size remained around 200 mm3 until 27 days when Pal-Rb was administered (p < 0.01), whereas tumor continued to grow over 600 mm3 when WT-Rb and PBS were injected. | |||
| 32781586 | 2020 | TAMRA-HPA3NT3-A2 | 15 | Free | Free | Linear | L | TAMRA labeled | HPA3NT3 analogue | Antimicrobial | Incubation times (0, 60, 120 min) at 37 °C | 128, 64, 32, 16, 8, 4, 2, 1, and 0.5 µM | Degradation occured initially after 10 min | Human serum protease | HPLC | Human serum | In Vitro | None | None | Hemolysis % =0.3 for 250 micromolar (Toxicity of HPA3NT3 analogue peptide against RBCs) | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 68.5 ± 12.0 µg/kg | 16.8±5.66 (Terminal Half Life) | (IP) corn oil treated rats plasma protease | ELISA | Corn oil treated rat plasma | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 64.5 ± 13.2 µg/kg | 24.5±0.05 (Terminal Half Life) | Untreated rats plasma protease | ELISA | untreated rats plasma | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 64.5 ± 13.2 µg/kg | 75.5 ± 17.9 (Terminal Half Life) | Untreated rats CSF protease | ELISA | untreated rats CSF | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 68.5 ± 12.0 µg/kg | 47.9 ± 20.9 (Terminal Half Life) | (IP) corn oil treated rats CSF protease | ELISA | Corn oil treated rat CSF | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32736262 | 2020 | EX | 39 | Free | Amidation | Linear | L | None | Produced by the salivary glands of Gila monster | Antiobesity | Blood was withdrawn at 0, 5 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h post-administratio | 50 nmol/kg | 0.69 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32736262 | 2020 | EX-AFF | 84 | Free | AFF | Linear | L | None | Synthetic | Antiobesity | Blood was withdrawn at 0, 5 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h post-administratio | 50 nmol/kg | 1.5 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32736262 | 2020 | EX-ABD | 84 | Free | ABD | Linear | L | None | Synthetic | Antiobesity | Blood was withdrawn at 0, 10 min, 1 h, 3 h, 8 h, 1 day, 2 day, 3 day, 4 day, 7 day, 10 day, and 14 day post-administratio | 50 nmol/kg | 84.02 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32736262 | 2020 | EX-ABD-AFF | 142 | Free | ABD-AFF | Linear | L | None | Synthetic | Antiobesity | blood was withdrawn at 0, 10 min, 1 h, 3 h, 8 h, 1 day, 2 day, 3 day, 4 day, 7 day, 10 day, and 14 day post-administratio | 50 nmol/kg | 166.4 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32736262 | 2020 | EX-ABD-AFF | 142 | Free | ABD-AFF | Linear | L | None | Synthetic | Antiobesity | blood was withdrawn at 0, 10 min, 1 h, 3 h, 8 h, 1 day, 2 day, 3 day, 4 day, 7 day, 10 day, and 14 day post-administratio | 50 nmol/kg | 140.2 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32608185 | 2020 | 125I-M-E5 | 22 | Free | Tyrosine (Y) residue was added to E5 sequence and 125I was added | Linear | L | None | Synthetic | Anticancer (Treatment of Acute Myeloid Leukemia) | N.A. | 50 µg/g | 14.53 ± 6.04 | Rats plasma protease | Gamma counter | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC4196105/#sec10 | None | The cells that were pretreated with M-E5 showed significantly reduced migration compared with the CXCL12 group, and the inhibitory rate was 82.9% for the leukemic cells separated from the spleen and 59.1% for those separated from the BM | |||
| 32603666 | 2020 | V-Gem | 1 | Free | Gemicitabine | Linear | L | None | Derived from Gemcitabine | Anticancer | 2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min | 76 nmol/g | 46.2 | Mice blood plasma protease | LC-MS/MS | Mice blood plasma (analyte = Gemcitabine) | In Vivo | None | None | N.A. | |||
| 32603666 | 2020 | V-Gem | 1 | Free | Gemicitabine | Linear | L | None | Derived from Gemcitabine | Anticancer | 2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min | 76 nmol/g | 128 | Mice blood plasma protease | LC-MS/MS | Mice blood plasma (analyte = dFdU) | In Vivo | None | None | N.A. | |||
| 32603666 | 2020 | V-Gem | 1 | Free | Gemicitabine | Linear | L | None | Derived from Gemcitabine | Anticancer | 2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min | 76 nmol/g | 3.7 | Mice blood plasma protease | LC-MS/MS | Mice blood plasma (analyte = Prodrug) | In Vivo | None | None | N.A. | |||
| 32603666 | 2020 | V-Gem | 1 | Free | Gemicitabine | Linear | L | None | Derived from Gemcitabine | Anticancer | 2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min | 228 nmol/g | 39.1 | Mice blood plasma protease | LC-MS/MS | Mice blood plasma (analyte = Gemcitabine) | In Vivo | None | None | N.A. | |||
| 32603666 | 2020 | V-Gem | 1 | Free | Gemicitabine | Linear | L | None | Derived from Gemcitabine | Anticancer | 2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min | 228 nmol/g | 216 | Mice blood plasma protease | LC-MS/MS | Mice blood plasma (analyte = dFdU) | In Vivo | None | None | N.A. | |||
| 32582624 | 2020 | NT(8-13) | 6 | Free | Free | Linear | L | None | Derived from NT | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 1.0 ± 0.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 1.5 ± 0.03 for hNTS1 | |||
| 32582624 | 2020 | Entry 1 | 6 | KK amino acid substiuitions | Free | Linear | L | None | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 1.6 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 4.0 ± 0.4 for hNTS1 | |||
| 32582624 | 2020 | Entry 2 | 6 | Kψ[CH2NH]K substiuition at position 1 | Free | Linear | L | None | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 8.4 ± 2.0 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 2.0 ± 0.8 for hNTS1 | |||
| 32582624 | 2020 | Entry 3 | 5 | KK amino acid substiuitions | TMSAla conjugation | Linear | L | None | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 1.6 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 0.018 ± 0.004 for hNTS1 | |||
| 32582624 | 2020 | Entry 4 | 5 | Kψ[CH2NH]K substiuition | TMSAla conjugation | Linear | L | None | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 2.0 ± 0.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 2.5 ± 0.2 for hNTS1 | |||
| 32582624 | 2020 | Entry 5 | 6 | KK amino acid substiuitions | Free | Linear | L | Sip amino acid substiution | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 4.5 ± 0.8 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 14 ± 11 for hNTS1 | |||
| 32582624 | 2020 | Entry 6 | 6 | Kψ[CH2NH]K substiuition | Free | Linear | L | Sip amino acid substiution | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 22 ± 2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 300 ± 50 for hNTS1 | |||
| 32582624 | 2020 | Entry 7 | 5 | Kψ[CH2NH]K substiuition | TMSAla conjugation | Linear | L | Sip amino acid substiution, TMSAla substuition | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 3.5 ± 0.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 55 ± 5 for hNTS1 | |||
| 32582624 | 2020 | Entry 8 | 5 | Kψ[CH2NH]K substiuition | TMSAla conjugation | Linear | L | Sip amino acid substiution, TMSAla substuition | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 20 ± 4 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 610 ± 30 for hNTS1 | |||
| 32582624 | 2020 | Entry 9 | 6 | KK amino acid substiuitions | Free | Linear | L | Substiution of Y amino acid with K | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 2.9 ± 0.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 7 600 ± 1 000 for hNTS1 | |||
| 32582624 | 2020 | Entry 10 | 6 | Kψ[CH2NH]K substiuition | Free | Linear | L | Substiution of Y amino acid with K | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 5.0 ± 0.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 6 600 ± 2 0003 for hNTS1 | |||
| 32582624 | 2020 | Entry 11 | 5 | KK amino acid substiuitions | TMSAla-OH conjugation | Linear | L | Substiution of Y amino acid with K | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 2.8 ± 0.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 710 ± 100 for hNTS1 | |||
| 32582624 | 2020 | Entry 12 | 5 | Kψ[CH2NH]K substiuition | TMSAla-OH conjugation | Linear | L | Substiution of Y amino acid with K | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 10 ± 1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 150 ± 60 for hNTS1 | |||
| 32582624 | 2020 | Entry 13 | 5 | KK amino acid substiuitions | TMSAla-OH conjugation | Linear | Mix | Substiution of Y amino acid with d-W | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 10 ± 2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 3 600 ± 600 for hNTS1 | |||
| 32582624 | 2020 | Entry 14 | 5 | Kψ[CH2NH]K substiuition | TMSAla-OH conjugation | Linear | L | Substiution of Y amino acid with d-W | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 19 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 55 ± 3 for hNTS1 | |||
| 32582624 | 2020 | Entry 15 | 6 | KK amino acid substiuitions | Free | Linear | L | Substiution of Y, I amino acid with Dmt, Tle | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 4.6 ± 0.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 57 ± 6 for hNTS1 | |||
| 32582624 | 2020 | Entry 16 | 5 | Kψ[CH2NH]K substiuition | Free | Linear | L | Substiution of Y, I amino acid with Dmt | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | >24 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 110 ± 2 for hNTS1 | |||
| 32512181 | 2020 | [3H]-THF | 8 | Free | Free | Linear | L | 3H labeling at proline5 residue | Isolated from calf thymus | Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment) | Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min | 93 nmol/mL | 3.7 ± 0.2 | Rats blood protease | N.A. | Rats blood sample | In Vitro | None | None | N.A. | |||
| 32512181 | 2020 | [3H]-THF | 8 | Free | Free | Linear | L | 3H labeling at proline5 residue | Isolated from calf thymus | Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment) | Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min | 93 nmol/mL | 5.6 ± 0.2 | Mouse blood protease | N.A. | Mouse blood sample | In Vitro | None | None | N.A. | |||
| 32512181 | 2020 | [3H]-THF | 8 | Free | Free | Linear | L | 3H labeling at proline5 residue | Isolated from calf thymus | Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment) | Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min | 93 nmol/mL | 5.2 ± 0.4 | Human blood protease | N.A. | Human blood sample | In Vitro | None | None | N.A. | |||
| 32506501 | 2020 | des-Ac-a-MSH | 14 | Free | Amidation | Linear | L | None | Derived from POMC | Antiinflammatory, Antipyretic | 37 °C | 2 µM | 0.21 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human plasma | In Vitro | None | None | EC50 (M) = 1.667E-09 for MC1R-des-Ac-a-MSH | |||
| 32506501 | 2020 | ACTH | 39 | Free | Free | Linear | L | None | Derived from POMC | Stimulates the adrenal glands to release cortisol | 37 °C | 2 µM | 3.79 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human plasma | In Vitro | None | None | EC50 (M) = 1.54E-09 for MC1R-ACTH | |||
| 32506501 | 2020 | gamma2-MSH | 12 | Free | Amidation | Linear | L | None | Derived from POMC | Antiobesity | 37 °C | 2 µM | 0.028 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human plasma | In Vitro | None | None | EC50 (M) = 7.749E-10 for MC1R-g2-MSH | |||
| 32506501 | 2020 | gamma3-MSH | 26 | Free | Free | Linear | L | None | Derived from POMC | Antiinflammatory and Cardiovascular function | 37 °C | 2 µM | 2.62 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human plasma | In Vitro | None | None | EC50 (M) = 9.37E-10 for MC1R-g3-MSH | |||
| 32506501 | 2020 | des-Ac-a-MSH | 14 | Free | Amidation | Linear | L | None | Derived from POMC | Antiinflammatory, Antipyretic | 37 °C | 2 µM | 32.06 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human CSF | In Vitro | None | None | EC50 (M) = 1.667E-09 for MC1R-des-Ac-a-MSH | |||
| 32506501 | 2020 | ACTH | 39 | Free | Free | Linear | L | None | Derived from POMC | Stimulates the adrenal glands to release cortisol | 37 °C | 2 µM | 86.33 | Human CSF protease | Glo-sensor transfected cell-based luminescence assay | Human CSF | In Vitro | None | None | EC50 (M) = 1.54E-09 for MC1R-ACTH | |||
| 32506501 | 2020 | gamma2-MSH | 12 | Free | Amidation | Linear | L | None | Derived from POMC | Antiobesity | 37 °C | 2 µM | 1.44 | Human CSF protease | Glo-sensor transfected cell-based luminescence assay | Human CSF | In Vitro | None | None | EC50 (M) = 7.749E-10 for MC1R-g2-MSH | |||
| 32464231 | 2020 | FP-EGCG-NPs | 3 | Free | Folate peptide (FA-Pep-1) conjugated to EGCG-loaded nanoparticles (EGCG-NPs) | Linear | L | None | Polyphenolic constituent of green tea | Antitumor (Against Mda-Mb-231 Tumor Xenograft) | blood samples were collected at different time intervals (0.5, 1, 2, 4, 6, 8, 12, 24 and 48 h post-administration | 0.1 mL | 25.13 ± 8.62 | Male SD rats plasma protease | HPLC | Male SD rats plasma | In Vivo | None | None | IC50 = 15.56 for FP-EGCG-NPs(µg/mL) in MDA-MB-231 | |||
| 32404523 | 2020 | PEG40-NC | 34 | Free | Free | Linear | L | PEGylation at Asn637 in native gp41 | Derived from the gp41 CHR | Therapeutic Efficacy In Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus Monkeys | Blood samples (300 μl) were collected from the tail vein before administration and at different intervals after injection (3, 6, 9, 20, 23, 29, 48, 72, and 96 h) | 1.7 μmol/kg | 10.39 | Rats plasma protease | HIV inhibition assay | Rats plasma | In Vivo | None | None | [EC50] = 18.51 nM for PEG40-NC (antiviral activity) | |||
| 32404523 | 2020 | C34 | 34 | Free | Free | Linear | L | None | Derived from the gp41 CHR | Therapeutic Efficacy In Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus Monkeys | Blood samples (300 μl) were collected from the tail vein before administration and at different intervals after injection (3, 6, 9, 20, 23, 29, 48, 72, and 96 h) | 1.7 μmol/kg | 0.6 | Rats plasma protease | HIV inhibition assay | Rats plasma | In Vivo | None | None | [EC50] = 18.51 nM for PEG40-NC (antiviral activity) | |||
| 32387412 | 2020 | DIG-2 | 62 | Free | bisMal-PEG(10KDa) | Linear | L | Radioiodinated , A8G, G31C modification in GLP-1 | DIG conjugates | Antidiabetes | The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C | 50 nmol/kg | 62.6 | Cynomolgus monkeys plasma protease | RP-HPLC | Cynomolgus monkeys plasma | In Vivo | None | None | kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD | |||
| 32387412 | 2020 | DIG-2 | 62 | Free | bisMal-PEG(10KDa) | Linear | L | Radioiodinated , A8G, G31C modification in GLP-1 | DIG conjugates | Antidiabetes | The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C | 100 nmol/kg | 97.2 | Cynomolgus monkeys plasma protease | RP-HPLC | Cynomolgus monkeys plasma | In Vivo | None | None | kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD | |||
| 32387412 | 2020 | DIG-2 | 62 | Free | bisMal-PEG(10KDa) | Linear | L | Radioiodinated , A8G, G31C modification in GLP-1 | DIG conjugates | Antidiabetes | The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C | 150 nmol/kg | 120.4 | Cynomolgus monkeys plasma protease | RP-HPLC | Cynomolgus monkeys plasma | In Vivo | None | None | kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD | |||
| 32380198 | 2020 | Apelin-12 | 12 | Free | Free | Linear | L | None | Smallest fragment of a 77 amino acid prepropeptide | Cardioprotective Properties | N.A. | 2-3 mg/ml | 165 (Terminus Half Life) | Human blood plasma protease | 1H-NMR | Human blood plasma | In Vitro | None | None | peptide M showed a significantly more pronounced effect in improving LV systolic function in Dox-induced cardiomyopathy compared to apelin-12 at a dose of 50 μg/kg | |||
| 32348108 | 2020 | SAH-GLP-1-A8J(16,23) | 28 | Aminoisobutyric acid | Free | Linear | L | Modifications include (R-octenyl alanine) and (Bis-pentenyl glycine) | Single-stapled analogs of GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | 120 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | PDB:3IOL | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | SAH-GLP-1-A8J(23,30) | 28 | Aminoisobutyric acid | Free | Linear | L | Modifications include (S-octenyl alanine) and (Bis-pentenyl glycine) | Single-stapled analogs of GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | 30 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | PDB:3IOL | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | stitched GLP-1 | 30 | Free | Free | Cyclic (I, I+7 Stitched GLP) | L | None | Stitched GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | 220 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | GLP-1 | 30 | Free | Free | Linear | L | None | Unstapled GLP-1 analogs | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | <10 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | GLP-1 | 30 | Free | Free | Linear | L | None | Unstapled GLP-1 analogs | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 10 μM | 14 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | SAH-GLP-1-A8J(16,23,30) | 28 | Aminoisobutyric acid | Free | Linear | L | Modifcations include (R-octenyl alanine) and (bis-pentenyl glycine) and (S-octenyl alanine) | Single-stapled analogs of GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 10 μM | 320 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | PDB:3IOL | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 10 μM | 170 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32332143 | 2020 | 68Ga‐NeoBOMB1 | 7 | 68Ga-DOTA-(p-aminomethylaniline)-(diglycolic acid), D-Phe at position 1 | NH-CH[CH2-CH(CH3)2]2 chemical group attached at C terminal | Linear | L | None | Synthetic | DOTA‐coupled GRPR‐antagonist | 2, 5, 10, 30 and 45 min and at 1, 2 and 3 h p.i | 50 µg | 27.3 | Human plasma protease | RP-HPLC | Human plasma | In Vivo | None | None | N.A. | |||
| 32332143 | 2020 | 68Ga‐NeoBOMB1 | 7 | 68Ga-DOTA-(p-aminomethylaniline)-(diglycolic acid), D-Phe at position 1 | NH-CH[CH2-CH(CH3)2]2 chemical group attached at C terminal | Linear | L | None | Synthetic | DOTA‐coupled GRPR‐antagonist | 2, 5, 10, 30 and 45 min and at 1, 2 and 3 h p.i | 50 µg | 35 | Human blood protease | RP-HPLC | Human blood sample | In Vivo | None | None | N.A. | |||
| 32316169 | 2020 | GLP1_16HSA | 615 | Free | Free | Linear | L | Incorporation of HSA at V16 of GLP_1C | Synthetic | Antidiabetes | Blood samples (below 70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 2, 4, 8, 12, and 24 h after administration | 10 nmol/kg | 8.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | EC50 = 0.70 μM | |||
| 32316169 | 2020 | GLP1_19HSA | 615 | Free | Free | Linear | L | Incorporation of HSA at Y19 of GLP_1C | Synthetic | Antidiabetes | Blood samples (below 70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 2, 4, 8, 12, and 24 h after administration | 10 nmol/kg | 7.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | EC50 = 1.91 μM | |||
| 32316169 | 2020 | GLP1_28HSA | 615 | Free | Free | Linear | L | Incorporation of HSA at F28 of GLP_1C | Synthetic | Antidiabetes | Blood samples (below 70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 2, 4, 8, 12, and 24 h after administration | 10 nmol/kg | 8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | EC50 = 6.85 μM | |||
| 32301996 | 2020 | 89Zr-NFP | 13 | mPEG2000, 89Zr labeling | Cy5.5 labelling | Linear | L | None | Synthetic | Diffuse intrinsic pontine glioma treatment | Mice were euthanized after 4 and 21 days for organ collection | 20 μCi | 60.3 | Mice brain homogenize protease | Gamma counter | Mice brain homogenize | In Vivo | None | None | IC50 (nM) = 5.6 ± 0.4 for DM1 in SF8628 | |||
| 32243177 | 2020 | FITC-labeled HFt | 183 | FITC labelled | Free | Linear | L | None | Derived from human Ft | Antidiabetes | At different time points (30 min, 1, 2, 4, 8, 10, 24, 48, 72, and 96 h) after injection | 100 μg | 51.1 | Mice plasma protease | BCA protein assay | Mice plasma | In Vivo | None | None | The GLP-HFt nanocage dose-dependently reduced the nonfasting blood glucose of the STZ-induced diabetic mice | |||
| 32243177 | 2020 | GLP-HFt | 217 | GLP-1 A8G modification linked by GSGG | Free | Linear | L | None | Synthetic | Antidiabetes | At different time points (30 min, 1, 2, 4, 8, 10, 24, 48, 72, and 96 h) after injection | 100 μg | 51.9 | Mice plasma protease | BCA protein assay | Mice plasma | In Vivo | None | None | The GLP-HFt nanocage dose-dependently reduced the nonfasting blood glucose of the STZ-induced diabetic mice | |||
| 32243137 | 2020 | OXM-1 | 37 | Free | Free | Linear | Mix | Incorporation of D-ser in place of L-ser at 2nd position | Derived from proglucagon | Antiobesity, Antisteatotic | N.A. | 40 μg/kg | 6 (Terminal Half Life) | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 10 for OXM-1 (in Vitro Potency of Stapled Peptides in Human GLP-1R- and GCGR-Mediated CRE-Luc Reporter Assays) | |||
| 32243137 | 2020 | O14 | 40 | Free | Addition of the 12 C-terminal residues of Ex-4 to a C-terminal truncated OXM, amidation | Linear | Mix | Two cysteine group conatins fatty acid moteity(L3 = Structure given in paper) , Incorporation of D-ser in place of L-ser at 2nd position | OXM analogs | Antiobesity, Antisteatotic | N.A. | 40 μg/kg | 8.3 (Terminal Half Life) | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.03 for O-14 (in Vitro Potency of Stapled Peptides in Human GLP-1R- and GCGR-Mediated CRE-Luc Reporter Assays) | |||
| 32235388 | 2020 | TxIB | 16 | Free | Free | Linear | L | None | α-conotoxin derived from the venom of the cone snail species Conus textile | Blocks the Α6/Α3Β2Β3 Nicotinic Acetylcholine Receptors | Aliquots of each peptide were taken out at 0, 12, 24, 36, and 48 h. | 100 μM | Stable | Male AB human serum protease | RP-UPLC | Male AB human serum | In Vitro | None | None | 42% inhibition of α6β2* nAChRs by TxIB | |||
| 32235388 | 2020 | cTxIB-4 | 20 | Linker | Free | Cyclic (C2-C8, C3-C16 Disulfide Bond And Linker-C16 Bond) | L | None | α-conotoxin TxIB analogue | Blocks the Α6/Α3Β2Β3 Nicotinic Acetylcholine Receptors | Aliquots of each peptide were taken out at 0, 12, 24, 36, and 48 h. | 100 μM | Slightly lower stability than TXIB | Male AB human serum protease | RP-UPLC | Male AB human serum | In Vitro | None | None | Inhibition of cTxIB-4 is 35% | |||
| 32235388 | 2020 | cTxIB-5 | 21 | Linker (GGAAG) | Free | Cyclic (C2-C8, C3-C16 Disulfide Bond And Linker-C16 Bond) | L | None | α-conotoxin TxIB analogue | Blocks the Α6/Α3Β2Β3 Nicotinic Acetylcholine Receptors | Aliquots of each peptide were taken out at 0, 12, 24, 36, and 48 h. | 100 μM | Slightly lower stability than TXIB | Male AB human serum protease | RP-UPLC | Male AB human serum | In Vitro | None | None | Inhibition of cTxIB-5 is 42% | |||
| 32235388 | 2020 | cTxIB-6 | 22 | Linker (GAGAAG) | Free | Cyclic (C2-C8, C3-C16 Disulfide Bond And Linker-C16 Bond) | L | None | α-conotoxin TxIB analogue | Blocks the Α6/Α3Β2Β3 Nicotinic Acetylcholine Receptors | Aliquots of each peptide were taken out at 0, 12, 24, 36, and 48 h. | 100 μM | Slightly lower stability than TXIB | Male AB human serum protease | RP-UPLC | Male AB human serum | In Vitro | None | None | Inhibition of cTxIB-6 is 48% | |||
| 35496622 | 2020 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 7.1 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.076 ± 0.013 for Lixisenatide (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1a | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 13.2 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.19 ± 0.02 for Lixisenatide 1a (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1b | 44 | Free | Amidation | Linear | L | (X2) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 19.1 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.49 ± 0.11 for Lixisenatide 1b (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1c | 44 | Free | Amidation | Linear | L | (X3) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 30 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.98 ± 0.24 for Lixisenatide 1c (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1d | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 13.1 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.085 ± 0.021 for Lixisenatide 1d (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1e | 44 | Free | Amidation | Linear | L | (X2) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 21.2 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.13 ± 0.03 for Lixisenatide 1e (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1f | 44 | Free | Amidation | Linear | L | (X3) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 33.4 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.32 ± 0.13 for Lixisenatide 1f (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1g | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 11.9 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.59 ± 0.16 for Lixisenatide 1g (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1h | 44 | Free | Amidation | Linear | L | (X2) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 17.8 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 1.97 ± 0.53 for Lixisenatide 1h (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1i | 44 | Free | Amidation | Linear | L | (X3) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 31.6 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 4.68 ± 0.85 for Lixisenatide 1i (in vitro GLP-1 receptor activation potency) | |||
| 32169063 | 2020 | IFN-1CTPON | 216 | Free | Carboxyl-terminal peptide (CTP) of the human chorionic gonadotropin β subunit and N-linked glycosylation sequences were linked to rhIFN-α2b at C terminus | Linear | L | None | Derived from rhIFN-α2b | Antiviral, Antitumor | Intraocular venous blood was collected at 0.5, 1, 2, 4, 8, and 24 h postinjection | 50 μg/kg | 2.62 ± 0.34 | Mice blood protease | ELISA | Mice blood sample | In Vivo | PDB id: 1ITF | None | Antiviral activities of IFN-1CTPON = 8.22 × 106 IU/mg | |||
| 32169063 | 2020 | IFN-2CTPON | 244 | Carboxyl-terminal peptide (CTP) of the human chorionic gonadotropin β su bunit and N-linked glycosylation sequences were linked to rhIFN-α2b at N terminus | Carboxyl-terminal peptide (CTP) of the human chorionic gonadotropin β su bunit and N-linked glycosylation sequences were linked to rhIFN-α2b at C terminus | Linear | L | None | Synthetic | Antiviral, Antitumor | Intraocular venous blood was collected at 0.5, 1, 2, 4, 8, and 24 h postinjection | 50 μg/kg | 3.45 ± 0.87 | Mice blood protease | ELISA | Mice blood sample | In Vivo | PDB id: 1ITF | None | Antiviral activities of IFN-2CTPON = 3.12 × 106 IU/mg | |||
| 32169063 | 2020 | rhIFN-α2b | 165 | Free | Free | Linear | L | None | Synthetic | Antiviral, Antitumor | Intraocular venous blood was collected at 0.5, 1, 2, 4, 8, and 24 h postinjection | 50 μg/kg | 1.34 ± 0.48 | Mice blood protease | ELISA | Mice blood sample | In Vivo | PDB id: 1RH2 | None | Antiviral activities of rhIFN-α2b = 5.29 × 107 IU/mg | |||
| 32141733 | 2020 | TB1-RS6 | 6 | Fluorescein | Amidation | Linear | L | Single atom O toS substitution (X=S) | Thioamide-stabilized version | Stabilization of cancer imaging peptides | 37 °C | 50 μM | >24 | Mouse serum protease | HPLC | Mouse serum | In Vitro | https://sci-hub.se/10.1021/acs.molpharmaceut.6b00464 | None | KI = 101 ± 24 nM, The IC50 values determined for TB1 and TB1-RS6 (719 ± 143 nM and 1363 ± 323 nM, respectively | |||
| 32141733 | 2020 | TB1 | 6 | Fluorescein | Amidation | Linear | L | None | Fluorescein analog of BVD15 | Stabilization of cancer imaging peptides | 37 °C | 50 μM | 1.5 | Mouse serum protease | HPLC | Mouse serum | In Vitro | https://sci-hub.se/10.1021/acs.molpharmaceut.6b00464 | None | KI = 53 ± 10 nM, The IC50 values determined for TB1 and TB1-RS6 (719 ± 143 nM and 1363 ± 323 nM, respectively | |||
| 32133341 | 2020 | Apamin based analogs 3 | 25 | Free | Free | Cyclic (C1-C11, C3-C15) | L | None | Apamin based analogs | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 12.8 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.65 ± 0.18 | |||
| 32133341 | 2020 | Apamin based analogs 9 | 21 | Free | Amidation | Cyclic(C1-C11, C3-C15 ) | L | None | Apamin based analogs | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 6.6 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.76 ± 0.03 | |||
| 32133341 | 2020 | R3 B1-27 | 27 | Free | Free | Linear | L | None | Native relaxin-3 | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 3.1 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 5.91 ± 0.21 | |||
| 32133341 | 2020 | R3 B1-22R | 23 | Free | Amidation | Linear | L | None | Synthetic | Relaxin-3 antagonist | N.A. | 0.05 μg/μl | 4 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.76 ± 0.03 | |||
| 32082972 | 2020 | LMRAP | 291 | Free | hIgG4 Fc-linker-AP25 | Linear | L | None | Synthetic | Antitumor | The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration | 12.5 mg/kg | 45.237 (Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively | |||
| 32082972 | 2020 | LMRAP | 291 | Free | hIgG4 Fc-linker-AP25 | Linear | L | None | Synthetic | Antitumor | The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration | 12.5 mg/kg | 29.187 (Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively | |||
| 32082972 | 2020 | LMRAP | 291 | Free | hIgG4 Fc-linker-AP25 | Linear | L | None | Synthetic | Antitumor | The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration | 12.5 mg/kg | 50.979 (Eliminatoin Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively | |||
| 32082972 | 2020 | LMRAP | 291 | Free | hIgG4 Fc-linker-AP25 | Linear | L | None | Synthetic | Antitumor | The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration | 12.5 mg/kg | 18.256 (Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively | |||
| 32082972 | 2020 | LMRAP | 291 | Free | hIgG4 Fc-linker-AP25 | Linear | L | None | Synthetic | Antitumor | The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration | 12.5 mg/kg | 27.879 (Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively | |||
| 32082972 | 2020 | LMRAP | 291 | Free | hIgG4 Fc-linker-AP25 | Linear | L | None | Synthetic | Antitumor | The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration | 12.5 mg/kg | 28.452 (Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively | |||
| 32075870 | 2020 | hGLP-2 | 33 | Free | Free | Linear | L | None | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 1 mg/kg | 6.4 ± 0.2 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.07 for hGLP-2 receptor | |||
| 32075870 | 2020 | Glepaglutide | 39 | Free | KKKKKK amino acids substiuitions at C terminal | Linear | L | G,E,T,S,L,A,A,A,A amino acid substuitions at positions 2,3,5,8,10,11,16,24,28 respectively | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.2 mg/kg | 19 ± 1.9 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.03 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.2 mg/kg | 16 ± 0.8 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.2 mg/kg | 159 ± 27(Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.100 mg/kg | 474 ± 80 (Elimination Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.025 mg/kg | 782 ± 365 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.100 mg/kg | 43 ± 4 (Elimination Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.100 mg/kg | 88 ± 11 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 1 mg/kg | 11.7 ± 1.4 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 5 mg/kg | 22.5 ± 1.3 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 1 mg/kg | 0.5 ± 0.1 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 5 mg/kg | 0.5 ± 0.0 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.25 mg/kg | 32.4 ± 6.1 (Terminal Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.15 mg/kg | 30.1 ± 3.1 (Terminal Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.25 mg/kg | 0.9 ± 0.1 (Terminal Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.15 mg/kg | 2.7 ± 0.8 (Terminal Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32034289 | 2020 | α-GD2 scFv TM | N.A. | Radiolabelled with 64Cu | E5B9 | Linear | L | VH and VL joined by linker (GGGGS)3 | Synthetic | Antitumor | N.A. | N.A. | 1.6 | Mice blood protease | PET scanning | Mice blood sample | In Vivo | E5B9 sequence available on this link: https://pmc.ncbi.nlm.nih.gov/articles/PMC6805801/ | None | EC50 = 0.7 nM (target cell lysis) | |||
| 32023048 | 2020 | ICP NPs | 8 | Free | One 4-carboxy-3-fluorophenylboronic acid (PBA), Three cholic acids (CA) | Linear | L | None | Synthetic | Transcellular Tumor Penetration And Photo−Chemo Combination Therapy | Blood samples (∼0.2 mL each time point) were collected from the jugular vein cannula to centrifuge tubes containing 20 μL of 10 IU heparin at predetermined time points (5, 10, 15, 30, 60, 120, 180, 240, 360, 720, 1440 min) | 3 mg/kg | 3.34 ± 0.86 | Female wistar rats plasma protease | HPLC | Female wistar rats plasma | In Vivo | None | None | Additional phototherapy by treatment with laser further enhanced the antitumor activity of both ICP and hICP NPs, leading to a complete cure rate of 10% and 50%, respectively | |||
| 32023048 | 2020 | hICP NPs | 8 | Free | One 4-carboxy-3-fluorophenylboronic acid (PBA), Three cholic acids (CA) | Linear | L | ICP NPs were stacked into nanoparticle clusters upon coating with DA modified HA, Folic acid | Synthetic | Transcellular Tumor Penetration And Photo−Chemo Combination Therapy | Blood samples (∼0.2 mL each time point) were collected from the jugular vein cannula to centrifuge tubes containing 20 μL of 10 IU heparin at predetermined time points (5, 10, 15, 30, 60, 120, 180, 240, 360, 720, 1440 min) | 3 mg/kg | 7.97 ± 2.38 | Female wistar rats plasma protease | HPLC | Female wistar rats plasma | In Vivo | None | None | Additional phototherapy by treatment with laser further enhanced the antitumor activity of both ICP and hICP NPs, leading to a complete cure rate of 10% and 50%, respectively | |||
| 31996466 | 2020 | D6PV | 40 | Free | Free | Linear | L | Replaces 18A with a modified central region of apoC-II | Derived from apoC-II | TG-Lowering Effects | N.A. | 46.7 mg/kg | 3 (Initial Elimination Half Life) | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | Equilibrium dissociation constant (Kd) of D6PV binding to HDL was determined to be 18.5 μM | |||
| 31996466 | 2020 | D6PV | 40 | Free | Free | Linear | L | Replaces 18A with a modified central region of apoC-II | Derived from apoC-II | TG-Lowering Effects | N.A. | 46.7 mg/kg | 9 (Terminal Elimination Half Life) | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | Equilibrium dissociation constant (Kd) of D6PV binding to HDL was determined to be 18.5 μM | |||
| 31926774 | 2020 | Leuprolide | 10 | Free | NHEt (Ethylamine) | Linear | L | None | Synthetic | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 0.43 ± 0.025 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The administration of same dose of PEGylated leuprolides also results in an initial testosterone surge. In addition, the extent of the testosterone surge is almost the same for all three peptides, either PEGylated or not | |||
| 31926774 | 2020 | Leuprolide | 10 | Free | NHEt (Ethylamine) | Linear | L | None | (GnRH) agonist | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 0.43 ± 0.06 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The administration of same dose of PEGylated leuprolides also results in an initial testosterone surge. In addition, the extent of the testosterone surge is almost the same for all three peptides, either PEGylated or not | |||
| 31926774 | 2020 | PEG2K-LEU | 10 | Free | Free | Linear | L | PEGylation at His2 | Derived from leuprolide | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 0.53 ± 0.032 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group | |||
| 31926774 | 2020 | PEG2K-LEU | 10 | Free | Free | Linear | L | PEGylation at His2 | Derived from leuprolide | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 0.59 ± 0.023 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group | |||
| 31926774 | 2020 | PEG5K-LEU | 10 | Free | Free | Linear | L | PEGylation at His2 | Derived from leuprolide | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 1.28 ± 0.64 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group | |||
| 31926774 | 2020 | PEG5K-LEU | 10 | Free | Free | Linear | L | PEGylation at His2 | Derived from leuprolide | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 1.51 ± 0.127 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group | |||
| 31901754 | 2020 | Compound 16a | 39 | Free | Amidation | Linear | L | Amino acid residues located at 24 substituted by the residues of Exenatide in the same location, Position 16 was replaced by Cys for coupling hybrid peptides with fatty chains | OXM analogs | Antiobesity, Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72 and 96 h time points, 100 μL of mixture was aliquoted | 1000 ng/mL | 71.79 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | EC50 = 3.8 ± 0.4 pM for mGLP1R | |||
| 31866565 | 2020 | YSNSG peptide | 5 | Free | Free | Cyclic | L | None | Synthetic | Antitumor | Blood samples from blood vessel in the tail were taken at the following time intervals: 15, 30, 60, 90 and 120 min | 20 mg/kg | 25.8 ± 8.2 | B16F1 melanoma mice plasma protease | UPLC-MS/MS | B16F1 melanoma mice plasma | In Vivo | None | None | The relative recoveries of the microdialysis probes of YSNSG peptide in mice using the reverse dialysis method were 79.3 ± 6.6% in the region 1 of the tumor and 79.1 ± 7.4% in the region 2 of the tumor | |||
| 31841696 | 2020 | P9 | 11 | Free | Amidation | Linear | L | None | Synthetic | Anticancer | 37 °C for 5, 10, 20, 25, 30, 45 min | N.A. | 19 | Human plasma protease | HPLC | Human plasma | In Vitro | https://sci-hub.se/10.1007/s13277-015-3435-x | None | IC50 of P48 for Hela229 = 0.6 nM | |||
| 31841696 | 2020 | P48 | 10 | Leucine reduction | Amidation | Linear | L | None | Generated with P9 degradation | Anticancer | 1, 2, 3, 4, 5, 10, 12 h. | N.A. | 4 | Human plasma protease | HPLC | Human plasma | In Vitro | https://sci-hub.se/10.1007/s13277-015-3435-x | None | IC50 of P48 for Hela229 = 0.6 nM | |||
| 31809037 | 2020 | ApoE-Ms-SF | 19 | Free | PEG-P(CL-DTC) | Linear | L | None | Synthetic | Targeted Delivery Of Sorafenib To Hepatocellular Carcinoma | At fixed time points, 75 μL of blood was taken from the ophthalmic vein into a heparinized tube | 6 mg SF equiv/kg | 6.8 (Elimination Half-Lives) | BALB/c mice plasma protease | HPLC | BALB/c mice plasma | In Vivo | None | None | IC50: 8.5 μg/mL for ApoE-MS-SF | |||
| 31786794 | 2020 | DR10601 | 15 | Free | IgG4 hinge-Fc fragment | Linear | L | None | Synthetic | Antiobesity, Antidiabetes | Blood samples were collected at 3, 8, 24, 36, 48, 72, 96, 120, 144 and 168 h after administration | 16.3 nmol/kg | 51.9 ± 12.2 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | (EC50) value of DR10601 for GCGR was 37.39±3.95 nmol/L | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hour after sHDL administration | 50 mg/kg | 2.1 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A-P | 23 | Free | Proline addition at C terminal | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hour after sHDL administration | 50 mg/kg | 4.2 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration | 50 mg/kg | 3.3 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration | 50 mg/kg | 3 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration | 50 mg/kg | 3.3 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration | 50 mg/kg | 3.3 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31765157 | 2020 | CPN-116 | 7 | X = Struture given in paper (6b) | Amidation | Linear | L | None | Synthetic | Antiobesity | At 30 min | 50 mg/mL | 20% of the initial concentration | Rats serum protease | LC-MS | Rats serum after i.p. pentobarbital sodium | In Vitro | https://sci-hub.se/10.1021/jm500599s | None | CPN exhibits a selective agonistic activity to mouse NMUR2 with an EC50 value of 28 ± 2 nM | |||
| 31765157 | 2020 | CPN-116 | 7 | X = Struture given in paper (6b) | Amidation | Linear | L | None | Synthetic | Antiobesity | at 30 min | 50 mg/mL | 90% of initial concentration | Rats CSF protease | LC-MS | Rats CSF after i.p. pentobarbital sodium | In Vitro | https://sci-hub.se/10.1021/jm500599s | None | CPN exhibits a selective agonistic activity to mouse NMUR2 with an EC50 value of 28 ± 2 nM | |||
| 31765157 | 2020 | CPN-116 | 7 | X = Struture given in paper (6b) | Amidation | Linear | L | None | Synthetic | Antiobesity | 4 hours | 50 mg/mL | 20% of the initial concentration | Rats CSF protease | LC-MS | Rats CSF after i.p. pentobarbital sodium | In Vitro | https://sci-hub.se/10.1021/jm500599s | None | CPN exhibits a selective agonistic activity to mouse NMUR2 with an EC50 value of 28 ± 2 nM | |||
