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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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 10541299 | 1999 | Epoetin | 166 | Free | Free | Cyclic | L | Three N-linked carbohydrate chains | Recombinant human erythropoietin | Stimulates erythropoiesis | Not mentioned | Not mentioned | 8.5 ±2.4 | Human blood proteases | ELISA | Subcutaneously injected into patients with end-stage renal failure | in vivo | http://www.drugbank.ca/drugs/DB00016 | None | Not reported | |||
| 10541299 | 1999 | Novel erythropoiesis stimulating protein (NESP) | 166 | Free | Free | Cyclic | L | Five N-linked carbohydrate chains | Hyperglycosylated analogue of recombinant human erythropoietin | Stimulates erythropoiesis | Not mentioned | Not mentioned | 25.3 ±2.2 | Human blood proteases | ELISA | Subcutaneously injected into patients with end-stage renal failure | in vivo | http://www.drugbank.ca/drugs/DB00017 | None | Not reported | |||
| 20418955 | 2010 | Gcg-XTEN 288 | 319 | Free | XTEN | Linear | L | None | Glucagon derivative | Regulate blood glucose | Not mentioned | 12 nmol/kg | 9 | Cynomolgus monkey plasma proteases | Sandwich ELISA | Injected subcutaneouly into cynomolgus monkeys | in vivo | None | None | Elevated blood glucose levels for 10 €“12 hours | |||
| 20418955 | 2010 | Gcg-XTEN 144 | 175 | Free | XTEN | Linear | L | None | Glucagon derivative | Regulate blood glucose | Not mentioned | 12 nmol/kg | 8 to 10 | Cynomolgus monkey plasma proteases | Sandwich ELISA | Injected subcutaneouly into cynomolgus monkeys | in vivo | None | None | Not reported | |||
| 18481852 | 2008 | 3A | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 580 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | 3A' | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 910 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | 3B | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 345 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | 3B' | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 655 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | A.A.B | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 190 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | A.A.B' | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 300 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | A'.A'.B | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 325 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | A'.A'.B' | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 470 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 11962721 | 2001 | CTR-S domain | 124 | Free | Free | Linear | L | None | CTR (Calreticulin) | It binds to C1q, prevents the formation of C1 and so inhibits activation of the classical pathway | Not reported | Not mentioned | 1.21 ± 0.34 in distribution phase | Serine Proteases | Radioactivity measured with a gamma counter | Rat plasma | in vivo | None | None | Biological activity =2 m Ci/nmol | |||
| 11962721 | 2001 | CTR-S domain | 124 | Free | Free | Linear | L | None | CTR (Calreticulin) | It binds to C1q, prevents the formation of C1 and so inhibits activation of the classical pathway | Not reported | Not mentioned | 40.5 ± 2.7 in elimination phase | Serine Proteases | Radioactivity measured with a gamma counter | Rat plasma | in vivo | None | None | Biological activity =2 m Ci/nmol | |||
| 15369394 | 2004 | PEG40-FMS-IFNα2 | 146 | Pegylation [40kdaPEG linked to INFα2 via 2-sulfo-9-fluorenylmethoxycarbonyl (FMS)] | Free | Cyclic(C1-C98, C29-138) | L | None | IFNα2 derivative | Antiviral and antiproliferative | 0-150 hours | 10 µg | 65 (t1/2 of rate of regeneration of native interferon) | Rat blood proteases | BIAcore binding assay | Intravenously administered to wistar rats | in vivo | http://www.drugbank.ca/drugs/DB00105 | None | Following subcutaneous administration to rats and monitoring circulating antiviral activity, active IFNα2 levels peaked at 50 h, with substantial levels still being detected 200 h after administration. | |||
| 15369394 | 2004 | Interferon α2 (IFNα2) | 146 | Free | Free | Cyclic(C1-C98, C29-138) | L | Glycosylation at Thr-105 | IFNα2 | Antiviral and antiproliferative | 0-25 hours | 10 μg/rat in 0.2 mL of PBS | ~1 | Rat blood proteases | BIAcore binding assay | Intravenously administered to wistar rats | in vivo | http://www.uniprot.org/uniprot/P01563 | None | Following administration of IFNα2 (100 μg/rat), the circulating antiviral activity declined with a t1/2 value of ˆ¼1 h, reaching a level lower than 20 pM IFNα2, 12 h after administration. | |||
| 1490668 | 1992 | rhGH(Recombinant DNA derived human growth hormone) | 191 | Free | Free | Linear | L | None | Recombinant DNA derived human growth hormone | Promotes growth and development | Not mentioned | 4 IU rhGH/m2 BSA | 18 | Proteases from Human serum | Radioimmunoassay | (Intravenous route of injection) human serum | in vivo | None | None | In a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight. | |||
| 1490668 | 1992 | rhGH(Recombinant DNA derived human growth hormone) | 191 | Free | Free | Linear | L | None | Recombinant DNA derived human growth hormone | Promotes growth and development | Not mentioned | 4 IU rhGH/m2 BSA | 2.59 ±1.32 | Proteases from Human serum | Radioimmunoassay | (Subcutaneous route of injection) human serum | in vivo | None | None | In a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight. | |||
| 1490668 | 1992 | rhGH(Recombinant DNA derived human growth hormone) | 191 | Free | Free | Linear | L | None | Recombinant DNA derived human growth hormone | Promotes growth and development | Not mentioned | 10 IU rhGH/m2 BSA | 4.29 ±1.89 | Proteases from Human serum | Radioimmunoassay | (Subcutaneous route of injection) human serum | in vivo | None | None | In a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight. | |||