| 31529097 | 2020 | GH | 191 | Free | Free | Linear | L | None | Produced by the somatotroph cells in the anterior pituitary gland | Involved in the regulation of growth and metabolism | N.A. | N.A. | 13.9 ± 3.6 | Human blood plasma protease | 2-site immunoassay | Human blood plasma | In Vivo | pdb id: 1HWG | None | N.A. | |||
| 31529097 | 2020 | GH | 191 | Free | Free | Linear | L | None | Produced by the somatotroph cells in the anterior pituitary gland | Involved in the regulation of growth and metabolism | N.A. | N.A. | 17.0 ± 6.8 | Human blood plasma protease | 2-site immunoassay | Human blood plasma after Sitagliptin | In Vivo | pdb id: 1HWG | None | N.A. | |||
| 31529097 | 2020 | GH | 191 | Free | Free | Linear | L | None | Produced by the somatotroph cells in the anterior pituitary gland | Involved in the regulation of growth and metabolism | GH levels were obtained every 10 minutes from 8 PM until 8 AM | N.A. | 13.9 | Human blood plasma protease | 2-site immunoassay | Human blood plasma | In Vivo | pdb id: 1HWG | None | N.A. | |||
| 31529097 | 2020 | GH | 191 | Free | Free | Linear | L | None | Produced by the somatotroph cells in the anterior pituitary gland | Involved in the regulation of growth and metabolism | GH levels were obtained every 10 minutes from 8 PM until 8 AM | N.A. | 14.5 | Human blood plasma protease | 2-site immunoassay | Human blood plasma after 1month of Sitagliptin | In Vivo | pdb id: 1HWG | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 43 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 9.9 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 52 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 12 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 32 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 8.3 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 38 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 13 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| N.A. | 2020 | Ac-(06-34-18) (wildtype) | 12 | Acetylation | Free | Linear | L | None | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 2.3 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 1.7 | |||
| N.A. | 2020 | Ac-(06-34-18) (HomoArg5) | 12 | Acetylation | Free | Linear | L | HomoArg6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 10.7 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 64 | |||
| N.A. | 2020 | Ac-(06-34-18) ( 4GuanPhe5) | 12 | Acetylation | Free | Linear | L | 4GuanPhe6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 2.8 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 21 | |||
| N.A. | 2020 | Ac-(06-34-18) (NMeArg5) | 12 | Acetylation | Free | Linear | L | NMeArg6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | >20 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 98 | |||
| N.A. | 2020 | Ac-(06-34-18) Aze3 (HomoArg5) | 12 | Acetylation | Free | Linear | L | Aze replaces Pro (P)at position 4 , HomoArg6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Aze3 (4GuanPhe5) | 12 | Acetylation | Free | Linear | L | Aze replaces Pro (P)at position 4 , 4GuanPhe6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Aze3 (NMeArg5) | 12 | Acetylation | Free | Linear | L | Aze replaces Pro (P)at position 4, NMeArg replaces Arg (R) at position 6 | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 | 12 | Acetylation | Free | Linear | L | Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 0.9 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 13.8 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 HomoArg5 | 12 | Acetylation | Free | Linear | L | HomoArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 12.2 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 19.7 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 4GuanPhe5 | 12 | Acetylation | Free | Linear | L | 4GuanPhe replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 5 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 2.5 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 NMeArg5 | 12 | Acetylation | Free | Linear | L | NMeArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | >20 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 60.2 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Aze3 Tyr4 HomoArg5 | 12 | Acetylation | Free | Linear | L | HomoArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr, Aze substituitons at position 4 | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Aze3Tyr4 4GuanPhe5 | 12 | Acetylation | Free | Linear | L | 4GuanPhe replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr, Aze substituitions at position 4 | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Aze3Tyr4 NMeArg5 | 12 | Acetylation | Free | Linear | L | NMeArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr, Aze substituitions at position 4 | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | HA-Aib-Linker-SEQ ID No. 5 | 40 | HA = Hyaluronic acid hydrogel linked with GLP-1 analogue | Amidation | Linear | Mix | Linker Z = Structure mentioned in patent, dSer substituitions at position 2 | GLP-1-Linker-Ha Conjugate | Antidiabetes, Antiobesity | Plasma sample were taken at 0,1,4,8,24,48 H And Once A Day On Day 3 to 21 at the same time | 0.623 mg/kg | 139 | Minipigs plasma protease | LC-MS/MS | Minipigs plasma | In Vivo | None | US 201715829596 A | EC50 hGLP-1R = 1.9 pM for Sequence No. 5 | |||
| 32454120 | 2020 | Uox-WT | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Treatment of hyperuricemia | Incubated for 4 h at room temperature | 28 μM | 1.1 (Enzymatic Activity Half Life) | Mice serum protease | Uric acid degradation assay | Mice serum | In Vivo | None | None | N.A. | |||
| 32454120 | 2020 | Uox-HSA | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Treatment of hyperuricemia | Incubated for 4 h at room temperature | 28 μM | 17.4 (Enzymatic Activity Half Life) | Mice serum protease | Uric acid degradation assay | Mice serum | In Vivo | None | None | N.A. | |||
| 32454120 | 2020 | PEG-PAEU + Uox-HSA | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Treatment of hyperuricemia | Incubated for 4 h at room temperature | 28 μM | 43.6 (Enzymatic Activity Half Life) | Mice serum protease | Uric acid degradation assay | Mice serum | In Vivo | None | None | N.A. | |||
| 32454120 | 2020 | PEG-PAEU-ABP + Uox-HSA | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Treatment of hyperuricemia | Incubated for 4 h at room temperature | 28 μM | 96.3 (Enzymatic Activity Half Life) | Mice serum protease | Uric acid degradation assay | Mice serum | In Vivo | None | None | N.A. | |||
| 32803073 | 2020 | Pal-Rb | 169 | Free | Free | Linear | L | Conjugation of palmitic acid, biotinylated labelling, , (AzF) was incorporated into the position 126 on the repebody followed by lipid conjugation | Synthetic | Antitumor | Blood was collected in predetermined time points postinjection (n = 5; 0.05, 0.5, 1, 2, 4, 6, 12 and 24 h) | 10 mg/kg | 4.2 (Distribution Half-Life) | Mice plasma protease | Sandwich ELISA | mice plasma | In Vivo | None | None | The tumor size remained around 200 mm3 until 27 days when Pal-Rb was administered (p < 0.01), whereas tumor continued to grow over 600 mm3 when WT-Rb and PBS were injected. | |||
| 31845578 | 2020 | Man25 | 449 | Free | Free | Linear | L | None | β-mannanase from Thermoanaerobacterium aotearoense | Role in cellulosic biomass degradation | 55 °C | N.A. | 40.2 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | Man25 retaining more than 50% activity at its optimal pH of 5.5 | |||
| 31845578 | 2020 | ManM3-3 | 449 | Free | Free | Linear | L | D143A amino acid substituition | Derived from Man25 | Role in cellulosic biomass degradation | 55 °C | N.A. | 143.4 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | Man25 retaining more than 50% activity at its optimal pH of 5.5 | |||
| 31845578 | 2020 | ManM5-10 | 449 | Free | Free | Linear | L | E32K, E34S amino acid substituition | Derived from Man25 | Role in cellulosic biomass degradation | 55 °C | N.A. | 74.4 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | Man25 retaining more than 50% activity at its optimal pH of 5.5 | |||
| 31840306 | 2020 | conjugate 1 b | 16 | 2A-Gossypol Conjugate Linked By Thiazolidine Imine Linkage | Free | Linear | L | None | Synthetic | Cancer‐cell‐specific drug delivery | After 10 hours | 0.1 mg | 52% Cleavage of the peptide | N.A. | HPLC | 50 μL of 6M Gn·HCl, 200 mM phosphate buffer at pH 7 | In Vitro | None | None | N.A. | |||
| 33270417 | 2020 | Peptide 1a | 8 | Free | Free | Linear | L | None | From human α-1-acid glycoprotein 1 | Used to study glycosylation effects on deamidation | 48 hours under 37 C | N.A. | 31.08 (Deamidation Half Life) | N.A. | HPLC-MS | N.A. | In Vitro | None | None | N.A. | |||
| 33270417 | 2020 | Peptide 2a | 8 | Free | Free | Linear | L | None | From peptidyl-prolyl cis−trans isomerase FKBP10 | Used to study glycosylation effects on deamidation | 12 days under 37 C | N.A. | 6.4 (Deamidation Half Life) | N.A. | HPLC-MS | N.A. | In Vitro | None | None | N.A. | |||
| 33270417 | 2020 | Peptide 3a | 8 | Free | Free | Linear | L | None | From deoxyribonuclease-2-alpha | Used to study glycosylation effects on deamidation | 15 days under 37 C | N.A. | 13 (Deamidation Half Life) | N.A. | HPLC-MS | N.A. | In Vitro | None | None | N.A. | |||
| 33270417 | 2020 | Peptide 4a | 8 | Free | Free | Linear | L | None | From protein sidekick-1 | Used to study glycosylation effects on deamidation | 13 days under 37 C | N.A. | 13.2 (Deamidation Half Life) | N.A. | HPLC-MS | N.A. | In Vitro | None | None | N.A. | |||
| 33270417 | 2020 | Peptide 5a | 8 | Free | Free | Linear | L | None | From the smoothened homologue | Used to study glycosylation effects on deamidation | 13 days under 37 C | N.A. | 18.78(Deamidation Half Life) | N.A. | HPLC-MS | N.A. | In Vitro | None | None | N.A. | |||
| 33270417 | 2020 | INGAP-P | 15 | Free | Free | Linear | L | None | Synthetic | N.A. | N.A. | N.A. | 55.9 (Deamidation Half Life) | N.A. | HPLC | N.A. | In Vitro | None | None | N.A. | |||
| 33115231 | 2020 | ASL | 5 | Bodipy Tr-X Ester Linked Via (Peg)12 | Free | Linear | Mix | None | Synthetic | Anticancer | N.A. | N.A. | Stable (Release Half Life) | N.A. | Fluorescent assay | PBS containing 0.05% (w/v) Tween 80 | In Vitro | None | None | IC50 = 4.908 ± 0.739 μM for dEx | |||
| 31843919 | 2019 | ZY4 | 17 | Free | Amidation | Cyclic (C2-C16 Disulfide Bond) | L | None | Cathelicidin-BF15 analogs | Antimicrobial | Blood samples were drawn retroorbitally under short-term anesthesia at different time points (1, 5, 10, 30, 60 min, and 2, 5, 10, 18, 24 h) | 8 mg/kg | 1.859 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | MIC (µM) = 1.9 for ZY4 in P. aeruginosa CICC21625 , MIC (µM) = 2 for ZY4 in B. subtilis , MIC (µM) = 2 for ZY4 in S. aureus , MIC (µM) = 2 for ZY4 in C. albicans | |||
| 31818212 | 2019 | RELAX10 | 309 | Free | Free | Linear | L | Fusion of Human Relaxin 2 with Fc IgG using linker | Human Relaxin analogue | Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart | Blood samples were collected at various time points after drug administration | 4 mg/kg | 3.59 | Wistar rats plasma protease | ELISA | Wistar rats plasma | In Vivo | https://www.lens.org/lens/patent/078-521-931-782-236/fulltext | None | RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L | |||
| 31818212 | 2019 | RELAX10 | 309 | Free | Free | Linear | L | Fusion of Human Relaxin 2 with Fc IgG using linker | Human Relaxin analogue | Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart | Blood samples were collected at various time points after drug administration | 4 mg/kg | 3.75 | Wistar rats plasma protease | ELISA | Wistar rats plasma | In Vivo | https://www.lens.org/lens/patent/078-521-931-782-236/fulltext | None | RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L | |||
| 31818212 | 2019 | RELAX10 | 309 | Free | Free | Linear | L | Fusion of Human Relaxin 2 with Fc IgG using linker | Human Relaxin analogue | Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart | Blood samples were collected at various time points after drug administration | 6 mg/kg | 5.58 | Wistar rats plasma protease | ELISA | Wistar rats plasma | In Vivo | https://www.lens.org/lens/patent/078-521-931-782-236/fulltext | None | RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L | |||
| 31818212 | 2019 | RELAX10 | 309 | Free | Free | Linear | L | Fusion of Human Relaxin 2 with Fc IgG using linker | Human Relaxin analogue | Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart | Blood samples were collected at various time points after drug administration | 6 mg/kg | 7.06 | Wistar rats plasma protease | ELISA | Wistar rats plasma | In Vivo | https://www.lens.org/lens/patent/078-521-931-782-236/fulltext | None | RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L | |||
| 31818212 | 2019 | RELAX10 | 309 | Free | Free | Linear | L | Fusion of Human Relaxin 2 with Fc IgG using linker | Human Relaxin analogue | Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart | Blood samples were collected at various time points after drug administration | 1, 6, or 30 mg/kg | 4.59 - 7.06 | Wistar rats plasma protease | ELISA | Wistar rats plasma | In Vivo | https://www.lens.org/lens/patent/078-521-931-782-236/fulltext | None | RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L | |||
| 31805154 | 2019 | CP24 | 24 | Free | Free | Linear | L | None | Synthetic | Antiviral (HIV-1 Fusion Inhibitory Peptide) | Serial blood samples were collected from monkeys that received CP24 or IBP-CP24 before injection and at 2, 4, 6, 24, 72 and 144 h post-injection | 10 mg/kg | 1.69 | Rhesus monkeys plasma protease | Sandwich ELISA | Rhesus monkeys plasma | In Vivo | None | None | IC50(nM) = 0.8±0.2 for CP24 in virus subtype A (92UG029) | |||
| 31805154 | 2019 | IBP-CP24 | 37 | IBP conjugation to the N-terminus of CP24 | Free | Linear | L | None | Synthetic | Antiviral (HIV-1 Fusion Inhibitory Peptide) | Serial blood samples were collected from monkeys that received CP24 or IBP-CP24 before injection and at 2, 4, 6, 24, 72 and 144 h post-injection | 10 mg/kg | 46.11 | Rhesus monkeys plasma protease | Sandwich ELISA | Rhesus monkeys plasma | In Vivo | None | None | IC50(nM) = 0.7±0.3 for IBP-CP24 in virus subtype A (92UG029) | |||
| 31774631 | 2019 | BAY55-9837 | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | N.A. | 5 mg/kg | 0.31 | Kunming mice plasma protease | ELISA | Kunming mice plasma | In Vivo | https://sci-hub.se/10.2337/diabetes.51.5.1453 | None | N.A. | |||
| 31774631 | 2019 | BAY-exosome | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | N.A. | 5 mg/kg | 7.76 | Kunming mice plasma protease | ELISA | Kunming mice plasma | In Vivo | https://sci-hub.se/10.2337/diabetes.51.5.1453 | None | N.A. | |||
| 31774631 | 2019 | BAY-exosome-SPION | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | N.A. | 5 mg/kg | 8.39 | Kunming mice plasma protease | ELISA | Kunming mice plasma | In Vivo | https://sci-hub.se/10.2337/diabetes.51.5.1453 | None | N.A. | |||
| 31654685 | 2019 | Off-target repebody-fused GLP-1 | 50 | Repebody | GLP-1(7-36) (A8G) fused to the off-target repebody through linker (A(EAAAAK)3A) at C terminus | Linear | L | None | Synthetic | Antidiabetes | Mice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis | 25 nmol/kg | 1.3 (Initial Half Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB id: 5VAI | None | C57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases | |||
| 31654685 | 2019 | Repebody-fused GLP-1 in complex with HSA | 50 | Repebody | GLP-1(7-36) (A8G) fused to the repebody in complex with HSA through linker (A(EAAAAK)3A) at C terminus | Linear | L | None | Synthetic | Antidiabetes | Mice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis | 25 nmol/kg | 4.2 (Initial Half Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB id: 5VAI | None | C57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases | |||
| 31654685 | 2019 | Repebody-fused GLP-1 in complex with HSA | 50 | Repebody | GLP-1(7-36) (A8G) fused to the repebody in complex with HSA through linker (A(EAAAAK)3A) at C terminus | Linear | L | None | Synthetic | Antidiabetes | Mice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis | 25 nmol/kg | 10.7 (Terminal Half Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB id: 5VAI | None | C57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases | |||
| 31632382 | 2019 | Api137 | 18 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O: L-ornithine at position 2 | Apidaecin analog | Antimicrobial | N.A. | 20 mg/kg | < 30 | Mice plasma protease | RP-HPLC | Mice plasma | In Vivo | None | None | N.A. | |||
| 31615671 | 2019 | Free-ADI | 100 | Free | Free | Linear | L | None | Purified from the mycelia of A. nidulan | Anticancer | 20 days | 100 μl | 50.14 | Mice serum protease | HPLC | Mice serum | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 100 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Purified from the mycelia of A. nidulan | Anticancer | 20 days | 100 μl | 66.8 | Mice serum protease | HPLC | Mice serum | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31594790 | 2019 | RLYE | 4 | Free | Free | Linear | L | None | Synthetic | Antitumor | 4 hours at 37°C | 2 µg/µl | 73 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 = 89.1 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC) | |||
| 31594790 | 2019 | Ac-RLYE | 4 | Acetylation | Free | Linear | L | None | Synthetic | Antitumor | 4 hours at 37°C | 2 µg/µl | 8.8 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 = 37.1 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC) | |||
| 31594790 | 2019 | RLYE-NH2 | 4 | Free | Amidation | Linear | L | None | Synthetic | Antitumor | 4 hours at 37°C | 2 µg/µl | 1.3 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 = 326.6 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC) | |||
| 31594790 | 2019 | rLYE | 4 | L-Arg replaced with D-Arg at position 1 | Free | Linear | Mix | None | Synthetic | Antitumor | 4 hours at 37°C | 2 µg/µl | 7 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 >1,000 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC) | |||
| 31594790 | 2019 | Ac-RLYE-NH2 | 4 | Acetylation | Amidation | Linear | L | None | Synthetic | Antitumor | 4 hours at 37°C | 2 µg/µl | 9.4 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 = 52.5 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC) | |||
| 31580912 | 2019 | Exenatide | 39 | Free | Amidation | Linear | L | Fluorescence dye | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 1.6 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | PDB id: 7MLL | None | EC50(M) = 6.1 × 10−10 ± 9.3 × 10−11 | |||
| 31580912 | 2019 | Exenatide K12C | 39 | Free | Amidation | Linear | L | K12C modification, fluorescence dye | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 2.5 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 4.0 × 10−11 ± 1.4 × 10−12 for K12C-PEG 5KDa | |||
| 31580912 | 2019 | K12C-PEG 5kD | 39 | Free | Amidation | Linear | L | K12C modification, fluorescence dye, PEG(5KDa) conjugation at Lys27 | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 1.7 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 4.0 × 10−11 ± 1.4 × 10−12 | |||
| 31580912 | 2019 | K12C-PEG 40 kD | 39 | Free | Amidation | Linear / Branched | L | Fluorescence dye, PEG40 conjugation at Lys27 | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 5.5 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 1.0 × 10−10 ± 2.9 × 10−11 | |||
| 31580912 | 2019 | C40-PEG 40 kD | 40 | Free | Cys40 conjugation at C terminal, PEG(40 KDa) | Linear | L | Fluorescence dye | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 5.1 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 1.9 × 10−10 ± 7.1 × 10−11 | |||
| 31580912 | 2019 | K12C-PEG 10 kD-K12C | 39 | Free | Free | Linear | L | Lys27 conjugaged with (PEG(10KDa)-HGEGTFTSDLSCQMEEEAVRLFIEWLKNGGPSSGAPPPS) | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 2.1 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 4.4 × 10−11 ± 4.9 × 10−12 | |||
| 31443181 | 2019 | FcRn | 365 | Free | Free | Linear | L | None | Isolated from human gastric juice | Role in extending the serum half life of therapeutic antibodies | Blood collection at 0, 1.5, 3, 4.5, 6, 7.5, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36 hrs | N.A. | 10.6 | PBMC lysate protease (African American) | LC-MS/MS | PBMC lysate (African American) | In Vitro | Uniprot id: P55899 | None | N.A. | |||
| 31443181 | 2019 | FcRn | 365 | Free | Free | Linear | L | None | Isolated from human gastric juice | Role in extending the serum half life of therapeutic antibodies | Blood collection at 0, 1.5, 3, 4.5, 6, 7.5, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36 hrs | N.A. | 11.6 | PBMC lysate protease (African American) | LC-MS/MS | PBMC lysate (African American) | In Vitro | Uniprot id: P55899 | None | N.A. | |||
| 31413801 | 2019 | PrRP31 analog 18-S4 | 31 | Free | Amidation | Cyclic (C6-C13 Disulfide Bond) | L | C6 and C13 linked with S4 = Structure given in paper, residue 8 modification with Nle, residue 23 modifcation with hArg | Prolactin releasing peptide analogs | Antiobesity | Blood samples (70 μL) were collected from retro-orbital or saphenous vein at the following time points: 0.25, 0.5, 1, 3, 7, 24, 48 and 72 h | 5 mg/kg | 8.44 | CD-1 female mice plasma protease | LC-MS | CD-1 female mice plasma | In Vivo | None | None | EC50 = 7.8nM towards GPR10 receptor | |||
| 31389463 | 2019 | OXM | 37 | Free | Free | Linear | L | None | Secreted postprandially by intestine L-cells | Antidiabetes, Antiobesity | blood was sampled pre-dose and at 0.5, 1, 2, 4, 8, 24, 48, 72, and 96 h post-dose | 30 nmoL/kg | 2.1 ± 0.6 | SD rats plasma protease | LC-MS, ELISA | SD rats plasma | In Vivo | pdb id: 7LLY_5 | None | EC50(nM) = 0.691 for Human GLP-1R | |||
| 31389463 | 2019 | PP18 | 49 | Free | Free | Linear | L | Ser23 linked with X3 = Structure givven in paper | OXM analogs | Antidiabetes, Antiobesity | blood was sampled pre-dose and at 0.5, 1, 2, 4, 8, 24, 48, 72, and 96 h post-dose | 30 nmoL/kg | 38.5 ± 5.9 | SD rats plasma protease | LC-MS, ELISA | SD rats plasma | In Vivo | None | None | EC50(nM) = 0.487 for Human GLP-1R | |||
| 31368418 | 2019 | EX | 39 | Free | Free | Linear | L | O=Ornithine | GLP-1 analogs | Antidiabetes | Blood samples were collected before and after administration at 1, 3, and 6 h and 1–35 d | 2 mg/kg | 2.59 ± 0.05 | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The blood glucose levels of saline-treated controls remained at 20 mM, while EX or LA-EX rapidly decreased the levels of blood glucose to approximately 10 mM after administration, which were maintained for approximately 6 h | |||
| 31368418 | 2019 | LA-EX | 39 | EX acylation with LA (Lactic acid) | Free | Linear | L | O=Ornithine | GLP-1 analogs | Antidiabetes | Blood samples were collected before and after administration at 1, 3, and 6 h and 1–35 d | 2 mg/kg | 5.95 | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The blood glucose levels of saline-treated controls remained at 20 mM, while EX or LA-EX rapidly decreased the levels of blood glucose to approximately 10 mM after administration, which were maintained for approximately 6 h | |||
| 31341417 | 2019 | PSG4R | 25 | hIgG4 Fc conjugation through linker AEAAAKEAAAKEAAAKEAAAKA | Free | Cyclic (Two Disulfide Bonds Arranged As Cys2-Cys10 And Cys4-Cys8 In Ap25) | L | None | RGD-4C and endostatin fragment ES-2 fusion protein derived | Antitumor | 100 to 200 µL orbital blood samples were taken at 5 min before drug administration or 0 min, 5 min, 10 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 18 h, 24 h, 36 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, 216 h after drug administration | 5 mg/kg | 56.27 (Elimination Half Life) | Rats plasma protease | Indirect competitive ELISA | Rats plasma | In Vivo | None | None | IC50 = 1.82 ± 0.25 μmol/L for PSG4R on HUVEC proliferation | |||
| 31341417 | 2019 | AP25 | 25 | Free | Free | Cyclic (Two Disulfide Bonds Arranged As Cys2-Cys10 And Cys4-Cys8) | L | None | Synthetic | Antitumor | 100 to 200 µL orbital blood samples were taken at 5 min before drug administration or 0 min, 5 min, 10 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 18 h, 24 h, 36 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, 216 h after drug administration | 5 mg/kg | 50 (Elimination Half Life) | Rats plasma protease | ELISA | rats plasma | In Vivo | None | None | IC50 = 1.60 ± 0.15μmol/L for AP25 on HUVEC proliferation | |||
| 31480738 | 2019 | PEG2kC34 | 35 | 2 kDa PEG conjugated to the N-terminus of cC34 through Mal linker | Free | Linear | L | None | Synthetic | Antiviral (HIV-1 fusion inhibitory peptides) | Blood samples (300 μL) were harvested from the tail vein before injection and at different time intervals after injection (0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 10.0 and 24.0 h | 1.7 μmol/kg | 2.57 ± 0.71 | Rats plasma protease | N.A. | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC7343207/ | None | EC50 =4.14 ± 1.89 for NL4-3 strain | |||
| 31480738 | 2019 | PEG5kC34 | 35 | 5 kDa PEG conjugated to the N-terminus of cC34 through Mal linker | Free | Linear | L | None | Synthetic | Antiviral (HIV-1 fusion inhibitory peptides) | Blood samples (300 μL) were harvested from the tail vein before injection and at different time intervals after injection (0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 10.0 and 24.0 h | 1.7 μmol/kg | 5.11 ± 3.54 | Rats plasma protease | N.A. | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC7343207/ | None | EC50 =4.59 ± 1.83 for NL4-3 strain | |||
| 31453257 | 2019 | Pept. A | N.A. | Free | Free | Cyclic | L | N.A. | N.A. | Therapeutic agent against a CNS-related disorder | Blood (100 µl) and CSF (100 µl) aliquots for drug concentration assessment were collected pre-dose, on study day 1 at 0.5, 1.5, 3, 6, and 24 h post first dose, and on study day 2 at 1.5 h post the second dose (corresponding to 25.5 h from study start) | 4.2 mg/kg | 3.5 ± 0.7 (Terminal Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 31453257 | 2019 | Pept. A | N.A. | Free | Free | Cyclic | L | N.A. | N.A. | Therapeutic agent against a CNS-related disorder | Blood (100 µl) and CSF (100 µl) aliquots for drug concentration assessment were collected pre-dose, on study day 1 at 0.5, 1.5, 3, 6, and 24 h post first dose, and on study day 2 at 1.5 h post the second dose (corresponding to 25.5 h from study start) | 4.2 mg/kg | 14.3 ± 5.5 (Terminal Half Life) | göttingen Minipig Csf Lumbar Protease | LC-MS/MS | Göttingen minipigs CSF lumbar | In Vivo | None | None | N.A. | |||
| 31443263 | 2019 | LL-37 | 37 | Free | Free | Linear | L | None | Synthetic | Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions) | 37 °C | N.A. | 242.47 ± 45.09 | Rats plasma proteaes | HPLC | 10 μg/mL rats plasma | In Vitro | None | None | Among the peptides, LTP exhibited a lower cytotoxicity than LL-37 and TP5. In addition, LTP exhibited no significant cytotoxicity towards RAW264.7 cells, even at the highest concentration of 60 µg/mL | |||
| 31443263 | 2019 | TP5 | 5 | Free | Free | Linear | L | None | Arg32–Tyr36 fragment derived from thymopoietin | Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions) | 37 °C | N.A. | 1.32 ± 0.24 | Rats plasma proteaes | HPLC | 10 μg/mL rats plasma | In Vitro | None | None | Among the peptides, LTP exhibited a lower cytotoxicity than LL-37 and TP5. In addition, LTP exhibited no significant cytotoxicity towards RAW264.7 cells, even at the highest concentration of 60 µg/mL | |||
| 31443263 | 2019 | LTP | 29 | Free | TP5 conjugated with LTP(13-36) at C terminus | Linear | L | None | Synthetic | Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions) | 37 °C | N.A. | 240.03 ± 55.14 | Rats plasma proteaes | HPLC | 10 μg/mL rats plasma | In Vitro | None | None | Among the peptides, LTP exhibited a lower cytotoxicity than LL-37 and TP5. In addition, LTP exhibited no significant cytotoxicity towards RAW264.7 cells, even at the highest concentration of 60 µg/mL | |||
| 31310433 | 2019 | K9-C-peptide hydrogel | 624 | Free | Human C-peptide genetically conjugated at the C-terminus of nine repeats of lysine-containing elastin-like polypeptide | Linear | L | Cy3 conjugation | ELP analogues | Antidiabetes | 120 minutes | N.A. | 72.3% Degradation | Elastase-2 | Confocal microscopy | Reaction buffer + elastase-2 | In Vitro | None | None | EC50 values of the four enzymes (collagenase-2, elastase-2, pepsin, and trypsin) were 0.17, 0.23, 510.00, and 124.60 U m/L for K9-C peptide | |||
| 31310433 | 2019 | K9-C-peptide hydrogel | 624 | Free | Human C-peptide genetically conjugated at the C-terminus of nine repeats of lysine-containing elastin-like polypeptide | Linear | L | Cy3 conjugation | ELP analogues | Antidiabetes | N.A. | N.A. | <10% Degradation | N.A. | Confocal microscopy | Reaction buffer | In Vitro | None | None | EC50 values of the four enzymes (collagenase-2, elastase-2, pepsin, and trypsin) were 0.17, 0.23, 510.00, and 124.60 U m/L for K9-C peptide | |||
| 31310433 | 2019 | K9-C-peptide hydrogel | 624 | Free | Human C-peptide genetically conjugated at the C-terminus of nine repeats of lysine-containing elastin-like polypeptide | Linear | L | Cy3 conjugation | ELP analogues | Antidiabetes | Repeated 30-min elastase-2 treatments | N.A. | 48.6 ± 0.8% Degradation After First Treatment | Elastase-2 | Confocal microscopy | Reaction buffer + elastase-2 | In Vitro | None | None | EC50 values of the four enzymes (collagenase-2, elastase-2, pepsin, and trypsin) were 0.17, 0.23, 510.00, and 124.60 U m/L for K9-C peptide | |||
| 31310433 | 2019 | K9-C-peptide hydrogel | 624 | Free | Human C-peptide genetically conjugated at the C-terminus of nine repeats of lysine-containing elastin-like polypeptide | Linear | L | Cy3 conjugation | ELP analogues | Antidiabetes | N.A. | N.A. | 89.7 ± 0.2% Degradation After Fifth Elastase Treatment | Elastase-2 | Confocal microscopy | Reaction buffer + elastase-2 | In Vitro | None | None | EC50 values of the four enzymes (collagenase-2, elastase-2, pepsin, and trypsin) were 0.17, 0.23, 510.00, and 124.60 U m/L for K9-C peptide | |||
| 31310433 | 2019 | K9-C-peptide hydrogel | 624 | Free | Human C-peptide genetically conjugated at the C-terminus of nine repeats of lysine-containing elastin-like polypeptide | Linear | L | Cy3 conjugation | ELP analogues | Antidiabetes | N.A. | N.A. | 1.3 ± 0.6% Degradation After 1St Buffer Treatment | N.A. | Confocal microscopy | Reaction buffer | In Vitro | None | None | EC50 values of the four enzymes (collagenase-2, elastase-2, pepsin, and trypsin) were 0.17, 0.23, 510.00, and 124.60 U m/L for K9-C peptide | |||
| 31310433 | 2019 | K9-C-peptide hydrogel | 624 | Free | Human C-peptide genetically conjugated at the C-terminus of nine repeats of lysine-containing elastin-like polypeptide | Linear | L | Cy3 conjugation | ELP analogues | Antidiabetes | N.A. | N.A. | 27.9 ± 2.5% Degradation After 5Th Buffer Treatment | N.A. | Confocal microscopy | Reaction buffer | In Vitro | None | None | EC50 values of the four enzymes (collagenase-2, elastase-2, pepsin, and trypsin) were 0.17, 0.23, 510.00, and 124.60 U m/L for K9-C peptide | |||
| 31278957 | 2019 | Ex-(EBP)10-6xHis | 96 | Free | Ten repeats of EBP without a linker sequence, (EBP)10 fused at the C-terminus of the exenatide for Ex-(EBP)10, 6xHis tag | Linear | L | Inserting valine to the X amino acid position in the EBP (VPGXG) sequence, labeled with Flamma® 675 vinylsulfone | Fusion protein of exenatide and elastin-based polypeptide from recombinant Saccharomyces cerevisiae | Antidiabetes | The fluorescence images of the mice were measured at 0, 1, 2, 4, 8, 12, 24, 48, 72, 96, and 147 h after injection | 20 μg | 7.7 | Mouse body protease | In vivo imaging system | Mouse body | In Vivo | None | None | N.A. | |||
| 31278957 | 2019 | Exenatide | 39 | Free | Amidation | Linear | L | Labeled with Flamma® 675 vinylsulfone | Exendin-4 analogs | Antidiabetes | The fluorescence images of the mice were measured at 0, 1, 2, 4, 8, 12, 24, 48, 72, 96, and 147 h after injection | 20 μg | 2.2 | Mouse body protease | In vivo imaging system | Mouse body | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31277465 | 2019 | Dox-peptide conjugate 13 | 14 | DOX | Free | Cyclic (Lys6-Glu14 bond) | L | C6 fatty acid linked between | Synthetic | Anticancer | An aliquot (40 µL) was removed at different time intervals, such as 4, 24, and 84 h | 0.25 mM | 10 | N.A. | RP-HPLC | PBS having pH values ranging from 6.5 to 7.4 | In Vitro | None | None | Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25–35% as compared to Dox which reduced cell proliferation in the range of 20–34% for all selected four cell lines | |||
| 31277465 | 2019 | Dox-peptide conjugate 13 | 14 | DOX | Free | Cyclic (Lys6-Glu14 bond) | L | C6 fatty acid linked between | Synthetic | Anticancer | Several aliquots (55 µL) were removed at 2, 5, 10, 15, 30, 60, 90, and 120 min | 125 µM | 11.8 | Human serum protease | HPLC | 25% human serum | In Vitro | None | None | Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25–35% as compared to Dox which reduced cell proliferation in the range of 20–34% for all selected four cell lines | |||
| 31276085 | 2019 | RWRWR peptide | 12 | Acetylation | Amidation | Linear | Mix | R amino acid substituition at 1,4, 11, FAM denotes 5,6-carboxyfluorescein conjugated with Orn,p=D-Proline6,O=Ornithine8 | Synthetic | Cell penetrating peptide | 37°C | 2 mg/ml | 420 | HeLa lysates protease | RP-HPLC | HeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6) | In Vitro | None | None | N.A. | |||
| 31276085 | 2019 | S-RWRWR peptide | 12 | Acetylation | Amidation | Linear | Mix | R amino acid substituition at 1,4, 11, FAM denotes 5,6-carboxyfluorescein conjugated with Orn,p=D-Proline11,O=Ornithine7 | scrambled version of the RWRWR peptide | Cell penetrating peptide | 37°C | 2 mg/ml | 30 | HeLa lysates protease | RP-HPLC | HeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6) | In Vitro | None | None | N.A. | |||
| 31276085 | 2019 | III-67B | 12 | FAM denotes 5,6-carboxyfluorescein | Amidation | Linear | L | None | Synthetic | Cell penetrating peptide | 37°C | 2 mg/ml | 9.5 | HeLa lysates protease | RP-HPLC | HeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6) | In Vitro | None | None | N.A. | |||
| 31235532 | 2019 | CNP-39 | 39 | Proline substituition (amino acid 1) | Free | Cyclic (1 Disulfide Bond) | L | Glycine (amino acid 2) modifcation | CNP derivative | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | Samples from animals treated with the daily CNP-39 molecule were also obtained after the 1st and the 26th dose: at pre-dose, 0.08, 0.25, 0.5, 1, 2, and 4 hours postdose | 20 μg/kg per day for 26 weeks | 0.35 | Cynomolgus monkeys plasma protease | competitive radioimmunoassay | Cynomolgus monkeys plasma | In Vivo | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity) | |||
| 31235532 | 2019 | TransCon CNP (CNP-38) | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | 4xPEG10KDa modification at Lys26 through transient linker | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | Blood samples for CNP38 analysis were collected and analyzed following the 1st and the 26th dose at the following time points: 0 (prior to dosing), 6, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose | 40 μg/kg per week for 26 weeks | 92.6 | Cynomolgus monkeys plasma protease | HPLC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity) | |||
| 31235532 | 2019 | TransCon CNP (CNP-38) | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | 4xPEG10KDa modification at Lys26 through transient linker | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | Blood samples for CNP38 analysis were collected and analyzed following the 1st and the 26th dose at the following time points: 0 (prior to dosing), 6, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose | 100 μg/kg per week for 26 weeks | 86.7 | Cynomolgus monkeys plasma protease | HPLC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity) | |||
| 31235532 | 2019 | CNP-38 | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | None | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | 4 days | 100 μg/ml | 12.6 ± 3.9 | Recombinant human NEP protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = 100 (NPR-C Affinity) | |||
| 31235532 | 2019 | 5-kDa PEG-linker CNP-38 | 38 | PEG5KDa through permanent linker | Free | Cyclic (1 Disulfide Bond) | L | None | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | 4 days | 100 μg/ml | Stable | Recombinant human NEP protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = 199 ± 12 (NPR-C Affinity) | |||
| 31235532 | 2019 | 5-kDa PEG-linker CNP-38 | 38 | PEG5KDa through permanent linker | Free | Cyclic (1 Disulfide Bond) | L | None | CNP-38 analog | Treatment of Comorbidities associated with Fibroblast Growth Factor Receptor 3–Related Skeletal Dysplasias | 4 days | 100 μg/ml | 65.4 | Recombinant Human Nep Protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = 83 ± 7 (NPR-C Affinity) | |||
| 31235532 | 2019 | 4x 10-kDa PEG-linker CNP-38 | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | PEG40KDa modification at Lys26 through permanent linker | CNP-38 analog | Treatment of Comorbidities associated with Fibroblast Growth Factor Receptor 3–Related Skeletal Dysplasias | 4 days | 100 μg/ml | Stable | Recombinant Human Nep Protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate < 2 (NPR-C Affinity) | |||
| 31194563 | 2019 | Fasudil in CAR-liposome | 9 | Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys | Amidation | Linear | L | None | Synthetic | Treatment of Pulmonary Arterial Hypertension | N.A. | 3 mg/kg | 0.7 ± 0.3 | Sham rats plasma protease | LC–MS/MS | Sham rats plasma | In Vivo | None | None | N.A. | |||
| 31194563 | 2019 | Fasudil in CAR-liposome | 9 | Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys | Amidation | Linear | L | None | Synthetic | Treatment of Pulmonary Arterial Hypertension | N.A. | 3 mg/kg | 1.1 ± 0.3 | PAH rats plasma protease | LC–MS/MS | PAH rats plasma | In Vivo | None | None | N.A. | |||
| 31194563 | 2019 | Fasudil in CAR-liposome | 9 | Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys | Amidation | Linear | L | None | Synthetic | Treatment of Pulmonary Arterial Hypertension | N.A. | 3 mg/kg | 12.9 ± 4.6 | Sham rats plasma protease | LC–MS/MS | Sham rats plasma | In Vivo | None | None | N.A. | |||
| 31194563 | 2019 | Fasudil in CAR-liposome | 9 | Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys | Amidation | Linear | L | None | Synthetic | Treatment of Pulmonary Arterial Hypertension | N.A. | 3 mg/kg | 16.1 ± 4.1 | PAH rats plasma protease | LC–MS/MS | PAH rats plasma | In Vivo | None | None | N.A. | |||
| 31181805 | 2019 | TxID | 15 | Free | Amidation | Cyclic (C2-C8, C3-C15 Disulfide Linkage) | L | None | Cloned from Hainan native Conus textile | Treatment of Neuropathic Pain, Addiction And Small Cell Lung Cancer | At 37 °C for 0, 1, 3, 6, 12, 24, and 48 h, respectively | 0.25 mM | Less Stable | Human serum protease | RP-UPLC | Human serum | In Vitro | None | None | DSPE-PEG-TxID was still effective in inhibiting the α3β4 receptor, relative to TxID with slower reversible recovery. | |||
| 31181805 | 2019 | DSPE-PEG-TxID | 15 | DSPE-PEG | Amidation | Cyclic (C2-C8, C3-C15 Disulfide Linkage) | L | None | Derived from TXID | Treatment of Neuropathic Pain, Addiction And Small Cell Lung Cancer | At 37 °C for 0, 1, 3, 6, 12, 24, and 48 h, respectively | 0.25 mM | Stable | Human serum protease | RP-UPLC | Human serum | In Vitro | None | None | DSPE-PEG-TxID was still effective in inhibiting the α3β4 receptor, relative to TxID with slower reversible recovery. | |||
| 31181805 | 2019 | DSPE-PEG-TxID | 15 | DSPE-PEG | Amidation | Cyclic (C2-C8, C3-C15 Disulfide Linkage) | L | None | Derived from TXID | Treatment of Neuropathic Pain, Addiction And Small Cell Lung Cancer | Investigations were made at 0, 30, 60, 90, 120, and 180 min (SIF) incubations | N.A. | Stable | Simulated intestinal fluid serum protease | N.A. | Simulated intestinal fluid serum | In Vitro | None | None | DSPE-PEG-TxID was still effective in inhibiting the α3β4 receptor, relative to TxID with slower reversible recovery. | |||
| 31181805 | 2019 | TxID | 15 | Free | Amidation | Cyclic (C2-C8, C3-C15 Disulfide Linkage) | L | None | Cloned from Hainan native Conus textile | Treatment of Neuropathic Pain, Addiction And Small Cell Lung Cancer | Investigations were made at 0, 30, 60, 90, 120, and 180 min (SIF) incubations | N.A. | Less Stable | Simulated intestinal fluid serum protease | N.A. | Simulated intestinal fluid serum | In Vitro | None | None | DSPE-PEG-TxID was still effective in inhibiting the α3β4 receptor, relative to TxID with slower reversible recovery. | |||
| 31156041 | 2019 | AD-114-Im7-FH | 118 | Free | lm7-FH fusion | Linear | L | None | Fusion protein of AD-114 with lm7 and FH | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 3 mg/kg | 0.18 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 9.1 (Human CXCR4 affinity) | |||
| 31156041 | 2019 | AD-114-Im7-FH-SA21 | 118 | Free | lm7-FH-SA21 | Linear | L | None | Fusion protein of AD-114 with lm7 and FH, SA21 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 2 mg/kg | 0.95 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 9.2 (Human CXCR4 affinity) | |||
| 31156041 | 2019 | AD-114-Im7 PEG 30K | 118 | Free | lm7-PEG30K | Linear | L | None | Fusion protein of AD-114 with lm7 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 3 mg/kg | 11.85 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 0.7 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-Im7 PEG 2×20K | 118 | Free | lm7-PEG2*20K | Linear | L | None | Fusion protein of AD-114 with lm7 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 1.25 mg/kg | 19.24 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 0.7 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600-6H | 118 | Free | PA-600-6H | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 10 mg/kg | 7.77 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600-6H | 118 | Free | PA-600-6H | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected at 15, 30 min, 1, 2, 3, 4, 8, 12,18, 24, 36, 48 and 72 h post dosing | 10 mg/kg | 7.03 | Mouse plasma protease | ELISA | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600-6H | 118 | Free | PA-600-6H | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected at 15, 30 min, 1, 2, 3, 4, 8, 12,18, 24, 36, 48 and 72 h post dosing | 10 mg/kg | 10.25 | Mouse plasma protease | ELISA | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected immediately post dosing and at 5, 30 min, 2, 8, 24, 72 h post dosing | 3.5 mg/kg | 9.5 | Rats plasma protease | LC–MS/MS | Rats plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600-6H | 118 | Free | PA-600-6H | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected immediately following dosing and at 5, 15, and 30 min and 1, 2, 4, 8, 12, 24, 36, 48, 60, 72, 84, 96, 120, 144, 168, and 192-h post-dosing | 2 mg/kg | 24.27 ± 0.24 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected pre-dosing and at the following time points post each dosing: 30 min, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, and 144 h | 3 mg/kg | 25.41 ± 5.17 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected pre-dosing and at the following time points post-dosing: 5 min, 1, 4, 12, 24, 48, 96, 168 h. | 3 mg/kg | 10.2 ± 3.9 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma dosed at Day 1 | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected pre-dosing and at the following time points post-dosing: 5 min, 1, 4, 12, 24, 48, 96, 168 h. | 0.1 mg/kg | 23.53 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma dosed at Day 1 | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected pre-dosing and at the following time points post-dosing: 5 min, 1, 4, 12, 24, 48, 96, 168 h. | 3 mg/kg | 8.31 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma dosed at Day 8 | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected pre-dosing and at the following time points post-dosing: 5 min, 1, 4, 12, 24, 48, 96, 168 h. | 10 mg/kg | 6.7 ± 1.1 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma dosed at Day 8 | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31100806 | 2019 | Lysostaphin | 255 | Free | Free | Linear | L | None | Produced by Staphylococcus simulans | Antibacterial | The blood was sampled from the tail vein at 25 min, 40 min, 1 h, 2 h, and 4 h time points in the group that received lysostaphin | 1 mg/ml | 1.5 ± 0.7 | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | PDB id: 4LXC | None | Minimum inhibitory concentration (MIC) of Lst-HDD towards S. aureus ATCC 29,213 was 3.2 µg/mL and concentration is 0.1 µg/mL | |||
| 31100806 | 2019 | Lst-HDD | 320 | Free | Free | Linear | L | None | Derived from Lysostaphin | Antibacterial | 25 min, 40 min, 1 h, 2 h, 4 h, and 6 h time points in the group that received Lst-HDD | 1 mg/ml | 3.1 ± 0.6 | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | None | None | MIC of Lst-HDD is 32 times higher than the MIC of lysostaphin in S. aureus ATCC 29,213 in —0.1 µg/mL | |||
| 31100806 | 2019 | lysostaphin | 255 | Free | Free | Linear | L | None | Produced by Staphylococcus simulans | Anti-Staphylococcal lysin | Blood was collected by orbital bleeding at 1, 4, 7, and 24 h postadministration | 40 mg/kg | <1 | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | Unconjugated lysostaphin shows a standard antibody binding response from 0.3 to 20 ng/ml. | |||
| 31100806 | 2019 | Cpl-1 | 568 | Free | Free | Linear | L | None | Lytic enzyme of a pneumococcal bacteriophage | Antimicrobial for Pneumococcal Bacteremia | Blood was collected after 5, 10, and15 min from three animals and after 30, 60, and 120 min from the other three animals | 1.6 mg | 20.5 | Mice plasma protease | Western blotting and spot densitometry | Mice serum | In Vivo | None | None | MICs of Cpl-1 = 32 μg/ml | |||
| 31100806 | 2019 | LytA | 318 | Free | Free | Linear | L | None | Derived from Streptococcus pneumoniae | Therapeutic agent in experimental peritonitis sepsis caused by highly Β-lactam resistant Streptococcus Pneumoniae | Blood samples were obtained from three animals per group, which were killed at 5, 15, 60, and 120 min | 3.1 mg/ml | 22.5 | Adult swiss mice plasma protease | N.A. | Adult swiss mice plasma | In Vivo | None | None | MICs of LytA = 16 μg/ml | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous | 10 µg/kg | 5.4 ± 0.3 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 10 µg/kg | 5.8 ± 0.4 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 30 µg/kg | 5.4 ± 0.3 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 100 µg/kg | 5.2 ± 0.2 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous | 17.4 µ/kg | 9.0 ± 1.8 (Elimination Half Life) | Cynomolgus monkeys plasma protease | LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 17.4 µ/kg | 11.4 ± 1.0 (Elimination Half Life) | Cynomolgus monkeys plasma protease | LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous | 17.4 µ/kg | 12.9 ± 1.0 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 17.4 µ/kg | 15.4 ± 0.3 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 31079216 | 2019 | NT | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Isolated from bovine hypothalamus | Dual function as a neurotransmitter/neuromodulator in the Central Nervous System (CNS) and as a hormone/cellular mediator in peripheral tissues, such as the gastrointestinal tract and adipose tissue | 24 h incubation at 37 °C | 160 μM | Lower Stability | Human plasma protease | UHPLC | Human plasma | In Vitro | PDB id: 2LNE | None | −LogIC50±SE = 9.54±0.42 in Neurotensin (1–13) for NTS1 receptor | |||
| 31079216 | 2019 | NT-5 | 4 | AOPC8 = 1‑(2‑(2‑aminophenyl)‑2‑oxoethyl)‑1H‑pyrrole‑2‑ carboxylic acid (AOPC) | Free | Linear | Mix | Lys9, d-Tyr(Et)11 modification in NT(8–13) | NT analogue | Dual function as a neurotransmitter/neuromodulator in the Central Nervous System (CNS) and as a hormone/cellular mediator in peripheral tissues, such as the gastrointestinal tract and adipose tissue | 24 h incubation at 37 °C | 160 μM | Higher stability than NT | Human plasma protease | UHPLC | Human plasma | In Vitro | None | None | −LogIC50±SE = 5.63±0.15 in Neurotensin (1–13) for NTS1 receptor | |||
| 31079216 | 2019 | NT-6 | 5 | AOPC8 = 1‑(2‑(2‑aminophenyl)‑2‑oxoethyl)‑1H‑pyrrole‑2‑ carboxylic acid (AOPC), d-Arg9 modification at N terminal | Free | Linear | Mix | d-Tyr(Et)11 modification in NT(8–13) | NT analogue | Dual function as a neurotransmitter/neuromodulator in the Central Nervous System (CNS) and as a hormone/cellular mediator in peripheral tissues, such as the gastrointestinal tract and adipose tissue | 24 h incubation at 37 °C | 160 μM | Higher stability than NT | Human plasma protease | UHPLC | Human plasma | In Vitro | None | None | −LogIC50±SE = 5.53±0.31 in Neurotensin (1–13) for NTS1 receptor | |||
| 31079216 | 2019 | NT-8 | 6 | AOPC8 = 1‑(2‑(2‑aminophenyl)‑2‑oxoethyl)‑1H‑pyrrole‑2‑ carboxylic acid (AOPC) | Free | Linear | Mix | Lys8, d-Arg9, d-Tyr(Et)11] modification in NT(7–13) | NT analogue | Dual function as a neurotransmitter/neuromodulator in the Central Nervous System (CNS) and as a hormone/cellular mediator in peripheral tissues, such as the gastrointestinal tract and adipose tissue | 24 h incubation at 37 °C | 160 μM | Higher stability than NT | Human plasma protease | UHPLC | Human plasma | In Vitro | None | None | −LogIC50±SE = 5.28±0.20 in Neurotensin (1–13) for NTS1 receptor | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 3 mg | 0.242 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 9 mg | 0.326 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 18 mg | 0.392 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 24 mg | 0.521 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 30 mg | 0.485 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31064153 | 2019 | Triazolopeptides compounds 3 | 4 | Free | Free | Linear | L | Lys1 linked with Har = Homo-Arginine, GlyΨ[Trl] is a glycyl-1,2,3-triazole unit mimicking glycine (triazole ring substitution instead of peptide bond) | Derived from triazolopeptide | Inhibits the interaction between Neuropilin-1 and Vascular Endothelial Growth Factor-165 | 37 °C | 1.1 µmol/mL | >> 48 | Human plasma protease | HPLC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 8.39 μM | |||
| 31064153 | 2019 | Triazolopeptides compounds 4 | 4 | D-Lys at the first position which contains Har = Homo-Arginine side chain | Free | Linear | Mix | GlyΨ[Trl] is a glycyl-1,2,3-triazole unit mimicking glycine (triazole ring substitution instead of peptide bond) | Derived from triazolopeptide | Inhibits the interaction between Neuropilin-1 and Vascular Endothelial Growth Factor-165 | 37 °C | 1.1 µmol/mL | >> 48 | Human plasma protease | HPLC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 10.22 μM | |||
| 31064153 | 2019 | Lys(Har)-Dab | 2 | Lys at the first position contains Har = Homo-Arginine side chain | Dab (2,4-diaminobutyric acid) | Linear | L | None | KPPR analogs | Peptidic inhibitor of the VEGF165/NRP-1 interaction | All samples were incubated at 37 °C and 100 µL of aliquots were withdrawn at different time intervals (for 4 and 5: 0, 10, 20, 30, 40, 50, 60, 70, 80 min, 1.5h, 2h, 2.5h, 3h, 4h, 6h | 1.1 µmol/mL | 34 | Human plasma protease | HPLC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 0.2 μM | |||
| 31064153 | 2019 | Peptidotriazoles | 3 | Dap (2,3-diaminopropionic acid) substiuition at 1st position | Free | Linear | L | None | KPPR analogs | Peptidic inhibitor of the VEGF165/NRP-1 interaction | All samples were incubated at 37 °C and 100 µL of aliquots were withdrawn at different time intervals (for 4 and 5: 0, 10, 20, 30, 40, 50, 60, 70, 80 min, 1.5h, 2h, 2.5h, 3h, 4h, 6h | 1.1 µmol/mL | 41 | Human plasma protease | HPLC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 0.2 μM | |||
| 31064153 | 2019 | Lys(Har)-PA | 3 | Side chain of the Lys residue in the first position was extended by attaching additional homoarginine (Har) | Free | Linear | L | None | KPPR analogs | Peptidic inhibitor of the VEGF165/NRP-1 interaction | 100 µL of aliquots were withdrawn at different time intervals (for 8 and 10: 0 min, 2h, 4h, 6h, 10h, 12h, 24h, 48h, 72h, 96h) | 1.1 µmol/mL | 39 | Human plasma protease | HPLC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 0.2μM | |||
| 31064153 | 2019 | Dab-R | 2 | Dab (2,4-diaminobutyric acid) substiuition at 1st position | Free | Linear | L | None | KPPR analogs | Peptidic inhibitor of the VEGF165/NRP-1 interaction | 100 µL of aliquots were withdrawn at different time intervals (for 8 and 10: 0 min, 2h, 4h, 6h, 10h, 12h, 24h, 48h, 72h, 96h) | 1.1 µmol/mL | 44 | Human plasma protease | HPLC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 0.3 μM | |||
| 31040673 | 2019 | ES2-AF | 21 | Free | VEGFR1-selective hexapeptide (GNQWFI, AF) ,amidation | Linear | L | FITC labeled | Synthetic | Antiangiogenic | Blood samples were collected through the fundus venous plexus, 0.5–24 hours after administration | 20 mg/kg | 2.34 ± 0.43 | Mice plasma protease | Fluorescence spectrometry | Mice plasma | In Vivo | None | None | The inhibitory rates of ES2-AF and CS-ES2-AF were similar (5 μg/mL–100 μg/mL), which indicated that the activity of ES2-AF was similar to CS-ES2-AF at relatively low concentrations | |||
| 31040673 | 2019 | CS-ES2-AF | 21 | CS (chondroitin sulfate) | VEGFR1-selective hexapeptide (GNQWFI, AF) ,amidation | Linear | L | FITC labeled | Synthetic | Antiangiogenic | Blood samples were collected through the fundus venous plexus, 0.5–24 hours after administration | 20 mg/kg | 7.57 ± 2.65 | Mice plasma protease | Fluorescence spectrometry | Mice plasma | In Vivo | None | None | The inhibitory rates of ES2-AF and CS-ES2-AF were similar (5 μg/mL–100 μg/mL), which indicated that the activity of ES2-AF was similar to CS-ES2-AF at relatively low concentrations | |||
| 31038930 | 2019 | Exenatide | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration | 25 nmol/kg | 0.9 | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 7MLL | None | Exenatide presented similar GLP-1 activities with EC50 values of 1.1 | |||
| 31038930 | 2019 | Exenatide-Fc | 261 | Free | Conjugation between Ex-Mal-DBCO and N3−Lys-Fc | Linear | L | None | Derived from the Lys-Fc directly expressed by Expi293F | Antidiabetes | Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration | 3.13 nmo/kg | 43.8 | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 7MLL | None | Exenatide-Fc presented similar GLP-1 activities with EC50 values of 1.5 nM | |||
| 31038930 | 2019 | Exenatide-Fc | 261 | Free | Conjugation between Ex-Mal-DBCO and N3−Lys-Fc | Linear | L | None | Derived from the Lys-Fc directly expressed by Expi293F | Antidiabetes | Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration | 12.5 nmol/kg | 40.4 | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 7MLL | None | Exenatide-Fc presented similar GLP-1 activities with EC50 values of 1.5 nM | |||
| 31038930 | 2019 | Exenatide-Fc | 261 | Free | Conjugation between Ex-Mal-DBCO and N3−Lys-Fc | Linear | L | None | Derived from the Lys-Fc directly expressed by Expi293F | Antidiabetes | Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration | 25 nmol/kg | 87.8 | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 7MLL | None | Exenatide-Fc presented similar GLP-1 activities with EC50 values of 1.5 nM | |||
| 30986342 | 2019 | T4-Cy5.5 | 7 | Free | Conjugated with Cy5.5 | Linear | L | None | Synthetic | Antitumor | N.A. | N.A. | 1 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Free T4 or P-T4 slowed tumor regrowth after chemotherapy, whereas the P-T4 treatment group exhibited a better suppressive effect | |||
| 30986342 | 2019 | P-T4-Cy5.5 | 11 | PEGylation | Conjugated with Cy5.5 | Linear | L | Diethylaminopropyl isothiocyanate (DEAP) conjugation at Lys1 side chain | Synthetic | Antitumor | N.A. | N.A. | 2 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Free T4 or P-T4 slowed tumor regrowth after chemotherapy, whereas the P-T4 treatment group exhibited a better suppressive effect | |||
| 30973007 | 2019 | GBAP | 11 | Free | Free | Cyclic (Ser3-Met11 bond) | L | None | Produced by Enterococcus faecalis | Antibacterial | Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, and 24 hr | 0.28 mM | 4 | N.A. | HPLC | pH 7.2 buffer | In Vitro | None | None | EC50 (nM) = 1.15 for GBAP | |||
| 30973007 | 2019 | GBAP 12 | 11 | Free | Free | Linear | L | None | GBAP analogs | Antibacterial | Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, and 24 hr | 0.28 mM | >20 | N.A. | HPLC | pH 7.2 buffer | In Vitro | None | None | EC50 (nM) = 1.15 for GBAP | |||
| 30973007 | 2019 | GBAP 11 | 14 | Free | Free | Cyclic (Ser3-Met11 bond) | L | N-methylation at Phe7 | GBAP analogs | Antibacterial | Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, and 24 hr | 0.28 mM | Highly Stable | Chymotrypsin | HPLC | PBS buffer + chymotrypsin | In Vitro | None | None | EC50(nM) = 6.3 for GBAP-[N-MeF7] | |||
| 30973007 | 2019 | GBAP | 11 | Free | Free | Cyclic (Ser3-Met11 bond) | L | None | Produced by Enterococcus faecalis | Antibacterial | Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8hr, and 24 hr | 0.28 mM | <30 | Human plasma protease | HPLC | Human plasma | In Vitro | None | None | EC50 (nM) = 1.15 for GBAP | |||
| 30973007 | 2019 | GBAP 11 | 14 | Free | Free | Cyclic (Ser3-Met11 bond) | L | N-methylation at Phe7 | GBAP analogs | Antibacterial | Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8hr, and 24 hr | 0.28 mM | <30 | Human plasma protease | HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 6.3 for GBAP-[N-MeF7] | |||
| 30938069 | 2019 | ESA-CJC-1295 | 30 | Free | (DAC) maleimidopropionic acid conjugated with Equine serum albumin | Cyclic | Mix | None | Synthetic | Stimulates The Production Of Growth Hormone (Gh) From The Pituitary Gland | One mL aliquots were removed for analysis at 0, 24, 48, 72 and 96 hours at 4°C | 700 pg/mL | 20 | Equine plasma protease | Mass spectrometry | Equine plasma | In Vivo | None | None | N.A. | |||
| 35520704 | 2019 | Liraglutide | 32 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At each predetermined times (1, 2, 3, 4, 6, 12, 24 and 36 h), there mice were sacrificed and ∼200 μL of blood samples were collected | 50 nmol/kg | 3.9 ± 0.3 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | None | None | EC50 = 0.72 ± 0.27 nM | |||
| 35520704 | 2019 | Di-GLP-1 | 62 | Free | Bis-maleimide-NH2 | Linear | L | None | GLP-1 analogs | Antidiabetes | At each predetermined times (1, 2, 3, 4, 6, 12, 24 and 36 h), there mice were sacrificed and ∼200 μL of blood samples were collected | 50 nmol/kg | 1.8 ± 0.2 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | PDB id: 5VAI | None | EC50 = 0.039 ± 0.007 nM | |||
| 35520704 | 2019 | Lip-Di-GLP-1 | 62 | Free | Bis-maleimide-C16 conjugation at C terminal | Linear | L | None | GLP-1 analogs | Antidiabetes | At each predetermined times (1, 2, 3, 4, 6, 12, 24 and 36 h), there mice were sacrificed and ∼200 μL of blood samples were collected | 50 nmol/kg | 7.0 ± 0.7 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | PDB id: 5VAI | None | EC50 = 0.056 ± 0.018 nM | |||
| 30904618 | 2019 | PAK | 253 | KLA linked with PsTag216 using flexible linker GGGGS at N terminal | Free | Linear | L | None | Fusion protein of PsTag216 and KLA | Antitumor | At 0.25 h, 0.5 h, 1 h, 2 h, 4 h, 8 h, 24 h, and 48 h post injection, a blood sample was obtained from the eye socket vein in mice | 1 μmol/kg | 5.05 ± 0.26 | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | IC50 (μM) = 11.05 ± 0.73 for the cell line A375 (In vitro antitumor effects) | |||
| 30901967 | 2019 | YIK-C16 | 37 | Free | palmitic acid (C16) was conjugated to the C-terminus of YIK (at Lys37) with a linker GSG between C16 and YIK | Linear | L | T639I mutation | HP23-E6-IDL analogue | Antiviral (Anti-Hiv Activity) | Mouse serum samples were collected before (0 h) and after injection 1, 3, 7, 11, 13, 15, 17, and 19 h for lipopeptide YIK-C16 | 5 mg/kg | 5.9 ± 3.2 | Mice serum protease | N.A. | Mice serum | In Vivo | None | None | IC50(pM) = 69 ± 8 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of YIK-C16 against infection by HIV-1 mutants resistant to T20) | |||
| 30901967 | 2019 | YIK | 34 | Free | Free | Linear | L | T639I mutation | HP23-E6-IDL analogue | Antiviral (Anti-Hiv Activity) | Mouse serum samples were collected before (0 h) and after injection (0.5, 1, 2, 4, and 6 h for peptides YIK | 5 mg/kg | 1.3 | Mice serum protease | N.A. | Mice serum | In Vivo | None | None | IC50(pM) = 784 ± 32 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of YIK against infection by HIV-1 mutants resistant to T20) | |||
| 30901967 | 2019 | HP23-E6-IDL | 32 | Free | Free | Linear | L | None | Synthetic | Antiviral (Anti-Hiv Activity) | Mouse serum samples were collected before (0 h) and after injection (0.5, 1, 2, 4, and 6 h for peptides HP23-E6-IDL | 5 mg/kg | 1 | Mice serum protease | N.A. | Mice serum | In Vivo | None | None | IC50(pM) = 912 ± 29 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of HP23-E6-IDL against infection by HIV-1 mutants resistant to T20) | |||
| 30900390 | 2019 | Ac-SDKP | 4 | Acetylation | Free | Linear | L | None | Synthetic | Antifibrotic effects on Hepatic Fibrosis | At 2, 4, 6, 8, 10, 18, 30, 120, 360, 480, and 540 min after the injection, 50 μL of blood was sampled from each animal through the caudal vein | 1 mg/kg | 9.65 ± 1.78 | Rats serum protease | RP-HPLC | Rats serum | In Vivo | None | None | Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro | |||
| 30900390 | 2019 | Ac-SD(d)K(d)P | 4 | Acetylation | Free | Linear | Mix | Asp2 and Lys3 were replaced with their D-isomers | Synthetic | Antifibrotic effects on Hepatic Fibrosis | At 2, 4, 6, 8, 10, 18, 30, 120, 360, 480, and 540 min after the injection, 50 μL of blood was sampled from each animal through the caudal vein | 1 mg/kg | 176.5 ± 6.45 | Rats serum protease | RP-HPLC | Rats serum | In Vivo | None | None | Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro | |||
| 30900390 | 2019 | Ac-SDKP | 4 | Acetylation | Free | Linear | L | None | synthetic | Antifibrotic Effects On Hepatic Fibrosis | 9 h at 37 C | 100 μM | 6.47 ± 1.53 | Human Serum Protease | HPLC | human serum | In Vitro | None | None | Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro | |||
| 30900390 | 2019 | Ac-SD(d)K(d)P | 4 | Acetylation | Free | Linear | Mix | Asp2 and Lys3 were replaced with their D-isomers | synthetic | Antifibrotic Effects On Hepatic Fibrosis | 9 h at 37 C | 100 μM | 161.5 ± 5.79 | Human Serum Protease | HPLC | human serum | In Vitro | None | None | Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro | |||
| 30853651 | 2019 | DiR dye-loaded PAS40 nanoghosts | 120 | Free | Free | Linear | L | None | Synthetic | Increases the circulation time of a cell membrane based nanotherapeutic | Measuring the residual fluorescence intensity of the dye in serum at 0, 8, 24 and 48 h | 50 mg/kg | 37 | Mouse serum protease | Fluorescence assay | Mouse serum | In Vivo | None | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 1, 2, 5, 15, 30, 60, 90, and 120 minutes | 200 pmol/kg | 4.3 ± 1.2 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 5, 15, 30, 60, 90 and 120 minutes after intraperitoneal injection | 200 pmol/kg | 92 ± 21 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 1, 2, 5, 15, 30, 60, 90, and 120 minutes | 2000 pmol/kg | 6.9 ± 2.5 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 5, 15, 30, 60, 90 and 120 minutes after intraperitoneal injection | 2000 pmol/kg | 53 ± 14 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30814652 | 2019 | Adnectin C | 20 | Free | Free | Linear | L | None | Derived from the tenth domain of fibronectin type III (10thFn3) | Anticancer | Blood samples were taken after 5 min, 15 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 36 h, 48 h, 72 h, and 96 h | 5 mg/kg | 49.41 | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | Kd(1/s) = 5.643E − 5 | |||
| 30814652 | 2019 | Adnectin C-PAS#1(200) | 20 | Free | PAS#1(200) | Linear | L | None | Adnectin C analogs | Anticancer | Blood samples were taken after 5 min, 15 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 36 h, 48 h, 72 h, and 96 h | 5 mg/kg | 226.2 | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | Kd(1/s) =2.476E − 5 | |||
| 30809901 | 2019 | FITC-AAR029b | 6 | FITC labelled | Free | Macrocyclic | L | X=Structure given in paper | Derived from a class of peptides known as cyclic peptide triazoles (cPTs) | Antiviral | N.A. | 0.01 mg/kg | 2.92 ± 0.93 (T1/2b-Elimination Half Life) | Rats plasma protease | Fluorescence assay | Rats plasma | In Vivo | None | None | EC50(nM) = 210±16 for AAR029b in Bal.01 virus | |||
| 30809901 | 2019 | FITC-AAR029b in Liposome | 6 | FITC labelled | Free | Macrocyclic | L | X=Structure given in paper | Derived from a class of peptides known as cyclic peptide triazoles (cPTs) | Antiviral | N.A. | 0.01 mg/kg | 8.87 ± 3.17(T1/2b-Elimination Half Life) | Rats plasma protease | Fluorescence assay | Rats plasma | In Vivo | None | None | EC50(nM) = 210±16 for AAR029b in Bal.01 virus | |||
| 30794654 | 2019 | CNP(1–22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | CNP C terminal cleavage | Improved endochondral ossification and accelerated bone growth in mice | N.A. | 20 nmol/kg | 1.42 ± 0.45 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30794654 | 2019 | ASB20123 | 39 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | C-type natriuretic peptide derivative | Treatment of Growth failure and Dwarfism | N.A. | 20 nmol/kg | 31.3 ± 4.8 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30794654 | 2019 | CNP(1–22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | CNP C terminal cleavage | Improved Endochondral Ossification And Accelerated Bone Growth In Mice | N.A. | 50 nmol/kg | 10.0 ± 5.0 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30794654 | 2019 | ASB20123 | 39 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | C-type natriuretic peptide derivative | Treatment Of Growth Failure And Dwarfism | N.A. | 50 nmol/kg | 32.1 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30756483 | 2019 | ABD–Dox | 47 | Free | Dox conjugation | Linear | L | None | Derived from streptococcal protein G | Anticancer | Blood samples were collected at 40 s, 15 and 30 min, and 2, 4, 8, 24, 48, 72, and 96 h post injection | 5 mg/kg | 29.4 ± 0.8 (Elimination Half Life) | Mice plasma protease | Flurorescence assay | Mice plasma | In Vivo | None | None | (IC50) of ABD–Dox was 6.4 × 10−6 for C26 cell | |||
| 30742145 | 2019 | n(BMP-2) | 116 | Free | Free | Linear | L | None | Synthetic | Promotes Bone repair | N.A. | 0.5 mg/kg | 48 | N.A. | Fluorescence spectrometry | Rats | In Vivo | PDB id: 1ES7 | None | n(BMP-2) did not enhance ALP expression in MSCs compared with native BMP-2 unless pretreated with IV collagenase, which significantly enhanced ALP expression and calcium deposition | |||
| 30742145 | 2019 | Native BMP-2 | 116 | Free | Free | Linear | L | None | Synthetic | Promotes Bone repair | N.A. | 0.5 mg/kg | <30 | N.A. | Fluorescence spectrometry | Rats | In Vivo | PDB id: 1ES7 | None | n(BMP-2) did not enhance ALP expression in MSCs compared with native BMP-2 unless pretreated with IV collagenase, which significantly enhanced ALP expression and calcium deposition | |||
| 30709867 | 2019 | PNA5 | 7 | Free | Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus | Linear | L | None | Ang-(1-7) analogs | Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction | N.A. | 100 µM | 1.0 ± 0.2 | Rats serum protease | Tandem mass spectrometry (MS) | Rats serum | In Vitro | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease Brain ROS production and Inflammation in Preclinical models of HF | N.A. | 100 µM | 0.25 ± 0.05 | Rats serum protease | Tandem mass spectrometry (MS) | Rats serum | In Vitro | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | PNA5 | 7 | Free | Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus | Linear | L | None | Ang-(1-7) analogs | Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction | N.A. | 10 mg/kg | 18.2 ± 3 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease Brain ROS production and Inflammation in Preclinical models of HF | N.A. | 10 mg/kg | 20.9 ± 0.7 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | PNA5 | 7 | Free | Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus | Linear | L | None | Ang-(1-7) analogs | Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction | N.A. | 10 mg/kg | 26.6 ± 3.6 | CSF protease | LC-MS | CSF | In Vivo | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease Brain ROS production and Inflammation in Preclinical models of HF | N.A. | 10 mg/kg | 24.7 ± 5 | CSF protease | LC-MS | CSF | In Vivo | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30690406 | 2019 | Apelin1 | 17 | Free | Free | Linear | L | None | Native apelin 17 | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.4 | RHNEP | LC-MS | Apelin1 | In Vitro | None | None | EC50(nM) = 1.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin2 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=H | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 1 | RHNEP | LC-MS | Apelin2 | In Vitro | None | None | EC50(nM) = 4.1 ± 1.0 | |||
| 30690406 | 2019 | Apelin3 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=Me, Methylation at Glu8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | >30 | RHNEP | LC-MS | Apelin3 | In Vitro | None | None | EC50(nM) = 4.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin4 | 17 | Free | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | RHNEP | LC-MS | Apelin4 | In Vitro | None | None | EC50(nM) = 568 ± 34 | |||
| 30690406 | 2019 | Apelin5 | 17 | Free | Free | Linear | L | R2=Me, Methylation at Gln5 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | RHNEP | LC-MS | Apelin5 | In Vitro | None | None | EC50(nM) = 176 ± 21 | |||
| 30690406 | 2019 | Apelin6 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 1.5 | RHNEP | LC-MS | Apelin6 | In Vitro | None | None | EC50(nM) = 2.6 ± 0.8 | |||
| 30690406 | 2019 | Apelin7 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | >30 | RHNEP | LC-MS | Apelin7 | In Vitro | None | None | EC50(nM) = 6.3 ± 1.0 | |||
| 30690406 | 2019 | Apelin8 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | >30 | RHNEP | LC-MS | Apelin8 | In Vitro | None | None | EC50(nM) = 11.3 ± 2.1 | |||
| 30690406 | 2019 | Apelin9 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | >30 | RHNEP | LC-MS | Apelin9 | In Vitro | None | None | EC50(nM) = 2.5 ± 1.5 | |||
| 30690406 | 2019 | Apelin1 | 17 | Free | Free | Linear | L | None | Native apelin 17 | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.4 | RhKLKB1 | LC-MS | Apelin1 | In Vitro | None | None | EC50(nM) = 1.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin2 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=H | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.7 | RhKLKB1 | LC-MS | Apelin2 | In Vitro | None | None | EC50(nM) = 4.1 ± 1.0 | |||
| 30690406 | 2019 | Apelin3 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=Me, Methylation at Glu8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.9 | RhKLKB1 | LC-MS | Apelin3 | In Vitro | None | None | EC50(nM) = 4.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin4 | 17 | Free | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | RhKLKB1 | LC-MS | Apelin4 | In Vitro | None | None | EC50(nM) = 568 ± 34 | |||
| 30690406 | 2019 | Apelin5 | 17 | Free | Free | Linear | L | R2=Me, Methylation at Glu5 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | RhKLKB1 | LC-MS | Apelin5 | In Vitro | None | None | EC50(nM) = 176 ± 21 | |||
| 30690406 | 2019 | Apelin6 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 1 | RhKLKB1 | LC-MS | Apelin6 | In Vitro | None | None | EC50(nM) = 2.6 ± 0.8 | |||
| 30690406 | 2019 | Apelin7 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 1.4 | RhKLKB1 | LC-MS | Apelin7 | In Vitro | None | None | EC50(nM) = 6.3 ± 1.0 | |||
| 30690406 | 2019 | Apelin8 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 2.1 | RhKLKB1 | LC-MS | Apelin8 | In Vitro | None | None | EC50(nM) = 11.3 ± 2.1 | |||
| 30690406 | 2019 | Apelin9 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 2.9 | RhKLKB1 | LC-MS | Apelin9 | In Vitro | None | None | EC50(nM) = 2.5 ± 1.5 | |||
| 30690406 | 2019 | Apelin1 | 17 | Free | Free | Linear | L | None | Native apelin 17 | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.02 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 1.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin2 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=H | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.3 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 4.1 ± 1.0 | |||
| 30690406 | 2019 | Apelin3 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=Me, Methylation at Glu8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 1.2 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 4.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin4 | 17 | Free | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 568 ± 34 | |||
| 30690406 | 2019 | Apelin5 | 17 | Free | Free | Linear | L | R2=Me, Methylation at Glu5 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 176 ± 21 | |||
| 30690406 | 2019 | Apelin6 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 4.5 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 2.6 ± 0.8 | |||
| 30690406 | 2019 | Apelin7 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 18 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 6.3 ± 1.0 | |||
| 30690406 | 2019 | Apelin8 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 20.5 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 11.3 ± 2.1 | |||
| 30690406 | 2019 | Apelin9 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 27 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 2.5 ± 1.5 | |||
| 30658804 | 2019 | ES2 | 11 | Free | FITC | Linear | L | None | derived from the C-terminus of endostatin | Antiangiogenic | Immediately, 0.5, 1, 2, 4, 6, 8, 12, 24, and 36 h after injection, blood was collected | 20 mg/kg | 18.04 ± 2.38 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Antitumor activity = 35.31% | |||
| 30658804 | 2019 | HTCOSC-ES2 | 11 | Chitooligosaccharide chloride | FITC | Linear | L | None | derived from the C-terminus of endostatin | Antiangiogenic | Immediately, 0.5, 1, 2, 4, 6, 8, 12, 24, and 36 h after injection, blood was collected | 80 mg/kg | 29.17 ± 3.91 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Antitumor activity = 68.21% | |||
| 30624060 | 2019 | Compound 7 | 9 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | sTyr = Sulfated-Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated DAsp | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 115 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.35 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 8 | 9 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | L | Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, MeAsp = N-methylated Asp | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 145 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.97 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 9 | 9 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 113 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.60 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 14 | 9 | yGlu-(OEG)2 linker between C14 fatty acid and peptide | Amidation | Linear | Mix | Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 2 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.74 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 15 | 9 | yGlu-(OEG)2 linker between C16 fatty acid and peptide | Amidation | Linear | Mix | Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 37 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.72 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 16 | 9 | yGlu-(OEG)2 linker between C20 fatty acid and peptide | Amidation | Linear | Mix | Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 153 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.43 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 17 | 9 | yGlu-PEG10-PEG10 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 103 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.54 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 18 | 9 | yGlu-PEG10-PEG10 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 161 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.50 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 19 | 10 | C18 fatty acid | Amidation | Linear | Mix | sTyr = Sulfated-Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated DAsp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 36 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.67 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 20 | 8 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 2.6 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.14 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 25 | 9 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 45 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.81 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 27 | 6 | Lys(C18d-yGlu-(OEG)2) linker between hydroxyphenylacetic acid and peptide | Amidation | Linear | Mix | Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 7.1 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.80 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 30 | 9 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 112 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.44 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 48 | 9 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Me1Nal = N-methyl-1-naphthylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 147 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.39 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 49 | 9 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Me1Nal = N-methyl-1-naphthylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 140 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.44 (In Vitro CCK-1R Potency) | |||
| 30624060 | 2019 | Compound 56 | 9 | yGlu-(OEG)2 linker between C18 fatty acid and peptide | Amidation | Linear | Mix | sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Phe(4sm) = 4-sulfomethylphenylalanine, βAsp at position 1 | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 106 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.50 (In Vitro CCK-1R Potency) | |||
| 30606721 | 2019 | BCY-B5 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | 11.5 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | N.A. | |||
| 30606721 | 2019 | BCY-B3 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Mouse plasma protease | Radio-HPLC | Mouse plasma | In Vitro | None | None | KD(nM) = 1.22 ± 0.40 | |||
| 30606721 | 2019 | BCY-C3 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15) | Mix | (1Nal),(D-Ala) at position 3,(tBuGly) at Asp14 | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | N.A. | |||
| 30606721 | 2019 | BCY-C2. | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15) | Mix | (1Nal),(D-Ala) at position 3,(tBuGly) at Asp14 | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Mouse plasma protease | Radio-HPLC | Mouse plasma | In Vitro | None | None | KD(nM) = 0.5 ± 0.2 | |||
| 30606721 | 2019 | BCY-B5 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | N.A. | |||
| 30606721 | 2019 | BCY-B3 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Human plasma protease | Radio-HPLC | Human plasma | In Vitro | None | None | KD(nM) = 1.22 ± 0.40 | |||
| 30606721 | 2019 | BCY-C3 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15) | Mix | (1Nal),(D-Ala) at position 3,(tBuGly) at Asp14 | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Human plasma protease | LC-MS | Human plasma | In Vitro | None | None | N.A. | |||
| 30606721 | 2019 | BCY-C2. | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15) | Mix | (1Nal),(D-Ala) at position 3,(tBuGly) at Asp14 | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Human plasma protease | Radio-HPLC | Human plasma | In Vitro | None | None | KD(nM) = 0.5 ± 0.2 | |||
| 30606721 | 2019 | BCY-B2 | 14 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C1, C7, C14) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | Blood samples were taken from two animals per time-point, at 0.08, 0.5, 1, 2, and 4 hours post injection (p.i.), | 5.925 mg/kg | 14 (Elimination Half Life) | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | KD(nM) = 25 ± 0.3 | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 50 mg/kg | 13 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 50 mg/kg | 16 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 50 mg/kg | 11 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 10 mg/kg | 3.6 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 10 mg/kg | 11 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 30600870 | 2019 | cot-biPEPEDB-VEGF | 20 | Acetylation | Amidation | Cyclic (C5-C13 Disulfide Bond In pepVEGF) | Mix | Lys10 linked with (OEG-Cotinine-OEG-SSSPIQGSWTWENGKWTWKGIIRLEQ-NH2), D-alanine | Synthetic | Antitumor | N.A. | 200nM | 1.18 (Clearance Half Life) | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | tumor growth inhibition was not significantly different between cot-biPEPEDB-VEGF and PBS control groups, despite a trend toward greater inhibition in the cot-biPEPEDB-VEGF group | |||