| 1490668 | 1992 | rhGH(Recombinant DNA derived human growth hormone) | 191 | Free | Free | Linear | L | None | Recombinant DNA derived human growth hormone | Promotes growth and development | Not mentioned | 4 IU rhGH/m2 BSA | 6.06 ±2.64 | Proteases from Human serum | Radioimmunoassay | (Intramuscular route of injection)human serum | in vivo | None | None | In a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight. | |||
| 7994807 | 1994 | Prothrombin fragment 1.2 | 273 | Free | Free | Linear | L | None | Prothrombin | Not mentioned | Not reported | Not reported | 90 | Human blood proteases in presence of Hirudin (anti-coagulant) | Radioimmunoassay ,ELISA | Human blood plasma sample | in vivo | 3759958, 2824564 | None | Not mentioned | |||
| 7787827 | 1994 | 125I-β-NGF | 120 | Free | Free | Cyclic (3 disulphide bonds between C15-C80, C58-C108, C68-C110) | L | None | β-nerve growth factor | Nerve growth promoting peptide | Blood samples (250 µl) were obtained from the catheterized carotid artery 15, 30, 45 and 60 min afte | 800 000 cpm of 125I-7S-NGF or 125I-β-NGF (diluted in 200 µl of saline) | 36.3 + 2.20 | Rats blood proteases | Column chromatography | Intravenouly injected in adult male Wistar rats | in vivo | http://www.drugbank.ca/drugs/DB00188 | None | Not reported | |||
| 8353280 | 1993 | Interleukin-3 (IL-3) | 140 | Free | Free | Cyclic (C17-C80,C79-C140) | L | Glycosylation at 84thand 112th position | IL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophils | Hematopoietic growth factor | Not mentioned | 1,000 biologic units | 2.1 (α half life) | Balb/c mice blood proteases | ELISA | Injected intravenously in Balb/c mice blood | in vivo | http://www.uniprot.org/uniprot/P01586 | None | Mice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field | |||
| 8353280 | 1993 | Interleukin-3 (IL-3) | 140 | Free | Free | Cyclic (C17-C80,C79-C140) | L | Glycosylation at 84thand 112th position | IL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophils | Hematopoietic growth factor | Not mentioned | 1,000 biologic units | 10.0 (β half life) | Balb/c mice blood proteases | ELISA | Injected intravenously in Balb/c mice blood | in vivo | http://www.uniprot.org/uniprot/P01586 | None | Mice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field | |||
| 8353280 | 1993 | Interleukin-3 (IL-3) | 140 | Free | Free | Cyclic (C17-C80,C79-C140) | L | Glycosylation at 84thand 112th position | IL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophils | Hematopoietic growth factor | Not mentioned | 1,000 biologic units | 3.6 (α half-life) | Balb/c mice blood proteases | ELISA | Injected intravenously in Balb/c mice blood | in vivo | http://www.uniprot.org/uniprot/P01586 | None | Mice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field | |||
| 8353280 | 1993 | Interleukin-3 (IL-3) | 140 | Free | Free | Cyclic (C17-C80,C79-C140) | L | Glycosylation at 84thand 112th position | IL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophils | Hematopoietic growth factor | Not mentioned | 1,000 biologic units | 30.8 (β half life) | Balb/c mice blood proteases | ELISA | Injected intravenously in Balb/c mice blood | in vivo | http://www.uniprot.org/uniprot/P01586 | None | Mice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field | |||
| 19115392 | 2009 | Interleukin-1 Receptor Antagonist (IL-1ra) | 152 | Free | Free | Cyclic(66-116) | L | Glycosylation at 84th position | Interleukin-1 Receptor Antagonist | The natural specific receptor antagonist (IL-1ra) binds to IL-1RI but does not initiate signaling as it does not engage the IL1R accessory protein and therefore acts as a receptor antagonist. | Not mentioned | Not mentioned | 6 to 15 | Rats blood proteases | Not mentioned | Rat blood | in vivo | http://www.uniprot.org/uniprot/P25086 | None | Significant depression of LTP in the group of animals that received intracerebroventricular injection of Aβ-peptide (1 €“40) compared with control animals injected with vehicle. | |||
| 38340726 | 2024 | A1L35HR2m | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Free | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | Sera were collected from these mice before (0 h) and 2, 4, 8, 12, 24, 48, 72, 120, 168, 240 and 336 h after injection | 5 mg/kg | 2.64 | Balb/c mice serum protease | N.A. | BALB/c mice serum | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Chol conjugation at C terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | Sera were collected from these mice before (0 h) and 2, 4, 8, 12, 24, 48, 72, 120, 168, 240 and 336 h after injection | 5 mg/kg | 81.83 | Balb/c mice serum protease | N.A. | BALB/c mice serum | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Chol conjugation at C terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | N.A. | 5 mg/kg | 89.8 | Balb/c mice serum protease | N.A. | Balb/c mice lung tissue homogenate | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Chol conjugation at C terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | N.A. | 5 mg/kg | 10.6 | Balb/c mice serum protease | N.A. | Balb/c mice trachea tissue homogenate | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Chol conjugation at C terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | N.A. | 5 mg/kg | 49 | Balb/c mice serum protease | N.A. | Balb/c mice nose tissue homogenate | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38293540 | 2024 | GLP-ABD-XTEN144 | 257 | GLP-1 molecule was linked to the N-terminus of ABD via a (GGGGS)3 linker (GLP-ABD), His-tag | ABD was connected to the N-terminus of the XTEN polypeptide (144 amino acids) through a (GGGGS)3 linker | Linear | L | None | Fusion protein of GLP-1, ABD, XTEN (either 144 or 288) | Antidiabetes, Antiobesity | At 1, 3, 7, 12, 18, 24, 30, 36 h, approximately 30 μL of blood was drawn from the tail vein | 5 nmol | 12.9 | C57Bl/6 mice plasma protease And DPP-4 | ELISA | C57BL/6 mice plasma | In Vivo | None | None | GLP-ABD-XTEN144 has a Kd value of only 5.50 nM | |||