| 30600066 | 2019 | GSHP-ES2 | 11 | FITC-GSHP | Free | Linear | L | None | Synthetic | Antitumour, Antiangiogenic | Blood samples were collected through the fundus venous plexus 0.5–72 h after administration | 20 mg/kg | 9.11 | Mice plasma protease | fluorescence spectrometry | mice plasma | In Vivo | None | None | When the concentration was 5, 25, 50, 75, 100 and 125 μg/ml, the inhibitory rate of GSHP-ES2 was 6.47%, 16.47%, 24.57%, 31.36%, 44.45%, and 67.26%, respectively | |||
| 30543420 | 2019 | R2 | 53 | Free | Free | Linear | L | B-D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 0.3 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.025 ± 0.004 | |||
| 30543420 | 2019 | R2 | 53 | Free | Free | Linear | L | B-D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 7 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.025 ± 0.55 | |||
| 30543420 | 2019 | R3-01 | 53 | Free | FA-01 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | N.A. | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 4.3 ± 0.005 | |||
| 30543420 | 2019 | R3-02 | 53 | Free | FA-02 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 1 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.028 ± 0.18 | |||
| 30543420 | 2019 | R3-02 | 53 | Free | FA-02 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role In Hemodynamics And Renal Function And Has Shown Preclinical Efficacy In Multiple Disease Models, Including Acute Heart Failure, Fibrosis, Preeclampsia, And Corneal Wound Healing | N.A. | 0.3 mg/kg | 1 | Mouse plasma protease | LC-MS | mouse plasma | In Vivo | None | None | EC50(nM) = 0.028 ± 0.10 | |||
| 30543420 | 2019 | R3-08 | 53 | Free | FA-08 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role In Hemodynamics And Renal Function And Has Shown Preclinical Efficacy In Multiple Disease Models, Including Acute Heart Failure, Fibrosis, Preeclampsia, And Corneal Wound Healing | N.A. | 0.3 mg/kg | N.A. | Mouse plasma protease | LC-MS | mouse plasma | In Vivo | None | None | EC50(nM) = 1.5 | |||
| 30543420 | 2019 | R3-09 | 53 | Free | FA-09 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role In Hemodynamics And Renal Function And Has Shown Preclinical Efficacy In Multiple Disease Models, Including Acute Heart Failure, Fibrosis, Preeclampsia, And Corneal Wound Healing | N.A. | 0.3 mg/kg | N.A. | Mouse plasma protease | LC-MS | mouse plasma | In Vivo | None | None | EC50(nM) = 0.8 | |||
| 30521347 | 2019 | cot-APTEDB-SN38 | 26 | Free | Free | Cyclic (2 Trp-Trp Bond) | L | Lys15 linked with (Cot-Mal-PEG4-Ala-SN38) | Linker is Mal-PEG4 | Anticancer | Those mice were sacrificed at 0.08, 0.5, 1, 3, 6, 12, 24, and 48 h post injection | 1 mg/kg | 1.36 | ICR mice plasma protease | HPLC | ICR mice plasma | In Vivo | https://sci-hub.st/10.1016/j.jconrel.2012.08.029 | None | HC[cot-APTEDB−SN38/Abcot] at an SN38/kg dose-equivalent of 2 mg effectively suppressed tumor growth and showed much greater antitumor activity (49.8% inhibition) than both cotAPTEDB-SN38 alone (23.9% inhibition) and CPT-11 (10.6% inhibition) | |||
| 30517073 | 2019 | D6.2 | 178 | Free | Free | Linear | L | V69M/I80T/F83L mutation in D6.1 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 1.5 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) = 790 | |||
| 30517073 | 2019 | EI.1 | 178 | Free | Free | Linear | L | K46M/K75X/N79M/ K142I mutations on D6.2 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 3.1 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) = 829 | |||
| 30517073 | 2019 | EI.3 | 178 | Free | Free | Linear | L | K30E/I41F/X75K/T135I/I142K mutation on El.1 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 3.4 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) = 548 | |||
| 30517073 | 2019 | D6.4 | 178 | Free | Free | Linear | L | K142I mutation in El.3 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 5.3 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) =622 | |||
| 30517073 | 2019 | D6.4 | 178 | Free | Free | Linear | L | Q77E mutation | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 6.7 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) =451 | |||
| 30517073 | 2019 | D6.5 | 178 | Free | Free | Linear | L | T136V mutation in D6.4 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 6.8 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) = 620 | |||
| 30517073 | 2019 | D6.6 | 178 | Free | Free | Linear | L | Q77E mutation in D6.5 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 9.4 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) = 702 | |||
| 30504081 | 2019 | VPGAG80 | 400 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 5.0 ± 0.1 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPGAG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 5.2 ± 0.1 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPGAG160 | 800 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 7.3 ± 0.2 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPKEG80 | 400 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 12.4 ± 0.1 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 17 nM for GLP1-VPKEG120 | |||
| 30504081 | 2019 | VPKEG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 12.9 ± 0.2 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 17 nM for GLP1-VPKEG120 | |||
| 30504081 | 2019 | VPGAG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 4.5 ± 0.2 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPGAG160 | 800 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 6.6 ± 0.3 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPKEG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 12.0 ± 0.4 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 17 nM for GLP1-VPKEG120 | |||
| 30504081 | 2019 | VPREG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =R, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 9.6 ± 0.5 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30504081 | 2019 | VPKDG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= D | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 10.8 ± 0.2 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30504081 | 2019 | VPRDG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =R, X2= D | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 8.2 ± 0.3 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30504081 | 2019 | VPGAG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 10.6 ± 1.6 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPGAG160 | 800 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 12.4 ± 0.8 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPKEG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 15.6 ± 0.6 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 17 nM for GLP1-VPKEG120 | |||
| 30504081 | 2019 | VPKDG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= D | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 11.8 ± 1 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30334171 | 2019 | rhIFN-α2b | 165 | Free | Free | Linear | L | None | Synthetic | Antiviral, Antitumor, And Immunomodulatory Effects | N.A. | 500 μg/kg | 0.54 (Elimination Half Life) | Rats plasma protease | sandwich ELISA | Rats plasma | In Vivo | PDB id: 1RH2 | None | rhIFN-α2b had a high specific antiviral activity (2.5 × 108 ± 1.1 × 108IU/mg protein) | |||
| 30165247 | 2019 | PoIFNα -C2 | 781 | Free | SPG C2 domain | Linear | L | None | Fusion protein of Ig-binding C2 domain of streptococcal protein G (SPG) with PoIFN-α | Antiviral And Immune Regulatory Effects | Serum samples were collected at 0.5, 2.0, 4.0, 8.0, 12, 24,48, 72, 96, 120 and 144 h post injection | 2.5 mg/kg | 56.82 ± 0.70 | Rats serum protease | ELISA | Rats serum | In Vivo | GenBank accession no. AY345969, X06173.1 | None | On MDBK cell, PoIFNα-C2 protein showed almost 10-fold lower anti-VSV activity (3.0 × 107 U/μM) than that (2.4 × 108 U/μM) of PoIFN-α standard | |||
| 30165247 | 2019 | PoIFN-α | 189 | Free | Free | Linear | L | None | Porcine IFN-α | Antiviral And Immune Regulatory Effects | Serum samples were collected at 0.5, 2.0, 4.0, 8.0, 12, 24,48, 72, 96, 120 and 144 h post injection | 2.5 mg/kg | 4.02 ± 0.06 | Rats serum protease | ELISA | Rats serum | In Vivo | None | None | On MDBK cell, PoIFNα-C2 protein showed almost 10-fold lower anti-VSV activity (3.0 × 107 U/μM) than that (2.4 × 108 U/μM) of PoIFN-α standard | |||
| 30165247 | 2019 | PoIFNα -C2 | 781 | Free | SPG C2 domain | Linear | L | None | Fusion protein of Ig-binding C2 domain of streptococcal protein G (SPG) with PoIFN-α | Antiviral And Immune Regulatory Effects | Serum samples were collected at 0.5, 2.0, 4.0, 8.0, 12, 24,48, 72, 96, 120 and 144 h post injection | 2.5 mg/kg | 61.58 ± 1.998 | Rats serum protease | ELISA | Rats serum | In Vivo | None | None | On MDBK cell, PoIFNα-C2 protein showed almost 10-fold lower anti-VSV activity (3.0 × 107 U/μM) than that (2.4 × 108 U/μM) of PoIFN-α standard | |||
| 30165247 | 2019 | PoIFN-α | 189 | Free | Free | Linear | L | None | Porcine IFN-α | Antiviral And Immune Regulatory Effects | Serum samples were collected at 0.5, 2.0, 4.0, 8.0, 12, 24,48, 72, 96, 120 and 144 h post injection | 2.5 mg/kg | 6.54 ± 0.16 | Rats serum protease | ELISA | Rats serum | In Vivo | None | None | On MDBK cell, PoIFNα-C2 protein showed almost 10-fold lower anti-VSV activity (3.0 × 107 U/μM) than that (2.4 × 108 U/μM) of PoIFN-α standard | |||
| 31615671 | 2019 | Free-ADI | 85 | Free | Free | Linear | L | None | Isolated from Thermophilic Aspergillus nidulans | Anticancer | 4°C | N.A. | 1445 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 85 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Synthetic | Anticancer | 4°C | N.A. | 2440 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Free-ADI | 85 | Free | Free | Linear | L | None | Isolated from Thermophilic Aspergillus nidulans | Anticancer | 30 °C | N.A. | 23.5 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 85 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Synthetic | Anticancer | 30 °C | N.A. | 40.2 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Free-ADI | 85 | Free | Free | Linear | L | None | Isolated from Thermophilic Aspergillus nidulans | Anticancer | 37°C | N.A. | 17.3 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 85 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Synthetic | Anticancer | 37°C | N.A. | 34.2 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Free-ADI | 85 | Free | Free | Linear | L | None | Isolated from Thermophilic Aspergillus nidulans | Anticancer | 45°C | N.A. | 3.4 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 85 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Synthetic | Anticancer | 45°C | N.A. | 8.4 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31536939 | 2019 | ALL*labeled nanocarriers | 12 | Free | D-Α-Tocopherol Succinate Linked Via Peg | Linear | L | Peptides are attached via a GGGSK linker to the nanocarrier surface via a thioether-mediated conjugation | Synthetic | Anticancer (therapy of hepatocellular carcinoma) | 37 °C for 0, 1, 2, 6, 12, and 24 h | 30 μM | 22.7 ( Sorafenib Release Half Life) | Mouse serum protease | HPLC | Mouse serum | N.A. | None | None | IC50 = 3.6 μM show greater toxicity to Hep3B cells in vitro | |||
| 31536939 | 2019 | QLE* labeled nanocarriers | 12 | Free | D-Α-Tocopherol Succinate Linked Via Peg | Linear | L | Peptides are attached via a GGGSK linker to the nanocarrier surface via a thioether-mediated conjugation | Synthetic | Anticancer (therapy of hepatocellular carcinoma) | 37 °C for 0, 1, 2, 6, 12, and 24 h | 30 μM | 19.5 (Sorafenib Release Half Life) | Mouse serum protease | HPLC | Mouse serum | N.A. | None | None | IC50 = 6.0 μM show lesser toxicity to Hep3B cells in vitro | |||
| 31376486 | 2019 | Recombinant XynRA1 | 379 | Free | Free | Linear | L | None | Derived from Rhodothermaceae bacterium RA | Endo-1,4-β-xylanase | 60 °C | N.A. | 1 (Activity Half Life) | N.A. | BCA Protein Assay | N.A. | In Vitro | Uniprot id: A0A1V0DJ74 | None | XynRA1 enzyme retained 80% of its maximal activity for 5 h | |||
| 31281949 | 2019 | FUD | 49 | Free | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 0.81 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 10K PEG-FUD | 49 | 10K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 3.28 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 20K PEG-FUD | 49 | 20K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 6.77 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 40K PEG-FUD | 49 | 40K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 10.09 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | mFUD | 49 | Free | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 0.86 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 10K PEG-mFUD | 49 | 10K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 3.06 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 20K PEG-mFUD | 49 | 20K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 5.25 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 40K PEG-mFUD | 49 | 40K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 8.36 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31067782 | 2019 | Rhodamine-labeled V96 | 482 | Free | Free | Linear | L | Rhodamine labeling | Synthetic | Increases half life | 37°C, Small aliquots of the solution (100 µL) were withdrawn at predetermined intervals (5, 15, 30 min, 1, 2, 4, 8, 24, 48, 72, 96, 120, 168 h) | 100 µM | 0.2 (T1/2 Fast Release Kinetics) | N.A. | Fluorescence assay | Proclear CompatiblesTM contact lenses | In Vivo | None | None | N.A. | |||
| 31067782 | 2019 | Rhodamine-labeled V96 | 482 | Free | Free | Linear | L | Rhodamine labeling | Synthetic | Increases half life | 37°C, Small aliquots of the solution (100 µL) were withdrawn at predetermined intervals (5, 15, 30 min, 1, 2, 4, 8, 24, 48, 72, 96, 120, 168 h) | 100 µM | 4615 (T1/2 Slow Release Kinetics) | N.A. | Fluorescence assay | Proclear CompatiblesTM contact lenses | In Vivo | None | None | N.A. | |||
| 31067782 | 2019 | Rhodamine-labeled V96 | 482 | Free | Free | Linear | L | Rhodamine labeling | Synthetic | Increases half life | 4°C, Small aliquots of the solution (100 µL) were withdrawn at predetermined intervals (5, 15, 30 min, 1, 2, 4, 8, 24, 48, 72, 96, 120, 168 h) | 100 µM | 0.2 (T1/2 Fast Release Kinetics) | N.A. | Fluorescence assay | Proclear CompatiblesTM contact lenses | In Vivo | None | None | N.A. | |||
| 31067782 | 2019 | Rhodamine-labeled V96 | 482 | Free | Free | Linear | L | Rhodamine labeling | Synthetic | Increases half life | 4°C, Small aliquots of the solution (100 µL) were withdrawn at predetermined intervals (5, 15, 30 min, 1, 2, 4, 8, 24, 48, 72, 96, 120, 168 h) | 100 µM | 96.2 (T1/2 Slow Release Kinetics) | N.A. | Fluorescence assay | Proclear CompatiblesTM contact lenses | In Vivo | None | None | N.A. | |||
| 31067782 | 2019 | Rhodamine-labeled S96 | 482 | Free | Free | Linear | L | Rhodamine labeling | Synthetic | Increases half life | 37°C, Small aliquots of the solution (100 µL) were withdrawn at predetermined intervals (5, 15, 30 min, 1, 2, 4, 8, 24, 48, 72, 96, 120, 168 h) | 100 µM | 0.2 (T1/2 Fast Release Kinetics) | N.A. | Fluorescence assay | Proclear CompatiblesTM contact lenses | In Vivo | None | None | N.A. | |||
| 31067782 | 2019 | Rhodamine-labeled S96 | 482 | Free | Free | Linear | L | Rhodamine labeling | Synthetic | Increases half life | 37°C, Small aliquots of the solution (100 µL) were withdrawn at predetermined intervals (5, 15, 30 min, 1, 2, 4, 8, 24, 48, 72, 96, 120, 168 h) | 100 µM | 137.1 (T1/2 Slow Release Kinetics) | N.A. | Fluorescence assay | Proclear CompatiblesTM contact lenses | In Vivo | None | None | N.A. | |||
| 31067782 | 2019 | V96 | 482 | Free | Free | Linear | L | None | Synthetic | Increases half life | N.A. | N.A. | 4 (Retention Half Life) | N.A. | N.A. | Solution | N.A. | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 9 | Free | Free | Linear | L | N23G24 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 400 ± 100 (Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N29G30 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 1100 ± 700(Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 14 | Free | Free | Linear | L | N111G112 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 18 ± 2 (Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 9 | Free | Free | Linear | L | N184G185 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 12 ± 1 (Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 20 | Free | Free | Linear | L | N238G239 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | N.A. | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N196A197 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 120 ± 10 (Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N360A361 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 630 ± 30 ( Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 9 | Free | Free | Linear | L | N23G24 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 200 ± 40 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N29G30 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 500 ± 200 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 14 | Free | Free | Linear | L | N111G112 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 12 ± 5 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 9 | Free | Free | Linear | L | N184G185 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 2.0 ± 0.5 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 20 | Free | Free | Linear | L | N238G239 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | N.A. | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N196A197 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 50 ± 2 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N360A361 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 120 ± 4 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30676716 | 2019 | APA1 | 7 | SATHA-FBA | Free | Linear | L | R=OMe | Synthetic | Increase half life of H2S | N.A. | 0.1 mg/mL | 31 ± 8 (H2S Release Half Life) | Dilute APA solution protease | Methylene blue method | Dilute APA solution | In Vitro | None | None | N.A. | |||
| 30676716 | 2019 | APA2 | 7 | SATHA-FBA | Free | Linear | L | R=Me | Synthetic | Increase half life of H2S | N.A. | 0.1 mg/mL | 22±4 (H2S Release Half Life) | Dilute APA solution protease | Methylene blue method | Dilute APA solution | In Vitro | None | None | N.A. | |||
| 30676716 | 2019 | APA3 | 7 | SATHA-FBA | Free | Linear | L | None | Synthetic | Increase half life of H2S | N.A. | 0.1 mg/mL | 19±8 (H2S Release Half Life) | Dilute APA solution protease | Methylene blue method | Dilute APA solution | In Vitro | None | None | N.A. | |||
| 30676716 | 2019 | APA4 | 7 | SATHA-FBA | Free | Linear | L | R=F | Synthetic | Increase half life of H2S | N.A. | 0.1 mg/mL | 14±2 (H2S Release Half Life) | Dilute APA solution protease | Methylene blue method | Dilute APA solution | In Vitro | None | None | N.A. | |||
| 30676716 | 2019 | APA5 | 7 | SATHA-FBA | Free | Linear | L | R=Cl | Synthetic | Increase half life of H2S | N.A. | 0.1 mg/mL | 13±4 (H2S Release Half Life) | Dilute APA solution protease | Methylene blue method | Dilute APA solution | In Vitro | None | None | N.A. | |||
| 33224505 | 2019 | AR-Bi@SiO2-Gd/DOX NPs | 23 | Free | C-Terminal End Of The Ar Peptide Was Added With An Nh2-Rich Linker (GGGGKKKK) | Linear | L | None | Synthetic | Antitumor (Tumor homing ) | N.A. | N.A. | 104.5 (Tumor Retention Half Life) | N.A. | ICP-MS | N.A. | In Vivo | None | None | N.A. | |||
| 30344018 | 2019 | ASN | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | B. cereus BDRD-ST26 (P43-amyE-BcA) | Production of acrylamide-free food | 50 C | N.A. | 17.35 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | Km = 9.38 mM | |||
| 30344018 | 2019 | ASN | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | B. cereus BDRD-ST26 (P43-BcA) | Production of acrylamide-free food | 50 C | N.A. | 17.57 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | km = 9.41 mM | |||
| 30344018 | 2019 | ASN | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | B. subtilis 168 | Production of acrylamide-free food | 65 C | N.A. | 61 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | km = 5.3 mM | |||
| 30344018 | 2019 | ASN | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | T. kodakaraensis 1656 | Production of acrylamide-free food | 85 C | N.A. | 130 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | km = 5.5 mM | |||
| 30684538 | 2019 | Tryptic peptide | 17 | Free | Free | Linear | L | N216A217 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 17 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 17 | Free | Free | Linear | L | N216A217 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 17 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N23G24 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 980 ± 60 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 13 | Free | Free | Linear | L | N29G30 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 1300 ± 100 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 7 | Free | Free | Linear | L | N111G112 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 150 ± 10 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 8 | Free | Free | Linear | L | N184G185 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N238G239 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 10,900 ± 400 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 14 | Free | Free | Linear | L | N196A197 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 19 | Free | Free | Linear | L | N360A361 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 15 | Free | Free | Linear | L | N216A217 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 270 ± 30 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 13 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 3800 ± 400 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 19 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 35,000 ± 900 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N23G24 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 700 ± 60 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 13 | Free | Free | Linear | L | N29G30 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 600 ± 20 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 7 | Free | Free | Linear | L | N111G112 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 130 ± 5 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 8 | Free | Free | Linear | L | N184G185 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N238G239 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 7800 ± 100 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 14 | Free | Free | Linear | L | N196A197 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 19 | Free | Free | Linear | L | N360A361 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 15 | Free | Free | Linear | L | N216A217 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 13 | Free | Free | Linear | L | N278A279 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 2600 ± 100 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 19 | Free | Free | Linear | L | N278A279 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 16,700 ± 20 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30809901 | 2019 | FITC-AAR029b | N.A. | Fluorescein isothiocynate labeled | Free | Macrocyclic | L | None | Derived from a class of peptides known as cyclic peptide triazoles (cPTs) | Antiviral | N.A. | 0.01 mg/kg | 0.029 ± 0.01 (T1/2Α-Distribution Half Life) | Rats plasma protease | Fluorescence assay | Rats plasma | In Vivo | None | None | EC50(nM) = 210±16 for AAR029b in Bal.01 virus | |||
| 30809901 | 2019 | FITC-AAR029b in Liposome | N.A. | Fluorescein isothiocynate labeled | Free | Macrocyclic | L | None | Derived from a class of peptides known as cyclic peptide triazoles (cPTs) | Antiviral | N.A. | 0.01 mg/kg | 0.032 ± 0.005 (T1/2Α-Distribution Half Life) | Rats plasma protease | Fluorescence assay | Rats plasma | In Vivo | None | None | EC50(nM) = 210±16 for AAR029b in Bal.01 virus | |||
| 30565900 | 2018 | DOX@PLEPMPss-cRGD | 3 | PCL-PEG | Free | Cyclic (N-C terminal end) | L | None | Synthetic | Anticancer | The plasma was collected after injection at predetermined time points (1, 3, 6, 12, and 24 h) | 2 mg/kg | 11.81 ± 0.67 (T1/2b) | Mice plasma protease | fluorescence spectrometry | mice plasma | In Vivo | None | None | The IC50 value (i.e., the concentration resulting in 50% cell inhibition) forDOX@Cu-PLEPMPsscRGD micelles was 2.884 µg mL−1 | |||
| 30565900 | 2018 | DOX@Cu-PLEPMPss-cRGD | 3 | PCL-PEG | Free | Cyclic (N-C terminal end) | L | None | Synthetic | Anticancer | The plasma was collected after injection at predetermined time points (1, 3, 6, 12, and 24 h) | 2 mg/kg | 12.20 ± 0.73 (T1/2b) | Mice plasma protease | fluorescence spectrometry | mice plasma | In Vivo | None | None | The IC50 value (i.e., the concentration resulting in 50% cell inhibition) forDOX@Cu-PLEPMPsscRGD micelles was 2.884 µg mL−1 | |||
| 30555549 | 2018 | AuNp-DPA | 13 | Free | Au | Linear | L | None | Synthetic | Antitumor | N.A. | 2 mg/kg | 7.5 ± 0.8 | Mice blood protease | HPLC | Mice blood sample | In Vivo | None | None | AuNP-DPA inhibited tumor growth by 88% on day 13 compared to the control, even better than DOX (inhibition ratio of 64.3% in comparison with the control) | |||
| 30496575 | 2018 | rhIFN-λ1 | 181 | Free | Human chorionic gonadotropin β subunit carboxyl-terminal peptide (CTP) and an N-glycosylation sequence linked to its C-terminus | Linear | L | None | Recombinant human interferon-λ1 | Antiviral, Antiproliferation, And Nk Cell Cytotoxicity-Promoting Activities | Venous blood was collected at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h post-injection | 40 μg/kg | 3.37 ± 0.70 | Mice blood protease | ELISA | Mice blood sample | In Vivo | None | None | Antiviral activity of the purified rhIFN-λ1 expressed by CHO cells was 2.5 × 105 IU/mg | |||
| 30496575 | 2018 | rhIFN-λ1-CTPON | 218 | Free | Human chorionic gonadotropin β subunit carboxyl-terminal peptide (CTP) and an N-glycosylation sequence linked to its C-terminus via linker | Linear | L | None | Recombinant human interferon-λ1 derivative | Antiviral, Antiproliferation, And Nk Cell Cytotoxicity-Promoting Activities | Venous blood was collected at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h post-injection | 40 μg/kg | 10.326 ± 0.87 | Mice blood protease | ELISA | Mice blood sample | In Vivo | None | None | Antiviral activity of the purified rhIFN-λ1 expressed by CHO cells was 2.5 × 105 IU/mg | |||
| 30411073 | 2018 | sPIF | 15 | Free | Free | Linear | L | None | Human embryo‐derived peptide analogs | Treatment of Autoimmune Hepatitis | Patients’ serum samples were collected and analyzed at five different time points: screening (day ‐28 to day 0), pre‐injection (day 0), and postinjection days 1, 2, and 8 | 0.1 mg/kg | N.A. | Human serum protease | LC-MS | Human serum | In Vivo | None | None | N.A. | |||
| 30411073 | 2018 | sPIF | 15 | Free | Free | Linear | L | None | Human embryo‐derived peptide analogs | Treatment Of Autoimmune Hepatitis | Patients’ serum samples were collected and analyzed at five different time points: screening (day ‐28 to day 0), pre‐injection (day 0), and postinjection days 1, 2, and 8 | 0.5 mg/kg | 63 | Human serum protease | LC-MS | Human serum | In Vivo | None | None | N.A. | |||
| 30411073 | 2018 | sPIF | 15 | Free | Free | Linear | L | None | Human embryo‐derived peptide analogs | Treatment Of Autoimmune Hepatitis | Patients’ serum samples were collected and analyzed at five different time points: screening (day ‐28 to day 0), pre‐injection (day 0), and postinjection days 1, 2, and 8 | 1 mg/kg | 109 | Human serum protease | LC-MS | Human serum | In Vivo | None | None | N.A. | |||
| 30407790 | 2018 | GENP-Gem-Ola | 12 | C18-EEG | Amidation | Linear | L | None | Synthetic | Treat Pancreatic Cancer With Breast Cancer 2 (Brca2) Mutation | Blood samples were collected at 0.5, 1, 2, 3, 5, 8, 12, and 24 h postinjection | equivalent concentrations of Gem (5 mg/kg) and Ola (50 mg/kg) | 4 | Mice plasma protease | HPLC | Mice plasma | In Vivo | None | None | Tumors from the GENP-Gem-Ola group showed extensive apoptosis (51% c-caspase-3 positive) | |||
| 30314880 | 2018 | SA-5K | 2 | Stearic acid conjugation | Substituition of Phe with Lys at C terminal | Linear | L | chemical group (S)-3-amino-3-(1-naphthyl)-propionic acid- conjugated between R1 and Lys2 | Synthetic | Anticancer | 0, 15, 30, min, 1, 2, 6, 12, 24 h | 2 mM | 5 | Human serum protease | HPLC, MS | Human serum | In Vitro | None | None | IC50 μM = 1.0 ± 0.05 for SA-5 in BT-474 | |||
| 30314880 | 2018 | Compound 5 | 2 | Free | Free | Linear | L | chemical group (S)-3-amino-3-(1-naphthyl)-propionic acid- conjugated between R1 and F2 | Synthetic | Anticancer, Antiproliferative | 0, 15, 30, min, 1, 2, 6, 12, 24 h | 2 mM | 2 | Human serum protease | HPLC, MS | Human serum | In Vitro | None | None | IC50 μM = 0.895 ±0.029 for compound 5 in BT-474 | |||
| 30309736 | 2018 | PE | 40 | Free | PEG(20k) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h | 100 nmoL/kg | 31.4 ± 1.6 | SD rats serum protease | ELISA | SD rats serum | In Vivo | PDB id: 1JRJ | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30309736 | 2018 | PE | 40 | Free | PEG(20k) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h | 200 nmol/kg | 31.7 ± 1.5 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30309736 | 2018 | PE | 40 | Free | PEG(20k) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h | 400 nmol/kg | 30.7 ± 2.2 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30309736 | 2018 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Exendin-4 | Antidiabetes | Blood samples were collected at 0, 0.25, 0.5, 0.75, 1, 2, 4, 6,8, and 12 h after injection | 100 nmoL/kg | 1.7 ± 0.3 | SD rats serum protease | ELISA | SD rats serum | In Vivo | PDB id: 7MLL | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30309736 | 2018 | PE | 40 | Free | PEG(20k) | Linear | L | Introduction of Cys at C terminal of Exendin-4 | Exendin-4 analogs | Antidiabetes | For 33 consecutive days, after the first administration for 6 days,eight rats received PE (100 nmoL/kg, 200 mL, s.c.) once every 84 h | 100 nmoL/kg | 27.6 ± 5.1 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30226777 | 2018 | E1 | 18 | Free | Free | Linear | L | None | Derived from the E1 envelope protein of GBV-C | HIV-1 fusion inhibitor peptide | At different incubation times (30 min, 1, 2, 4, 8, and 24 h) | 1 mg/mL | 8 | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 30226777 | 2018 | E1-NP | 18 | Free | Free | Linear | L | None | Derived from the E1 envelope protein of GBV-C | HIV-1 fusion inhibitor peptide | At different incubation times (30 min, 1, 2, 4, 8, and 24 h) | 1 mg/mL | 24 | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 30175919 | 2018 | Myristoylated peptide | 14 | 6FAM labelled | Additional C terminal cysteine linked to peptide using dislufide bond | Linear | L | MeAla, MeArg,Lys1 modified with Myr | Synthetic | Substrate reporter for PKB | RT | 1 µM | 12 ± 1 | N.A. | N.A. | Axenic D. discoideum K-AX3 DB or SorCM after myristoylated peptide loading | In Vitro | None | None | N.A. | |||
| 30175919 | 2018 | Electroporation peptide | 9 | 6FAM labelled | Free | Linear | L | MeAla, MeArg | Synthetic | Substrate reporter for PKB | RT | 35 µM | 53 ± 15 | N.A. | N.A. | Axenic D. discoideum K-AX3 SorCM buffer after electroporation | In Vitro | None | None | N.A. | |||
| 30175919 | 2018 | Pinocystosis peptide | 9 | 6FAM labelled | Free | Linear | L | MeAla, MeArg | Synthetic | Substrate reporter for PKB | RT | 150 µM | 19 ± 2 | N.A. | N.A. | Axenic D. discoideum K-AX3 DB after pinocytosis | In Vitro | None | None | N.A. | |||
| 30174173 | 2018 | GsMTx4 | 35 | Free | Free | Linear | L | None | Isolated from the venom of the spider Grammostola spatulata | Treatment of Duchenne Muscular Dystrophy | 6 times over 14 days – sacrifice on day 28 | 10 mg/kg | 1 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC2217226/ | None | 1 μM GsMTx4 in vitro experiments shows 0.1–5.0 μM effective in suppressing MSC activity in various disease models | |||
| 30170067 | 2018 | ES2-AF | 33 | ES2 | Free | Linear | L | None | Synthetic | Treatment of diseases caused by Diabetic Eye Disease, Rheumatoid Arthritis And Other Neo-Vascularization, Anti-Angiogenesis Activity | Blood samples were collected through the jugular vein at 5 min, 15 min, 30 min, 1 h, 2 h, 6 h, 12 h, 24 h, and 48 h after administration | 25 mg/kg | 2.785 | Wistar rats plasma protease | Fluorescence spectrometry | Wistar rats plasma | In Vivo | None | None | KD (mol· L−1) = 3.011 × 10−4 | |||
| 30170067 | 2018 | HA-ES2-AF | 33 | ES2-AF peptide was conjugated with HA by the formation of an amide linkage between the amino group of the ES2-AF peptide and the activated carboxyl of HA | Free | Linear | L | None | Synthetic | Treatment of diseases caused by Diabetic Eye Disease, Rheumatoid Arthritis And Other Neo-Vascularization, Anti-Angiogenesis Activity | Blood samples were collected through the jugular vein at 5 min, 15 min, 30 min, 1 h, 2 h, 6 h, 12 h, 24 h, and 48 h after administration | 25 mg/kg | 18.07 | Wistar rats plasma protease | Fluorescence spectrometry | Wistar rats plasma | In Vivo | None | None | KD (mol· L−1) = 4.779 × 10−10 | |||
| 30165332 | 2018 | DV1 | 21 | Free | Amidation | Linear | D | All D-amino acids | Synthetic | CXCR4 antagonist | Blood samples were collected into heparin-coated polypropylene centrifuge tubes at 0, 5, 10, 15, 30 min and 1, 2, 4, 6, 8, 12, 24, 36 and 48 h after the dose | 10 mg/kg | 8.7 ± 2.4 | Rats plasma protease | HPLC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30161002 | 2018 | P16 | 21 | Free | Free | Linear | L | None | TNF-a cleaved fragment | Antitumor | Orbital blood samples were collected from 3 mice at different time points (0, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, and 48 h) | 5 mg/kg | 0.07 | BALB/c mice plasma protease | LC-MS | BALB/c mice plasma | In Vivo | None | None | N.A. | |||
| 30161002 | 2018 | TNF-a | 158 | Free | Free | Linear | L | None | TNF-a | Antitumor | Orbital blood samples were collected from 3 mice at different time points (0, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, and 48 h) | 5 mg/kg | 0.43 | BALB/c mice plasma protease | LC-MS | BALB/c mice plasma | In Vivo | PDB id: 6OP0 | None | N.A. | |||
| 30096651 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At 1, 2, 3, 4, 6, 12, 24 and 48 h after injection, three Kunming mice were sacrificed at each time point and blood samples (~200 mL) were collected through extracting eyeball | 50 nmol/kg | 3.6 ± 0.2 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | None | None | the potency of 6 was 5.2 times higher than liraglutide | |||
| 30096651 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Blood samples (100e150 mL) were obtained from fundus venous plexus and stored in polyethylene tubes containing heparin | 50 nmol/kg | 4.2 ± 0.3 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | the potency of 6 was 5.2 times higher than liraglutide | |||
| 30096651 | 2018 | Analogue 6 | 80 | Free | C terminal Cys extension for bis-maleimide linkage | Linear | L | Conjugation of Palmitic acid at Lys20 (single monomer) , dimerization | Dimeric lipidated Xenopus GLP-1 analogues | Antidiabetes | At 1, 2, 3, 4, 6, 12, 24 and 48 h after injection, three Kunming mice were sacrificed at each time point and blood samples (~200 mL) were collected through extracting eyeball | 50 nmol/kg | 10.8 ± 0.8 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | None | None | EC50 = 1.4 ± 0.5 nM in HEK293 cells | |||
| 30096651 | 2018 | Analogue 6 | 80 | Free | C terminal Cys extension for bis-maleimide linkage | Linear | L | Conjugation of Palmitic acid at Lys20 (single monomer) , dimerization | Dimeric lipidated Xenopus GLP-1 analogues | Antidiabetes | Blood samples (100e150 mL) were obtained from fundus venous plexus and stored in polyethylene tubes containing heparin | 50 nmol/kg | 12.9 ± 3.6 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50 = 1.4 ± 0.5 nM in HEK293 cells | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 1 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 2 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 4 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | > 4 | Rats SCT protease | LC-HRMS | 1 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 3.43 | Rats SCT protease | LC-HRMS | 2 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 0.56 | Rats SCT protease | LC-HRMS | 4 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 50 µM | > 4 | Rats SCT protease | LC-HRMS | 1 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 50 µM | > 4 | Rats SCT protease | LC-HRMS | 2 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 50 µM | > 4 | Rats SCT protease | LC-HRMS | 4 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 3 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 0.9 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Attenuates Renal Fibrosis | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | None | None | N.A. | |||
| 30023916 | 2018 | Conjugate 2 | 31 | CH90 linked by linker EDA–(LMDS) | Free | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 25.3 (T1/2 Elimination Half life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | EC50 = 9.9 nM | |||
| 30023916 | 2018 | Conjugate 2 | 31 | CH90 linked by linker EDA–(LMDS) | Free | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 30.3 (T1/2 Elimination Half life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | EC50 = 9.9 nM | |||
| 30023916 | 2018 | Conjugate 3 | 31 | Free | HPN50 linked by linker EDA–(LMDS) | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 33.6 (T1/2 Elimination Half life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | EC50 = 7.0 nM | |||
| 30023916 | 2018 | Conjugate 3 | 31 | Free | HPN50 linked by linker EDA–(LMDS) | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 25.8 (T1/2 Elimination Half life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | EC50 = 7.0 nM | |||
| 30023916 | 2018 | CH10-conjugated peptides | 31 | Free | CH10 linked by linker | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | 37 °C for 2 h | N.A. | 16 (T1/2 Elimination Half life) | 0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii | HPLC | N.A. | In Vitro | None | None | N.A. | |||
| 30023916 | 2018 | (CH30,CH40,CH70)-conjugated peptides | 31 | CH30/CH40/CH70 linker by linker | Free | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | 37 °C for 2 h | N.A. | 22 - 25 (T1/2 Elimination Half life) | 0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii | HPLC | N.A. | In Vitro | None | None | N.A. | |||
| 30023916 | 2018 | PEG30k-conjugated GLP-1C peptide | 31 | PEG30K | Free | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | 37 °C for 2 h | N.A. | 17.5 (T1/2 Elimination Half life) | 0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii | HPLC | N.A. | In Vitro | None | None | EC50 = 5.2 nM | |||
| 30023916 | 2018 | 10 kDa PEG-modified GLP-1 | 31 | PEG10K | Free | Linear | L | None | Synthetic | Antidiabetes | 37 °C for 2 h | N.A. | 105.5 (T1/2 Elimination Half life) | 0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii | HPLC | N.A. | In Vitro | None | None | N.A. | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment | 2.2 mg/kg | 14.1 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Mild Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment | 2.2 mg/kg | 15.9 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Moderate Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment | 2.2 mg/kg | 24.1 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Severe Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion | 2.2 mg/kg | 7.7 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Healthy Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 29958697 | 2018 | 125I-TLQP-21 | 21 | 125I labelled | Free | Linear | L | None | Derived from the proteolytic cleavage of the 617-aa VGF | Isoproterenol stimulated lipolysis | At the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL) | 1 mM | 1.7 (T1/2 Initial Phase) | Rats plasma protease | LC-MS | Rats plasma | In Vitro | None | None | N.A. | |||
| 29958697 | 2018 | 125I-TLQP-21 | 21 | 125I labelled | Free | Linear | L | None | Derived from the proteolytic cleavage of the 617-aa VGF | Isoproterenol stimulated lipolysis | At the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL) | 1 mM | 0.97 (T1/2 Initial Phase) | Rats plasma protease | LC-MS | Rats plasma volume reduced to 12.5 ml | In Vitro | None | None | N.A. | |||
| 29958697 | 2018 | 125I-TLQP-21 | 21 | 125I labelled | Free | Linear | L | None | Derived from the proteolytic cleavage of the 617-aa VGF | Isoproterenol stimulated lipolysis | At the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL) | 1 mM | 110 (T1/2 Terminal Phase) | Rats plasma protease | LC-MS | Rats plasma | In Vitro | None | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 30 μg | 11.43 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 100 μg | 12.07 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 150 μg | 10.97 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 300 μg | 9.54 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29799205 | 2018 | 4i | 39 | Free | Free | Linear | L | X3 = structure given in paper | GLP-1 analogs | Antidiabetes | Serial blood samples (100–200 µL) were collected from fundus venous plexus in microcentrifuge tubes (EDTA containing) at 0, 1, 2, 3, 4, 6, 12, 24 and 48 h | 50 nmol/kg | 5.4 ± 1.0 | SD rats plasma protease | LC-MS/MS. | SD rats plasma | In Vivo | None | None | EC50(nM) = 0.88 ± 0.43 | |||
| 29799205 | 2018 | 5b | 39 | Free | Free | Linear | L | X4 = structure given in paper | GLP-1 analogs | Antidiabetes | Serial blood samples (100–200 µL) were collected from fundus venous plexus in microcentrifuge tubes (EDTA containing) at 0, 1, 2, 3, 4, 6, 12, 24 and 48 h | 50 nmol/kg | 11.0 ± 1.2 | SD rats plasma protease | LC-MS/MS. | SD rats plasma | In Vivo | None | None | N.A. | |||
| 29799205 | 2018 | Liraglutide | 32 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 35.4 | SD rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | N.A. | |||
| 29799205 | 2018 | 4a | 29 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 17.4 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.29 ± 0.04 | |||
| 29799205 | 2018 | 4b | 29 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 27.7 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.97 ± 0.11 | |||
| 29799205 | 2018 | 4c | 29 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 37.7 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 1.49 ± 0.13 | |||
| 29799205 | 2018 | 4d | 29 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 20.2 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.49 ± 0.07 | |||
| 29799205 | 2018 | 4e | 29 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 29.4 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 1.68 ± 0.18 | |||
| 29799205 | 2018 | 4f | 29 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 37.3 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) =6.35 ± 0.39 | |||
| 29799205 | 2018 | 4g | 38 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 21.5 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) =0.18 ± 0.02 | |||
| 29799205 | 2018 | 4h | 38 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 31.6 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.57 ± 0.19 | |||
| 29799205 | 2018 | 4i | 38 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 39.5 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) =0.88 ± 0.43 | |||
| 29799205 | 2018 | 4j | 38 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 24.1 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.31 ± 0.03 | |||
| 29799205 | 2018 | 4k | 38 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 30.1 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.68 ± 0.24 | |||
| 29799205 | 2018 | 4l | 38 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 40.5 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 2.09 ± 0.21 | |||
| 29799205 | 2018 | 4m | 43 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 18.8 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.18 ± 0.06 | |||
| 29799205 | 2018 | 4n | 43 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 26.6 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.44 ± 0.11 | |||
| 29799205 | 2018 | 4o | 43 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 36.4 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.98 ± 0.18 | |||
| 29799205 | 2018 | 4p | 43 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 16.9 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.14 ± 0.02 | |||
| 29799205 | 2018 | 4q | 43 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 27.2 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.48 ± 0.08 | |||
| 29799205 | 2018 | 4r | 43 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 38.7 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.61 ± 0.24 | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 27 ± 1 | NEP (5.687 Nm) | RP-HPLC | Tris–HCl buffer (50 mM, pH 7.4) | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 78 ± 2 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM Sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 94 ± 2 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM Opiorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 47 ± 1 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Ala1]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 74 ± 2 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Ala2]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 109 ± 8 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Ala3]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 42 ± 2 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM[Ala4]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 52 ± 2 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Ala5]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 116 ± 1 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [His2]opiorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 53 ± 1 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Ser4]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 114 ± 2 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Arg2]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 139 ± 3 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Pro4]opiorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29738954 | 2018 | γTatM4 | 12 | Acetylation | Amidation | Linear | L | None | Tat peptide analogue | Antibacterial and Anti-Tb | N.A. | 10 mM | 16 | Trypsin | RP-HPLC | Tris-EDTA buffer | In Vitro | None | None | MIC(micrmolar) = 1.12 ± 0.01 for E.coli | |||
| 29738954 | 2018 | CtrlTat | 11 | Acetylation | Amidation | Linear | L | None | Derived from the human immunodeficiency virus 1 (HIV-1) tat protein | Antibacterial and Anti-Tb | N.A. | 10 mM | 4 | Trypsin | RP-HPLC | Tris-EDTA buffer | In Vitro | None | None | MIC (micromolar) = 6.27 ± 0.05 for E.coli | |||
| 29732120 | 2018 | Analogue 6 | 5 | Free | Free | Macrocyclic (N-C terminal end) | Mix | D-Phe | Synthetic | Inhibits pro-angiogenic integrins | At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h) | 1 mg/ml | 9 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50(μM) = 140 ± 95 against αvβ3 | |||
| 29732120 | 2018 | Analogue 12 | 5 | Free | Free | Macrocyclic (N-C terminal end) | L | None | Synthetic | Inhibits pro-angiogenic integrins | At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h) | 1 mg/ml | 7 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50(μM) = 166 ± 98 against αvβ3 | |||
| 29732120 | 2018 | Analogue 11 and 9b | 5 | Free | Free | Macrocyclic (N-C terminal end) | Mix | Thio substiuition in Asp (analogue 11) and Phe (analogue 9b) | Synthetic | Inhibits pro-angiogenic integrins | At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h) | 1 mg/ml | 36 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 value of 11 shows that 11 is poorer than Cilen | |||
| 29732120 | 2018 | Cilen | 5 | Free | Free | Macrocyclic (N-C terminal end) | Mix | Methylation at Phenylalanine (D-form) | Synthetic | Glioblastoma therapy | At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h) | 1 mg/ml | 12 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 value of 11 shows that 11 is poorer than Cilen | |||
| 29721065 | 2018 | 64Cu-DOTA-F56-CM | 12 | 64Cu-DOTA | maleimidopropionic acid (MPA) at the C-terminal | Linear | L | None | Maleimidopropionic acid-conjugated peptide | Antiangiogenic | At 10, 30, 60, and 120 min | 7.4 mBq | 6.967 | SD rats blood protease | Radioactivity assay | SD rats blood | In Vivo | None | None | F56 and F56-CM reduced the angiogenesis of zebrafish embryos in a dose-dependent way | |||
| 29721065 | 2018 | 64Cu-DOTA-F56 | 12 | 64Cu-DOTA | Free | Linear | L | None | Synthetic | Antiangiogenic | At 10, 30, 60, and 120 min | 7.4 mBq | 0.4249 | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | F56 and F56-CM reduced the angiogenesis of zebrafish embryos in a dose-dependent way | |||
| 29693715 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose | 5 mg for 5 days followed by 10 mg for 5 days | 156.4 | Human plasma protease | LC‐MS/MS | Human plasma (Normal hepatic function) after 10th dosing | In Vivo | None | None | N.A. | |||
| 29693715 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose | 5 mg for 5 days followed by 10 mg for 5 days | 142.1 | Human plasma protease | LC‐MS/MS | Human plasma (Mild hepatic function) after 10th dosing | In Vivo | None | None | N.A. | |||
| 29693715 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose | 5 mg for 5 days followed by 10 mg for 5 days | 146.7 | Human plasma protease | LC‐MS/MS | Human plasma (Moderate hepatic function) after 10th dosing | In Vivo | None | None | N.A. | |||
| 29693715 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose | 5 mg for 5 days followed by 10 mg for 5 days | 153.7 | Human plasma protease | LC‐MS/MS | Human plasma (Severe hepatic function) after 10th dosing | In Vivo | None | None | N.A. | |||
| 29685037 | 2018 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease brain ROS production and inflammation in preclinical models of HF | 15 h at 37°C | 100 µM | 13.8 ± 5.7 | Rats serum protease | HPLC | Rats serum | In Vitro | None | None | Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice | |||
| 29685037 | 2018 | Ang-AA | 7 | Acetylation | Amidation | Linear | L | None | Ang-(1-7) analogs | Antifibrosis, Antihypertension, Antihypertrophic and Antiarrhythmia Activities | 15 h at 37°C | 100 µM | 171.1 ± 40.7 | Rats serum protease | HPLC | Rats serum | In Vitro | None | None | Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice | |||
| 29685037 | 2018 | Ang-AA | 7 | Acetylation | Amidation | Linear | L | None | Ang-(1-7) analogs | Antifibrosis, Antihypertension, Antihypertrophic and Antiarrhythmia Activities | After a 30 min incubation at 37°C | 0.1 mM | 135.7 ± 37.7 | ACE, LAP and NEP | HPLC | PBS solution containing all three hydrolytic enzymes (0.5 IU/mL), ACE, LAP and NEP | In Vitro | None | None | Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice | |||
| 29685037 | 2018 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease brain ROS production and inflammation in preclinical models of HF | After a 30 min incubation at 37°C | 0.1 mM | 9.2 ± 0.5 | ACE, LAP and NEP | HPLC | PBS solution containing all three hydrolytic enzymes (0.5 IU/mL), ACE, LAP and NEP | In Vitro | None | None | Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice | |||
| 29685037 | 2018 | Ang-AA | 7 | Acetylation | Amidation | Linear | L | None | Ang-(1-7) analogs | Antifibrosis, Antihypertension, Antihypertrophic and Antiarrhythmia Activities | At 2, 4, 6, 8, 10, 15, 50, 120, 240, 480, 720 and 960 min after the injection, 100 µL of blood were sampled from each animal through the caudal vein | 400 µg/kg | 238.7 ± 61.3 | Rats serum protease | RP-HPLC | Rats serum | In Vivo | None | None | Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice | |||
| 29673717 | 2018 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | 3.6 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | PDB id: 7MLL | None | EC50 (pM) = 1.8 ± 0.8 | |||
| 29673717 | 2018 | Liraglutide | 32 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | 15.4 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | N.A. | |||
| 29673717 | 2018 | I-1 | 30 | Free | Amidation | Linear | L | Cys17-Gly8-GLP-1(7-36) modification and fatty acid modification through Mal referred to as X1 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | EC50(pM) = 5.6 ± 1.1 | |||
| 29673717 | 2018 | I-2 | 30 | Free | Amidation | Linear | L | Cys17-Gly8-GLP-1(7-36) modification and fatty acid modification through Mal referred to as X2 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | EC50(pM) = 14.3 ± 2.0 | |||
| 29673717 | 2018 | I-3 | 30 | Free | Amidation | Linear | L | Cys17-Gly8-GLP-1(7-36) modification and fatty acid modification through Mal referred to as X3 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | EC50(pM) = 26.3 ± 2.5 | |||
| 29673717 | 2018 | I-4 | 31 | Free | Amidation | Linear | L | Cys37-Gly8-GLP1(7-36) modification and fatty acid conjugation through Mal at Cys37 referred to as X1 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/ MS | Rats plasma | In Vitro | None | None | EC50(pM) = 6.1 ± 1.9 | |||
| 29673717 | 2018 | I-5 | 31 | Free | Amidation | Linear | L | Cys37-Gly8-GLP1(7-36) modification and fatty acid conjugation through Mal at Cys37 referred to as X2 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/ MS | Rats plasma | In Vitro | None | None | EC50(pM) = 9.3 ± 1.1 | |||
| 29673717 | 2018 | I-6 | 31 | Free | Amidation | Linear | L | Cys37-Gly8-GLP1(7-36) modification and fatty acid conjugation through Mal at Cys37 referred to as X3 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/ MS | Rats plasma | In Vitro | None | None | EC50(pM) = 19.8 ± 2.1 | |||
| 29669811 | 2018 | 125I-3E8.G4S | 278 | 125I labelled | Free | Linear | L | 125I-labeled, VH and VL joined by G4S linker | Derived from the 3E8 antibody | Optimizes biophysical properties, serum half-life and high-specificity tumor imaging | Blood samples (5 μl) were drawn from the saphenous vein by puncture, using a 30-gauge syringe needle, at 0.5, 1, 5, 24, 48, and 72 h postinjection for 3E8.G4S | 5 μCi | 0.67 | Mice blood protease | Radioiodination assay | Mice blood sample | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/instance/5995523/bin/supp_RA118.002538_136163_1_supp_109995_p6kvvq.pdf | None | KD of 3.6 nM for 3E8.G4S | |||
| 29669811 | 2018 | 125I-3E8.G4S dimer | 561 | 125I labelled | Free | Linear | L | 125I-labeled, 2 ScFv joined by G4S linker | Derived from the 3E8 antibody | Optimizes biophysical properties, serum half-life and high-specificity tumor imaging | Blood samples (5 μl) were drawn from the saphenous vein by puncture, using a 30-gauge syringe needle, at 0.5, 1, 5, 24, 48, and 72 h postinjection for 3E8.G4S | 5 μCi | 2 | Mice blood protease | Radioiodination assay | Mice blood sample | In Vivo | None | None | KD of 3.6 nM for 3E8.G4S | |||
| 29669811 | 2018 | 125I-3E8.G4S oligomer (Trimeric) | 844 | 125I labelled | Free | Linear | L | 125I-labeled, 3 ScFv joined by G4S linker | Derived from the 3E8 antibody | Optimizes biophysical properties, serum half-life and high-specificity tumor imaging | 0.5, 1.5, 3, 6, 24, 48, and 72 h | 5 μCi | 3.3 | Mice blood protease | Radioiodination assay | Mice blood sample | In Vivo | None | None | KD of 3.6 nM for 3E8.G4S | |||
| 29669811 | 2018 | 125I-3E8.G4S oligomer (Tetrameric) | 1127 | 125I labelled | Free | Linear | L | 125I-labeled, 4 ScFv joined by G4S linker | Derived from the 3E8 antibody | Optimizes biophysical properties, serum half-life and high-specificity tumor imaging | 0.5, 1.5, 3, 6, 24, 48, and 72 h | 5 μCi | 3.3 | Mice blood protease | Radioiodination assay | Mice blood sample | In Vivo | None | None | KD of 3.6 nM for 3E8.G4S | |||
| 29656472 | 2018 | [K6T]P8 peptide | 10 | Free | Amidation | Linear | L | K6T modification | Synthetic | IL‐15 antagonist peptide | At t = 0, 5, 8, 10, 20,30, 45, 60, 90, and 120 minutes | 100 μM. | 5.88 ± 1.73 | Human synovial fluids protease | RP-HPLC | Human synovial fluids | In Vitro | None | None | IC50 values of 27.7 μM | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 151.7 | Human plasma protease | LC–MS/MS | Human plasma (Normal renal function) | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/ | None | N.A. | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 159.3 | Human plasma protease | LC–MS/MS | Human plasma (Mild renal function ) | In Vivo | None | None | N.A. | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 162.8 | Human plasma protease | LC–MS/MS | Human plasma (Moderate renal function) | In Vivo | None | None | N.A. | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 164.9 | Human plasma protease | LC–MS/MS | Human plasma (Severe renal function group) | In Vivo | None | None | N.A. | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 152.8 | Human plasma protease | LC–MS/MS | Human plasma (ESRD Renal function group) | In Vivo | None | None | N.A. | |||
| 29617109 | 2018 | RNP-DFO | 30 | Free | PLGA linked through mPEG | Linear | L | None | Synthetic | Treatment of Parkinson in mice | Blood samples were harvested from the tail vein at 0.08, 0.5, 1, 2, 4, 6, 12, and 24 h post-dosing | 50 mg/kg | More Stable | Rats plasma protease | HPLC | Rats plasma | In Vivo | None | None | N.A. | |||
| 29602308 | 2018 | P4-Chlorambucil | 7 | Free | Chlorambucil | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 21.5 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Chlorambucil | 7 | Free | Chlorambucil | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 12.4 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Melphalan | 7 | Free | Melphalan | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 24.6 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Melphalan | 7 | Free | Melphalan | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 10.6 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Bendamustine | 7 | Free | Bendamustine | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 19.3 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Bendamustine | 7 | Free | Bendamustine | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 15.4 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Chlorambucil-PEG-AuNP | 7 | Free | Chlorambucil | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 21 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Chlorambucil-PEG-AuNP | 7 | Free | Chlorambucil | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 20 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Melphalan-PEG-AuNP | 7 | Free | Melphalan | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 22 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Melphalan-PEG-AuNP | 7 | Free | Melphalan | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 18.3 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Bendamustine-PEG-AuNP | 7 | Free | Bendamustine | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 22.3 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Bendamustine-PEG-AuNP | 7 | Free | Bendamustine | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 18.3 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29577579 | 2018 | Fc‐apelin‐13 fusion protein | 12 | Fc linked by (GGGS)3 linker at N terminus | Free | Linear | L | None | Fc‐apelin‐13 fusion protein | Antidiabetes and Anti‐Heart Failure Activities | About 10 μL of blood was collected at each time point of 0, 1, 2, 4, 8, 24, 32, 48, 56, and 72 hours after administration | 5 mg/kg | ~33 | Mice Plasma Protease | Western blotting | Mice plasma | In Vivo | None | None | EC50 values of the Fc‐apelin‐13 fusion protein= 12.0 ± 1.1 nM for cAMP suppression | |||
| 29550018 | 2018 | DTβ4 | 88 | Free | Free | Linear | L | Dimerization using GS linker | Dimeric Tβ4 | Protects post-ischemic cardiac function | N.A. | 50 μg | 59.1 | Mouse serum protease | HPLC | Mouse serum | In Vivo | Uniprot id: P62328 | None | In scratch wound and Boyden chamber assays, the migration of HUVECs induced by DTβ4 was significantly higher than that induced by wild-type Tβ4 at each applied concentration | |||
| 29550018 | 2018 | Tβ4 | 43 | Free | Free | Linear | L | None | Synthetic | Protects post-ischemic cardiac function | N.A. | 50 μg | 53.3 | Mouse serum protease | HPLC | Mouse serum | In Vivo | Uniprot id: P62328 | None | In scratch wound and Boyden chamber assays, the migration of HUVECs induced by DTβ4 was significantly higher than that induced by wild-type Tβ4 at each applied concentration | |||
| 29540315 | 2018 | GUB09-123 | 33 | Free | Amidation | Linear | L | None | Synthetic | GLP-1/GLP-2 co-agonist | Blood samples were collected by decapitation of the animals at nine different time points after administration (0.25, 0.5, 0.75, 1, 2, 4, 6, 10 and 24 hours, n=3 for each time point) | 800nmol/kg | 0.9 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | GLP-1R, EC50 (nM) = 0.07 | |||
| 29540315 | 2018 | GUB09-145 | 34 | Free | Amidation | Linear | L | Lipidation at Lys14 (C16-yE-) | GUB09-123 analogue | GLP-1/GLP-2 co-agonist | Blood samples were collected by decapitation of the animals at nine different time points after administration (0.25, 0.5, 0.75, 1, 2, 4, 6, 10 and 24 hours, n=3 for each time point) | 800nmol/kg | 2.7 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | GLP-1R, EC50 (nM) = 0.17 | |||
| 29536338 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | Antidiabetes | GLP-1R agonist | Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h). | 0.5 mg | 145 | Human plasma protease | LC–MS/MS | Human plasma (Japanese subjects) | In Vivo | None | None | N.A. | |||
| 29536338 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | Antidiabetes | GLP-1R agonist | Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h). | 1 mg | 163 | Human plasma protease | LC–MS/MS | Human plasma (Japanese subjects) | In Vivo | None | None | N.A. | |||
| 29536338 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | Antidiabetes | GLP-1R agonist | Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h). | 0.5 mg | 159 | Human plasma protease | LC–MS/MS | Human plasma (Caucasian subjects) | In Vivo | None | None | N.A. | |||
| 29536338 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | Antidiabetes | GLP-1R agonist | Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h). | 1 mg | 167 | Human plasma protease | LC–MS/MS | Human plasma (Caucasian subjects) | In Vivo | None | None | N.A. | |||
| 29531858 | 2018 | [68Ga]Ga-DOTA-RGD | 8 | CH2CO chemical group attached, DOTA conjugated with Lys1 | CCPEG | Cyclic (C2-C6 Disulfide Bond) | L | 68Ga labelling | Synthetic | PET imaging agent to visualize and quantify angiogenesis | Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection | N.A. | 24.6 (Slow Phase) | NHP plasma protease | UV-HPLC and LC-ESI-MS | NHP uterus plasma without NC-100717 | N.A. | None | None | N.A. | |||
| 29531858 | 2018 | [68Ga]Ga-DOTA-RGD | 8 | CH2CO chemical group attached, DOTA conjugated with Lys1 | CCPEG | Cyclic (C2-C6 Disulfide Bond) | L | 68Ga labelling | Synthetic | PET imaging agent to visualize and quantify angiogenesis | Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection | N.A. | 1.1 (Fast Phase) | NHP plasma protease | UV-HPLC and LC-ESI-MS | NHP uterus plasma without NC-100717 | N.A. | None | None | N.A. | |||
| 29531858 | 2018 | [68Ga]Ga-DOTA-RGD | 8 | CH2CO chemical group attached, DOTA conjugated with Lys1 | CCPEG | Cyclic (C2-C6 Disulfide Bond) | L | 68Ga labelling | Synthetic | PET imaging agent to visualize and quantify angiogenesis | Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection | 1 mg/kg | 26.4 (Slow Phase) | NHP plasma protease | UV-HPLC and LC-ESI-MS | NHP uterus plasma after administration of NC-100717 (1 mg/kg) | In Vivo | None | None | N.A. | |||
| 29531858 | 2018 | [68Ga]Ga-DOTA-RGD | 8 | CH2CO chemical group attached, DOTA conjugated with Lys1 | CCPEG | Cyclic (C2-C6 Disulfide Bond) | L | 68Ga labelling | Synthetic | PET imaging agent to visualize and quantify angiogenesis | Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection | 1 mg/kg | 1.9 (Fast Phase) | NHP plasma protease | UV-HPLC and LC-ESI-MS | NHP uterus plasma after administration of NC-100717 (1 mg/kg) | In Vivo | None | None | N.A. | |||
| 29528634 | 2018 | GLP2-2G | 33 | Free | Free | Linear | L | Ala2 was substituted with Gly | GLP-2 analogue | Treatment of Short Bowel Syndrome | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 25 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.035 ± 0.003 | |||
| 29528634 | 2018 | GLP-2 analog 8 | 42 | Free | Amidation | Cyclic (C17-C24 Stapled Using Linker L3) | L | None | GLP-2 analogues | Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 2.7 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.068 ± 0.003 | |||
| 29528634 | 2018 | GLP-2 analog 9 | 42 | Free | Amidation | Cyclic (C9-C16 Stapled Using Linker L3) | L | None | GLP-2 analogues | Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 3.1 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.041 ± 0.005 | |||
| 29528634 | 2018 | GLP-2 analog 10 | 42 | Free | Amidation | Cyclic (C11-C18 Stapled Using Linker L3) | L | None | GLP-2 analogues | Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 4.7 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.028 ± 0.002 | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | Serial blood samples were taken from each animal via temporary indwelling tail vein cannulae at 5, 10, 20, 30, 60, 120, 180, and 240 min postdose, | 5 mg/kg | 78 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 29517911 | 2018 | 2d | 13 | Acetylation | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | Serial blood samples were taken from each animal via temporary indwelling tail vein cannulae at 5, 10, 20, 30, 60, 120, 180, and 240 min postdose, | 5 mg/kg | 48 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | Serial blood samples were taken from each animal via temporary indwelling tail vein cannulae at 5, 10, 20, 30, 60, 120, 180, and 240 min postdose, | 10 mg/kg | N.A. | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29517911 | 2018 | 2d | 13 | Acetylation | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | The animals were sacrificed 15 min, 1 h, 4 h, 8 h, 24 h, 48, and 96 h after injection | 2 mg/mL | 39 ± 2 | Rabbit eye plasma protease | HPLC | Rabbit eye plasma | In Vivo | None | None | Ki Values (nM) = 3,400 ± 200 against PKal from Rabbit | |||
| 29517911 | 2018 | 4b | 17 | Acetylation | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C7, C14 By 1,3,5 Trismethylbenzene) | L | HArg, Aze substituitions | synthetic | Antidiabetes (Treatment of Diabetic Macular Edema) | The animals were sacrificed 15 min, 1 h, 4 h, 8 h, 24 h, 48, and 96 h after injection | 2 mg/mL | ~22 | Rabbit eye plasma protease | HPLC | Rabbit eye plasma | In Vivo | None | None | Ki Values (nM) = ∼2,650 against PKal from Rabbit | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Human vitreous protease | LC-MS/MS | Human vitreous | In Vitro | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 29517911 | 2018 | 2d | 13 | Acetylation | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Human vitreous protease | LC-MS/MS | Human vitreous | In Vitro | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Human vitreous protease | LC-MS/MS | Human vitreous | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 29517911 | 2018 | 2d | 13 | Acetylation | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | 1.5 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 29517911 | 2018 | 2d | 13 | Acetylation | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | 2.8 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes | 24 h at 37 °C | 0.16 mM | >24 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 29517911 | 2018 | 2d | 13 | Acetylation | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions | 2a analogue | Antidiabetes | 24 h at 37 °C | 0.16 mM | >24 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes | 24 h at 37 °C | 0.16 mM | 7 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29516741 | 2018 | Liraglutide | 32 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Serial blood samples were collected at the 0, 0.083, 0.25, 0.5, 1, 2, 4, 7 and 24-h time points | 30 μg/kg | 6.59 | Monkeys plasma protease | LC-MS/MS | Monkeys plasma | In Vivo | None | None | N.A. | |||
| 29464007 | 2018 | 99mTc-F1A | 18 | 99mTc-HHEDEG | Free | Cyclic (C-C Disulfide Bond In C Terminal) | L | Interconnected through a diethylene glycol (DEG) spacer | Fibrin-specific natural peptide analogue | 99MTC-F4A is a high-avidity prototype probe for characterizing thrombus in Lvads | Serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter | N.A. | 124.7 ± 41.3 (T1/2b Elimination Half Life) | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | 99mTc-F4A probe was not displaced by F1A | |||
| 29464007 | 2018 | 99mTc-F1A | 18 | 99mTc-HHEDEG | Free | Cyclic (C-C Disulfide Bond In C Terminal) | L | Interconnected through a diethylene glycol (DEG) spacer | Fibrin-specific natural peptide analogue | 99MTC-F4A is a high-avidity prototype probe for characterizing thrombus in Lvads | Serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter | N.A. | 174.2 ± 26.2 (T1/2b Elimination Half Life) | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | Kd ~10.2 µM for 99mTc-F1A (bound to uniform fibrin clots in PBS) | |||
| 29461833 | 2018 | Pyr analogue 2 | 13 | Free | Free | Cyclic (X1-X5 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 0.8 ± 0.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 5.7 ±3.5 for 2 | |||
| 29461833 | 2018 | Pyr analogue 3 | 13 | pGlu = Pyroglutamate | Free | Cyclic (Rx2-X6 Bond) | L | X= allylglycine, Rx=Na-ally-arginine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 2.2 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 4.5 ±1.4 for 3 | |||
| 29461833 | 2018 | Pyr analogue 4 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X1-X6 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 0.7 ± 0.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 523 ±165 for 4L | |||
| 29461833 | 2018 | Pyr analogue 5 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X3-X7 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 3.9 ± 0.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 3 ±0.1 for 5 | |||
| 29461833 | 2018 | Pyr analogue 6 | 13 | pGlu = Pyroglutamate | Free | Cyclic (Rx4-X8 Bond) | L | X= allylglycine, Rx=Na-ally-arginine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 7.7 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 9.1 ±1.4 for 6 | |||
| 29461833 | 2018 | Pyr analogue 7 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X4-X8 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 9.9 ± 1.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 489 ±186 for 7L | |||
| 29461833 | 2018 | Pyr analogue 8 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X5-X9 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 3.5 ± 0.8 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 3.9 ±1.4 for 8L | |||
| 29461833 | 2018 | Pyr analogue 9 | 13 | pGlu = Pyroglutamate | Free | Cyclic (Sx6-X10 Bond) | L | X= allylglycine, Sx=Na-allyl-serine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | >24 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 41 ±4 for 9L | |||
| 29461833 | 2018 | Pyr analogue 10 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X6-X10 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 4.1 ±0.8 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 194 ±70 for 10L | |||
| 29461833 | 2018 | Pyr analogue 11 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X7-X11 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 6.6 ±0.4 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 1.4 ±0.4 for 11 | |||
| 29461833 | 2018 | Pyr analogue 12 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X8-X12 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 4.6 ±0.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 14 ±7 for 12 | |||
| 29461833 | 2018 | Pyr analogue 13 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X9-X13 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 8.6 ±0.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 1.1 ±0.1 for 13 | |||
| 29461833 | 2018 | Pyr analogue 14 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X10-X14 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 7.8 ±1.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 445 ±62 for 14L | |||
| 29461833 | 2018 | Pyr analogue 15 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X9-X13 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 6.8 ±1.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 0.15 ±0.01 for 15 | |||
| 29436835 | 2018 | PIE 12-trimer | 48 | Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 0.6 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 2.1 ± 0.28 (antiviral potency) | |||
| 29436835 | 2018 | PIE 12-trimer | 48 | Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 0.8 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 2.1 ± 0.28 (antiviral potency) | |||
| 29436835 | 2018 | Palm-PIE12-trimer | 48 | Palm-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1.2 mg/kg | 1.8 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.54 ± 0.029 (antiviral potency) | |||
| 29436835 | 2018 | Palm-PIE12-trimer | 48 | Palm-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1.2 mg/kg | 2.2 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.54 ± 0.029 (antiviral potency) | |||
| 29436835 | 2018 | C16-PIE12-trimer | 48 | C16-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 0.9 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.11 ± 0.012 (antiviral potency) | |||
| 29436835 | 2018 | C16-PIE12-trimer | 48 | C16-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 1.2 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.11 ± 0.012 (antiviral potency) | |||
| 29436835 | 2018 | C18-PIE12-trimer | 48 | C18-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 1.1 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.087 ± 0.012(antiviral potency) | |||
| 29436835 | 2018 | C18-PIE12-trimer | 48 | C18-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 1.4 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.087 ± 0.012(antiviral potency) | |||
| 29436835 | 2018 | Chol-PIE12-trimer | 48 | Chol-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 1.8 | Rats plasma protease | UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.022 ± 0.0018 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PIE12-trimer | 48 | Chol-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 2.7 | Rats plasma protease | UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.022 ± 0.0018 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PIE12-trimer | 48 | Chol-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 1.6 | Rats plasma protease | UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.022 ± 0.0018 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PIE12-trimer | 48 | Chol-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 3.9 | Rats plasma protease | UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.022 ± 0.0018 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PEG5k-PIE12-trimer | 48 | Chol-PEG5K-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 5.6 | Rats plasma protease | UHPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.030 ± 0.0010 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PEG5k-PIE12-trimer | 48 | Chol-PEG5K-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 7.2 | Rats plasma protease | UHPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.030 ± 0.0010 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 3.3 | Rats plasma protease | Ultra-High Performance Liquid Chromatography (UHPLC) | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 5.4 | Rats plasma protease | Ultra-High Performance Liquid Chromatography (UHPLC) | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | One ml blood samples were collected by venipuncture of a femoral vein at 0.083, 0.167, 0.25, 0.5, 1, 2, 4, 8, 16 and 24 h | 1 mg/kg | 7.4 | Male cynomolgus monkeys plasma protease | LC-MS | Male cynomolgus monkeys plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | Plasma samples were collected pre-dose and 0.25, 0.5, 1, 2, 4, 8, 16, 24, 48 and 72 h post-dose | 3 mg/kg | 18.8 | Male cynomolgus monkeys plasma protease | LC-MS | Male cynomolgus monkeys plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29433929 | 2018 | CT105 | 38 | Amidation | Acetylation | Linear | L | None | Synthetic | Antiviral (against HIV Virus) | Serial blood samples were collected from each animal before injection and at 0.08, 0.25, 0.5, 1, 2, 4 and 8 h after injection | 6 mg/kg | 2.7 | Rats plasma protease | IC-ELISA | Rats plasma | In Vivo | None | None | IC50(nM) =0.26 against HIV variant R3A | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | Day 1 (cycle 1 - 28days) | 6 mg/m2 | 2.3 | Human plasma protease | ELISA | Human plasma | In Vivo | https://www.lens.org/lens/patent/124-764-042-412-641/fulltext?l=en | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 12 mg/m2 | 2.1 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 24 mg/m2 | 3.2 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 48 mg/m2 | 4.9 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 96 mg/m2 | 6 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 6 mg/m2 | 2.8 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 12 mg/m2 | 2 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 24 mg/m2 | 3.7 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 48 mg/m2 | 4.6 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 96 mg/m2 | 8.5 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29421564 | 2018 | HDL-SP | 34 | MPB-Mal modified, additional cysteine residue on N-terminus of SP | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis in Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 117 | Human serum protease | ELISA | Human serum | In Vitro | None | None | N.A. | |||
| 29421564 | 2018 | SP | 11 | Free | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis in Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 2 | Human serum protease | ELISA | Human serum | In Vitro | None | None | N.A. | |||
| 29421564 | 2018 | HDL-SP | 34 | MPB-Mal modified, additional cysteine residue on N-terminus of SP | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis in Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 30 | Diabetic rats serum protease | ELISA | Diabetic rats serum | In Vitro | None | None | N.A. | |||
| 29421564 | 2018 | SP | 11 | Free | Free | Linear | L | None | Synthetic | Therapeutic Regeneration By Facilitating Mobilization Of Endogenous Stem Cells From Bone Marrow To The Injured Sites | 0 to 72 h at 37°C | 5 nmol | 1.7 | Diabetic rats serum protease | ELISA | Diabetic rats serum | In Vitro | None | None | N.A. | |||
| 29421564 | 2018 | SP | 11 | Free | Free | Linear | L | None | Synthetic | Therapeutic Regeneration By Facilitating Mobilization Of Endogenous Stem Cells From Bone Marrow To The Injured Sites | 0 to 72 h at 37°C | 5 nmol | 0.8 | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 29421564 | 2018 | HDL-SP | 34 | MPB-Mal modified, additional cysteine residue on N-terminus of SP | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis In Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 60 | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 29421564 | 2018 | SP | 11 | Free | Free | Linear | L | None | Synthetic | Therapeutic Regeneration By Facilitating Mobilization Of Endogenous Stem Cells From Bone Marrow To The Injured Sites | 0 to 72 h at 37°C | 5 nmol | 5 | Diabetic rats serum protease | ELISA | Diabetic rats serum | In Vitro | None | None | N.A. | |||
| 29421564 | 2018 | HDL-SP | 34 | MPB-Mal modified, additional cysteine residue on N-terminus of SP | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis In Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 96 | Diabetic rats serum protease | ELISA | Diabetic rats serum | In Vitro | None | None | N.A. | |||
| 29391187 | 2018 | Peptide 6 | 41 | Free | ABD domain from Streptococcal G strain , Amidation | Linear | L | None | [Ser8]-GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein using a heparinised syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 h postdose | 0.01 mg/kg | 5.8 ± 0.4 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | EC50(nM) = 1.7 | |||
| 29391187 | 2018 | Peptide 6 | 41 | Free | ABD domain from Streptococcal G strain , Amidation | Linear | L | None | [Ser8]-GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein using a heparinised syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 h postdose | 0.01 mg/kg | 5.4 ± 0.3 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | EC50(nM) = 1.7 | |||
| 29335522 | 2018 | PAK2 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Role in PDAC cancer invasion and metastasis | N.A. | N.A. | 4.5 | Miapaca-2 cell lysate protease | Western blotting | Miapaca-2 cells lysate after PKM2 depletion (treated with 20 μg/ml cycloheximide (CHX)) | In Vitro | None | None | N.A. | |||