| 38293540 | 2024 | GLP-ABD-XTEN288 | 401 | GLP-1 molecule was linked to the N-terminus of ABD via a (GGGGS)3 linker (GLP-ABD), His-tag | ABD was connected to the N-terminus of the XTEN polypeptide (288 amino acids) through a (GGGGS)3 linker | Linear | L | None | Fusion protein of GLP-1, ABD, XTEN (either 144 or 288) | Antidiabetes, Antiobesity | At 1, 3, 7, 12, 18, 24, 30, 36 h, approximately 30 μL of blood was drawn from the tail vein | 5 nmol | 7.32 | C57Bl/6 mice plasma protease And DPP-4 | ELISA | C57BL/6 mice plasma | In Vivo | None | None | GLP-ABD-XTEN288 showed a Kd value of 27.78 nM | |||
| 38006944 | 2024 | Fatty Acid Modified TMP | 108 | Free | Free | Linear | L | C41H70O15N4 fatty acid modification | TMP analogue | Treatment of Thrombocytopenia | N.A. | 100 μg/kg | 128.5 | Beagle dogs plasma protease | ELISA | Beagle dogs plasma | In Vivo | None | None | The modified TMPs, particularly the C41H70O15N4 group, showed enhanced and prolonged activity, reaching peak platelet counts of 5047 × 10⁹/L at 216 hours (enhanced platelet counts) | |||
| 37827496 | 2024 | TTRA81V heterozygous | 508 | N.A. | N.A. | Linear | L | Alanine (Ala) is substituted with valine (Val) at position 81 | Derived from missense mutation in the TTR gene | Causes mild transthyretin amyloid cardiomyopathy | N.A. | 3.6 μM | 21 | Urea between 0.5 and 9 M in phosphate buffer (1 mM of EDTA, 10 mM of sodium phosphate, and 100 mM of potassium chloride, pH = 7.4 | UPLC | Human serum | In Vitro | None | None | N.A. | |||
| 37827496 | 2024 | TTRA81V homozygous | 508 | N.A. | N.A. | Linear | L | Alanine (Ala) is substituted with valine (Val) at position 81 | Derived from missense mutation in the TTR gene | Causes mild transthyretin amyloid cardiomyopathy | N.A. | 3.6 μM | 17.5 | Urea between 0.5 and 9 M in phosphate buffer (1 mM of EDTA, 10 mM of sodium phosphate, and 100 mM of potassium chloride, pH = 7.4 | UPLC | Human serum | In Vitro | None | None | N.A. | |||
| 37827496 | 2024 | TTRWT (wild-type transthyretin) | 508 | N.A. | N.A. | Linear | L | None | Liver‐secreted plasma protein | Causes mild transthyretin amyloid cardiomyopathy | N.A. | 3.6 μM | 44 | Urea between 0.5 and 9 M in phosphate buffer (1 mM of EDTA, 10 mM of sodium phosphate, and 100 mM of potassium chloride, pH = 7.4 | UPLC | Human serum | In Vitro | None | None | N.A. | |||
| 37827496 | 2024 | TTRL55P mutation | 508 | N.A. | N.A. | Linear | L | leucine (Leu) is substituted with proline (Pro) at position 55 | Derived from missense mutation in the TTR gene (L55P) | Causes mild transthyretin amyloid cardiomyopathy | N.A. | 3.6 μM | 4.4 | Urea between 0.5 and 9 M in phosphate buffer (1 mM of EDTA, 10 mM of sodium phosphate, and 100 mM of potassium chloride, pH = 7.4 | UPLC | Human serum | In Vitro | None | None | N.A. | |||
| 38116563 | 2023 | Ex-DARP-FGF21 | 327 | Exendin-4 peptide (Ex) fused to the N-terminus of the DARPin (DARP) protein via (GGGGS)3, His-tag and TEV protease site introduced at position 1 | FGF21 fused to the C-terminus of the DARPin (DARP) protein via (GGGGS)3 linker | Linear | L | L98R and P171A amino acid substitutions in FBGF21 | Exendin-4, DARPin, FGF21 fusion protein | Antidiabetes, Antiobesity | Approximately 40 µL of blood was collected from the orbital venous plexus at different time points (1, 3, 8, 12, 24, 36, 48, and 72 h) | 10 nmol/kg | 27.6 ± 3.2 | C57BL/6 mice plasma protease | ELISA | C57BL/6 mice plasma | In Vivo | None | None | Ex-DARP-FGF21 and Ex-DARP were efficaciously bound to HSA with half-maximal binding concentrations of 4.5 nM and 1.9 nM, respectively | |||
| 38092894 | 2023 | Tag-free rhMFG-E8 | 387 | 23 amino acid leader sequence of cystatin S introduced at N terminal | Free | Linear | L | None | Expressed in Expi293F cells | Antiinflammatory (Including Radiation Injury) | Blood samples (100 μl per time point) were collected starting from 2 to 6 hours | 50 µg | 1.45 (Terminal Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The tag-free rhMFG-E8 demonstrated markedly higher cell adhesion binding activity (to SVEC4-10 cells) compared to E. coli-expressed His-tagged rhMFG-E8, which binds to αVβ3 integrin on the membrane of phagocytes | |||
| 38092894 | 2023 | Tag-free rhMFG-E8 | 387 | 23 amino acid leader sequence of cystatin S introduced at N terminal | Free | Linear | L | None | Expressed in Expi293F cells | Antiinflammatory (Including Radiation Injury) | Blood samples (100 μl per time point) were collected starting from 2 to 12 hours | 50 µg | 2.33 (Terminal Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The tag-free rhMFG-E8 demonstrated markedly higher cell adhesion binding activity (to SVEC4-10 cells) compared to E. coli-expressed His-tagged rhMFG-E8, which binds to αVβ3 integrin on the membrane of phagocytes | |||
| 38027063 | 2023 | ScFv9-CD | 466 | Free | Fusion of CD | Linear | L | Biotinylation | CD sequence originates from the C1qTNF3 protein and scFv9 sequence is derived from an antibody fragment to target amyloid beta (Aβ) | Treatment of AD and Parkinson disease | Plasma was collected at 0, 2, 4, 8, and 24 h after injection | 250 μg | 1.82 | TgCRND8 mice plasma protease | Direct ELISA | TgCRND8 mice plasma | In Vivo | None | None | N.A. | |||
| 38027063 | 2023 | ScFv9 | 304 | Free | Free | Linear | L | Biotinylation | The scFv9 sequence is derived from an antibody fragment to target amyloid beta (Aβ) | Treatment of AD and Parkinson disease | Plasma was collected at 0, 2, 4, 8, and 24 h after injection | 250 μg | 0.74 | TgCRND8 mice plasma protease | Direct ELISA | TgCRND8 mice plasma | In Vivo | None | None | N.A. | |||
| 37874823 | 2023 | MDK-703 | 110 | Fused with IgG2 Fc chain via (Gly-Ser)10 linker, Fc-fragments consisting of the CH2 and CH3 domains of the heavy chain and hinge regions of human IgG2 Fc modified as follows: The first and second cysteines of the hinge region were replaced with serine to prevent detrimental disulfide bridge formation; the last amino acid (lysine) of the Fc region was replaced with an alanine | Free | Linear | L | None | Synthetic | IL-7R agonist peptide | Blood samples were collected at pre-Dose (day 1), 0.5, 1 h, 2 h, 4 h, 8 h, 24 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, and 216 h post-dose | 1 mg/kg | 46 (Terminal Half Life) | Cynomolgus monkeys serum protease | Sandwich ELISA | Cynomolgus monkeys serum | In Vivo | None | None | IC50(nM) = 190 (IC50 values in a competition ELISA for compound binding to Cyno IL-7Rα) | |||
| 37449781 | 2023 | NCL30 | 230 | Polysarcosine = poly(N-methyl glycine) | Free | Linear | L | fluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine) | synthetic | Improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation | Blood samples of 50 μL were collected from the tail vein at the defined time points after systemic administration: 10 min, 1 h, 6 h, 24 h, 72 h | 5 μg/μL | 11.4 | C57BL/6 mice plasma protease | Fluorescence spectrophotometry | C57BL/6 mice plasma | In Vivo | None | None | Not mentioned | |||
| 37449781 | 2023 | 2F-CL30 | 230 | Polysarcosine = poly(N-methyl glycine) | Free | Linear | L | fluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine) | synthetic | Improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation | Blood samples of 50 μL were collected from the tail vein at the defined time points after systemic administration: 10 min, 1 h, 6 h, 24 h, 72 h | 5 μg/μL | 11.3 | C57BL/6 mice plasma protease | Fluorescence spectrophotometry | C57BL/6 mice plasma | In Vivo | None | None | Not mentioned | |||
| 37449781 | 2023 | 3F-CL30 | 230 | Polysarcosine = poly(N-methyl glycine) | Free | Linear | L | fluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine) | synthetic | Improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation | Blood samples of 50 μL were collected from the tail vein at the defined time points after systemic administration: 10 min, 1 h, 6 h, 24 h, 72 h | 5 μg/μL | 19.1 | C57BL/6 mice plasma protease | Fluorescence spectrophotometry | C57BL/6 mice plasma | In Vivo | None | None | Not mentioned | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for Pk Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 20 mg/kg | 27 | Cynomolgus monkeys serum protease | Sandwich ELISA | Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 5 mg/kg | 28 ± 23 | Cynomolgus monkeys serum protease | Sandwich ELISA | Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 20 mg/kg | 26.5 | C2 Cynomolgus monkeys serum protease | Sandwich ELISA | C2 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 5 mg/kg | 13.4 | C4 Cynomolgus monkeys serum protease | Sandwich ELISA | C4 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 5 mg/kg | 54.4 | C5 Cynomolgus monkeys serum protease | Sandwich ELISA | C5 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 5 mg/kg | 16.9 | C6 Cynomolgus monkeys serum protease | Sandwich ELISA | C6 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | FcRN Antagonist | N.A. | 30 mg/kg | 15 | G1-1 Cynomolgus monkeys serum protease | Sandwich ELISA | G1-1 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | FcRN Antagonist | N.A. | 30 mg/kg | 9.3 | G1-2 Cynomolgus monkeys serum protease | Sandwich ELISA | G1-2 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | FcRN Antagonist | N.A. | 30 mg/kg | 4.5 | G1-3 Cynomolgus monkeys serum protease | Sandwich ELISA | G1-3 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | FcRN Antagonist | N.A. | 75 mg/kg | 13 | G2-1 Cynomolgus monkeys serum protease | Sandwich ELISA | G2-1 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | Fcrn Antagonist | N.A. | 75 mg/kg | 6.1 | G2-2 Cynomolgus monkeys serum protease | Sandwich ELISA | G2-2 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | Fcrn Antagonist | N.A. | 75 mg/kg | 12 | G2-3 Cynomolgus monkeys serum protease | Sandwich ELISA | G2-3 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | ZTPA001 | 108 | Free | ABD (albumin Binding Domain) | Linear | L | None | Tslp Binding Z Variants | Antiinflammatory | Blood samples (0.5 mL) were collected at the following time points: Predose, At 10 And 30 Min And 1 , 6, 10, 26, 50, 72, And 96 H Postdose And At Days 6, 7, 8, 11 , 13, 15, 18, And 22 | 1.33 mg/kg | 3-4 (Terminal Half Life) | Cynomolgus monkeys serum protease | Sandwich PK-ELISA | Cynomolgus monkeys serum | In Vivo | None | EP 2023053030 W | IC50(nM) = 0.5 | |||
| N.A. | 2023 | ZTPA104 | 111 | ABD (albumin Binding Domain) | Free | Linear | L | None | Tslp Binding Z Variants | Antiinflammatory | Blood sampling time points were divided into two cohorts as follows: Cohort A (N=3 Per Test Item) Were Bled Predose, At 5 Min And 1 , 8, 72, 168, 264, 408 And 504 H Postdose; And Cohort B (N=3 Per Test Item) Were Bled Predose, At 30 Min And 3, 24, 120, 216, 336 And 456 H Postdose | 1.2 mg/kg | 36 (Terminal Half Life) | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | EP 2023053030 W | IC50(nM) = 0.03 | |||
| N.A. | 2023 | ZTPA001 | 108 | Free | ABD (albumin Binding Domain) | Linear | L | None | Tslp Binding Z Variants | Antiinflammatory | Blood sampling time points were divided into two cohorts as follows: Cohort A (N=3 Per Test Item) Were Bled Predose, At 5 Min And 1 , 8, 72, 168, 264, 408 And 504 H Postdose; And Cohort B (N=3 Per Test Item) Were Bled Predose, At 30 Min And 3, 24, 120, 216, 336 And 456 H Postdose | 1.2 mg/kg | 29 (Terminal Half Life) | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | EP 2023053030 W | IC50(nM) = 0.5 | |||