| 29335522 | 2018 | PAK2 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Role in PDAC cancer invasion and metastasis | N.A. | N.A. | >24 | Miapaca-2 cell lysate protease | Western blotting | Miapaca-2 cells lysate with PKM2 expression (treated with 20 μg/ml cycloheximide (CHX)) | In Vitro | None | None | N.A. | |||
| 29329072 | 2018 | Compound 1 | 8 | Free | Amidation | Linear | L | None | NMU-analogs | Regulation of Feeding Behavior, the stress response and nociception | 37 °C | 112 µM | 4.3 ± 0.2 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 38.9, IC50(nM) = 0.78 for hNMUR1 and EC50(nM) = 30.8, IC50(nM) = 1.7 for hNMUR2 | |||
| 29329072 | 2018 | Compound 2 | 8 | Acetylation | Amidation | Linear | L | None | NMU-analogs | Regulation of Feeding Behavior, the stress response and nociception | 37 °C | 112 µM | 117.8 ± 0.7 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | N.A. | |||
| 29329072 | 2018 | Compound 16 | 7 | Acetylation, 7-OH-Tic = 7-hydroxy-L-1,2,3,4- tetrahydroisoquinoline-3-carboxylic acid at position 1 | Amidation | Linear | L | None | NMU-analogs | Regulation of Feeding Behavior, the stress response and nociception | 37 °C | 112 µM | 109.8 ± 3.1 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 5.1, IC50(nM) = 0.037 for hNMUR1 and EC50(nM) = 13.4, IC50(nM) = 12.3 for hNMUR2 | |||
| 29329072 | 2018 | Compound 18 | 8 | Ac-2'NaI = 2’-naphtylalanine at position 1 | Amidation | Linear | L | None | NMU-analogs | Regulation of Feeding Behavior, the stress response and nociception | 37 °C | 112 µM | 128.8 ± 1.7 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 1.6, IC50(nM) = 0.88 for hNMUR1 and EC50(nM) = 1.6, IC50(nM) = 5.6 for hNMUR2 | |||
| 29329072 | 2018 | Compound 28 | 8 | Acetylation | Amidation | Linear | L | Dmt = 2',6'-dimethyltyrosine at position 4 | NMU-analogs | Regulation Of Feeding Behavior, The Stress Response And Nociception | 37 °C | 112 µM | 253.5 ± 6 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 7.7, IC50(nM) = 0.36 for hNMUR1 and EC50(nM) = 3675, IC50(nM) = 1857 for hNMUR2 | |||
| 29329072 | 2018 | Compound 32 | 8 | Acetylation | Amidation | Linear | L | N(benzyl)Gly modfication at position 4 | NMU-analogs | Regulation Of Feeding Behavior, The Stress Response And Nociception | 37 °C | 112 µM | 837.4 ± 27.8 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 172.2, IC50(nM) = 83.1 for hNMUR1 and EC50(nM) = 1278, IC50(nM) = 1019 for hNMUR2 | |||
| 29329072 | 2018 | Compound 38 | 8 | Acetylation | Amidation | Linear | L | N(4-OH-Phenethyl)Gly at position 4 | NMU-analogs | Regulation Of Feeding Behavior, The Stress Response And Nociception | 37 °C | 112 µM | 1096.1 ± 56.1 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 216.6, IC50(nM) = 3.9 for hNMUR1 and EC50(nM) = 339.2, IC50(nM) = 206.9 for hNMUR2 | |||
| 29329072 | 2018 | Compound 42 | 7 | Acetylation | Amidation | Linear | L | Oic = octahydroindole carboxylic acid modification between R5 and R6 | NMU-analogs | Regulation Of Feeding Behavior, The Stress Response And Nociception | 37 °C | 112 µM | 1426.1 ± 67.4 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 28.8, IC50(nM) = 11.2 for hNMUR1 and EC50(nM) = 1.8, IC50(nM) = 13.9 for hNMUR2 | |||
| 29282303 | 2018 | SCRAP-mCherry | N.A. | DD | mCherry | N.A. | L | None | Synthetic | Affects Antigen Presentation | N.A. | N.A. | 41 ± 5 | El4 cells protease | BD cytoflex flow cytometry | EL4 cells after Shield-1 removal | N.A. | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 4.588 | Rats serum protease | LC-MS | Rats serum after 50 mg/kg sHDL | In Vivo | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 4.25 | Rats serum protease | LC-MS | Rats serum after 2.5 mg/kg sHDL-PEG2k | In Vivo | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 7.14 | Rats serum protease | LC-MS | Rats serum after 5 mg/kg sHDL-PEG2k | In Vivo | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 5.05 | Rats serum protease | LC-MS | Rats serum after 2.5 mg/kg sHDL-PEG5k | In Vivo | None | None | N.A. | |||
| 29122441 | 2018 | FAMP1 | 18 | FAM | Amidation | Cyclic (C10-C13 Disulfide Bond) | L | None | Synthetic | N.A. | 37 C | 10 µM | 7 | 293T cells lysates protease | RP-HPLC-FD | 293T cells lysate | In Vitro | None | None | N.A. | |||
| 29122441 | 2018 | FAMP1 | 18 | FAM | Amidation | Cyclic (C10-C13 Disulfide Bond) | L | None | Synthetic | Increases Half Life | 37 C | 10 µM | 21 | 293T cells lysates protease | RP-HPLC-FD | 293T cells lysate | In Vitro | None | None | N.A. | |||
| 29122441 | 2018 | FAM-P2 | 18 | FAM | Amidation | Cyclic (C10-C14 Disulfide Bond) | L | None | Synthetic | N.A. | 37 C | 10 µM | 16 | 293T cells lysates protease | RP-HPLC-FD | 293T cells lysate | In Vitro | None | None | N.A. | |||
| 29122441 | 2018 | FAM-P2.L5 | 18 | FAM | Amidation | Cyclic (C10-C14 Disulfide Bond) | L | 1,3-bis(bromomethyl)benzene linker (L5) for stapling i, i+4 spacing | Synthetic | Increases Half Life | 37 C | 10 µM | 10 | 293T cells lysates protease | RP-HPLC-FD | 293T cells lysate | In Vitro | None | None | N.A. | |||
| 29104145 | 2018 | AS16-Fc | 7 | Free | Fc | Linear | L | None | Fusion protein of AS16 and Fc | Antitumor | Blood samples were taken at 0 min, 5min,30 min, 2 h, 4 h, 6 h, 8 h, 10 h and 24h from orbit | 45 mg/kg | 231 | Rats serum protease | ELISA | Rats serum | In Vivo | https://sci-hub.st/10.1016/j.peptides.2010.01.007 | None | The activity value of AS16-Fc, as observed in vivo, is its significant inhibition of tumor growth and reduction in M2-polarized macrophages and vessel density in the MCA-205 tumor model | |||
| 29104145 | 2018 | AS16 | 7 | Free | Free | Linear | L | None | Synthetic | Antitumor | Blood samples were taken at 0 min, 5min,30 min, 2 h, 4 h, 6 h, 8 h, 10 h and 24h from orbit | 45 mg/kg | 1 | Rats serum protease | ELISA | Rats serum | In Vivo | None | None | The activity value of AS16-Fc, as observed in vivo, is its significant inhibition of tumor growth and reduction in M2-polarized macrophages and vessel density in the MCA-205 tumor model | |||
| 29051342 | 2018 | 68Ga-NOTA-UBI | 13 | 68Ga-NOTA | Free | Linear | L | None | Synthetic | Nuclear Imaging of Infectious Diseases | Image acquisition started 30, 60 and 120 min after IV | N.A. | 29 | NHP blood protease | PET-CT imaging | NHP blood sample | In Vivo | None | None | N.A. | |||
| 28954201 | 2018 | RTD-1 | 18 | Free | Free | Cyclic | L | None | Derived from rhesus | Attenuates Endotoxin-Induced Acute Lung Injury | Received RTD-1 at 0, 0.2, 1,5, or 25 mg/kg 0.5 hour before LPS challenge | 5 or 25 mg/kg | 30 (Terminal Half Life) | Mice plasma protease | LC-MS | Mice plasma (LPS-challenged ) | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3024902/ | None | IC50= 4.5 μg/ml | |||
| 28948296 | 2018 | GIP(3-30)NH2 | 27 | Free | Amidation | Linear | L | None | GIP analogue | GIP receptor antagonist | Blood samples were drawn 30, 15 and 0 min before and 20, 25, 30, 40, 50, 60, 67, 70, 75, 80, 95 and 125 min after the start of the GIP(3-30)NH2 infusion | 800 pmol/kg/min | 7.6 ± 1.4 (Elimination Half Life) | Human plasma protease | RIA | Human plasma | In Vivo | None | None | IC50 value of 87.6 nmol/l | |||
| N.A. | 2018 | TRAIL-ASPD | 347 | Free | C-type lectin domain of human SP-D joined with Strep-tag II using linker | Linear | L | None | Trail-SPD Fusion Protein | Therapeutic, diagnostic and/or research applications | Serum samples were collected after several time points (predose, 5 min., 30 min., 2H, 6H and 24H) | 10 μg | 7 | CD1 mice serum protease | ELISA | CD1 mice serum | In Vivo | None | EP 17197297 A | TRAIL-SPD fusion proteins induced no hepatotoxic effects, even if ligands were secondarily cross-linked by antibodies | |||
| N.A. | 2018 | TRAIL-ASPD_F335D | 347 | Free | C-type lectin domain of human SP-D joined with Strep-tag II using linker | Linear | L | Phe355 -> Asp355 modification | Trail-SPD Fusion Protein | Therapeutic, diagnostic and/or research applications | Serum samples were collected after several time points (predose, 5 min., 30 min., 2H, 6H and 24H) | 10 μg | 14 | CD1 mice serum protease | ELISA | CD1 mice serum | In Vivo | None | EP 17197297 A | Five hours of co-incubation of primary human hepatocytes with trimeric TRAIL-ASPD_F335D together with chemotherapeutic drugs induced no caspase activity (E) | |||
| N.A. | 2018 | Example 7 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, B3E, desB27, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 44 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 10.5 | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27 modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 45 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27 modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 52 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Prior Art analogue 2 | 50 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B28D,modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 121 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Prior Art analogue 2 | 50 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B28D, modifcations | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 159 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27,modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 29 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Example 5 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2×OEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27, modifcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 35 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 7.6 | |||
| N.A. | 2018 | Example 9 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, A21A, B3Q, desB27, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 30 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 16.7 | |||
| N.A. | 2018 | Example 7 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, B3E, desB27, modififcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 30 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 10.5 | |||
| N.A. | 2018 | Example 4 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2×OEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B3E, desB27,modificaitons | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 31 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 9.3 | |||
| N.A. | 2018 | Prior Art analogue 2 | 50 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B28D, modifcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 45 | SD rats plasma protease | ELISA | SD rats plasma with 3 Zinc Ion Per Hexamer | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Prior Art analogue 3 | 50 | Free | B29K(N(Eps)Tetradecanedioyl), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 50 | SD rats plasma protease | ELISA | SD rats plasma with 3 Zinc Ion Per Hexamer | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Example 15 | 49 | Free | B29K(N(Eps)Hexadecanedioyl-gGlu-2×OEG), desB30 modifications | cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27, modificaitons | Insulin Derivative | Treatment Of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 67 | SD rats plasma protease | ELISA | SD rats plasma with Zinc Ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 1.8 | |||
| N.A. | 2018 | Example 23 | 49 | Free | B29K(N(Eps)Hexadecanedioyl-4×gGlu), desB30 modifications | cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3Q, desB27, modifications | Insulin Derivative | Treatment Of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 55 | SD rats plasma protease | ELISA | SD rats plasma with Zinc Ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 1.54 | |||
| N.A. | 2018 | Prior Art analogue 7 | 50 | Free | B29K(N(Eps)Hexadecanedioyl-gGlu), desB30 modifications | cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,modifications | Insulin Derivative | Treatment Of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 200 | SD rats plasma protease | ELISA | SD rats plasma with 3 Zinc Ion Per Hexamer | In Vivo | None | US 201615754342 A | N.A. | |||
| 29633613 | 2018 | ThXylC | N.A. | Free | Free | Linear | L | None | Obtained from the soluble fractions of the recombinant E. coli BL21(DE3) cells | β-xylosidase | 65 °C | N.A. | 8.9 (Activity Half Life) | N.A. | N.A. | ThXylC | In Vitro | None | None | N.A. | |||
| 29633613 | 2018 | ThXylC-ELK | N.A. | Free | ELK16 short peptide was introduced to the C-terminus of ThXylC | Linear | L | None | Obtained from the soluble fractions of the recombinant E. coli BL21(DE3) cells | β-xylosidase | 65 °C | N.A. | 54.8 (Activity Half Life) | N.A. | N.A. | ThXylC-ELK | In Vitro | None | None | N.A. | |||
| 29316656 | 2018 | [125I]-Az | 21 | Free | Free | Linear | L | 125I labeld at His9 | Derived from Azemiops feae (Fea's viper) | Local muscle relaxant | Animal blood samples were taken from the orbital sinus 5, 15, 30, 60 min and 1, 2, 4 and 24 h after [125I]-Az administration | 0.25 mg/kg | 0.3 (Excretion Half Life) | ICR mice blood protease | Radioactivity assay | ICR mice blood | In Vivo | None | None | LD50 of Az (0.51 mg/kg) | |||
| 29316656 | 2018 | [125I]-Az | 21 | Free | Free | Linear | L | 125I labeld at His9 | Derived from Azemiops feae (Fea's viper) | Local muscle relaxant | Animal blood samples were taken from the orbital sinus 5, 15, 30, 60 min and 1, 2, 4 and 24 h after [125I]-Az administration | 0.5 mg/kg | 0.68 (Excretion Half Life) | ICR mice blood protease | Radioactivity assay | ICR mice blood | In Vivo | None | None | LD50 of Az (0.51 mg/kg) | |||
| 29316656 | 2018 | [125I]-Az | 21 | Free | Free | Linear | L | 125I labeld at His9 | Derived from Azemiops feae (Fea's viper) | Local Muscle Relaxant | Animal blood samples were taken from the orbital sinus 5, 15, 30, 60 min and 1, 2, 4 and 24 h after [125I]-Az administration | 0.25 mg/kg | 0.26(Excretion Half Life) | ICR mice blood protease | Radioactivity assay | ICR mice blood | In Vivo | None | None | LD50 of Az (0.51 mg/kg) | |||
| 29316656 | 2018 | [125I]-Az | 21 | Free | Free | Linear | L | 125I labeld at His9 | Derived from Azemiops feae (Fea's viper) | Local muscle relaxant | Animal blood samples were taken from the orbital sinus 5, 15, 30, 60 min and 1, 2, 4 and 24 h after [125I]-Az administration | 0.5 mg/kg | 0.29(Excretion Half Life) | ICR mice blood protease | Radioactivity assay | ICR mice blood | In Vivo | None | None | LD50 of Az (0.51 mg/kg) | |||
| 29373818 | 2018 | fibrinolytic enzyme | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | From the marine Serratia marcescens subsp sakuensis | Clot lysis | 37 °C | N.A. | 19 (Activity Half Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 29373818 | 2018 | fibrinolytic enzyme | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | From the marine Serratia marcescens subsp sakuensis | Clot lysis | 50°C | N.A. | 29 (Activity Half Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 29385666 | 2018 | Cel9K | 997 | Free | Free | Linear | L | None | Cloned using the shot-gun method from Paenibacillus sp. X4 | Endo-β-1,4-glucanase | 50°C | N.A. | 59.2 (Activity Half Life) | N.A. | N.A. | Cel9K | In Vitro | None | None | N.A. | |||
| 29464007 | 2018 | 99mTc-F4A | 72 | Free | Free | Cyclic (PEG2000 Linkage) | L | Tetramerization using PEG2000 | Fibrin-specific natural peptide analogue | 99mTc-F4A is a high-avidity prototype probe for characterizing thrombus in LVADs | serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter | N.A. | 5.0 ± 1.9 (T1/2A Distribution Half Life) | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 29464007 | 2018 | 99mTc-F1A | 18 | 99MTC-HHEDEG-DEG | Free | Cyclic (C-C Disulfide Bond In C Terminal) | L | None | Fibrin-specific natural peptide analogue | 99mTc-F4A is a high-avidity prototype probe for characterizing thrombus in LVADs | serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter | N.A. | 8.6 ± 1.9(T1/2A Distribution Half Life) | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30063837 | 2018 | MTG variant | 331 | Free | Free | Linear | L | ClY20/62/171 modifications, ClY = 3-Chloro-Tyrosine | Derived from Streptoverticillium mobaraense | Transglutaminase | 60°C for 10 min | N.A. | 5.1-Fold Longer Than That Of The Wild-Type Enzyme (Activity Half Life) | N.A. | N.A. | Buffer | In Vitro | pdb id: 1IU4 | None | N.A. | |||
| 29263923 | 2017 | FITC-conjugated E5 | 22 | FITC conjugation | Free | Linear | L | None | Synthetic | Inhibit Breast Tumor Progression | N.A. | 40 mg/kg | ~10 | Mouse serum protease | Fluorescence assay | Mouse serum | In Vivo | None | None | E5 (0.1 μM) had high affinity towards 4T1 cells and HUVECs | |||
| 29176766 | 2017 | M10 | 10 | Free | Free | Linear | L | None | Derived from the C-terminal part of the MET receptor tyrosine kinase | Antifibrotic | Plasma samples were collected by cardiac puncture in the presence of 0.01% of Na-Citrate at time intervals of 15 min, 30 min, 1h, 2h, 4h, 6h, 12 h, 24 h, and 48 h following injection | 1 mg/kg | 6.8 ± 0.7 | Mouse plasma protease | ELISA | Mouse plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC4789156/ | None | N.A. | |||
| 29029327 | 2017 | Alu-HCG | 31 | Free | HCG | Linear | L | None | Derived from the exonization of an Alu-J element in the glycoprotein hormone alpha (GPHA) gene | Role in Placental development | N.A. | 2 mg/ml | 82.3 | Rats serum protease | ELISA | Rats serum | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1 | 5 µg | 1.8 | Human plasma protease | ELISA | Human plasma | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1 | 5 µg | 1.6 | Human plasma protease | ELISA | Human plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1 | 5 µg | 1.8 | Human plasma protease | ELISA | Human plasma with Metformin | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8 | 5 µg | 1.9 | Human plasma protease | ELISA | Human plasma | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8 | 5 µg | 1.3 | Human plasma protease | ELISA | Human plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8 | 5 µg | 1.9 | Human plasma protease | ELISA | Human plasma with Metformin | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84 | 10 µg | 1.6 | Human plasma protease | ELISA | Human plasma | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84 | 10 µg | 1.8 | Human plasma protease | ELISA | Human plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84 | 10 µg | 1.3 | Human plasma protease | ELISA | Human plasma | In Vivo | None | None | N.A. | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 1.96 ± 0.05 | Rats plasma protease | RIA | Rats plasma without NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 9.94 ± 1.40 | Rats plasma protease | RIA | Rats plasma with NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 14.9 ± 3.1 | Rats plasma protease | RIA | Rats plasma without NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 12.7 ± 1.2 | Rats plasma protease | RIA | Rats plasma with NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 10 nmol/kg | 4.34 ± 0.20 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 11 nmol/kg | 15.03 ± 4.31 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22) | 34 | Ghrelin (12-28) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 12 nmol/kg | 17.75 ± 3.99 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The activity of ghrelin(12-28)CNP(6-22) was about ten-fold less potent than that of CNP(6-22)ghrelin(12-28) | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22) | 34 | Ghrelin (12-28) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 13 nmol/kg | 14.86 ± 2.64 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The activity of ghrelin(12-28)CNP(6-22) was about ten-fold less potent than that of CNP(6-22)ghrelin(12-28) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28)amide | 34 | Free | Ghrelin(12-28)amide | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 14 nmol/kg | 14.50 ± 0.85 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22)ghrelin(12-28) | 51 | Free | Ghrelin(12-28) | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 15 nmol/kg | 18.40 ± 2.05 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | Agonist activity of ghrelin(12-28)CNP(6-22)ghrelin(12-28) was also the lowest | |||
| 28899838 | 2017 | Ghrelin(28-12)CNP(6-22)ghrelin(12-28) | 51 | Reversed sequence ghrelin(28-12) fused to the N-terminal side of CNP(6-22) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 16 nmol/kg | 17.38 ± 1.00 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | Ghrelin(28-12)CNP(6-22)ghrelin(12-28) exhibited lower potency than that of ghrelin(28-12)CNP(6-22) and CNP(6-22)ghrelin(12-28) | |||
| 28821462 | 2017 | wtFN | 183 | Free | Free | Linear | L | Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages | Synthetic | Antitumor | N.A. | 50 mg/kg | 1.1 ± 0.1 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 1FHA | None | N.A. | |||
| 28821462 | 2017 | LCFN36 | 183 | Free | Fusing the XTEN peptide of 36 amino acids through a linker | Linear | L | Gly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages | wtFN derivative | Antitumor | N.A. | 50 mg/kg | 3.5 ± 0.3 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28821462 | 2017 | LCFN72 | 183 | Free | Fusing the XTEN peptide of 72 amino acids through a linker | Linear | L | Gly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages | wtFN derivative | Antitumor | N.A. | 50 mg/kg | 5.5 ± 0.1 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28821462 | 2017 | LCFN144 | 183 | Free | Fusing the XTEN peptide of 144 amino acids through a linker | Linear | L | Gly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages | wtFN derivative | Antitumor | N.A. | 50 mg/kg | 11.3 ± 1.0 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28821462 | 2017 | LCFN288 | 183 | Free | Fusing the XTEN peptide of 288 amino acids through a linker | Linear | L | Gly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages | wtFN derivative | Antitumor | N.A. | 50 mg/kg | 10.2 ± 0.3 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28800217 | 2017 | Peptide 22 | 34 | Free | Free | Linear | L | Ala5 substituition in GpTx-1 | derived from Grammostola porteri (Tarantula spider) (Lasiodora porteri) | Potently inhibits the voltage-gated sodium channels Nav1.7/Scn9A | At 0.5, 1, 1.25, 1.5,2,3, and 4 hours post-dose, 3 mice were euthanized and then blood samples were collected | 5 mg/kg | 0.605 | Mice plasma protease | LC-MS/MS | Mice serum | In Vivo | https://sci-hub.se/10.1021/jm501765v | None | IC50=0.58-10 nM for GpTx-1 | |||
| 28799326 | 2017 | GLP-1 | 31 | Free | Free | Linear | L | None | GLP-1 | Antidiabetes | Blood samples were collected from the tail vessel in time intervals of predose 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 and 192 hours | 5 mg/kg | 0.03 | NMR1 mice serum protease | AlphaLISA | NMR1 mice serum | In Vivo | PDB id: 5VAI | None | EC50 = 5.257*10-11 | |||
| 28799326 | 2017 | WT-albumin | 585 | Free | Free | Linear | L | None | Produced by secretion from yeast | Carrier protein | Blood samples were collected from the tail vessel in time intervals of predose 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 and 192 hours | 5 mg/kg | 21.5 | NMR1 mice serum protease | AlphaLISA | NMR1 mice serum | In Vivo | None | None | KD±SD (nM) = 548.7 ±90.2 against human FcRn receptor | |||
| 28799326 | 2017 | GLP-1-PEG-WT-albumin | 616 | Free | GLP-1 modified PEG-Mal group reacts with the free C34 of rHSA, chemical group attached between Lys31 (8-amino-3,6-dioxaoctanoyl-maleimidopropionyl) and D32 | Linear | L | None | Produced by secretion from yeast | Antidiabetes | Blood samples were collected from the tail vessel in time intervals of predose 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 and 192 hours | 5 mg/kg | 8.5 | NMR1 mice serum protease | AlphaLISA | NMR1 mice serum | In Vivo | None | None | KD±SD (nM) = 856.5±94.9 against human FcRn receptor | |||
| 28799326 | 2017 | GLP-1-PEG-HB-albumin | 616 | Free | GLP-1 modified PEG-Mal group reacts with the free C34 of rHSA, chemical group attached between Lys31 (8-amino-3,6-dioxaoctanoyl-maleimidopropionyl) and D32 | Linear | L | K573P modification in HSA,GLP-1 modified with PEG-maleimide | Produced by secretion from yeast | Antidiabetes | Blood samples were collected from the tail vessel in time intervals of predose 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 and 192 hours | 5 mg/kg | 9.9 | NMR1 mice serum protease | AlphaLISA | NMR1 mice serum | In Vivo | None | None | KD±SD (nM) = 26.1±2.7 against human FcRn receptor | |||
| 28771355 | 2017 | GLP-1 analogue 4 | 31 | Free | Free | Linear | L | K34R substituition at GLP-1, Conjugated with indomethacin via γGlu attached to the ε-amine of Lys26 of the GLP-1 analog | GLP-1 analogs | Antidiabetes | Blood sampled at eight time-points within 24 h | 5 mL/kg | 55 | Lean mice plasma protease | Luminescent Oxygen Channeling Immunoassay | Lean mice plasma | In Vivo | None | None | GLP-1R EC50 ± SEM (nM) = 0.068 ± 0.037 | |||
| 28771355 | 2017 | GLP-1 analogue 6 | 31 | Free | Diflunisal is linked to the GLP-1 peptide through its hydroxyl group | Linear | L | K34R substituition at GLP-1, at Lys20 indomethacin is linked through a γGlu residue-Lys, DIF=diflunisal, Dehydroxylation of DIF | GLP-1 analogs | Antidiabetes | Blood sampled at eight time-points within 24 h | 5 mL/kg | 299 | Lean mice plasma protease | Luminescent Oxygen Channeling Immunoassay | Lean mice plasma | In Vivo | None | None | GLP-1R EC50 ± SEM (nM) = 0.547 ± 0.211 | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | Chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 0.03 mg | 5.14 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC9488713/ | None | For human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | Chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 0.07 mg | 7.38 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | For human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 0.2 mg | 19.3 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 0.6 mg | 23.2 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 1.8 mg | 25.4 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 3.6 mg | 19.9 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 5 mg | 15.3 / 15.7 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28721592 | 2017 | G-CSF | 204 | Met addition at N terminal of G-CSF | Free | Linear | L | None | Human derived | Selectively stimulate proliferation | Blood samples were drawn from the rats at selected time points (0, 3, 6, 12, 18, and 24 h after injection) | 150 μg/kg | 1.2 | Rats serum protease | ELISA | Rats serum | In Vivo | Genbank accession no. NM_172219 | None | in vitro activity of GCSF-La reached 48% of that of the G-CSF monomer | |||
| 28721592 | 2017 | GCSF-Lα | 462 | Met addition at N terminal of G-CSF | Free | Linear | L | Dimer joined by linker La - SGLEA–(EAAAK)4–ALEA–(EAAAK)4–ALEGS | Homodimeric G-CSF | Selectively stimulate proliferation | Blood samples were drawn from the rats at selected time points (0, 3, 6, 12, 18, and 24 h after injection) | 150 μg/kg | 8.7 | Rats serum protease | ELISA | Rats serum | In Vivo | Genbank accession no. NM_172219 | None | in vitro activity of GCSF-La reached 48% of that of the G-CSF monomer | |||
| 28714475 | 2017 | tagPK128 | 22 | tag | Free | Bicyclic(C9-C15,C15-C21 Disulfide Bond In Pk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit plasma kallikrein | N.A. | 0.5 mg/kg | 0.9 ± 0.2 (T1/2a) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin | |||
| 28714475 | 2017 | tagPK128 | 22 | tag | Free | Bicyclic(C9-C15,C15-C21 Disulfide Bond In Pk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit plasma kallikrein | N.A. | 0.5 mg/kg | 2.9 ± 0.7 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin | |||
| 28714475 | 2017 | tagUK18 | 24 | tag | Free | Bicyclic(C9-C16,C16-C23 Disulfide Bond In Uk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit urokinase | N.A. | 0.5 mg/kg | 1.0 ± 0.1 (T1/2a) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 780±110 for rat albumin | |||
| 28714475 | 2017 | tagUK18 | 24 | tag | Free | Bicyclic(C9-C16,C16-C23 Disulfide Bond In Uk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit urokinase | N.A. | 0.5 mg/kg | 7.4 ± 0.2 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 780±110 for rat albumin | |||
| 28714475 | 2017 | UK18 | 17 | Free | Free | Bicyclic(C2-C9,C9-C16 Disulfide Bond) | L | None | Synthetic | Inhibit urokinase | N.A. | 0.3 mg/kg | 0.30 ± 0.02 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) > 100,000 for rat albumin | |||
| 28714475 | 2017 | Tag | 7 | Fluorescein (F) | Amidation | Linear | L | Lys4 linked with Palm fatty acid | Synthetic | Increases Half Life | N.A. | 0.25 mg/kg | 1.5 ± 0.4 (T1/2a) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 220±30 for rat albumin | |||
| 28714475 | 2017 | Tag | 7 | Fluorescein (F) | Amidation | Linear | L | Lys4 linked with Palm fatty acid | Synthetic | Increases Half Life | N.A. | 0.25 mg/kg | 12.3 ± 0.4 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 220±30 for rat albumin | |||
| 28714475 | 2017 | tag-3xPEG24-FXIIa inhibitor | N.A. | Tag-3xPEG24 | Amidation | Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor) | L | None | Synthetic | FXIIa Inhibitor | N.A. | 5 mg/kg | 1.0 ± 0.2 (T1/2a) | Rabbit plasma protease | RP-HPLC using fluorescence detector | Rabbit plasma | In Vivo | None | None | (EC5x) at 4.2±0.5 mM | |||
| 28714475 | 2017 | tag-3xPEG24-FXIIa inhibitor | N.A. | Tag-3xPEG24 | Amidation | Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor) | L | None | Synthetic | FXIIa Inhibitor | N.A. | 5 mg/kg | 5.2 ± 0.4 (T1/2b) | Rabbit plasma protease | RP-HPLC using fluorescence detector | Rabbit plasma | In Vivo | None | None | (EC5x) at 4.2±0.5 mM | |||
| 28714475 | 2017 | FXIIa inhibitor | N.A. | Fluorescein (F) | Amidation | Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor) | L | None | Synthetic | FXIIa Inhibitor | N.A. | 3.7 mg/kg | 0.21 ± 0.04 (T1/2b) | Rabbit plasma protease | A single quadrupole liquid chromatography mass spectrometer | Rabbit plasma | In Vivo | None | None | Ki FXIIa = 4±0.9 nM in presence of albumin | |||
| 28711730 | 2017 | rhCNTF | 187 | Free | Free | Linear | L | None | Synthetic | Treatment of Neurodegenerative or Metabolic diseases | At different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) | 1 mg/kg | 34.28 | SD rats serum protease | ELISA | SD rats serum | In Vivo | PDB id: 1CNT | None | EC50±SD = 0.48±0.12ng/ml for rhCNTF | |||
| 28711730 | 2017 | rhCNTF-ABD | 251 | Free | ABD035 | Linear | L | Linked by (G4S)3 linker | Fusion of recombinant human CNTF (rhCNTF) with an albumin-binding domain (ABD) | Treatment of Neurodegenerative or Metabolic diseases | At different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) | 1 mg/kg | 483.39 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50±SD = 0.51±0.18 for rhCNTF-ABD | |||
| 28711730 | 2017 | PEG-20k-rhCNTF | 187 | PEGylation (20KDa) | Free | Linear | L | None | Synthetic | Treatment of Neurodegenerative or Metabolic diseases | At different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) | 1 mg/kg | 441.24 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50±SD = 0.48±0.12ng/ml for rhCNTF | |||
| 28711730 | 2017 | PEG-40k-rhCNTF | 187 | PEGylation (40KDa) | Free | Linear | L | None | Synthetic | Treatment of Neurodegenerative or Metabolic diseases | At different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) | 1 mg/kg | 523.89 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50±SD = 0.48±0.12ng/ml for rhCNTF | |||
| 28691076 | 2017 | Cyclic D,L-α-Peptides | 8 | Free | free | Cyclic | Mix | D-amino acid substituitons | Synthetic | Antiatherosclerotic | Blood was drawn (30–60 μL) from the retro-orbital sinus into a heparinized capillary tube before dosing (0 min) and at different intervals from 30 min to 8 h after dosing | 20 g | 6 | BALB/c mouse plasma protease | LC-MS/SIM | BALB/c mouse plasma | In Vivo | None | None | cytotoxicity LD50 (μM) = 36 for NCI | |||
| 28668697 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (approximately 100 µL) were collected from the lateral tail vein at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 16 h | 50 nmol | 2.35 ± 0.23 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50(nM) = 1.79 ± 0.47 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation) | |||
| 28668697 | 2017 | 7b | 29 | Free | Free | Linear | L | X2 = Structure given in paper, n= 40 | Derived from Xenopus GLP-1 | Antidiabetes | Blood samples (approximately 100 µL) were collected from the lateral tail vein at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 16 h | 50 nmol | 2.78 ± 0.14 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 1.4 ± 0.2 for peptide 7 (potency on the cloned human GLP-1 receptor) | |||
| 28668697 | 2017 | 7c | 29 | Free | Free | Linear | L | X3= Structure given in paper, n = 108 | Derived from Xenopus GLP-1 | Antidiabetes | Blood samples (approximately 100 µL) were collected from the lateral tail vein at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 16 h | 50 nmol | 5.67 ± 0.30 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 1.4 ± 0.2 for peptide 7 (potency on the cloned human GLP-1 receptor) | |||
| 28623878 | 2017 | FITC-F9 hydrogel | 9 | Fluoresceinisothiocyanate labelled | Free | Linear | L | None | F9 analogue | Therapeutic drug delivery | 5 days | 0.01 M | 1 to 4 | Mice plasma protease | fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28619366 | 2017 | BPI-3016 | 30 | Free | Free | Linear | L | substituting –NHCO– amide bond of Ala2 with –CH(CF3)NH– to form (A'), Lys20 conjugation with C18, K34R modification | hGLP-1 analogs | Antidiabetes | Blood samples collected at −2 (pre-administration), 2, 8, 22, 46, 94, 118, 142, and 166 h after administration | 0.2 mg/kg | 95 ± 20 | Diabetic cynomoglus monkeys plasma protease | electrospray ionization LC–MS/MS | Diabetic cynomoglus monkeys plasma | In Vivo | None | None | Single subcutaneous injection of 0.4 mg/kg BPI-3016 significantly lowered the fasting glucose level at 46 h after administration | |||
| 28606508 | 2017 | SAPSP-Dox | 21 | Dox = Doxorubicin, Cys incorporation for linking | Amidation | Linear | L | None | SAPSP peptide | Anticancer | 37 °C | 0.1 mM | 9.58 | Fetal Bovine Serum protease | RP-HPLC | Fetal Bovine Serum | In Vitro | None | None | IC50 (microM) = 1.19±0.13 against MCF-7 cells | |||
| 28605180 | 2017 | MS-exenatide (MeSO2-) | 39 | Tetra PEG hydrogel linked with exenatide using linker MeSO2- | Amidation | Linear | L | None | Exenatide analogs | Antidiabetes | Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN | 1.3 µmol/g | 244 | Mouse serum protease | LC-MS/MS | Mouse serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | MS-exenatide (-CN) | 39 | Tetra PEG hydrogel linked with exenatide using linker -CN | Amidation | Linear | L | None | Exenatide analogs | Antidiabetes | Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN | 1.4 µmol/g | 730 | Mouse serum protease | LC-MS/MS | Mouse serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | MS-exenatide (MeSO2-) | 39 | Tetra PEG hydrogel linked with exenatide using linker MeSO2- | Amidation | Linear | L | None | Exenatide analogs | Antidiabetes | Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN | 1.3 µmol/g | 310 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | MS-exenatide (-CN) | 39 | Tetra PEG hydrogel linked with exenatide using linker -CN | Amidation | Linear | L | None | Exenatide analogs | Antidiabetes | Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN | 1.4 µmol/g | 880 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 80 µg/mL | 18 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 80 µg/mL | 50 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 | |||
| 28605180 | 2017 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Substituiting Asn28 with Gln28 | Exenatide analogs | Antidiabetes | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 49 µg/mL | 17 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 11 ±3.7 | |||
| 28605180 | 2017 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Substituiting Asn28 with Gln28 | Exenatide analogs | Antidiabetes | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 49 µg/mL | 48 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 11 ±3.7 | |||
| 28575099 | 2017 | Api134 | 18 | Gu: N,N,N′,N′-tetramethylguanidine, O denotes L-ornithine | Amidation | Linear | L | Orn=Ornithine | Apidaecin analog | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Highly Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Api137 | 18 | Gu: N,N,N′,N′-tetramethylguanidine, O denotes L-ornithine | Free | Linear | L | Orn=Ornithine | Apidaecin analog | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Highly Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Onc112 | 19 | Free | Amidation | Linear | Mix | D-amino acid substituitons | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Highly Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Onc18 | 19 | Free | Amidation | Linear | L | None | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Medium Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Onc72 | 19 | Free | Amidation | Linear | L | L-ornithine (Orn) | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Medium Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Api88 | 18 | Gu: N,N,N′,N′-tetramethylguanidine, O denotes L-ornithine | Amidation | Linear | L | Orn=Ornithine | Apidaecin analog | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Low Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | AAYR-Onc112 | 23 | AAYR | Amidation | Linear | Mix | None | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Low Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | LVPR-Onc112 | 23 | LVPR | Amidation | Linear | Mix | None | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Low Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28522195 | 2017 | [Gly2]GLP-2 | 33 | Free | Free | Linear | L | Ala2 to Gly2 | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood samples were collected from the tail vein at 0, 1, 2, 3, 4, 5,6, 9 and 12 h after administration | 2 mg/mL | 1.62 (Terminal Half Life) | Rats plasma protease | N.A. | Rats plasma | In Vivo | None | None | EC50 values of [Gly2]GLP-2 = 8.40 nM | |||
| 28522195 | 2017 | native GLP-2 | 33 | Free | Free | Linear | L | None | Glucagon | Treatment of Short Bowel Syndrome | Blood samples were collected from the tail vein at 0, 1, 2, 3, 4, 5,6, 9 and 12 h after administration | 2 mg/mL | 4.59 (Terminal Half Life) | Rats plasma protease | N.A. | Rats plasma | In Vivo | None | None | EC50 values of GLP-2 = 2.58 nM | |||
| 28494253 | 2017 | Peptide 22 | 20 | 111In-DTPA = diethylenetriaminepentaacetic acid | Free | Linear | L | X1=Asn at position 1, X2=Leu at position , X3=Lys,X4 = Thr, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 77% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 22 = 1.01 ± 0.21 | |||
| 28494253 | 2017 | Peptide 23 | 21 | 111In-DTPA-Gly = diethylenetriaminepentaacetic acid | Free | Linear | L | X1=Asn, X2=Leu, X3=Lys,X4 = Thr, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 60% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 23 = 1.28 ± 0.23 | |||
| 28494253 | 2017 | Peptide 24 | 20 | 111In-DTPA = diethylenetriaminepentaacetic acid | Amidation | Linear | L | X1=Asn, X2=Leu, X3=Lys,X4 = Thr, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 52% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 24 = 1.19 ± 0.30 | |||
| 28494253 | 2017 | Peptide 25 | 20 | 111In-DTPA = diethylenetriaminepentaacetic acid | Free | Linear | Mix | X1=D-Asn, X2=Leu, X3=Lys,X4 = Thr, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 80% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 25 = 1.36 ± 0.42 | |||
| 28494253 | 2017 | Peptide 26 | 20 | 111In-DTPA = diethylenetriaminepentaacetic acid | X4 = D-Thr at C terminal | Linear | Mix | X1=D-Asn, X2=Leu, X3=Lys, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 77% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 26 = 1.19 ± 0.40 | |||
| 28464043 | 2017 | KP-10 | 10 | Free | Amidation | Linear | L | None | kisspeptin analogue | Treatment of Specific Human Reproductive Disorders | 100 μl of blood was collected from the lateral tail vein from groups of mice (n = 4) for each time point (0, 1min, 2 min, 5 min, 10 min, 30 min, 60 min and 120 min) | 1 nmol | 4 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)77047-1/fulltext | None | N.A. | |||
| 28464043 | 2017 | KP-54 | 54 | Free | Amidation | Linear | L | None | kisspeptin analogue | Treatment of Specific Human Reproductive Disorders | 100 μl of blood was collected from the lateral tail vein from groups of mice (n = 4) for each time point (0, 1min, 2 min, 5 min, 10 min, 30 min, 60 min and 120 min) | 1 nmol | 32 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)77047-1/fulltext | None | N.A. | |||