| 38092894 | 2023 | tag-free rhMFG-E8 | 387 | Cystatin S | Free | Linear | L | Glycosylation | Derived from Expi293F Human cells | antiinflammatory | Blood samples (100 μl per time point) were collected at 0, 3, 6, 9, 12 and 15 min, then every 15 min for the first 60 min till 2 hours | 50 µg | 11.55 (Distribution Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | LD50/30 (lethal dose, 50% at 30 days) falls between 14.5 Gy and 15 Gy after partial body irradiation (PBI) in mice treated with vehicle (normal saline), | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 260 μg/kg | 54.5 | Mouse serum protease | ELISA | Mouse serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 260 μg/kg | 32.3 | Mouse serum protease | ELISA | Mouse serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 260 μg/kg | 66.4 ± 33.0 | Rats serum protease | ELISA | Rats serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 260 μg/kg | 40.9 ± 17.7 | Rats serum protease | ELISA | Rats serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 52 μg/kg | 24.9 ± 2.2 | Dogs serum protease | ELISA | Dogs serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 52 μg/kg | 26.6 ± 1.5 | Dogs serum protease | ELISA | Dogs serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36471433 | 2022 | [125I]sNEP-scFv8D3-scFc | 1456 | sNEP (amino acid 52–749 of NEP) recombinantly linked to a single-chain fragment constant (scFc) of mouse IgG2c antibody at N terminus using linker | ScFc then attached to the BBB transporter (scFv8D3) at C terminus using linker | Linear | L | 125I labeled | Fusion protein of sNEP-scFc-scFv8D3 | Treatment of Alzheimer's diseases | Blood samples collected from the tail vein at 1, 4, 6, 24, 48 and 72 h post-administration | 5 mg/kg | 16 | Tg-Arcswe Mice Plasma Protease | instant thin layer chromatography (iTLC) | Tg-ArcSwe mice plasma | In Vivo | None | None | N.A. | |||
| 36471433 | 2022 | [125I]muNEP-scFv8D3-scFc | 1456 | sNEP (amino acid 52–749 of NEP) recombinantly linked to a single-chain fragment constant (scFc) of mouse IgG2c antibody at N terminus using linker | ScFc then attached to the BBB transporter (scFv8D3) at C terminus using linker | Linear | L | 125I labeled | Fusion protein of sNEP-scFc-scFv8D3 | Treatment of Alzheimer's diseases | Blood samples collected from the tail vein at 1, 4, 6, 24, 48 and 72 h post-administration | 2.5 mg/kg | 18 | Tg-Arcswe Mice Plasma Protease | instant thin layer chromatography (iTLC) | Tg-ArcSwe mice plasma | In Vivo | None | None | N.A. | |||
| 36034808 | 2022 | uPAR | 335 | Free | Free | Linear | L | None | Derived from PLAUR gene | Plays role in thrombosis | N.A. | N.A. | 209.6 ± 0.2 | BEAS-2B cells lysate protease | Densitometry analysis using NIH Image J | BEAS-2B cells lysate with UK treatment +H/R (Hypoxia/Reoxygenation) + Cycloheximide | In Vivo | None | None | N.A. | |||
| 36034808 | 2022 | uPAR | 335 | Free | Free | Linear | L | None | Derived from PLAUR gene | Plays role in thrombosis | N.A. | N.A. | 48.2 ± 2.3 | BEAS-2B cells lysate protease | Densitometry analysis using NIH Image J | BEAS-2B cells lysate with UK treatment +H/R (Hypoxia/Reoxygenation) + Cycloheximide | In Vivo | None | None | N.A. | |||
| 35849214 | 2022 | HSA | 585 | Free | Free | Cyclic (17 Disulfide Bond) | L | None | Human derived | Carrier Protein | 30 minutes | 3 mL/kg of 20% albumin | 8 | Human intravascular sample protease | N.A. | Human intravascular sample | In Vivo | None | None | N.A. | |||
| 35849214 | 2022 | HSA | 585 | Free | Free | Cyclic (17 Disulfide Bond) | L | None | Human derived | Carrier Protein | 120 minutes | 3 mL/kg of 20% albumin | 6.3 | Human intravascular sample protease | N.A. | Human intravascular sample | In Vivo | None | None | N.A. | |||
| 35840338 | 2022 | BIF | 296 | Single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | Interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 3 nmol/kg | 128 ± 10 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Receptor Phosphorylation EC50, nM = 4241 (Functional activity of BIF as determined by phosphorylation of hIR-A expressed in 293 cells) | |||
| 35840338 | 2022 | BIF | 296 | Single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | Interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 10 nmol/kg | 104 ± 4 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Receptor Phosphorylation EC50, nM = 391 (Functional activity of BIF as determined by phosphorylation of hIR-B expressed in 293 cells) | |||
| 35840338 | 2022 | BIF | 296 | single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 30 nmol/kg | 120 ± 21 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Receptor Phosphorylation EC50, nM > 10,000 (Functional activity of BIF as determined by phosphorylation of hIGF-1R expressed in 293 cells) | |||
| 35840338 | 2022 | BIF | 296 | single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 30 nmol/kg | 120 ± 21 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Lipogenesis in 3T3-L1 Adipocytes, EC50 nM = 19 (Functional activity of BIF as assessed by lipogenesis and cellular proliferation) | |||
| 35840338 | 2022 | BIF | 296 | single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 30 nmol/kg | 120 ± 21 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Proliferation in Saos-2 Cells,EC50 nM = 134 (Functional activity of BIF as assessed by cellular proliferation) | |||
| 35840338 | 2022 | BIF | 296 | single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 30 nmol/kg | 120 ± 21 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Proliferation in H4IIE Cells,EC50 nM = 20 (Functional activity of BIF as assessed by cellular proliferation) | |||
| 35677307 | 2022 | rhG-CSF | 175 | Free | Free | Linear | L | None | Recombinant human methionyl-granulocyte colonystimulating factor | N.A. | Sampling time - 0, 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, 24 h | 1.0 mg/kg | 2.74 ± 0.33 | Mice Serum Protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 35677307 | 2022 | PEG10k-rhG-CSF | 175 | Free | Free | Linear | L | PEG10K-MAL fatty chain-modification of rhG-CSF at Cys18 position | rhG-CSF derivative | N.A. | sampling time - 0, 0.5, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168h | 1.0 mg/kg | 13.05 ± 0.45 | Mice Serum Protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 35677307 | 2022 | C15-rhG-CSF | 175 | Free | Free | Linear | L | C15-MAL fatty chain-modification of rhG-CSF at Cys18 position | rhG-CSF derivative | N.A. | sampling time - 0, 0.5, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 h | 1.0 mg/kg | 5.72 ± 0.43 | Mice Serum Protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 35458385 | 2022 | FL-EK1 | 162 | Flexible 35-mer linker (L35) connects the FN3 domain to the EK1 peptide at N terminus | Free | Linear | L | None | EK1 and 10th FN3 unit conjugate | Pan-cov fusion inhibitor | Serum samples were collected before (0 h) and after injection of EK1 (0.5 h, 1 h, 3 h, 7 h, and 12 h) or FL-EK1 (0.5 h, 1 h, 3 h, 7 h, 24 h, 48 h, 72 h, and 96 h) | 40 mg/kg | 30.0 ± 12.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | IC50(nM) = 114.5 ± 33.4 against B.1.1.7 (Alpha), IC50(nM) = 201.2 ± 16.8 against B.1.351 (Beta), IC50(nM) = 373.1 ± 16.9 against P.1 (Gamma), IC50(nM) = 133.0 ± 16.5 against B.1.617.2 (Delta), IC50(nM) = 179.2 ± 38.3 against B.1.525 (Eta), IC50(nM) = 230.9 ± 49.3 against B.1.617.1 (Kappa), IC50(nM) = 88.5 ± 58.2 against C.37 (Lambda), IC50(nM) = 297.5 ± 188.2 against B.1.1.529 (Omicron) | |||
| 35455421 | 2022 | FLT | 163 | FN3 domain | Free | Linear | L | None | FN3 ,T1144 fusion protein | Antiviral (HIV fusion inhibitor) | Blood samples were collected from the orbital sinus at 0, 0.5, 1.5, 3, 6, 9, 12, 24, 48, 72, 96 and 120 h after injection of the inhibitors tested | 5.94 mg/kg | 27.09 ± 6.9 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | None | None | IC50(nM)= 65.3 ± 2.6 against HIV-1 96USSN20 (X4/R5, A), IC50(nM) = 9.8 ± 0.9 against HIV-1 96USNG17 (X4, A), IC50(nM) = 6.5 ± 0.2 against HIV-1 90US_873 (R5, B), IC50(nM) = 8.8 ± 0.3 against HIV-1 BZ167 (X4, B), IC50(nM) = 12.5 ± 0.5 against HIV-1 SE364 (R5, C), IC50(nM) = 9.3 ± 0.5 against HIV-1 PBL288 (R5, C), IC50(nM) = 11.7 ± 0.8 against HIV-1 92UG001 (X4/R5, D), IC50(nM) = 6.4 ± 0.3 against HIV-1 J32228M4 (R5, D), IC50(nM) = 7.5 ± 0.3 against HIV-1 DJ263 (R5, CRF02_AG), IC50(nM) = 10.2 ± 0.6 against HIV-1 CAM1475MV (R5, CRF02_AG) (Infection on MT-4 cells) | |||
| 35414877 | 2022 | Native GIP | 153 | Free | Free | Linear | L | None | Glucagon | Glucose dependent insulinotropic | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | 45 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | N.A. | |||
| 35174698 | 2022 | eGFP | 239 | Free | Free | Linear | L | None | Enhanced GFP | Tagging | N.A. | N.A. | 565 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Ec | 250 | GFP | Ec (E.coli) SsrA tag sequences conjugation | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 6 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Mf | 266 | GFP | Mf (M.fluorum) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 56 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | eGFP | 239 | Free | Free | Linear | L | None | Enhanced GFP | Tagging | N.A. | N.A. | No Degradation | E. Coli Bl21(De3) star strain lysate protease | Fluorescence assay | E. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Ec | 250 | GFP | Ec (E.coli) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 14 | E. Coli Bl21(De3) star strain lysate protease | Fluorescence assay | E. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Mf | 266 | GFP | Mf (M.fluorum) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 424 | E. Coli Bl21(De3) star strain lysate protease | Fluorescence assay | E. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35046019 | 2022 | ELP(0FA)GFP | 400 | Free | GFP | Linear | L | None | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 1.6 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA - Mouse serum albumin (μM) = n.d. (Binding affinity of ELP-GFP constructs for serum albumin), KD HSA - Human serum albumin (μM) = n.d | |||
| 35046019 | 2022 | ELP(1FA)GFP | 400 | Free | GFP | Linear | L | 1 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 1.9 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) = 126 ± 32.2, KD HSA - Human serum albumin (μM) = n.d | |||
| 35046019 | 2022 | ELP(5FA)GFP | 400 | Free | GFP | Linear | L | 5 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 19.6 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) = 10.3 ± 4.0, KD HSA - Human serum albumin (μM) = n.d | |||
| 35046019 | 2022 | ELP(10FA)GFP | 400 | Free | GFP | Linear | L | 10 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 33.3 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) =2.76 ± 0.19, KD HSA - Human serum albumin (μM) = n.d | |||
| 35046019 | 2022 | ELP(1FA)GFP | 400 | Free | GFP | Linear | L | 1 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 18.5 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) =25.9 ± 7.1, KD HSA - Human serum albumin (μM) = 19.3 ± 3.9 | |||
| 35046019 | 2022 | ELP(5FA)GFP | 400 | Free | GFP | Linear | L | 5 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 31.7 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) =4.0 ± 1.6, KD HSA - Human serum albumin (μM) = 3.16 ± 0.60 | |||
| 35046019 | 2022 | ELP(10FA)GFP | 400 | Free | GFP | Linear | L | 10 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 27.9 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) = 2.22 ± 0.03, KD HSA - Human serum albumin (μM) = 1.64 ± 0.17 | |||
| N.A. | 2022 | TROP2 TCE (PC1) | 692 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 3 ug/kg | 1.02 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | EC50(nM) = 0.1477 (TROP binding) | |||
| N.A. | 2022 | TROP2 TRACTr PC complex (PC5) | 911 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 100 ug/kg | 90.16 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | EC50(nM) = 60.25 (TROP binding) | |||
| N.A. | 2022 | TROP2 TRACTr PC complex (PC18) | 916 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 100 μg/kg | 97.31 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | IC50(pM) = 3,253 | |||
| N.A. | 2022 | TROP2 TRACTr PC complex (PC21) | 1177 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 100 μg/kg | 100.73 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | N.A. | |||