| 28457895 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 1 hour | 25 nmol/kg | ~0.35 | ICR mice retro-orbital sinus protease | Exenatide ELISA | ICR mice retro-orbital sinus | In Vivo | PDB id: 7MLL | None | both exenatide and exenatide-APTHSA groups at an equal dose effectively cleared glucose from the bloodstream, showing similar anti-hyperglycemic activity | |||
| 28457895 | 2017 | Exenatide-APTHSA | 83 | Free | C-terminal part of exenatide was connected to the N-terminal part of APTHSA using a long (18-mer) linker | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 1 hour | 25 nmol/kg | ~1.3 | ICR mice retro-orbital sinus protease | Exenatide ELISA | ICR mice retro-orbital sinus | In Vivo | PDB id: 7MLL | None | both exenatide and exenatide-APTHSA groups at an equal dose effectively cleared glucose from the bloodstream, showing similar anti-hyperglycemic activity | |||
| 28437610 | 2017 | m-exendin-4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | N.A. | 25 nmol/kg | 43.11 | Murine plasma protease | ELISA | Murine plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28437610 | 2017 | Native Ex4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | N.A. | 25 nmol/kg | 1.9 | Murine plasma protease | ELISA | Murine plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28416744 | 2017 | cRGD-ZW800-1 | 5 | Free | ZW800-1 fluorophore | Cyclic (RGDyK) | Mix | y = D-Tyr | Synthetic | Generic tracer for Intraoperative Near-Infrared Fluorescence Imaging of Solid Tumors | Time points -5, 1, 6, 10, 20, 30, 40, 50, 60, 90, 120, and 240 min. post injection | 10 nmol | 25.3 ± 6.4 | Mice serum protease | Fluorescence assay | Mice serum | In Vivo | None | None | In vitro competition for binding cRGD-ZW800-1 (500 nM) with a 1:1 molar ratio of unlabeled cRGD (500 nM) resulted in a reduction of 32% on the HT-29 cells and 36% on the high integrin-expressing U-87 MG cells compared to cells treated without unlabeled cRGD | |||
| 28416744 | 2017 | cRGD-ZW800-1 | 5 | Free | ZW800-1 fluorophore | Cyclic (RGDyK) | Mix | y = D-Tyr | Synthetic | Generic tracer for Intraoperative Near-Infrared Fluorescence Imaging of Solid Tumors | Time points -5, 1, 6, 10, 20, 30, 40, 50, 60, 90, 120, and 240 min. post injection | 10 nmol | 71.1 ± 9.4 (Terminal Half Life) | Mice serum protease | Fluorescence assay | Mice serum | In Vivo | None | None | In vitro competition for binding cRGD-ZW800-1 (500 nM) with a 1:1 molar ratio of unlabeled cRGD (500 nM) resulted in a reduction of 32% on the HT-29 cells and 36% on the high integrin-expressing U-87 MG cells compared to cells treated without unlabeled cRGD | |||
| 28389388 | 2017 | PEG-HsTX1[R14A] | 34 | PEGylation | Amidation | Cyclic (C3-C24, C9-C29, C13-C34 Disulfide Linkage) | L | Substituting arginine 14 with alanine | From scorpion Heterometrus spinnifer | Immunomodulation in Inflammatory Arthritis | 2 hours | 1 mg/kg | 37.3 | Lewis rats serum protease | Anti-PEG ELISA | Lewis rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3968461/ | None | IC50 of 35.9 ± 6.3 nM | |||
| 28373972 | 2017 | Api88 | 18 | Gu: N,N,N',N' tetramethylguanidino | Amidation | Linear | L | O denotes L-ornithine | Apidaecin analog | Antibacterial | After 10, 20, 30, 60, or90 min animals (n = 7) | 5 mg/kg | 17.3 | Mice plasma protease | RP-HPLC-ESI-MS | Mice plasma | In Vivo | None | None | MIC = Api88 > Api137 | |||
| 28373972 | 2017 | Api88 | 18 | Gu: N,N,N',N' tetramethylguanidino | Amidation | Linear | L | O denotes L-ornithine | Apidaecin analog | Antibacterial | After 10, 20, 30, 60, or90 min animals (n = 7) | 20 mg/kg | 11.1 | Mice plasma protease | RP-HPLC-ESI-MS | Mice plasma | In Vivo | None | None | MIC = Api88 > Api137 | |||
| 28373972 | 2017 | Api137 | 18 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O denotes L-ornithine | Apidaecin analog | Antimicrobial | After 10, 20, 30, 60, or90 min animals (n = 7) | 5 mg/kg | 33.8 | Mice plasma protease | RP-HPLC-ESI-MS | Mice plasma | In Vivo | None | None | The minimum inhibitory concentration (MIC) value for Api137 against E. coli ATCC 25922 is 4 µg/mL. | |||
| 28373972 | 2017 | Api137 | 18 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O denotes L-ornithine | Apidaecin analog | Antimicrobial | After 10, 20, 30, 60, or90 min animals (n = 7) | 20 mg/kg | 16.9 | Mice plasma protease | RP-HPLC-ESI-MS | Mice plasma | In Vivo | None | None | The minimum inhibitory concentration (MIC) value for Api137 against E. coli ATCC 25922 is 4 µg/mL. | |||
| 28356733 | 2017 | SCD | 32 | Free | Chitosan-modified SeNP (SC) | Linear | L | None | Peptide-conjugated selenium nanoparticles | Antidiabetes | Orbital blood was collected at each time point before dosing and from 0.5 to 24 h post dosing | 1 mg/kg | 14.12 | DB/DB mice orbital blood protease | LC-MS/MS | DB/DB mice orbital blood sample | In Vivo | None | None | IC50 of SC for INS-1 cells was 66.10 μM | |||
| 28356733 | 2017 | DBAYL | 32 | Free | Free | Linear | L | None | PACAP-derived peptide | Antidiabetes | Orbital blood was collected at each time point before dosing and from 0.5 to 24 h post dosing | 1 mg/kg | 1.98 | DB/DB mice orbital blood protease | LC-MS/MS | DB/DB mice orbital blood sample | In Vivo | None | None | EC50 of DBAYL at VPAC1 was 804 nM | |||
| 28323965 | 2017 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Measured at the final randomized dose (following the second dose) | 0.25 mg/kg | 36.1 | Human serum protease | IDS-iSys chemiluminescence assay | Human serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU, https://sci-hub.se/10.1021/acs.molpharmaceut.5b00868 | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 28323965 | 2017 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Measured at the final randomized dose (following the second dose) | 0.48 mg/kg | 18.3 | Human serum protease | IDS-iSys chemiluminescence assay | Human serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU, https://sci-hub.se/10.1021/acs.molpharmaceut.5b00868 | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 28323965 | 2017 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Measured at the final randomized dose (following the second dose) | 0.66 mg/kg | 22.4 | Human serum protease | IDS-iSys chemiluminescence assay | Human serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU, https://sci-hub.se/10.1021/acs.molpharmaceut.5b00868 | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 28323965 | 2017 | r-HGH | 191 | Free | Free | Linear | L | None | Synthetic | Treatment of GHD | Measured following 2 weeks of daily administration | 0.24 mg/kg | 3.5 | Human serum protease | IDS-iSys chemiluminescence assay | Human serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU, https://sci-hub.se/10.1021/acs.molpharmaceut.5b00868 | None | EC50 = 0.36 ± 0.06 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 28281868 | 2017 | HSA-eTGFBR2 | 697 | Free | eTGFBR2 fused at the C-terminal of HSA | Linear | L | None | Synthetic | Neutralize TGF-Β1 activity | Blood samples were collected 5 min, 15 min, 30 min, 1 h, 2 h, 6 h,12 h, 24 h | 3 nmol/kg | 11.84 | Mice serum protease | Human TGF-b RII Duo Set ELISA | Mice serum | In Vivo | pdb id: 4P7U, 7DJN | None | KD = 1.42* 10-8M of HSA-eTGFBR2 for TGF-B1 | |||
| 28281868 | 2017 | eTGFBR2 | 112 | Free | Free | Linear | L | None | Synthetic | Neutralize TGF-Β1 activity | Blood samples were collected through the eyes at 5 min, 15 min, 30 min, 60 min, 120 min | 3 nmol/kg | 41.42 | Mice serum protease | Human TGF-b RII Duo Set ELISA | Mice serum | In Vivo | None | None | KD = 9.49* 10-9M of eTGFBR2 for TGF-B1 | |||
| 28209419 | 2017 | Native GLP-2 | 33 | Free | Free | Linear | L | None | Glucagon | Treatment of Short Bowel Syndrome | N.A. | 8 μg/kg | ~120 | Human plasma protease | GLP-2 (1–33) specific radioimmunoassay | Adult human plasma | In Vivo | PDB id: 2L63 | None | N.A. | |||
| 28209419 | 2017 | Native GLP-2 | 33 | Free | Free | Linear | L | None | Glucagon | Treatment of Short Bowel Syndrome | Samples were taken prior to GLP-2 administration and at 60, 90 and 180 min post injection on Day 3 of therapy or Day 42 | 2.5 μg/kg | ~45 | Human plasma protease | GLP-2 (1–33) specific radioimmunoassay | Infant human plasma | In Vivo | PDB id: 2L63 | None | N.A. | |||
| 28138743 | 2017 | CP-11 | 13 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | A plasma aliquot was withdrawn at each time-point(0, 0.16, 0.5, 1, 2, 4 h) | 10 μM | 0.21 | Mouse plasma protease | LC-HRMS. | Mouse plasma | In Vitro | None | None | N.A. | |||
| 28138743 | 2017 | Omiganan | 13 | Free | Amidation | Linear | L | None | Analogue of indolicidin | Antimicrobial | A plasma aliquot was withdrawn at each time-point(0, 0.16, 0.5, 1, 2, 4 h) | 10 μM | 0.83 | Mouse plasma protease | LC-HRMS. | Mouse plasma | In Vitro | None | None | N.A. | |||
| 28138743 | 2017 | Indolicidin | 13 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | A plasma aliquot was withdrawn at each time-point(0, 0.16, 0.5, 1, 2, 4 h) | 10 μM | 1.53 | Mouse plasma protease | LC-HRMS. | Mouse plasma | In Vitro | None | None | N.A. | |||
| 28097629 | 2017 | TP508 | 23 | Free | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | 2.16 mM | 13.7 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG5k-TP508 | 23 | PEG5K | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | 2.16 mM | 11.5 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG20k-Cys14-TP508 | 23 | Free | Amidation | Linear | L | PEGylation at Cys14 through Mal-modified PEG20K, TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | Molar equivalent of 5 mg/mL TP508 | 70 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG20k-TP508 | 23 | PEG20K | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | 2.16 mM | 93 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG30k-TP508 | 23 | PEG30K | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | Molar equivalent of 1 mg/mL TP508 | 258 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28068664 | 2017 | scFv57R | N.A. | Free | Free | Linear | L | None | Synthetic | Antiviral (against Rabies Virus) | 37o C for 0-72 hours | 0.5 mg/ml | 14.1 | N.A. | ELISA | PBS | In Vitro | None | None | Neutralizing potency (IU/ml) = 83.8 ± 9.4 for monomer | |||
| 28068664 | 2017 | scFv57R-ATS | N.A. | Free | (ATS) was fused to the C-terminus of the anti-RV scFv57R | Linear | L | None | scFv57R-ATS fusion protein | Antiviral (against Rabies Virus) | 37o C for 0-72 hours | 0.5 mg/ml | 33.9 | N.A. | ELISA | PBS | In Vitro | None | None | Neutralizing potency (IU/ml) = 2.9 ± 0.5 for polymer | |||
| 28068664 | 2017 | scFv57R-ATS | N.A. | Free | (ATS) was fused to the C-terminus of the anti-RV scFv57R | Linear | L | None | scFv57R-ATS fusion protein | Antiviral (against Rabies Virus) | 37o C | 0.5 mg/ml | 15.6 | Mouse serum protease | ELISA | Mouse serum | In Vitro | None | None | Neutralizing potency (IU/ml) = 2.9 ± 0.5 for polymer | |||
| 28065871 | 2017 | DOX-cRGD30-RCCMs | 5 | Free | RCCMs | Cyclic (RGDyK) | Mix | y = D-Tyr | Synthetic | Antitumor | -4 C for 10 h | 10 mg DOX equiv./kg | 4.7 (T1/2,b) | Kunming mice retro-orbital sinus protease | Fluorescence assay | Kunming mice retro-orbital sinus | In Vivo | None | None | IC50 value for DOX-cRGD30-RCCMs is 1.9 µg/mL | |||
| 28065871 | 2017 | DOX-cRGD30-PEG-PCL | 5 | Free | PEG-PLC | Cyclic (RGDyK) | Mix | y = D-Tyr | Synthetic | Antitumor | -4 C for 10 h | 10 mg DOX equiv./kg | 1.2 (T1/2,b) | Kunming mice retro-orbital sinus protease | Fluorescence assay | Kunming mice retro-orbital sinus | In Vivo | None | None | N.A. | |||
| 28010844 | 2017 | Octreotide | 8 | D-amino acid Phe | Free | Cyclic (C2-C7 Disulfide Linkage) | Mix | D-amino acid substituitons Trp | SST analog | Anticancer and treatment of Endocrine Diseases | The mice were sacrificed at 10, 20, 40, 60, 120, 240 and 360 min | 50 mg/kg | 28 | Mouse stomach tissue lysate protease | HPLC-MS | Mouse stomach tissue lysate | In Vivo | https://sci-hub.st/10.1177/106002808802201001 | None | N.A. | |||
| 28010844 | 2017 | Octreotide | 8 | D-amino acid Phe | Free | Cyclic (C2-C7 Disulfide Linkage) | Mix | D-amino acid substituitons Trp | SST analog | Anticancer and treatment of Endocrine Diseases | The mice were sacrificed at 10, 20, 40, 60, 120, 240 and 360 min | 50 mg/kg | 37.7 | Mouse intestine tissue lysate protease | MALDI-TOF-MSI and LC-MS/MS | Mouse intestine tissue lysate | In Vivo | None | None | N.A. | |||
| 28005375 | 2017 | DOX-ATN/SCID-Ps | 5 | Acetylation | PEG-P(TMC-DTC) | Linear | Mix | None | Synthetic | Anticancer | N.A. | 150 μL | 4.13 (Elimination Half Life) | Kunming mice retro-orbital sinus protease | Fluorescence assay | Kunming mice retro-orbital sinus blood | In Vivo | None | None | DOX-ATN56/SCID-Ps revealed a low IC50 of 5.2 μg/mL to B16F10 cells | |||
| 27990643 | 2017 | CN-105 | 5 | Acetylation | Amidation | Linear | L | None | APOE-derived peptide | Treatment of Spontaneous Intracranial Hemorrhage (Ich) | Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing | 0.01 mg/kg | 2.3 ± 0.5 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5054364/ | None | N.A. | |||
| 27990643 | 2017 | CN-105 | 5 | Acetylation | Amidation | Linear | L | None | APOE-derived peptide | Treatment of Spontaneous Intracranial Hemorrhage (Ich) | Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing | 0.03 mg/kg | 2.4 ± 0.5 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 27990643 | 2017 | CN-105 | 5 | Acetylation | Amidation | Linear | L | None | APOE-derived peptide | Treatment Of Spontaneous Intracranial Hemorrhage (Ich) | Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing | 0.1 mg/kg | 3.3 ± 0.6 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 27990643 | 2017 | CN-105 | 5 | Acetylation | Amidation | Linear | L | None | APOE-derived peptide | Treatment Of Spontaneous Intracranial Hemorrhage (Ich) | Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing | 0.3 mg/kg | 3.6 ± .4 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 27990643 | 2017 | CN-105 | 5 | Acetylation | Amidation | Linear | L | None | APOE-derived peptide | Treatment Of Spontaneous Intracranial Hemorrhage (Ich) | Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing | 1 mg/kg | 3.5 ± 0.3 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 27881716 | 2017 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 3.81 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 142.81 | |||
| 27881716 | 2017 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 4.43 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 142.81 | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 6.27 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 53.77 | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 4.14 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL)= 47.63 | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 150 mg/kg | 2.57 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 53.77 | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 150 mg/kg | 2.74 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL)= 47.63 | |||
| 27815337 | 2017 | pE13F | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 7.2 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 300 ± 182 | |||
| 27815337 | 2017 | P26 | 12 | Acetylation | Pro(4-Br)Phe substituition | Linear | Mix | Aib, DLeu,ProNle, D-Ala | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 86 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 138 ± 30 | |||
| 27815337 | 2017 | K17F | 17 | Free | Free | Linear | L | None | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 4.6 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 15 ± 3.6 | |||
| 27815337 | 2017 | P92 | 17 | Acetylation | Pro(4-Br)Phe substituition | Linear | Mix | Aib, DLeu,DGln, ProNle, D-Arg at position 3 | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 24 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 4 ± 2.4 | |||
| 27815337 | 2017 | LIT01-196 | 18 | CF3(CF2)7(CH2)2C(O) | Free | Linear | L | None | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 1440 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 16 ± 5.6 | |||
| 27784692 | 2017 | ELP | 815 | Free | Free | Linear | L | x = Val,Gly or Ala | Synthetic | Carrier protein | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 100 mg/kg | 52.6 (T1/2,Terminal) | Rats plasma protease | whole-body fluorescence imaging | Rats plasma | In Vivo | None | None | KTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours | |||
| 27784692 | 2017 | KTP-ELP | 822 | Conjugation of KTP cyclic peptide at N terminal | Free | Linear | L | x = Val,Gly or Ala | Fusion protein of KTP and ELP | Carrier protein | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 100 mg/kg | 234.83 (T1/2,Terminal) | Rats plasma protease | whole-body fluorescence imaging | Rats plasma | In Vivo | None | None | KTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours | |||
| 27784692 | 2017 | ELP | 815 | Free | Free | Linear | L | x = Val,Gly or Ala | Synthetic | Carrier protein | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 5 mg/kg | 90.3 (T1/2,Terminal) | Swine plasma protease | whole-body fluorescence imaging | Swine plasma | In Vivo | None | None | KTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours | |||
| 27784692 | 2017 | KTP-ELP | 822 | Conjugation of KTP cyclic peptide at N terminal | Free | Linear | L | x = Val,Gly or Ala | Fusion protein of KTP and ELP | Carrier protein | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 5 mg/kg | 118.6 (T1/2,Terminal) | Swine plasma protease | whole-body fluorescence imaging | Swine plasma | In Vivo | None | None | KTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours | |||
| 27689406 | 2017 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 3.2 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27689406 | 2017 | GLP-1 | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 1.2 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | PDB id: 5VAI | None | N.A. | |||
| 27689406 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Exendin-4 | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 35.1 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | PDB id: 7MLL | None | EC50 (pM) = 1.8 ± 0.8 | |||
| 27689406 | 2017 | X1 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Antiobesity | N.A. | N.A. | 3.9 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27689406 | 2017 | X2 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Antiobesity | N.A. | N.A. | 16.1 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27689406 | 2017 | X3 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Antiobesity | N.A. | N.A. | 21.3 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27539157 | 2017 | Anti‐VEGF PCCs Bi‐LV | 23 | X1 = biotin-PEG3 label | lfreW = D and L -amino acids | Cyclic | Mix | Tz4 = triazole linker | Synthetic | In vivo imaging probe and an Anti‐PA peptide | Blood was drawn from each of three animals at the following time points: 3, 10, 30, 60, 120, 240, 360, 1,440 min | 1 mg/kg | 7 (Elimination Half Life) | Mice plasma protease | LC‐MS/MS assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 27539157 | 2017 | Anti‐VEGF PCCs Tri‐LV | 28 | X1 = biotin-PEG3 label | eeird = D-amino acids | Cyclic | Mix | Tz4 = triazole linker | Synthetic | In vivo imaging probe and an Anti‐PA peptide | Blood was drawn from each of three animals at the following time points: 3, 10, 30, 60, 120, 240, 360, 1,440 min | 1 mg/kg | 36 (Elimination Half Life) | Mice plasma protease | LC‐MS/MS assay | Mice plasma | In Vivo | None | None | IC50 = 2.6 ± 0.5 nM | |||
| N.A. | 2017 | SEQ ID NO 62 | 152 | Free | Free | Linear | L | None | Lipocalin muteins | Pcsk9-Specific Lipocalin Muteins | N.A. | N.A. | 0.99 | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | None | US 201715445066 A | IC50(nM) = 1.36 without HSA for LDLR binding | |||
| N.A. | 2017 | SEQ ID NO 82 | 153 | Free | Free | Linear | L | None | Lipocalin muteins | Pcsk9-Specific Lipocalin Muteins | N.A. | N.A. | 0.86 | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | None | US 201715445066 A | IC50(nM) = 1.68 without HSA for LDLR binding | |||
| N.A. | 2017 | SEQ ID NO 83 | 203 | Free | ABP-G148 (Albumin binding protein) conjugation | Linear | L | None | Lipocalin muteins | Pcsk9-Specific Lipocalin Muteins | N.A. | N.A. | 24 | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | None | US 201715445066 A | IC50(nM) = 1.93 without HSA for LDLR binding | |||
| N.A. | 2017 | SEQ ID NO 84 | 210 | Free | ABP-G148 (Albumin binding protein) conjugation | Linear | L | None | Lipocalin muteins | Pcsk9-Specific Lipocalin Muteins | N.A. | N.A. | 32 | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | None | US 201715445066 A | IC50(nM) = 1.09 without HSA for LDLR binding | |||
| 28953210 | 2017 | 99mTc-exendin(9-39) | 31 | 99Mtc Radiolabeled | Free | Linear | L | None | Exendin4 analogs | Antidiabetes | Whole-body images from four healthy individuals were acquired at 20 min, 2, 6, and 24 h after 99mTc-exendin(9-39)/octreotide administration | N.A. | 1.2 (T1/2 a- Fast ) (Activity Half Life) | Human blood protease | N.A. | Human blood | N.A. | PDB id: 7MLL | None | N.A. | |||
| 28953210 | 2017 | 99mTc-exendin(9-39) | 31 | 99Mtc Radiolabeled | Free | Linear | L | None | Exendin4 analogs | Antidiabetes | Whole-body images from four healthy individuals were acquired at 20 min, 2, 6, and 24 h after 99mTc-exendin(9-39)/octreotide administration | N.A. | 8.7 (T1/2 b- Slow)(Activity Half Life) | Human blood protease | N.A. | Human blood | N.A. | PDB id: 7MLL | None | N.A. | |||
| 28953210 | 2017 | 99mTc-exendin(9-39) | 31 | 99Mtc Radiolabeled | Free | Linear | L | None | Exendin4 analogs | Antidiabetes | Whole-body images from four healthy individuals were acquired at 20 min, 2, 6, and 24 h after 99mTc-exendin(9-39)/octreotide administration | N.A. | 1.7(T1/2 b-Slow)(Activity Half Life) | Human blood protease | N.A. | Human blood | N.A. | PDB id: 7MLL | None | N.A. | |||
| 28870261 | 2017 | EXT-Sol | 39 | Free | Free | Linear | L | Substituition of amino acids G,L,K,Q,M,E,E,V,R,L,E,K,N,O,P,S,S,G,A,P,P,P,S | Exendin4 analogs | Antidiabetes | At specific time 0, 0.25, 0.5, 1,1.5, 2, 3, 4, 6, 8 h after injection | 50 μg/kg | 0.22 ± 0.03 (T1/2a- Distribution) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | EXT-SBA-15 exhibited efficacy that is comparable to EXT-Sol on 5 h | |||
| 28870261 | 2017 | EXT-SBA-15 | 39 | Free | Free | Linear | L | Substituition of amino acids G,L,K,Q,M,E,E,V,R,L,E,K,N,O,P,S,S,G,A,P,P,P,S | Exendin4 analogs | Antidiabetes | Collected at 0, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120 h | 50 μg/kg | 0.26 ± 0.05(T1/2a- Distribution) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | EXT-SBA-15 exhibited efficacy that is comparable to EXT-Sol on 5 h | |||
| 28870261 | 2017 | EXT-Sol | 39 | Free | Free | Linear | L | Substituition of amino acids G,L,K,Q,M,E,E,V,R,L,E,K,N,O,P,S,S,G,A,P,P,P,S | Exendin4 analogs | Antidiabetes | At specific time 0, 0.25, 0.5, 1,1.5, 2, 3, 4, 6, 8 h after injection | 50 μg/kg | 0.60 ± 0.08(T1/2b-Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | EXT-SBA-15 exhibited efficacy that is comparable to EXT-Sol on 5 h | |||
| 28870261 | 2017 | EXT-SBA-15 | 39 | Free | Free | Linear | L | Substituition of amino acids G,L,K,Q,M,E,E,V,R,L,E,K,N,O,P,S,S,G,A,P,P,P,S | Exendin4 analogs | Antidiabetes | Collected at 0, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120 h. | 50 μg/kg | 14.53 ± 0.70(T1/2b-Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | EXT-SBA-15 exhibited efficacy that is comparable to EXT-Sol on 5 h | |||
| 28714475 | 2017 | PK128 | 15 | Free | Free | Bicyclic (C2-C8,C8-C14 Disulfide Bond In Pk128) | L | None | Synthetic | Inhibit plasma kallikrein | Probes were taken at different time points (5 min, 0.5, 1, 2, 4, 8, 24 and 48 h) at 37 C , diluted to 3 mM (urokinase inhibitor) or 0.75 mM (plasma kallikrein inhibitor) with assay buffer (10 mM TrisCl, pH 7.4, 150 mM NaCl, 10 mM MgCl2, 1 mM CaCl2, 0.01% v/v Tween-20, and 0.1% (w/v) casein) | 20 microM | 1.8 ± 0.3 (Activity Half Life) | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin for tagPK128 | |||
| 28714475 | 2017 | tagPK128 | 22 | Tag | Free | Bicyclic (C2-C8,C8-C14 Disulfide Bond In Pk128) | L | Lys4 conjugated with Palm | Synthetic | Inhibit plasma kallikrein | Probes were taken at different time points (5 min, 0.5, 1, 2, 4, 8, 24 and 48 h) at 37 C , diluted to 3 mM (urokinase inhibitor) or 0.75 mM (plasma kallikrein inhibitor) with assay buffer (10 mM TrisCl, pH 7.4, 150 mM NaCl, 10 mM MgCl2, 1 mM CaCl2, 0.01% v/v Tween-20, and 0.1% (w/v) casein) | 20 microM | >48 (Activity Half Life) | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin for tagPK128 | |||
| 28416744 | 2017 | cRGD-ZW800-1 | 5 | Free | Zw800-1 | Cyclic (RGDyK) | Mix | y = D-Tyr, cyclic peptide linked with ZW800-1 | Synthetic | Generic tracer for intraoperative near-infrared fluorescence imaging of solid tumors | time points -5, 1, 6, 10, 20, 30, 40, 50, 60, 90, 120, and 240 min. post injection | 10 nmol | 14.6 ± 1.7 (Distribution Half Life) | Mice serum protease | Fluorescence assay | Mice serum | In Vivo | None | None | N.A. | |||
| 27784692 | 2017 | ELP | 815 | Free | Free | Linear | L | x = Val,Gly or Ala | Synthetic | Carrier protein | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 100 mg/kg | 3.63 (T1/2,Distribution) | Rats plasma protease | whole-body fluorescence imaging | Rats plasma | In Vivo | None | None | N.A. | |||
| 27784692 | 2017 | KTP-ELP | 822 | Conjugation of KTP cyclic peptide at N terminal | Free | Linear | L | x = Val,Gly or Ala | Fusion protein of KTP and ELP | Carrier protein | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 100 mg/kg | 39.12 (T1/2,Distribution) | Rats plasma protease | whole-body fluorescence imaging | Rats plasma | In Vivo | None | None | N.A. | |||
| 27784692 | 2017 | ELP | 815 | Free | Free | Linear | L | x = Val,Gly or Ala | Synthetic | Carrier protein | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 5 mg/kg | 3.8 (T1/2,Distribution) | Swine plasma protease | whole-body fluorescence imaging | Swine plasma | In Vivo | None | None | N.A. | |||
| 27784692 | 2017 | KTP-ELP | 822 | Conjugation of KTP cyclic peptide at N terminal | Free | Linear | L | x = Val,Gly or Ala | Fusion protein of KTP and ELP | carriers | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 5 mg/kg | 6 (T1/2,Distribution) | Swine plasma protease | whole-body fluorescence imaging | Swine plasma | In Vivo | None | None | N.A. | |||
| 28717654 | 2017 | RT1.14opt-in | 561 | Free | Free | Linear | L | (D185N, D186N, E478Q) amino acid modifications | Derived from HIV-1 MN | Induce oxidative stress | After 0, 2, 4, and 6 hours of incubation, the cells were harvested, lysed | N.A. | 2 (Activity Half Life) | HeLa cells lysate protease, E64 (10 μM),leupeptin (10 μg/ml), aprotinin (10 μg/ml), pepstatin A (7,5 μM), MG132 (5 μM), or epoxomicin (0,1 μM) | Cycloheximide chase assay and Western blot | HeLa cells lysate after treatment with cycloheximide | In Vivo | Transfection route** | None | Lysates of 105 cells expressing RT1.14opt-in retained 0,00012% activity | |||
| 28717654 | 2017 | RT1.14oil | 586 | N-Terminally fused to a leader signal sequence from the NS1 protein | Rt1.14 | Linear | L | (D185N, D186N, E478Q) amino acid modifications | Derived from HIV-1 MN | Induce oxidative stress | After 0, 2, 4, and 6 hours of incubation, the cells were harvested, lysed | N.A. | ~15 (Activity Half Life) | HeLa cells lysate protease, E64 (10 μM),leupeptin (10 μg/ml), aprotinin (10 μg/ml), pepstatin A (7,5 μM), MG132 (5 μM), or epoxomicin (0,1 μM) | Cycloheximide chase assay and Western blot | HeLa cells lysate after treatment with cycloheximide | In Vivo | Transfection route** | None | Lysates of 105 cells expressing RT1.14oil retained 0,00005% of the activity | |||
| 27804918 | 2016 | APTEDB–SN38 | 26 | Free | Free | Cyclic (2 Trp-Trp Bond) | L | Ala-modified SN38 (Cys-Mal-PEG4-Ala-SN38) linked with Cys-modified APT EDB through Lys15 | Linker is Mal-PEG4 | Anticancer | At different times (0.08, 0.5, 1, 3, 6, 12 h) after injection | 1 mg/kg | 1.77 | Mice plasma protease | HPLC | Mice plasma | In Vivo | https://sci-hub.st/10.1016/j.jconrel.2012.08.029 | None | IC50 = 472.6 nM | |||
| 27656777 | 2016 | VH434 | 8 | Acetylation | Amidation | Cyclic (C1-C8 Disulfide Bond) | L | None | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 1.16 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | KD = 196 nM | |||
| 27656777 | 2016 | VH445 | 8 | Acetylation | Amidation | Cyclic (C1-C8 Disulfide Bond) | Mix | c = D-Cys at position 1 | VH445 | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 3.03 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | KD = 76 nM | |||
| 27656777 | 2016 | VH4106 | 8 | Acetylation | Amidation | Cyclic | Mix | Pen, Thz = Penicillamine, Thiazolidine | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 1.89 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | KD = 9 nM | |||
| 27656777 | 2016 | VH4127 | 8 | Pr = propionylation, c = D-Cys at N terminal | Amidation | Cyclic | Mix | Pen, Thz = non-natural amino acid | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 4.27 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | KD = 18 nM | |||
| 27656777 | 2016 | VH4128 | 8 | Pr = propionylation, c = D-Cys at N terminal | Amidation | Cyclic | Mix | c = D-Cys and Pen, Thz, Sar = non-natural amino acid | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 4.35 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | Introduction of the non-natural Sar residue at the Gly7 position had only minor impact on the affinity (compare VH4128 to VH4127 and VH4131 to VH4130 | |||
| 27656777 | 2016 | VH4129 | 8 | Pr = propionylation, c = D-Cys at N terminal | Amidation | Cyclic (C1-C8 Disulfide Bond) | Mix | c = D-Cys and Sar modification , Pip = Pipecolic acid | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 6.66 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | N.A. | |||
| 27656777 | 2016 | VH4130 | 8 | Pr = propionylation, c = D-Cys at N terminal | Amidation | Cyclic | Mix | c = D-Cys and Pen, Pip = non-natural amino acid | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 4.03 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | Introduction of the non-natural Sar residue at the Gly7 position had only minor impact on the affinity (compare VH4128 to VH4127 and VH4131 to VH4130 | |||
| 27656777 | 2016 | VH4131 | 8 | Pr = propionylation, c = D-Cys at N terminal | Amidation | Cyclic | Mix | c = D-Cys and Sar,Pen, Pip = non-natural amino acid | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 10 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | Introduction of the non-natural Sar residue at the Gly7 position had only minor impact on the affinity (compare VH4128 to VH4127 and VH4131 to VH4130 | |||
| 27558296 | 2016 | Compound 1 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Inotropic Agent | Time points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h) | 1 µg/mL | 0.025 | Wistar rats plasma protease | ESI-MS | Wistar rats plasma | In Vitro | None | None | EC50(nM) = 2.6 ± 1.0 | |||
| 27558296 | 2016 | Compound 2 | 13 | pGlu = Pyroglutamate | Free | Linear | L | Nle = Norleucine at position 11 | Apelin analogs | Inotropic Agent | Time points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h) | 1 µg/mL | 0.13 | Wistar rats plasma protease | ESI-MS | Wistar rats plasma | In Vitro | None | None | EC50(nM) = 2.0 ± 0.3 | |||
| 27558296 | 2016 | Compound 26 | 14 | pGlu = Pyroglutamate | Free | Cyclic (C2-C7 Disulfide Linkage) | L | Nle = Norleucine at position 12 | Apelin analogs | Inotropic Agent | Time points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h) | 1 µg/mL | 0.1 | Wistar rats plasma protease | ESI-MS | Wistar rats plasma | In Vitro | None | None | EC50(nM) > 1000 | |||
| 27558296 | 2016 | Compound 31 | 13 | Palmitic acid conjugation | Free | Linear | L | Nle= Nor-leucine at position 11, Aib = 2-Aminoisobutyric acid at position 12 | Apelin analogs | Inotropic Agent | Time points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h) | 1 µg/mL | 29 | Wistar rats plasma protease | ESI-MS | Wistar rats plasma | In Vitro | None | None | EC50(nM) = 21.6 ± 4.5 for compound 31 | |||
| 27558296 | 2016 | Compound 31 | 13 | Palmitic acid conjugation | Free | Linear | L | Gly9 was exchanged with Lys, TAMRA = 5,6-carboxytetramethylrhodamine at Lys9 modification at Lysine , Nle= Nor-leucine at position 11, Aib = 2-Aminoisobutyric acid at position 12 | compound 31 analogues | Inotropic Agent | 37 C | 0.00001 M | ~4 | Porcine liver homogenate protease | HPLC using a fluorescence detector | Porcine liver homogenate | In Vitro | None | None | EC50(nM) = 21.6 ± 4.5 for compound 31 | |||
| 27558296 | 2016 | Compound 31 | 13 | Palmitic acid conjugation | Free | Linear | L | Gly9 was exchanged with Lys, TAMRA = 5,6-carboxytetramethylrhodamine at Lys9 modification at Lysine , Nle= Nor-leucine at position 11, Aib = 2-Aminoisobutyric acid at position 12 | compound 31 analogues | Inotropic Agent | 37 C | 0.00001 M | 0.36 | Wistar rats plasma protease | HPLC | Wistar rats plasma | In Vitro | None | None | EC50(nM) = 21.6 ± 4.5 for compound 31 | |||
| 27393654 | 2016 | IFN-α | 165 | Free | Free | Linear | L | None | Human derived | Antiproliferative, Immunoregulatory and Antiviral | At desired time points (1, 5, 15, 30 min, 1, 3, 6, 24,48, 72 and 96 h) | 1 mg IFN-α equivalent/kg | 1.49 (T1/2b-Terminal Half Life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 1ITF | None | IC50 = 10.77 pg/mL | |||
| 27393654 | 2016 | IFN-PMPC | 165 | Free | poly(2-methacryloyloxyethyl phosphorylcholine) | Linear | L | None | Human derived | Antiproliferative, Immunoregulatory and Antiviral | At desired time points (1, 5, 15, 30 min, 1, 3, 6, 24,48, 72 and 96 h) | 1 mg IFN-α equivalent/kg | 51.6 (T1/2b-Terminal Half Life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | IC50 = 20.02 pg/mL | |||
| 27364558 | 2016 | Biotinylated SSTN(IGF1R) | 28 | Free | Free | Linear | L | Biotinylation | Mouse derived | Dually Attack MM Tumor Cell Survival And Tumor Angiogenesis | terminally bled at 0, 0.1, 0.3, 1, 3, 6, 12 and 24 hr post-injection | 0.365 mg/kg | 27 | Female BALB/c mice serum | IR scanning using anti-biotin antibody | Female BALB/c mice serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3651771/ | None | The growth of human CAG, RPMI-8226, KMS-12, U266, MM.1R and the mouse P3X63Ag8 myeloma cells was significantly reduced by a three-day treatment with 30 μM SSTNIGF1R | |||
| 27337048 | 2016 | SFTI-a | 14 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | Sunflower trypsin inhibitor derivative | Immunomodulatory inhibitors of the CD2:CD58 protein–protein interaction | 37 °C at various time points from 0 min to 24 h | 2 mg/ml | <=24 | Human serum protease | HPLC, MS | Human serum | In Vitro | None | None | Cell adhesion inhibition IC50 (µM) = 0.043 ± 0.025 in T cell OVCAR-3 | |||
| 27243004 | 2016 | Api793 | 20 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (WO)2 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 246 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/L) = 0.64 ± 0.05 in HEK293 | |||
| 27243004 | 2016 | Api794 | 22 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (WO)3 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 311 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/l) = 0.28 ± 0.03 in HEK293 | |||
| 27243004 | 2016 | Api795 | 20 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (IO)2 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 354 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/l) > 0.6 in HEK293 | |||
| 27243004 | 2016 | Api796 | 22 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (IO)3 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 249 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/l) > 0.6 in HEK293 | |||
| 27240277 | 2016 | ENF | 36 | Free | Free | Linear | L | None | Synthetic | Antiviral (against HIV infection) | N.A. | 1.7 μmol/kg | 1.5 ± 0.1 (Elimination Half Life) | SD rats plasma protease | HPLC | SD rats plasma | In Vivo | None | None | EC50(nM) = 3 ± 0 | |||
| 27240277 | 2016 | PEG2k-ENF | 36 | mPEG(2KDa)-Maleimide | Free | Linear | L | None | Synthetic | Antiviral (against HIV infection) | N.A. | 1.7 μmol/kg | 16.1 ± 3.8 (Elimination Half Life) | SD rats plasma protease | HPLC | SD rats plasma | In Vivo | None | None | EC50(nM) = 4 ± 0 | |||
| 27232339 | 2016 | GLP-1-IgG2σ-Fc | 31 | Free | Human IgG2σ constant heavy-chain linked via a peptide linker (GGGSGGGSGGGS) with human GLP-1 (A8G/G26E/R36G) at C terminal | Linear | L | GLP-1 variant (A8G/G26E/R36G) linked to the human IgG2σ constant heavy-chain by a peptide linker (GGGSGGGSGGGS) | GLP-1 analogs | Antidiabetes | Blood (0.6 mL) was collected from the foreleg vein immediately pre-administration (time 0), and at 2, 4, 8, 12, 48, 72, 96, 192,240, and 288 h after a single subcutaneous injection of GLP-1-IgG2σ-Fc | 0.1 mg/kg | 57.1 ± 4.5 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | PDB id: 5VAI | None | Cells incubated with medium containing 16.8 mM glucose secreted significantly more insulin in the presence of 10 nM (5.2 ± 0.4 ng/mL) and 100 nM (7.3 ± 0.3 ng/mL) GLP-1-IgG2σ-Fc, as compared with control cells (2.5 ± 0.5 ng/mL) | |||
| 27217590 | 2016 | OT (oxytocin) | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | None | Produced in the hypothalamus and released by the posterior pituitary gland | Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia | Time points postdose: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 7, and 24 hours | 0.1 mg/kg | 0.12 | Wistar rats plasma protease | LC-MS/MS | Wistar rats plasma | In Vivo | https://sci-hub.st/10.1016/s0079-6123(08)00417-2 | None | EC50(nM) = 0.039 (OTR agonist) | |||
| 27217590 | 2016 | PF1 | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | Substitution of the Pro7 to Gly and Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group, Palm = Palmitic acid | OT analog | Non–brain-penetrant OT receptor agonist | Time points postdose: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 7, and 24 hours | 0.1 mg/kg | 8.5 | Wistar rats plasma protease | LC-MS/MS | Wistar rats plasma | In Vivo | None | None | EC50(nM) = 0.025 (OTR agonist) | |||
| 27217590 | 2016 | PF1 | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | Substitution of the Pro7 to Gly and Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group, Palm = Palmitic acid | OT analog | Non–brain-penetrant OT receptor agonist | Time points postdose: 0.25 (OT only), 0.5, 1, 2, 4, 6, and 24 hours (6- and 24-hour sampling limited to PF1 only) | 4 ml/kg | 3.2 | C57Bl/6J mice plasma protease | LC-MS/MS | C57BL/6J mice plasma | In Vivo | None | None | EC50(nM) = 0.025 (OTR agonist) | |||
| 27217590 | 2016 | OT (oxytocin) | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | None | Produced in the hypothalamus and released by the posterior pituitary gland | Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia | Time points postdose: 0.25 (OT only), 0.5, 1, 2, 4, 6, and 24 hours (6- and 24-hour sampling limited to PF1 only | 10 ml/kg | 0.5 | C57Bl/6J mice plasma protease | LC-MS/MS | C57BL/6J mice plasma | In Vivo | PDB id: 2MGO | None | EC50(nM) = 0.039 (OTR agonist) | |||
| 27217590 | 2016 | PF1 | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | Substitution of the Pro7 to Gly and Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group, Palm = Palmitic acid | OT analog | Non–brain-penetrant OT receptor agonist | Serial blood samples were collected from each mouse via the retro-orbital sinus at the following time points postdose: 0.5, 1, 2, 4, 6, and 24 hours | 20 mg/kg | 309 | C57Bl/6J mice plasma protease | LC-MS/MS | C57BL/6J mice plasma | In Vivo | None | None | EC50(nM) = 0.025 (OTR agonist) | |||
| 27217590 | 2016 | OT (oxytocin) | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | None | Produced in the hypothalamus and released by the posterior pituitary gland | Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia | Serial blood samples were collected from each mouse via the retro-orbital sinus at the following time points postdose: 0.5, 1, 2, 4, 6, and 24 hours | 20 mg/kg | 7.3 | C57Bl/6J mice plasma protease | LC-MS/MS | C57BL/6J mice plasma | In Vivo | None | None | EC50(nM) = 0.039 (OTR agonist) | |||