| N.A. | 2022 | PC-22 complex | 911 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 100 μg/kg | 68.97 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | N.A. | |||
| N.A. | 2022 | hIL-18BP | 194 | Free | Free | Linear | L | None | Synthetic | Antagonist of IL-18 | Single subcutaneous administration: 0, 0.33, 1, 1.5, 3, 5, 7, 12, 24, 48, 72, 120, And 168 Hours (13 Points In Total), Single Intravenous Administration: 0, 0.083, 0.25, 0.5, 1.25, 3, 5, 10, 24, 48, And 72 Hours (11 Points In Total) | 3 mg/kg + 1 mg/kg | 6.51 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | IB 2021058964 W | IC50 of IL-18BP-His was 0.0240 nM | |||
| N.A. | 2022 | hIL-18BP | 194 | Free | Free | Linear | L | None | Synthetic | Antagonist of IL-18 | Single intravenous administration: 0, 0.083, 0.25, 0.5, 1.25, 3, 5, 10, 24, 48, And 72 Hours (11 Points In Total) | 1 mg/kg | 6.51 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | IB 2021058964 W | IC50 of IL-18BP-His was 0.0240 nM | |||
| 35910276 | 2022 | KB-SP | 806 | Free | Free | Linear | L | None | Derived from Bacillus sp. KB111 strain | Haloprotease | 50°C | N.A. | 90 (Enzyme Activity) | N.A. | Zymography | EDTA + Tris-HCl + 0.5 M NaCl+ azocasein | In Vitro | GenBank id: KUL11341.1 | None | KB-SP exhibited more than 50% of the highest activity at pH=6.5–10 | |||
| 35910276 | 2022 | KB-SP | 806 | Free | Free | Linear | L | None | Derived from Bacillus sp. KB111 strain | Haloprotease | 60 °C | N.A. | 10 (Enzyme Activity) | N.A. | Zymography | EDTA + Tris-HCl + 0.5 M NaCl+ azocasein | In Vitro | GenBank id: KUL11341.1 | None | KB-SP exhibited more than 50% of the highest activity at pH=6.5–10 | |||
| 35910276 | 2022 | KB-SP | 806 | Free | Free | Linear | L | None | Derived from Bacillus sp. KB111 strain | Haloprotease | 50°C | N.A. | 5 (Enzyme Activity) | N.A. | Zymography | EDTA + Tris-HCl + 0.5 M NaCl+ azocasein | In Vitro | GenBank id: KUL11341.1 | None | KB-SP exhibited more than 50% of the highest activity at pH=6.5–10 | |||
| 35711755 | 2022 | R13 Fae | 393 | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Xylanase | pH 6.0 25 Celsius | N.A. | 23 (Half Life Activty) | N.A. | N.A. | Phosphate buffer | In Vitro | None | None | N.A. | |||
| 35711755 | 2022 | R13 Fae | 393 | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Xylanase | pH 6.0 ,35°C | N.A. | 16 (Half Life Activity) | N.A. | N.A. | Phosphate buffer | In Vitro | None | None | N.A. | |||
| 35133860 | 2022 | mTSS | 436 | Free | Free | Linear | L | None | Derived from preTSS | Collagenolytic protease | 75°C | N.A. | 1.5 (Activity Half Life) | N.A. | N.A. | 10 mM CaCl2 at pH 9.0 | In Viro Study | None | None | In the presence of 10 mM CaCl2 at pH 9.0, mTSS retained more than 80% or 70% of the original activity after 8 h of incubation at 60°C or 70°C | |||
| 35133860 | 2022 | mTSS | 436 | Free | Free | Linear | L | None | Derived from preTSS | Collagenolytic protease | 60°C | N.A. | 2 (Activity Half Life) | N.A. | N.A. | 10 mM CaCl2 at pH 11.0 | In Viro Study | None | None | In the presence of 10 mM CaCl2 at pH 9.0, mTSS retained more than 80% or 70% of the original activity after 8 h of incubation at 60°C or 70°C | |||
| 35133860 | 2022 | mTSS | 436 | Free | Free | Linear | L | None | Derived from preTSS | Collagenolytic protease | N.A. | N.A. | >12 (Activity Half Life) | N.A. | N.A. | 10 mM CaCl2 at pH 7.5 | In Viro Study | None | None | In the presence of 10 mM CaCl2 at pH 9.0, mTSS retained more than 80% or 70% of the original activity after 8 h of incubation at 60°C or 70°C | |||
| 35133860 | 2022 | mTSS | 436 | Free | Free | Linear | L | None | Derived from preTSS | Collagenolytic protease | 70°C | N.A. | 6 (Activity Half Life) | N.A. | N.A. | pH 9 | In Viro Study | None | None | In the presence of 10 mM CaCl2 at pH 9.0, mTSS retained more than 80% or 70% of the original activity after 8 h of incubation at 60°C or 70°C | |||
| 34630378 | 2021 | ABD-VP1 | 330 | ABD | Free | Linear | L | None | Synthetic | Treatment of Coxsackievirus B3 (Cvb3)-Induced Viral Myocarditis | 1h at RT | 0.25 μg/μL | 280 | Murine serum protease | ELISA | Murine serum | In Vivo | None | None | ABD-VP1 increased the 28-day survival rate from about 40% (VP1) to 73% | |||
| 34630378 | 2021 | VP1 vaccine | 284 | Free | Free | Linear | L | None | Synthetic | Treatment of Coxsackievirus B3 (Cvb3)-Induced Viral Myocarditis | 1h at RT | 0.25 μg/μL | <15 | Murine serum protease | ELISA | Murine serum | In Vivo | None | None | ABD-VP1 increased the 28-day survival rate from about 40% (VP1) to 73% | |||
| 34459035 | 2021 | CODD | 120 | Free | Free | Linear | L | FLAG tag | C-Terminal oxygen-dependent degradation domain | Regulates gene expression | N.A. | N.A. | 5.8‐Fold Increase | Cells lysate protease | CHX assay, Western blotting | HEK293 Flp‐In T‐REx cells lysate after neddylation inhibition | In Vitro | None | None | N.A. | |||
| 33918853 | 2021 | HFn/DOX | 172 | Free | Free | Linear | L | None | Synthetic | Antitumor | Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C | 3.0 mg/kg | 3.07 ± 0.06 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.49 ± 0.11 | |||
| 33918853 | 2021 | HFn-PAS/DOX | 235 | Free | 15aa linker, enzyme cleavable site, PAS(40), 5 aa flexible linker conjugated at C terminus | Linear | L | None | Synthetic | Antitumor | Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C | 3.0 mg/kg | 14.96 ± 0.29 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.38 ± 0.09 | |||
| 33918853 | 2021 | HFn-GFLG-PAS-RGDK/DOX | 239 | Free | Add RGDK tretapeptide to HFn-PAS C-terminus | Linear | L | None | Synthetic | Antitumor | Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C | 3.0 mg/kg | 17.61 ± 0.39 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.17 ± 0.01 | |||
| 33918853 | 2021 | HFn-PLGLAG-PAS-RGDK/DOX | 241 | Free | Add RGDK tretapeptide to HFn-PAS C-terminus and substituite enzyme cleavable linker with PLGLAG | Linear | L | None | Synthetic | Antitumor | Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C | 3.0 mg/kg | 18.93 ± 0.61 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.18 ± 0.04 | |||
| 33656323 | 2021 | IL-2 | 132 | Free | Free | Cyclic (C57-C104 Disulfide Bond) | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.041 ± 0.006 (T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.613 ± 0.063(T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 control | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 0, 5, and 30 min and 2, 6, and 12 h for group I and 2, 10, and 60 min and 4, 8, and 24 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.035 ± 0.014(T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | IL-2 | 132 | Free | Free | Cyclic (C57-C104 Disulfide Bond) | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.273 ± 0.040(T1/2b) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 3.595 ± 0.518(T1/2b) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 control | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 0, 5, and 30 min and 2, 6, and 12 h for group I and 2, 10, and 60 min and 4, 8, and 24 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.196 ± 0.114(T1/2b) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33650155 | 2021 | 3XFLAG-hDASPO_341 | 365 | 3XFLAG labelling | Free | Linear | L | None | Found in the hippocampus of female patients affected by Alzheimer's disease | Degradation Of D-Aspartate ( D-Asp) | 10 hours | 2 μg | ≈ 100 | U87 cells lysate protease | Western blotting | U87 cells lysate with cycloheximide (CHX) | In Vivo | None | None | N.A. | |||
| 33650155 | 2021 | 3XFLAG-hDASPO_369 | 393 | 3XFLAG labelling | Free | Linear | L | None | Found in the hippocampus of female patients affected by Alzheimer's disease | Degradation Of D-Aspartate ( D-Asp) | 10 hours | 2 μg | ≈ 100 | U87 cells lysate protease | Western blotting | U87 cells lysate with cycloheximide (CHX) | In Vivo | None | None | N.A. | |||
| 33391505 | 2021 | [125I]SST-scFv8D3 | 115 | 125I labeled | scFv of 8D3 is added to SST | Cyclic (Disulfide Bond Bw C-C Of SST) | L | Serine, threonine and glycine were added to the linker | Synthetic | Treatment of Alzheimer's diseases | Eight microliter blood samples from the tail vein were obtained at 0.5, 1, 2, 4, 6 and 24-h post injection | 0.44±0.08 MBq | 6 | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | The measured activation of neprilysin by SST-scFv8D3 preserved around 70% of the activation obtained by SST alone | |||
| 33387593 | 2021 | Wild-type (IFN) | 165 | Free | Free | Linear | L | None | Human derived | Antiviral, Antiproliferative | Blood samples were taken at different times post-injection | 100000 U | 0.9 ± 0.1 (T1/2 Elimination) | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | PDB id: 1ITF | None | Antiviral SBA (IU/ng) = 201 ± 9 in wild-type IFN, Antiproliferative SBA (IU/ng) = 240 ± 50 | |||
| 33387593 | 2021 | GMOP-IFN | 179 | GM-CSF O-glycosylated Peptide | Free | Linear | L | None | Synthetic | Antiviral, Antiproliferative | Blood samples were taken at different times post-injection | 100000 U | 3.0 ± 0.4(T1/2 Elimination) | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | PDB id: 1ITF | None | Antiviral SBA (IU/ng) = 190 ± 30 in GMOP-IFN, Antiproliferative SBA (IU/ng) = 280 ± 40 | |||
| 33387593 | 2021 | mGMOP-IFN | 180 | Modified GOMP | Free | Linear | L | None | Synthetic | Antiviral, Antiproliferative | Blood samples were taken at different times post-injection | 100000 U | 2.5 ± 0.2 (T1/2 Elimination) | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | PDB id: 1ITF | None | Antiviral SBA (IU/ng) = 280 ± 50 in mGMOP-IFN, Antiproliferative SBA (IU/ng = 95 ± 5 | |||
| 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 | |||
| 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 | |||
| 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 | ALM6-1F7 | 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 | |||
| 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. | |||
| 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) | |||
| 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. | |||
| 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)) | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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. | |||
| 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 | |||
| 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 | |||
| 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. | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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) | |||
| 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. | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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. | |||
| 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 | |||
| 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. | |||
| 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 | |||
| 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) | |||
| 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. | |||
| 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. | |||
| 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. | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 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. | |||
| 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) | |||
| 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. | |||
| 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 | |||
| 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 | |||
| 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. | |||
| 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. | ||||
| 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 | |||
| 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 | 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 | |||
| 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 |