| 27166982 | 2016 | ADM analogue 3 | 39 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (C3-C8 Disulfide Linkage) | L | None | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 9.7 | Human blood plasma protease | RP-HPLC | Human blood plasma | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 17 | 38 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (Dpr3-E8 Lactam Bridge) | L | K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1 | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 84.6 | Human blood plasma protease | RP-HPLC | Human blood plasma | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 20 | 38 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (Dpr3-E8 Lactam Bridge) | L | Nα-Methylation of Lysine at position 33, K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1 | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 126.2 | Human blood plasma protease | RP-HPLC | Human blood plasma | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 3 | 39 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (C3-C8 Disulfide Linkage) | L | None | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 3.3 | Porcine liver homogenate protease | RP-HPLC | Porcine liver homogenate | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 20 | 38 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (Dpr3-E8 Lactam Bridge) | L | Nα-Methylation of Lysine at position 33, K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1 | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 38 | Porcine liver homogenate protease | RP-HPLC | Porcine liver homogenate | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27157666 | 2016 | cMBP2-PEG-Stp/NIS Polyplex | 12 | Free | PEG-Stp = succinoyl-tetraethylene pentamine/NIS gene | Linear | L | 123I labeling | Synthetic | Antitumor | 48 hours after polyplex administration, mice received an intraperitoneal injection of 18.5 MBq 123I | 18.5 MBq 123I | 3 | Huh7 subcutaneous mice xenografts protease | Gamma counter | Huh7 subcutaneous mice xenografts | In Vivo | https://sci-hub.st/10.1016/j.nucmedbio.2009.01.005 | None | N.A. | |||
| 27155328 | 2016 | I-3 | 38 | Free | Amidation | Linear | L | X3(Fatty acid structure given in paper) linked with Ser11 | Exendin-4 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points, 100 lL mixture was aliquoted | 1000 ng/mL | 35.6 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vitro | None | None | EC50(pM) =38.47 ± 9.86 | |||
| 27115755 | 2016 | HSA-dTMP | 63 | HSA joined using a linker | Free | Linear | L | None | Fusion protein of dTMP and HSA | Treatment of Thrombocytopenia | Serum was sampled from mice eyes at 5 min, 30 min, 1 h,1.5 h, 2 h, 4 h, 12 h, 24 h, and 48 h after dosing | 300 μg/kg | 17.1 | Mice serum protease | Immunoenzymetric assay | Mice serum | In Vivo | None | None | both HSA-dTMP and dTMP-HSA could significantly increase peripheral platelet counts in a dose-dependent manner in normal mice | |||
| 27115755 | 2016 | dTMP-HSA | 63 | Free | HSA joined using a linker | Linear | L | None | Fusion protein of dTMP and HSA | Treatment of Thrombocytopenia | Serum was sampled from mice eyes at 5 min, 30 min, 1 h,1.5 h, 2 h, 4 h, 12 h, 24 h, and 48 h after dosing | 300 μg/kg | 16.1 | Mice serum protease | Immunoenzymetric assay | Mice serum | In Vivo | None | None | both HSA-dTMP and dTMP-HSA could significantly increase peripheral platelet counts in a dose-dependent manner in normal mice | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Bicarinalin displayed no cytotoxicity against human lymphocytes in concentrations ranging from 0.066 to 8.5 mol L−1 and its LC50 value was 67.8 mol L−1 | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [micromole/L] = 24.4, 5.8, 12.2, 8.7, 5.4 for E.coli, C.sakazakii, P.aeruginosa CIP 82118, P.aeruginosa [R]ATCC 15442, S.enterica respectively. | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [micromole/L] = 12.2, 3, 8.7, 0.45, 24.4 for E.hirae, S.aureus, MRSA, S.xylosus, B.subtilis respectively | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [micromole/L] = 0.75, 17.3, 17.3, 97.5, 6.1 for A.niger, C.albicans, C.albicans[R], G.candidum, S.cerevisiae and MIC[micromole/L] = 1.5 for L.infantum | |||
| 32263229 | 2016 | iT-P/PTX NPs | 5 | Free | TPGS(D-a-tocopherol polyethylene glycol succinate) linked with poly(lactide) using disulfide linkage, cRGD further conjugated to NP surface | Cyclic (RGDfC) | Mix | D-Phe at position 4 | Synthetic | Anticancer | Blood samples were collected in EP tubes containing 20 mL of 1000 U heparin per mL at 0.5, 1, 2, 4, 8, 12, 24, 48 and 72 h for each group. | 10 mg/ kg | 12.68 ± 0.81 | SD rats plasma protease | HPLC | SD rats plasma | In Vivo | None | None | IC50 = 1.90 ± 0.28 mg/mL incubated with A2780 cell | |||
| 26982623 | 2016 | Peptide -5 (LTX-315) | 9 | Free | Amidation | Linear | L | Replacing Trp8 with the more bulky unnatural Dip = Diphenyalanine | Synthetic | Anticancer | 100 µl samples were taken after 0, 10, 20, 45 and 90 min | 1 µM | 71 | Cryopreserved rats hepatocyte protease | LC-MS/MS | Cryopreserved rats hepatocytes at a cell density of 0.5 million cells/ml | In Vitro | None | None | IC50 ± SD in µM = 34.3 ± 2.3 for MRC-5 cells | |||
| 26982623 | 2016 | Peptide -5 (LTX-315) | 9 | Free | Amidation | Linear | L | Replacing Trp8 with the more bulky unnatural Dip = Diphenyalanine | Synthetic | Anticancer | 100 µl samples were taken after 0, 10, 20, 45 and 90 min | 1 µM | 64 | Cryopreserved rats hepatocyte protease | LC-MS/MS | Cryopreserved rats hepatocytes at a cell density of 0.5 million cells/ml | In Vitro | None | None | IC50 ± SD in µM = 34.3 ± 2.3 for MRC-5 cells | |||
| 26905040 | 2016 | WT-EX4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | 37 °C | 200 μg/mL | 16.9 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM | |||
| 26905040 | 2016 | EX4-2K | 40 | Free | PEG(2KDa) linked with Ex-4 through Mal (Maleimide) | Linear | L | None | Exendin-4 analogs | Antidiabetes | 37 °C | 200 μg/mL | 69.2 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM | |||
| 26905040 | 2016 | EX4-5K | 40 | Free | PEG(5KDa) linked with Ex-4 through Mal (Maleimide) | Linear | L | None | Exendin-4 analogs | Antidiabetes | 37 °C | 200 μg/mL | 62.8 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM | |||
| 26905040 | 2016 | EX4-20K | 40 | Free | PEG(20KDa) linked with Ex-4 through Mal (Maleimide) | Linear | L | None | Exendin-4 analogs | Antidiabetes | 37 °C | 200 μg/mL | 69.7 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM | |||
| 26905040 | 2016 | EX4-50K | 40 | Free | (PEG(50KDa))3 linked with Ex-4 through Mal (Maleimide) | Linear | L | None | Exendin-4 analogs | Antisepsis | 37 °C | 200 μg/mL | 234.2 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | A dissociation constant of Kd(app) ≈ 0.159 nM was obtained for the interaction between GLP-1R and EX4-50 | |||
| 26877782 | 2016 | Native Extendin-4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At predetermined times (0, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96 h), blood samples were collected from tail vein of each animal | 25 nmol/kg | 5.16 ± 5.23 | DB/DB mice plasma protease | Exendin-4 EIA | DB/DB mice plasma | In Vivo | None | None | IC50 = 0.21 ± 0.08 nM | |||
| 26877782 | 2016 | Abextide | 40 | Free | tEB (Truncated Evans blue) dye linked via Maleimide | Linear | L | Cys addition at C terminal of Ex4 | Exendin-4 analogs | Antidiabetes | At predetermined times (0, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96 h), blood samples were collected from tail vein of each animal | 25 nmol/kg | 36.28 ± 7.01 | DB/DB mice plasma protease | Exendin-4 EIA | DB/DB mice plasma | In Vivo | None | None | IC50 = 0.18 ± 0.06 nM | |||
| 26869426 | 2016 | HsTX1[R14A] | 34 | Free | Amidation | Cyclic (C3-C24, C9-C29, C13-C31 Disulfide Linkage) | L | R14A substituitions | Isolated from the scorpion Heterometrus spinnifer | Treatment of Autoimmune Diseases | Blood samples (500 mL) were collected at 5, 15,30, 60, 120, 180, 240, and 300 min | 2 mg/kg | 79.6 ± 6.5 (Terminal elimination half life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/instance/2144240/pdf/10631983.pdf | None | IC50 value of 45 pM (affinity for Kv1.3 channels) | |||
| 26835125 | 2016 | IONP-HA-GEM-CTX-Cy5.5 | 36 | Conjugation of HA into CTX at N terminal in IONP-HA-GEM | Cy5.5 labeled | Linear | L | None | Synthetic | Glioblastoma therapy | At 1.5, 3, 6, 16, 24 and 48 h after injection, blood (20-50 L) was collected from tail veins | 2 mg/ml | ~2.8 | BALB/c mice blood plasma protease | Fluorescence spectrometry | BALB/c mice blood plasma | In Vivo | PDB id: 1CHL | None | N.A. | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 10.1 ± 0.5 (Elimination Half Life) | Human blood plasma protease | RIA | Human blood plasma with 2 × 100 mg sitagliptin | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 9.4 ± 0.8 (Elimination Half Life) | Human blood plasma protease | RIA | Human blood plasma | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY3-36 | 34 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 14.9 ± 1.3 (Elimination Half Life) | Human blood plasma protease | RIA (total PYY assay) | Human blood plasma | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Samples were taken regularly (t = 0, 0.5, 1, 2, 3, 4, 6, 8, 21, and 24 h) | 0.6 pmol/mL | 22.8 ± 8.0 − 3.6 ± 0.6 | Human blood plasma protease | RIA (when correcting for NH2-terminal degradation) | Human blood with EDTA, aprotinin (500 KIE/ml), and the DPP-4 inhibitor valine pyrrolidide (0.01 mmol/l, final concentration (when correcting for NH2-terminal degradation) | In Vitro | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Samples were taken regularly (t = 0, 0.5, 1, 2, 3, 4, 6, 8, 21, and 24 h) | 0.6 pmol/mL | 8.6 ± 3.6 | Human blood plasma protease | RIA (when we corrected for NH2-terminal degradation) | Human blood plasma with EDTA, aprotinin (500 KIE/ml), and the DPP-4 inhibitor valine pyrrolidide (0.01 mmol/l, final concentration (when correcting for NH2-terminal degradation) | In Vitro | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26808305 | 2016 | αAnalogue | 37 | Fatty acid moiety attached to Ser1 at N terminal | Amidation | Cyclic (Disulfide Bridge Between Positions 2 And 7) | L | None | CGRP analogue | Vasodilatory effect | Blood (200 µl) was sampled from vena sublingualis from anaesthetised rats at pre-dose and at 0.5, 1, 3, 7 and 24 h post dosing | 151 nmol/kg | 10.2 ± 0.9 | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | https://sci-hub.st/10.1126/science.2994212, | None | N.A. | |||
| 26808199 | 2016 | PYY24–36 | 13 | Free | Amidation | Linear | L | None | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | <0.5 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 8 | 13 | R8( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | 24 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 2 | 13 | R2( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | >20 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 5 | 13 | R5( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 7 | 13 | R7( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 9 | 13 | R9( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26806490 | 2016 | Wild-type IFN | 165 | Free | Free | Linear | L | None | Recombinant human IFN-α2b | Antiviral, Anticancer | N.A. | 1*106 U / 200 g | 1.4 ± 0.3 (Elimination Half Life) | Wistar rats plasma protease | N.A. | Female Wistar rats plasma | In Vivo | PDB id: 1RH2 | None | Specific antiviral bioactivity (U ng−1) = 185 ± 30, Specific antiproliferative bioactivity (U ng−1) = 309 ± 65 | |||
| 26806490 | 2016 | CTP-IFN | 193 | CTP ( the terminal peptide of the β subunit of human chorionic gonadotropin (hCG)) | Free | Linear | L | None | Recombinant human IFN-α2b | Antiviral, Anticancer | N.A. | 1*106 U / 200 g | 7.8 ± 0.7 (Elimination Half Life) | Wistar rats plasma protease | N.A. | Female Wistar rats plasma | In Vivo | PDB id: 1HCN | None | Specific antiviral bioactivity (U ng−1) = 65 ± 3, Specific antiproliferative bioactivity (U ng−1) = 19 ± 9 | |||
| 26806490 | 2016 | IFN-CTP | 193 | Free | CTP ( the terminal peptide of the β subunit of human chorionic gonadotropin (hCG)) | Linear | L | None | Recombinant human IFN-α2b | Antiviral, Anticancer | N.A. | 1*106 U / 200 g | 8.4 ± 1.5 (Elimination Half Life) | Wistar rats plasma protease | N.A. | Female Wistar rats plasma | In Vivo | None | None | Specific antiviral bioactivity (U ng−1) = 58 ± 6, Specific antiproliferative bioactivity (U ng−1) = 26 ± 8 | |||
| 26806490 | 2016 | CTP-IFN-CTP | 221 | CTP ( the terminal peptide of the β subunit of human chorionic gonadotropin (hCG)) | CTP ( the terminal peptide of the β subunit of human chorionic gonadotropin (hCG)) | Linear | L | None | Recombinant human IFN-α2b | Antiviral, Anticancer | N.A. | 1*106 U / 200 g | 13.4 ± 1.5 (Elimination Half Life) | Wistar rats plasma protease | N.A. | Female Wistar rats plasma | In Vivo | None | None | Specific antiviral bioactivity (U ng−1) = 44 ± 3, Specific antiproliferative bioactivity (U ng−1) = 9 ± 1 | |||
| 26774588 | 2016 | PYY3-36 | 34 | Free | Amidation | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 175 | Minipigs heparin-plasma protease | LC-MS | Minipigs heparin-plasma | In Vitro | None | None | N.A. | |||
| 26774588 | 2016 | PYY3-36 | 34 | Free | Amidation | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 220 | Minipigs heparin-plasma protease | LC-MS | minipigs heparin-plasma with 10 mM EDTA | In Vitro | None | None | N.A. | |||
| 26774588 | 2016 | PYY3-35 | 33 | Free | Free | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 6 | Minipigs heparin-plasma protease | LC-MS | minipigs heparin-plasma | In Vitro | None | None | N.A. | |||
| 26774588 | 2016 | PYY3-35 | 33 | Free | Free | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 39 | Minipigs heparin-plasma protease | LC-MS | minipigs heparin-plasma with 10 mM EDTA | In Vitro | None | None | N.A. | |||
| 26754785 | 2016 | TfCuMT | 108 | Free | Free | Cyclic (4 Disulfide Bond Cys-Cys) | L | None | Copper metallothionein derived from ciliate Tetrahymena farahensis | Involved in metal homeostasis and metal detoxification by forming metal-thiolate complex | 37°C | N.A. | 103 | N.A. | SDS PAGE | Sonicated sample (20ml) +5 ml SDS loading buffer (50% glycerol, 10% SDS,0.5 M dithiothreitol, 0.25% bromophenol blue, 0.25 M Tris-Cl pH6.8) | In Vitro | None | None | N.A. | |||
| 26752086 | 2016 | ABB28 | 38 | 7 mer ABD domain conjugated at N terminus | Amidation | Linear | L | Biotinylation | Synthetic | Antitumor | N.A. | 30 nmol | 2 | BALB/c mice plasma protease | ELISA | BALB/c mice plasma | In Vivo | None | None | IC50 ranges from 2.1–2.5 mM (In the absence of FBS) for ABB28 | |||
| 26752086 | 2016 | BB28 | 31 | conjugating a truncated antimicrobial peptide B28 to the N-terminus of the tumor-homing peptide bombesin | Amidation | Linear | L | Biotinylation | Synthetic | Antitumor | N.A. | 30 nmol | <5 | BALB/c mice plasma protease | ELISA | BALB/c mice plasma | In Vivo | None | None | IC50 ranges from 2.5–3.0 mM (In the absence of FBS) for BB28 | |||
| 26741458 | 2016 | Peptide 1 | 6 | Free | Free | Linear | L | None | Synthetic | Hydrogelators | Degradation was monitored after 0, 1, 2, 3, 4, 5, and 10 min | 34 μM | 3.43 ± 0.06 | Human blood plasma protease | HPLC | Human blood plasma | In Vitro | None | None | N.A. | |||
| 26741458 | 2016 | Peptide 2 | 8 | Free | Free | Linear | L | β3-homophenylalanine (β3-hPhe) at position 3 and 6 | Synthetic | Hydrogelators | During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min. | 33 μM | 19.53 ± 0.55 | Human blood plasma protease | HPLC | Human blood plasma | In Vitro | None | None | N.A. | |||
| 26741458 | 2016 | Peptide 3 | 8 | Free | Amidation | Linear | L | β3-homophenylalanine (β3-hPhe) at position 3 and 6 | Synthetic | Hydrogelators | During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min. | 33 μM | 40.00 ± 1.28 | Human blood plasma protease | HPLC | Human blood plasma | In Vitro | None | None | N.A. | |||
| 26741458 | 2016 | Peptide 4 | 8 | Free | Amidation | Linear | L | β3-homophenylalanine (β3-hPhe) at position 3 and 6, substitution of Phe with Tyr at positions 4 and 7 | Synthetic | Hydrogelators | During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min. | 33 μM | 18.71 ± 0.44 | Human blood plasma protease | HPLC | Human blood plasma | In Vitro | None | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 0.05784 | Chymotrypsin | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with Chymotrypsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 3.53 | Aminopeptidase N | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with APN (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 10.16 | Carboxy-Peptidase A | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with CPA (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 12.38 | Trypsin | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with Trypsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 14.28 | Pepsin | Mass spectrometry | Gastric fluid solution (pH 1.2) with Pepsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 37°C | 100 µg/mL | 1.718 | Intestinal duodenum homogenate protease | Ultraviolet spectroscopy | Intestinal duodenum homogenate | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 37°C | 100 µg/mL | 1.462 | Intestinal jejunum homogenate protease | Ultraviolet spectroscopy | Intestinal jejunum homogenate | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 37°C | 100 µg/mL | 1.229 | Intestinal ileum homogenate protease | Ultraviolet spectroscopy | Intestinal ileum homogenate | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 28989813 | 2016 | Exendin | 39 | Free | Amidation | Linear | L | Fluorescently labeled with Alexa Fluor | Derived from Heloderma suspectum | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 1.7 ± 0.2 (T1/2 Elimination Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 0.08 ± 0.01 | |||
| 28989813 | 2016 | 54.6 kDa EG9 | 43 | Free | AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(54.6KDa) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-4 analogs | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 42.4 ± 2.9 (T1/2 Elimination Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50(nM) = 1.91 ± 0.35 | |||
| 28989813 | 2016 | 55.6 kDa EG3 | 43 | Free | AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(55.6KDa) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-4 analogs | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 61.2 ± 5.0 (T1/2 Elimination Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50(nM) = 4.17 ± 0.13 | |||
| 28989813 | 2016 | 71.6 kDa EG3 | 43 | Free | AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(71.6KDa) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-4 analogs | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 61.5 ± 3.2 (T1/2 Elimination Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50(nM) = 5.11 ± 0.23 | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 3.6 mg/kg | 3.12 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 3.6 mg/kg | 4.33 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 36 mg/kg | 3.69 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 36 mg/kg | 5.18 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 180 mg/kg | 4.79 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 180 mg/kg | 5.5 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 3.6 mg/kg | 6.6 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 3.6 mg/kg | 7.75 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 36 mg/kg | 3.71 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 36 mg/kg | 5.36 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 180 mg/kg | 6.24 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 180 mg/kg | 6.2 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 1.5 mg/kg | 12.76 ± 2.06 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 1.5 mg/kg | 16.17 ± 2.30 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 15 mg/kg | 15.88 ± 0.98 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 15 mg/kg | 15.47 ± 1.84 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 30 mg/kg | 16.66 ± 2.41 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 30 mg/kg | 16.93 ± 2.01 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 181 | 1.5 mg/kg | 15.40 ± 7.39 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 181 | 1.5 mg/kg | 17.01 ± 6.91 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 181 | 15 mg/kg | 16.57 ± 6.32 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 181 | 15 mg/kg | 19.94 ± 8.77 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 181 | 30 mg/kg | 22.44 ± 12.53 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 181 | 30 mg/kg | 22.54 ± 19.55 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26628555 | 2016 | HLDF-6-NH2 | 6 | 3H labeling at N terminal | Amidation | Linear | L | None | Isolated from the culture medium of retinoic acid-treated HL-60 cells | Neuroprotective And Nootropic Activities | N.A. | N.A. | 8 | Wistar rats blood plasma protease | N.A. | Wistar rats blood plasma | In Vivo | None | None | ChAT activity, dpm/mg of tissue = 5.61±0.40 in (βA + HLDF-6-NH2,250 µg/kg) | |||
| 26628555 | 2016 | HLDF-6-OH | 6 | 3H labeling at N terminal | Free | Linear | L | None | Isolated from the culture medium of retinoic acid-treated HL-60 cells | Neuroprotective And Nootropic Activities | N.A. | N.A. | 2 | Wistar rats blood plasma protease | N.A. | Wistar rats blood plasma | In Vivo | None | None | ChAT activity, dpm/mg of tissue = 5.29±0.34 in (βA + HLDF-6-OH,250 µg/kg) | |||
| 26574515 | 2016 | CII-a | 40 | Free | Free | Linear | L | Two amphipathic helices linked by proline19 | Synthetic | Treatment of Hypertriglyceridemia | 0, 0.5, 1, 4, 7, 24, and 48 hours | 1.0μmol/kg of body weight | 1.33 ± 0.72 | Apoc2 Mutant Mice Plasma Protease | MALDI-TOF MS | Apoc2 mutant mice plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC4293430/ | None | peptide C-II-a dose of 5 μmol/kg achieved a maximum decrease of approximately 90% after 30 minutes, with plasma TG remaining below baseline levels for up to 48 hours | |||
| 26574515 | 2016 | CII-a | 40 | Free | Free | Linear | L | Two amphipathic helices linked by proline19 | Synthetic | Treatment of Hypertriglyceridemia | 0, 0.5, 1, 4, 7, 24, and 48 hours | 1.0 μmol/kg of body weight | 1.33 ± 0.72 | Apoc2 mutant mice plasma protease | MALDI-TOF MS | Apoc2 mutant mice plasma | In Vivo | None | None | peptide C-II-a dose of 5 μmol/kg achieved a maximum decrease of approximately 90% after 30 minutes, with plasma TG remaining below baseline levels for up to 48 hours | |||
| 26565554 | 2016 | NG29-TFacetate | 10 | SarLys = N-methyl glycine and Lysine | TFacetate = Trifluoroacetate addition at C terminal | Linear | Mix | D-Phenyalanine substituitions for L-Phenylanine and Arg9 removal from C terminal | BK analogue | Role in Neurological and Ischemic Cardiovascular diseases and brain cancer | N.A. | 75 mg/kg | 2.28 (Elimination Half Life) | Wistar Han rats plasma protease | LC-MS/MS | Wistar Han rats plasma | In Vivo | https://sci-hub.st/10.1139/y02-053 | None | IC50(nM) = 0.3 for SarLys[dPhe8]desArg9BK ( for hB1R ) | |||
| 26565554 | 2016 | NG29-acetate | 10 | SarLys = N-methyl glycine and Lysine | Acetate addition at C terminal | Linear | Mix | (f) D-Phenyalanine substituitions for L-Phenylanine (F) and Arg9 removal from C terminal | BK analogue | Role in Neurological and Ischemic Cardiovascular diseases and brain cancer | N.A. | 75 mg/kg | 2.38 (Elimination Half Life) | Wistar Han rats plasma protease | LC-MS/MS | Wistar Han rats plasma | In Vivo | None | None | IC50(nM) = 0.3 for SarLys[dPhe8]desArg9BK ( for hB1R ) | |||
| 26507721 | 2016 | Dulaglutide | 275 | Free | IgG4 Fc fused at C terminal using GS linker | Linear | L | None | GLP-1 analogs | Antidiabetes | 4 to 6 weeks | 0.75 mg | 5.5 (GM) | Human plasma protease | RIA | Human plasma after multiple doses of dulaglutide once weekly, ranging from 4 to 6 weeks | In Vivo | DB id: DB09045 | None | N.A. | |||
| 26507721 | 2016 | Dulaglutide | 275 | Free | IgG4 Fc fused at C terminal using GS linker | Linear | L | None | GLP-1 analogs | Antidiabetes | 4 to 6 weeks | 1.5 mg | 4.7 (GM) | Human plasma protease | RIA | Human plasma after multiple doses of dulaglutide once weekly, ranging from 4 to 6 weeks | In Vivo | DB id: DB09045 | None | N.A. | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 3 min, 5 min, 10 min, 15 min, 30 min, 1 h, 4 h, 1 d, 2 d, 7 d, 28 d | 3.3 mg/kg | 59 (Terminal Half Life) | Mouse plasma protease | TLC | Mouse plasma | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d | 10 mg/kg | 62 (Terminal Half Life) | Mouse plasma protease | TLC | Mouse plasma | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d | 10 mg/kg | 60 (Terminal Half Life) | Mouse plasma protease | TLC | Mouse plasma | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 18 h, 1 d, 2 d, 3 d, 7 d, 28 d | 10 mg/kg | 58 (Terminal Half Life) | Mouse plasma protease | TLC | Mouse plasma | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 3 min, 5 min, 10 min, 15 min, 30 min, 1 h, 4 h, 1 d, 2 d, 7 d, 28 d | 3.3 mg/kg | 60 (Terminal Half Life) | Mouse brain homogenate protease | TLC | Mouse brain homogenate | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d | 10 mg/kg | 61 (Terminal Half Life) | Mouse brain homogenate protease | TLC | Mouse brain homogenate | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d | 10 mg/kg | 94 (Terminal Half Life) | Mouse brain homogenate protease | TLC | Mouse brain homogenate | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 18 h, 1 d, 2 d, 3 d, 7 d, 28 d | 10 mg/kg | 73 (Terminal Half Life) | Mouse brain homogenate protease | TLC | Mouse brain homogenate | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 20 mg | 5.9 | Human serum protease | HPLC–MS/MS | Human serum (Japanese) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 80 mg | 13.7 | Human serum protease | HPLC–MS/MS | Human serum (Japanese) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 240 mg | 23.5 | Human serum protease | HPLC–MS/MS | Human serum (Japanese) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 20 mg | 6.9 | Human serum protease | HPLC–MS/MS | Human serum ( Caucasians) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 80 mg | 14.4 | Human serum protease | HPLC–MS/MS | Human serum ( Caucasians) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 240 mg | 26.1 | Human serum protease | HPLC–MS/MS | Human serum ( Caucasians) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 27393654 | 2016 | IFN-α | 165 | Free | Free | Linear | L | None | Human derived | Antiproliferative, immunoregulatory and antiviral | At desired time points (1, 5, 15, 30 min, 1, 3, 6, 24,48, 72 and 96 h) | 1 mg IFN-α equivalent/kg | 0.33 (T1/2a- Distribution Half Life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 1ITF | None | IC50 = 10.77 pg/mL | |||
| 27393654 | 2016 | IFN-PMPC | 165 | Free | Poly(2-Methacryloyloxyethyl Phosphorylcholine) | Linear | L | None | Human derived | Antiproliferative, immunoregulatory and antiviral | At desired time points (1, 5, 15, 30 min, 1, 3, 6, 24,48, 72 and 96 h) | 1 mg IFN-α equivalent/kg | 2 (T1/2a- Distribution Half Life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 1ITF | None | IC50 = 20.02 pg/mL | |||
| 28989813 | 2016 | Exendin | 39 | Free | Amidation | Linear | L | Fluorescently labeled with Alexa Fluor | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 0.7 ± 0.1 (T1/2 Absorption Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 0.08 ± 0.01 | |||
| 28989813 | 2016 | 54.6 kDa EG9 | 40 | Free | Poly[Oligo(Ethylene Glycol)9 Methyl Ether Methacrylate] = Poegma(54.6 Kda) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-C-POEGMA conjugates | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 6.2 ± 0.5 (T1/2 Absorption Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 1.91 ± 0.35 | |||
| 28989813 | 2016 | 55.6 kDa EG3 | 40 | Free | Poly[Oligo(Ethylene Glycol)3 Methyl Ether Methacrylate] = Poegma(55.6Kda) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-C-POEGMA conjugates | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 7.6 ± 0.7 (T1/2 Absorption Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 4.17 ± 0.13 | |||
| 28989813 | 2016 | 71.6 kDa EG3 | 40 | Free | Poly[Oligo(Ethylene Glycol)3 Methyl Ether Methacrylate] = Poegma(71.6Kda) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-C-POEGMA conjugates | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 9.0 ± 1.7 (T1/2 Absorption Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 5.11 ± 0.23 | |||
| 26552936 | 2016 | DDD | 591 | Free | Free | Linear | L | His-tag | Wild-type KerSMD | Keratinase | 60°C | N.A. | 41 ± 15 (Activity Half Life) | N.A. | Enzyme activity assay | DDD | In Vitro | None | None | Activity with Casein (U mg−1) = 3779 ± 20 | |||
| 26552936 | 2016 | DDF | 590 | Free | T1 From KERsmf | Linear | L | His-tag | KerSMD mutants | Keratinase | 60°C | N.A. | 105.3 ± 5 (Activity Half Life) | N.A. | Enzyme activity assay | DDF | In Vitro | None | None | Activity with Casein (U mg−1) = 4467 ± 14 | |||
| 26552936 | 2016 | FDD | 572 | P1 Substituitions From Kersmf | Free | Linear | L | His-tag | KerSMD mutants | Keratinase | 60°C | N.A. | 152.2 ± 2 (Activity Half Life) | N.A. | Enzyme activity assay | FDD | In Vitro | None | None | Activity with Casein (U mg−1) =7844 ± 25 | |||
| 26552936 | 2016 | FDF | 571 | P1 Substituitions From Kersmf | T1 Substituitions From Kersmf | Linear | L | His-tag | KerSMD mutants | Keratinase | 60°C | N.A. | 244.6 ± 2 (Activity Half Life) | N.A. | Enzyme activity assay | FDF | In Vitro | None | None | Activity with Casein (U mg−1) =8229 ± 50 | |||
| 26552936 | 2016 | DD | 486 | Free | T2 Removed | Linear | L | His-tag | KerSMD mutants | Keratinase | 60°C | N.A. | 5.6 ± 2 (Activity Half Life) | N.A. | Enzyme activity assay | DD | In Vitro | None | None | Activity with Casein (U mg−1) = 4328 ± 18 | |||
| 26552936 | 2016 | FD | 467 | P1 From KERsmf | T2 Removed | Linear | L | His-tag | KerSMD mutants | Keratinase | 60°C | N.A. | 36.5 ± 6 (Activity Half Life) | N.A. | Enzyme activity assay | FD | In Vitro | None | None | Activity with Casein (U mg−1) = 9876 ± 50 | |||
| 26673564 | 2016 | H3 | 30 | Free | Free | Linear | L | None | Histone 3 | Structural role | preincubated for 1 h | 3.0 μM | 9.63 (Activity Half Life) | N.A. | Resorufin-derived absorbance assay | Assay buffer containing 25 μM peptide substrate, 50 μM Amplex Red, and 1 unit/mL HRP and H3 | In Vitro | None | None | IC50(nM) =153 | |||
| 133-353-120-049-121 | 2016 | rHuEPO-Fc | 399 | Free | Free | Linear | L | Fusion with IgG Fc fragment | Human erythropoietic protein Fusion with IgG Fc fragment | Immunogenic | N.A. | 5 ug/kg | 35.24+/-5.15 | Not mentioned | ELISA | Blood | in vivo | https://lens.org/133-353-120-049-121 | US 9,375,487 B2 | N.A. | |||
| 076-262-596-914-468 | 2016 | GLP-1 ELP1-120 | NA | His7 of GLP1 | Free | Linear | L | Fusion with ELP | preproglucagon | N.A. | N.A. | 10mg/kg | 12.9 | Tev protease | Bioassay | Rat | in vivo | https://www.lens.org/lens/patent/076-262-596-914-468 | US 9,458,218 B2 | N.A. | |||
| 076-262-596-914-468 | 2016 | GLP-1 ELP1-120 | NA | His7 of GLP1 | Free | Linear | L | Fusion with ELP | preproglucagon | N.A. | N.A. | 1 mg/kg | 20 | Tev protease | Bioassay | Rabbit | in vivo | https://www.lens.org/lens/patent/076-262-596-914-468 | US 9,458,218 B2 | N.A. | |||
| 107-968-725-190-134 | 2016 | Ex-4 | 39 | Free | Free | Linear | L | None | NA | N.A. | 30 min | 25 μM | 38 | chymotrypsin | ELISA | male C57BL/6 mice serum | in vivo | https://lens.org/107-968-725-190-134 | US 9,296,805 B2 | N.A. | |||
| 107-968-725-190-134 | 2016 | singly stapled SAH-Ex(A) | 39 | Stapled | Free | Linear | L | None | NA | N.A. | 30 min | 25 μM | 94 | chymotrypsin | ELISA | male C57BL/6 mice serum | in vivo | https://lens.org/107-968-725-190-134 | US 9,296,805 B2 | N.A. | |||
| 107-968-725-190-134 | 2016 | singly stapled SAH-Ex(B) | 39 | Stapled | Free | Linear | L | None | NA | N.A. | 30 min | 25 μM | 128 | chymotrypsin | ELISA | male C57BL/6 mice serum | in vivo | https://lens.org/107-968-725-190-134 | US 9,296,805 B2 | N.A. | |||
| 107-968-725-190-134 | 2016 | doubly stapled peptide SAH-Ex(A, B) | 39 | Stapled | Stapled | Linear | L | None | NA | N.A. | 30 min | 25 μM | 295 | chymotrypsin | ELISA | male C57BL/6 mice serum | in vivo | https://lens.org/107-968-725-190-134 | US 9,296,805 B2 | N.A. | |||
| 106-160-175-860-210 | 2016 | P28 | 28 | acetylate | amidated | Cyclic | L | enzymatically cyclized | P. aeruginosa azurin | Therapeutic | 72 hours | 10 μl | Increased | NA | MTT | Human Cancer Cells | in vivo | https://lens.org/106-160-175-860-210 | US 9,434,770 B2 | N.A. | |||
| 059-320-765-410-102 | 2016 | FGF21 | NA | 6-his tag, free cysteine | 182P | Linear | L | Vitamin D3-PEG-maleimide | E. coli | Therapeutic | NA | 0.1 mg/kg | 675-fold increase | NA | ELISA | Rats | in vivo | https://www.lens.org/lens/patent/059-320-765-410-102 | US 9,289,507 B2 | N.A. | |||
| 059-320-765-410-102 | 2016 | rGhrelin-carrier conjugate | NA | Free | cysteine | Linear | L | Vitamin D3-PEG-maleimide | E. coli | Therapeutic | NA | 0.1 mg/kg | 8 | NA | ELISA | Rats | in vivo | https://www.lens.org/lens/patent/059-320-765-410-102 | US 9,289,507 B2 | N.A. | |||
| 043-207-181-799-34X | 2016 | Coagulation Factor VII | 444 | Free | 3CTPs | Linear | L | CTP | hepatocytes | 60 sec | 100 μl | 4.07 | serine protease | ELISA | Blood Stream | in vivo | https://www.lens.org/lens/patent/043-207-181-799-34X | US 9458444 B2 | N.A. | ||||
| 136-103-666-814-603 | 2016 | bi-specific fusion protein | 19 | Free | Free | Linear | L | None | NA | non-immunogenic protein | NA | NA | between 2 hours and 24 hours, greater than 24 hours, or greater than one week | NA | ELISA | in vivo | https://www.lens.org/lens/patent/136-103-666-814-603 | US 9238080 B2 | N.A. | ||||
| 032-864-902-079-483 | 2016 | glucagon-like peptide-2 | 33 | removing α-carbon of histidine | thiol group | Linear | L | None | NA | NA | NA | NA | Increased | NA | NA | NA | in vivo | https://lens.org/032-864-902-079-483 | US 9504757 B2 | NA | |||
| 191-672-090-004-249 | 2016 | human albumin | NA | Free | Free | Linear | L | None | Human | NA | NA | NA | NA | NA | NA | NA | in vivo | https://lens.org/191-672-090-004-249 | US 9352016 B2 | NA | |||
| 023-486-744-040-716 | 2016 | Factor Xa variant | NA | Free | Free | Linear | L | None | Human | NA | NA | NA | 1 | intracellular protease | aPTT-based assay | CHO cells | in vivo | https://lens.org/023-486-744-040-716 | US 9371522 B2 | NA | |||
| 130-503-305-403-520 | 2016 | IL-22 dimer | 308 | Free | Free | Linear | L | None | Human | NA | 20-30 min | 100 μg/kg | 1.3 | NA | MTT | PC12 cells | in vitro | https://lens.org/130-503-305-403-520 | US 9352024 B2 | NA | |||
| 033-015-326-560-809 | 2016 | Lipocalin 2 mutein | 178 | Free | Free | Linear | L | None | Human | antagonist | 30 min | NA | NA | serine protease | ELISA | NA | in vivo | https://lens.org/033-015-326-560-809 | US 9260492 B2 | NA | |||
| 030-841-916-119-277 | 2017 | GLP-1 | 30 | Free | Fusion with ELP | Linear | L | None | synthetic | agonists | 15-60 min | 300-500 mg/dl | 20 | NA | cAMP assay | rabbits | in vivo | https://lens.org/030-841-916-119-277 | US 9821036 B2 | NA | |||
| 030-841-916-119-277 | 2017 | GLP-1 | 30 | Free | Fusion with ELP | Linear | L | None | synthetic | agonists | 15-60 min | 300-500 mg/dl | 24 | NA | cAMP assay | rabbits | in vivo | https://lens.org/030-841-916-119-277 | US 9821036 B2 | NA | |||
| 030-841-916-119-277 | 2017 | GLP1 | 30 | Free | Fusion with ELP | Linear | L | None | synthetic | agonists | 15-60 min | 300-500 mg/dl | 12.9 | NA | cAMP assay | rats | in vivo | https://lens.org/030-841-916-119-277 | US 9821036 B2 | NA | |||
| 030-841-916-119-277 | 2017 | GLP1 | 30 | Free | Fusion with ELP | Linear | L | None | synthetic | agonists | 15-60 min | 300-500 mg/dl | 8.6 | NA | cAMP assay | rats | in vivo | https://lens.org/030-841-916-119-277 | US 9821036 B2 | NA | |||
| 179-033-965-606-598 | 2017 | insulin | 21 | Free | Free | Linear | L | None | Human | NA | 0.02 mg/kg | Less than 20K-PEG-insulin | NA | enzyme immunoassay | Rat Blood | in vivo | https://lens.org/179-033-965-606-598 | US 9616109 B2 | EC50 = 7.9ng/ml | ||||
| 179-033-965-606-598 | 2017 | 20K-PEG-insulin | NA | 20K-PEG | Free | Linear | L | None | Human | NA | 15 min | NA | improved | NA | enzyme immunoassay | Rat Blood | in vivo | https://lens.org/179-033-965-606-599 | US 9616109 B2 | EC50 =26.3ng/ml | |||
| 179-033-965-606-598 | 2017 | VitD-(25)-PEG2K-insulin | NA | VitD-(25)-PEG2K | Free | Linear | L | None | Human | NA | 2-16 hours | NA | improved | NA | enzyme immunoassay | Rat Blood | in vivo | https://lens.org/179-033-965-606-600 | US 9616109 B2 | EC50 =15.8ng/ml | |||
| 179-033-965-606-598 | 2017 | VitD-(3)-PEG1.2K-insulin | NA | VitD-(3)-PEG1.2K | Free | Linear | L | None | Human | NA | 20 min | NA | Drastically Improved | NA | enzyme immunoassay | Rat Blood | in vivo | https://lens.org/179-033-965-606-601 | US 9616109 B2 | EC50= 282.2ng/ml | |||
| 025-814-764-427-267 | 2017 | PB1120 | 28 | VIP with a Met | ELP(1-120) | linear | L | None | Synthetic | NA | 30 min | 3 mg/kg | 45.8 | NA | cell-based bioassay | Monkeys | in vivo/vitro | https://www.lens.org/lens/patent/025-814-764-427-267 | US 9,700,598 B2 | NA | |||
| 138-792-131-275-411 | 2017 | HRS (1-60) | 67 | Free | Free | Linear | L | None | Synthetic | Therapeutic | 1.5 hr | 8 mg/kg | 0.5 | NA | ELISA | mice | in vivo | https://lens.org/138-792-131-275-411 | US 9587235 B2 | NA | |||
| 138-792-131-275-411 | 2017 | Fc-HRS (2-60) | 293 | Fc | Free | Linear | L | None | Synthetic | Therapeutic | 1.5 hr | 8 mg/kg | 72 | NA | ELISA | mice | in vivo | https://lens.org/138-792-131-275-411 | US 9587235 B2 | NA | |||
| 138-792-131-275-411 | 2017 | HRS (1-60)-Fc | 293 | Free | Fc | Linear | L | None | Synthetic | Therapeutic | 1.5 hr | 8 mg/kg | 33 | NA | ELISA | mice | in vivo | https://lens.org/138-792-131-275-411 | US 9587235 B2 | NA | |||
| 138-792-131-275-411 | 2017 | HRS (1-60) | 67 | Free | Free | Linear | L | None | Synthetic | Therapeutic | 1.5 hr | 8 mg/kg | 0.7 | NA | ELISA | mice | in vivo | https://lens.org/138-792-131-275-411 | US 9587235 B2 | NA | |||
| 138-792-131-275-411 | 2017 | Fc-HRS (2-60) | 293 | Fc | Free | Linear | L | None | Synthetic | Therapeutic | 1.5 hr | 8 mg/kg | 71 | NA | ELISA | mice | in vivo | https://lens.org/138-792-131-275-411 | US 9587235 B2 | NA | |||
| 138-792-131-275-411 | 2017 | HRS (1-60)-Fc | 293 | Free | Fc | Linear | L | None | Synthetic | Therapeutic | 1.5 hr | 8 mg/kg | 37 | NA | ELISA | mice | in vivo | https://lens.org/138-792-131-275-411 | US 9587235 B2 | NA | |||
| 159-909-893-044-968 | 2017 | adrenomedullin | 44 | lipid | free | Linear | D | None | human adrenomedullin peptide | agonistic | NA | NA | 1.5 | NA | ELISA | SHR rat | in vivo | https://lens.org/159-909-893-044-968 | US 9694051 B2 | NA | |||
| 013-179-165-807-035 | 2017 | hFc-Apelin13 | 298 | hFC | free | Linear | L | None | human adrenomedullin peptide | na | 2 HRS | 10 μg/mL | 01-Oct | NA | ELISA | C57/Bl6 mice | in vivo | https://lens.org/038-310-729-099-192 | US 9789197 B2 | NA | |||
| 013-179-165-807-035 | 2017 | Apelin13-hFc | 289 | free | hFC | Linear | L | None | human adrenomedullin peptide | na | 2 HRS | 3 μg/mL | 01-Oct | NA | ELISA | C57/Bl6 mice | in vivo | https://lens.org/038-310-729-099-192 | US 9789197 B2 | NA | |||
| 092-334-515-289-964 | 2017 | PB1120 | 29 | VIP | ELP (1-120) | Linear | L | None | NA | anti-hypertensive | NA | NA | 45.8 | NA | NA | Monkeys | in vitro | https://lens.org/092-334-515-289-964 | US 9561262 B2 | NA | |||
| 034-343-155-162-302 | 2017 | Ex4 | 87 | Free | Free | Linear | L | None | NA | NA | NA | NA | 38 | chymotrypsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA | |||
| 034-343-155-162-302 | 2017 | singly stapled SAH-Ex(A) | NA | SAH | Free | Linear | L | None | NA | NA | NA | NA | 94 | chymotrypsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA | |||
| 034-343-155-162-302 | 2017 | singly stapled SAH-Ex(B) | NA | SAH | Free | Linear | L | None | NA | NA | NA | NA | 128 | chymotrypsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA | |||
| 034-343-155-162-302 | 2017 | doubly stapled SAH-Ex(A, B) | NA | SAH | Free | Linear | L | None | NA | NA | NA | NA | 295 | chymotrypsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA | |||
| 034-343-155-162-302 | 2017 | exenatide | 87 | Free | Free | Linear | L | None | NA | NA | NA | NA | 13 | pepsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA | |||
| 034-343-155-162-302 | 2017 | singly stapled SAH-Ex(A) | NA | Free | SAH | Linear | L | None | NA | NA | NA | NA | 81 | pepsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA | |||
| 034-343-155-162-302 | 2017 | SAH-Ex(A, B) | NA | Free | SAH | Linear | L | None | NA | NA | NA | NA | 172 | pepsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA |