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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	Protease	Assay	Test Sample	Vivo/Vitro	Reference	Patent No.	Activity
1083	11099487	2000	RQIKIWFQNRRMKWKKNELKRAFAALRDQI	Int-H1-S6A,F8A	30	Free	Free	Linear	L	None	C-Myc derivative	Antiproliferative and proapoptotic	Not reported	Not mentioned	18.73	Fetal calf serum proteases	HPLC	Fetal bovine serum batch2	in vitro	None	None	Not reported
1216	21114599	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVK-Aib-R	[Aib35]hGLP-1(7-36)NH2	30	Free	Amidation	Linear	L	Aib--Aminoisobutyric acid	Analogue of glucagon like peptide-1	Regulate blood glucose	Not mentioned	Not mentioned	18.4	Human plasma proteases	HPLC	Human plasma	in vitro	14759771	None	EC50=0.05 ±0.01nM for cAMP stimulation
1754	16467916	2005	(Pen)-Y(Me)-ARGDN-Tic-C	RGD	9	Acetylation	Amidation	Linear	L	Pen=Penicillamine, Methylation at Tyrosine, Tic=tetrahydroisoquinoline carboxylic acid	Human Glioma cells	Integrin Protein	Not reported	Not mentioned	~20	Proteases present in rat brain homogenates suspended in aCSF	RP-HPLC	Rat brain homogenates suspended in aCSF	in vitro	None	None	No activity found
1769	16892368	2006	WDREINNYTSLIH	C46	13	Glycosylation	Amidation	Linear	L	None	Derived from T20	HIV-1 fusion inhibitory peptide	Not reported	40 ng peptide/200 mL buffer	0.75	Not mentioned	ELISA	PBS/1% BSA	in vitro	None	None	IC50=90nM
1806	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAALREL	T-2635	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	16.3	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.007 µg/ml against IIIB virus
1807	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAALREL	T-2635	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	16.3	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.018 µg/ml against 098 virus
1808	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAALREL	T-2635	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	16.3	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.025 µg/ml against 098-T20 virus
1809	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAALREL	T-2635	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	16.3	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.015 µg/ml against 098-T1249 virus
1810	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAALREL	T-2635	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	16.3	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.021 µg/ml against 098-T651 virus virus
1821	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAALREL	T-267221	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	15.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.011 µg/ml against IIIB virus
1822	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAALREL	T-267221	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	15.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.035 µg/ml against 098 virus
1823	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAALREL	T-267221	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	15.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.028 µg/ml against 098-T20 virus virus
1824	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAALREL	T-267221	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	15.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.035 µg/ml against 098-T1249 virus
1825	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAALREL	T-267221	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	15.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.050 µg/ml against 098-T651 virus
1836	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAALREL	T-267227	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	17.9	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.012 µg/ml against IIIB virus
1837	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAALREL	T-267227	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	17.9	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.045 µg/ml against 098 virus
1838	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAALREL	T-267227	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	17.9	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.028 µg/ml against 098-T20 virus
1839	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAALREL	T-267227	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	17.9	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.025 µg/ml against 098-T1249 virus
1840	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAALREL	T-267227	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	17.9	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.044 µg/ml against 098-T651 virus
1948	18307313	2007	R-X-R	CAP 22	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 11 µM for S.aureus
1949	18307313	2007	R-X-R	CAP 22	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 10 µM for Methicillin- resistant S.aureus
1950	18307313	2007	R-X-R	CAP 22	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.epidermis
1954	18307313	2007	R-X-R	CAP 24	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for S.aureus
1955	18307313	2007	R-X-R	CAP 24	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for Methicillin- resistant S.aureus
1956	18307313	2007	R-X-R	CAP 24	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for Methicillin- resistant S.epidermis
2009	15587934	2004	SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH	AlbuBNP	32	Human serum albumin	Free	Linear	L	None	B-type cardiac natriuretic peptides fused to HAS at N-terminal	Vasodilator	Not reported	2.19 mg/kg	19.3	Mouse blood proteases	EIA	Mice plasma (Subcutaneous injection)	in vivo	None	None	EC50 =28.4 ± 1.2 nM
2064	23318685	2013	GGLYACHMGPIT-Nal-VCQPLRSar-Peg-SarRLPQCV-Nal-TIPGMHCAYLGG	Peginesatide	40	Acetylation	Dimerization using PEGylation	Cyclic (C6-C15, C26-C35)	L	Nal, Pegylation	Synthetic peptide	Erythropoiesis-stimulating agent	Not reported	0.1 mg/kg	19.0 ± 2.0	Monkey blood proteases	ELISA	Monkey blood plasma	in vitro	None	None	Increase in RBCs of 1.67 106/ µl 21 days after the administration
2072	3348603	1987	N-MeVal-EtPro-N-MeThr-Leu-MePro-AMHA-Pro-N-MeLeu- Gly	DihydromycoplanecinA (DHMP A)	10	alpha-hydroxybutyric acid	Free	Cyclic	L	N-MeVal; N-methylvaline, EtPro; Ethylproline, N-MeThr; N-methylthreonine MePro; Methylproline, AMHA; 2-amino-5-methylhexanoic acid, N-MeLeu; N-methylleucine	Active metabolite in urine of mice and dogs	Antibiotic	Not reported	10 mg/kg	19.3	Mouse blood proteases	Not mentioned	Mice serum (Intravenous)	in vivo	None	None	LD50>6000mg/kg administered orally to mice
2092	N.A.	2004	ELAGIGILTV	[Î²El, amide]-Melan-A	10	Beta-Glu1	Amidation	Linear	L	None	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	20	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= 0.3 nM
2173	N.A.	2012	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4-Î±1AT(P357N)	39	Free	Fusion of Alpha-1 Antitrypsin Monovariant [Î±1AT(P357N)]	Linear	L	None	Venom of Heloderma horridum	Insulinotropic peptide	N.A.	520 micro g/Kg	19.1	Not mentioned	EIA	Rat plasma (Subcutaneous)	in vivo	None	EP2423233A2	Blood glucose after 24 hour ~10 mM
2176	N.A.	2006	HGDGSFSDEMNTILDNLAARDFINWLIQTLITDK	Derivative of Glucagon Like Peptide-2 (GLP-2)	34	Free	Addition of maleimidopropionic acid (MPA) and amidation	Linear	L	None	GLP-2	Intestine function modulator	N.A.	500 nM/ Kg	16.2	Rat blood proteases	Radioimmunoassay	Rat plasma (Intravenous)	in vivo	None	US7112567B2	Increase in wet-weight of small intestine ~0.3 g
2179	15817669	2007	YaDAIFTQSYRKVLAQLSARKLLQDILSRL	Derivative of Growth hormone releasing factor	30	Free	Addition of maleimidopropionic acid (MPA) and amidation	Linear	Mix	None	GRF peptide	Growth harmone and somatostatin releasing factor	N.A.	100 nM/ Kg	18.7	Rat blood proteases	Radioimmunoassay	Rat plasma (Intravenous)	in vivo	None	US7268113B2	Not mentioned
2184	N.A.	2010	K-Sar-htrGtf	Peptide-B	8	Free	Amidation	Linear	Mix	Sar= sarcosine	Glucagon superfamily Peptide A	Insulinotropic peptide	N.A.	2 mg/ ml	18.6	Not mentioned	LC/MS	plasma	in vitro	None	US20110288003	Not mentioned
2266	1418002	1992	GPETLCGAELVDALQFVCGDRGFYFNKPTGYGYGSSRRAPQTGIVDECCFRSCDLRRLMYCAPLKPAKSA	Somatomedin c	70	Free	Free	Linear	L	None	Human liver	Growth hormone	Not given	129.4 ng	20	Human serum proteases	Peptide specific immunoassay	Human serum sample	in vitro	PMID 632300	None	Somatomedin C is a prerequisite for normal muscle homeostasis which is disrupted in fibromyalgia. Regression analysis shows that ~7 % low level of somatomedin c in case of fibromyalgia patients.
2273	4034413	1985	YaGFL	Leucine enkephalin analogue	5	Free	Free	Linear	Mix	Thiomethylene bond replacement between residue 3-4	Derivative of Natural enkephalin	Analgesic	20 minutes	0.9 nM	>1000	Human serum protease	HPLC	Human serum	in vitro	None	None	Not reported
2565	16828890	2006	pGlu-NSPR	NC-1900 (Analogue of arginine vasopressin)	5	Free	Addition of lycinamide	Linear	L	pGlu=pyroglutamic acid	Synthetic analogue of arginine vasopressin	Neuropeptide	0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36 and 48 h	0.55mM	19	Mice blood proteases	HPLC-UV	Subcutaneously and Intravenously injected in mice	in vitro	None	None	Single subcutaneous injection of NC-1900 tended to improve the scopolamine-induced memory deficits, but the effects were far from enough to make the animals €™ memory recover, which suggested that either a higher dose or multi- injections of NC-1900 were needed to promote its effects
2603	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	0.1 mg/kg	16.4 ±1.7	Monkey plasma proteases	Competitive ELISA	Monkey plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2690	25039358	2014	HAEGTFTSDVSSYLEGQAAK(Î³-Glu-palmitoyl)EFIAWLVRGRG	Liraglutide	31	Free	Free	Linear	L	Î³-Glu-palmitoyl at 21 st position	Analog of human GLP-1	GLP-1 receptor agonist, Hypoglycaemic	37 °C for 2-72 hours	1000ng/ml	17.1	Rat plasma proteases	LC-MS/MS	Rat Plasma	in vitro	None	None	GLP-1 receptor Activation potency with EC50 =9.5 ± 0.8 pM in HEK-293 cells
2698	25039358	2014	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRX2	Coumarin-modified GLP-1 derivative 13	31	Free	Amidation	Linear	L	X-2 = Cys- conjugated-7-hydroxyCoumarin maleimide	Analog of human GLP-1	Hypoglycaemic	37 °C for 2-72 hours	1000ng/ml	18.4	Rat plasma proteases	LC-MS/MS	Rat Plasma	in vitro	None	None	GLP-1 receptor Activation potency with EC50 = 16.8 ± 0.7 pM in HEK-293 cells
2719	25771000	2015	MWQRPSSWIEGRFPHSDAVFTDQYTRLRKQLAAKKYLQSLKQKRY	MHDBAY (Recombinant PACAP-derived peptide)	45	Free	Free	Linear	L	None	Synthetic (Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide)	Insulin secretion stimulant	37 C, 48 Hours	10 µM	16.31	Fxa(Facor Xa)	HPLC-ESI/MS/MS	Peptide sample + HAS	in vitro	None	None	AUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control
2720	25771000	2015	MWQRPSSWIEGRFPHSDAVFTDQYTRLRKQLAAKKYLQSLKQKRY	MHDBAY (Recombinant PACAP-derived peptide)	45	Free	Free	Linear	L	None	Synthetic (Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide)	Insulin secretion stimulant	0.5-24 hours	0.5 mg/kg	16.72	Fxa(Facor Xa) and DPP-IV	LC-MS/MS	Peptide sample + HSA +Fxa + DPP IV(Dose i/v injected)	in vitro	None	None	AUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control
2988	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	18	Proteases from Fetal calf serum	HPLC	Fetal calf serum + 1Î¼M catropril	in vitro	None	None	Not reported
3054	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	2000Î¼g/kg	18.2	Rats blood proteases	Radioimmunoassay	Intravenous injection of the peptide in Hans Wistar Male rat	in vivo	None	None	Platelet count increased from 1,504Ã—103/mm3 to 2,304Ã—103/mm3,Neutophil count increased from 941/mm3 to 27,439/mm3,Monocyte count increased from 160/mm3 to 8,246/mm3,Eosinophil count increased from 86/mm3 to 986/mm3,Basophil count increased from 11/mm3 to 863/mm3,Lymphocyte count increased from 4,210/mm3 to 27,439/mm3,RBC count decreased form 7.05Ã—106/mm3 to 5.52Ã—106/mm3,Prothrombin time increased from 13.7 to 17.5 seconds.
3055	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	2000Î¼g/kg	19.4	Rats blood proteases	Radioimmunoassay	Intravenous injection of the peptide in Hans Wistar Female rat	in vivo	None	None	Platelet count increased from 1,504Ã—103/mm3 to 2,304Ã—103/mm3,Neutophil count increased from 941/mm3 to 27,439/mm3,Monocyte count increased from 160/mm3 to 8,246/mm3,Eosinophil count increased from 86/mm3 to 986/mm3,Basophil count increased from 11/mm3 to 863/mm3,Lymphocyte count increased from 4,210/mm3 to 27,439/mm3,RBC count decreased form 7.05Ã—106/mm3 to 5.52Ã—106/mm3,Prothrombin time increased from 13.7 to 17.5 seconds.
3115	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[K18,E22]-c[K30,E34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K42)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	18 ±2.2	Neutral endopeptidase 24.11	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human NEP 24.11 enzyme (1.0 Î¼g/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00134	None	EC50=1.0nM,pEC50=9.0 ±0.09
4011	38785334	2024	IsoV-DTHFPCIKFEPRSKGCK	Rusfertide (PTG-300)	18	IsoV = Isovaeryl at position 1	Amidation	Cyclic(C7-C17 Disulfide Linkage)	L	Lys8 conjugation with palmitoyl-Glu(2)-OH	Synthetic	Provides therapy for PV and Hemochromatosis	N.A.	1 mg	17.9 ± 2.1	Human plasma protease	HPLC-MS	Human plasma	In Vivo	None	None	N.A.
4023	38721043	2024	SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFC	EXT607 (R=OH)	35	Free	Cys modified PTH-1 linked with VitD3 through (PEG)36	Linear	L	R= OH for Cys35	PTH-1 derivative	Treatment of Hypoparathyroidism	Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose	30 µg/kg	15.4	Rats plasma protease	ELISA	Rats plasma	In Vivo	None	None	EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1)
4030	38642503	2024	VPALR	VPALR-SUL	5	Free	Sul = Sulpiride	Linear	L	None	Derived from the Ku70 domain	Antidepressant	Blood samples were collected from the orbital venous plexus at various time points (5 min, 15 min, 30 min, 1 h, 2 h, 3 h, 5 h, 7 h, 9 h, 12 h, 24 h	Equivalent of 3 mg/kg of sulpiride	17.49 ± 13.50	Male SD rats plasma protease	LC-MS/MS	Male SD rats plasma	In Vivo	None	None	VPALR-SUL showed almost 100% cell viability at all tested concentrations, which indicates excellent biocompatibility with HT22 nerve cells and minimal cytotoxicity
4042	38486997	2024	HsQGTFTSDKSKYLE-Aib-KAAQDFVEWLKAGGPSSGAPPPS	1907-B	40	Free	Replacing the amide bond with a C-terminal acid	Cyclic (Lactam Bridge K17 & D21)	Mix	At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine	GLP-1 analogs	Antidiabetes	Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration	0.05 mg/kg	∼16.8	SD rats plasma protease	LC-MS/MS	SD rats plasma	In Vivo	None	None	GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B)
4166	38097378	2023	CR	Au_CR	2	Au gold particle conjuagtion at N terminal through formation of Au-S bond	Amidation	Linear	L	None	Synthetic	Antimicrobial	Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h	10 mg/kg	∼17.5	Mice plasma protease	ICP-MS	Mice plasma	In Vivo	None	None	MIC(μg/mL) = 1.56 against S. aureus
4167	38097378	2023	CR	Au_CR	2	Au gold particle conjuagtion at N terminal through formation of Au-S bond	Amidation	Linear	L	None	Synthetic	Antimicrobial	Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h	10 mg/kg	∼17.5	Mice plasma protease	ICP-MS	Mice plasma	In Vivo	None	None	MIC(μg/mL) >100 against E.coli
4168	38097378	2023	CR	Au_CR	2	Au gold particle conjuagtion at N terminal through formation of Au-S bond	Amidation	Linear	L	None	Synthetic	Antimicrobial	Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h	10 mg/kg	∼17.5	Mice plasma protease	ICP-MS	Mice plasma	In Vivo	None	None	MIC(μg/mL) >100 against B.subtilis
4169	38097378	2023	CR	Au_CR	2	Au gold particle conjuagtion at N terminal through formation of Au-S bond	Amidation	Linear	L	None	Synthetic	Antimicrobial	Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h	10 mg/kg	∼17.5	Mice plasma protease	ICP-MS	Mice plasma	In Vivo	None	None	MIC(μg/mL) = 1.56 against C.albicans
4188	37449781	2023	pSar200-b-pCys(SO2Et)30	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
4192	37384895	2023	HRHTKQRHTALH	CLA-coated PTX-SPIONs@HRH	12	Free	Free	Linear	L	None	Synthetic	Antiangiogenic (used for targeted delivery of Paclitaxel in non-small cell lung carcinoma)	Mice were euthanized over 24 h at t = 0.5, 1, 4, 8, and 24 h	15.6 μg/mL	17.1	Mice Plasma Protease	HPLC	Mice plasma	In Vivo	None	None	The activity value for CLA-coated PTX-SPIONs@HRH at the maximal therapeutic concentration (100 μg/mL) resulted in 12.8% cell viability on A549 lung adenocarcinoma cells
4193	37384895	2023	HRHTKQRHTALH	CLA-coated PTX-SPIONs@HRH	12	Free	Free	Linear	L	None	Synthetic	Antiangiogenic (used for targeted delivery of Paclitaxel in non-small cell lung carcinoma)	Mice were euthanized over 24 h at t = 0.5, 1, 4, 8, and 24 h	15.6 μg/mL	17.1	Mice Plasma Protease	HPLC	Mice plasma	In Vivo	None	None	The activity value for CLA-coated PTX-SPIONs@HRH at the maximal therapeutic concentration (100 μg/mL) resulted in 12.8% cell viability on A549 lung adenocarcinoma cells
4294	N.A.	2023	Y-Aib-EGTFISDLSI-Aib-KEEIHQ-Aib-EFIEWLLAQGPSSGAPPPS	SEQ ID NO 19	39	Free	Amidation	Linear	L	Aib = α-aminoisobutyric acid	Exendin-4 analogs	Antidiabetes	Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application	0.25 mg/kg	19.6	Rats plasma protease	LC-MS	Rats plasma	In Vivo	None	EP 2022074607 W	IC50 hGIPR (nM) = 2
4299	N.A.	2023	Y-Aib-EGTFISDLSI-Aib-KDR-Aib-HQ-Aib-EFIEWLLAQRPSSGAPPPS	SEQ ID NO 22	39	Free	Amidation	Linear	L	Aib = α-aminoisobutyric acid	Exendin-4 analogs	Antidiabetes	Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application	0.5 mg/kg	15.5	Rats plasma protease	LC-MS	Rats plasma	In Vivo	None	EP 2022074607 W	IC50 hGIPR (nM) = 1
4306	N.A.	2023	PSXFLSPEHQRVQQRKESKKPPAKLQPRK	SEQ ID NO 2	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>19	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 1.9
4309	N.A.	2023	PXXFLSPTHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 25	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3, NMeS = N-Methyl-L-Serine at position 2	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	17	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 70.5
4433	36471433	2022	EVQLVESGGGLYQPGNSLTLSCVASGFTFSNYGMHWIRQAPKKGLEWIAMITYDSSKMNYADTVKGRFTISRDNSKNTLYEMNSLRSEDTAMYYCAYPTSHYVVDVWGQGYSVTVSSGSTSGGGSGGGSGGGGSSDIQMTQSPASLSASLEEIVTITCQASQDIGNWLAWTQQKPGKSPQLLIYGATSLADGVPSRFSQSRSGTQFSLKISRYQVEDIGIYYCLQAYNTPWTFGGGTKLELKRASAPGSGGGSAPGEPRYPITQNPSPPLKECPPCAAPDLLGGPSYFIFPPKIKDVLMISLSPMYTCVVVDVSEDDPDYQISWFVNNYEVHTAQTQTHREDYNSTLRVVSALPIQHQDWMSGKEFKCKYNNRALPSPIEKTISKPRGPVRAPQVYVLPPPAEEMTKKEFSLTCMITGFLPAEIAVDWTSNGRTEQNYKNTATYLDSDGSYFMYSKLRVQKSTWERGSLFACSVVHEGLHNHLTTKTISRSLGPGGGGSGGGGSGGGGSEPRYPITQNPSPPLKECPPCAAPDLLGGPSVFIFPPKIKDVLMISLSPMVTCVVVDVSEDDPDYQISWFVNNVEVHTAQTQTHREDYNSTLRYVSALPIQHQDWMSGKEFKCKVNNRALPSPIEKTISKPRGPYRAPQVYVLPPPAEEMTKKEFSLTCMITGFLPAEIAVDWTSNGRTEQNYKNTATVLDSDGSYFMYSKLRVQKSTWERGSLFACSVVHEGLHNHLTTKTISRSLG-APGSGGGSAPG-YDDGICKSSDCIKSAARLIQNMDASVEPCTDFFKYACGGWLKRNVIPETSSRYSNFDILRDELEVILKDVLQEPKTEDIVAVQKAKTLYRSCINESAIDSRGGQPLLKLLPDIYGWPVASDNWDQTYGTSWTAEKSIAQLNSKYGKKVLINFFVGTDDKNSTQHIIHFDQPRLGLPSRDYYECTGIYKEACTAYVDFMISVARLIRQEQSLPIDENQLSLEMNKVMELEKEIANATTKPEDRNDPMLLYNKMTLAKLQNNFSLEYNGKSFSWSNFTNEIMSTVNINIQNEEEVVVYAPEYLTKLKPILTKYSPRDLQNLMSWRFIMDLVSSLSRNYKESRNAFRKALYGTTSETATWRRCANYVNGNMENAVGRLYVEAAFAGESKHVVEDLIAQIREVFIQTLDDLTWMDAETKKKAEEKALAIKERIGYPDDIISNENKLNNEYLELNYREDEYFENIIQNLKFSQSKQLKKLREKVDKDEWISGAAVVNAFYSSGRNQIVFPAGILQPPFFSAQQSNSLNYGGIGMVIGHEITHGFDDNGRNFNKDGDLVDWWTQQSANNFKDQSQCMVYQYGNFSWDLAGGQHLNGINTLGENIADNGGIGQAYRAYQNYVKKNGEEKLLPGLDLNHKQLFFLNFAQVWCGTYRPEYAYNSIKTDVHSPGNFRIIGTLQNSAEFADAFHCRKNSYMNPERKCRVW	[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.
4434	36471433	2022	EVQLVESGGGLYQPGNSLTLSCVASGFTFSNYGMHWIRQAPKKGLEWIAMITYDSSKMNYADTVKGRFTISRDNSKNTLYEMNSLRSEDTAMYYCAYPTSHYVVDVWGQGYSVTVSSGSTSGGGSGGGSGGGGSSDIQMTQSPASLSASLEEIVTITCQASQDIGNWLAWTQQKPGKSPQLLIYGATSLADGVPSRFSQSRSGTQFSLKISRYQVEDIGIYYCLQAYNTPWTFGGGTKLELKRASAPGSGGGSAPGEPRYPITQNPSPPLKECPPCAAPDLLGGPSYFIFPPKIKDVLMISLSPMYTCVVVDVSEDDPDYQISWFVNNYEVHTAQTQTHREDYNSTLRVVSALPIQHQDWMSGKEFKCKYNNRALPSPIEKTISKPRGPVRAPQVYVLPPPAEEMTKKEFSLTCMITGFLPAEIAVDWTSNGRTEQNYKNTATYLDSDGSYFMYSKLRVQKSTWERGSLFACSVVHEGLHNHLTTKTISRSLGPG-GGGSGGGGSGGGGS-EPRYPITQNPSPPLKECPPCAAPDLLGGPSVFIFPPKIKDVLMISLSPMVTCVVVDVSEDDPDYQISWFVNNVEVHTAQTQTHREDYNSTLRYVSALPIQHQDWMSGKEFKCKVNNRALPSPIEKTISKPRGPYRAPQVYVLPPPAEEMTKKEFSLTCMITGFLPAEIAVDWTSNGRTEQNYKNTATVLDSDGSYFMYSKLRVQKSTWERGSLFACSVVHEGLHNHLTTKTISRSLG-APGSGGGSAPG-YDDGICKSSDCIKSAARLIQNMDASVEPCTDFFKYACGGWLKRNVIPETSSRYSNFDILRDELEVILKDVLQEPKTEDIVAVQKAKTLVRSCINESAIDSRGGQPLLKLLPDIYGWPVASDNWDQTYGTSWTAEKSIAQLNSKYGKKVLINFFVGTDDKNSTQHIIHFDQPRLGLPSRDYYECTGIYKEACTAYVDFMISVARLIRQEQSLPIDENQLSLEMNKVMELEKEIANATTKPEDRNDPMLLYNKMTLAKLQNNFSLEYNGKSFSWSNFTNEIMSTVNINIQNEEEVVVYAPEYLTKLKPILTKYSPRDLQNLMSWRFIMDLVSSLSRNYKESRNAFRKALYVTTSETATWRRCANYVNGNMENAVGRLYVEAAFAGESKHVVEDLIAQIREVFIQTLDDLTWMDAETKKKAEEKALAIKERIGYPDDIISNENKLNNEYLELNYREDEYFENIIQNLKFSQSKQLKKLREKVDKDEWISGAAVVNAFYSSGRNQIVFPAGILQPPFFSAQQSNSLNYGGIGMVIGHEITHGFDDNGRNFNKDGDLVDWWTQQSANNFKDQSQCMVYQYGNFSWDLAGGQHLNGINTLGENIADNGGIGQAYRAYQNYVKKNGEEKLLPGLDLNHKQLFFLNFAQVWCGTYRPEYAYNSIKTDVHSPKNFRIIGTLQNSAEFADAFHCRKNSYMNPERKCRVW	[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.
4479	36323988	2022	HGEGTFSSELATILDALAARDFIAWLIATKITDKK	Glepaglutide M1	35	Free	Two lysines has been added at C terminal	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	5 mg	17	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.068 nM In vitro potency
4530	35990007	2022	desH-AEGTFTSDVSSYLEEQAAREFIAWLVRGRKX	Peptides 1	31	desH indicates the non-natural amino acid deamino-histidine	Free	Linear	L	X = R1, R2 = H (R2 group present in R1)	GLP-1R agonist	Antidiabetes, Antiobesity	200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h	17872 pmol/kg	18.6	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	N.A.
4594	35688476	2022	DNPSLSIDLTFHLLRTLLELEKQEKEKQQACQNRIIFDSV	PEG-hUCN1	40	Free	Amidation	Linear	L	Insertion of a cysteine residue at position 31 for pegylation	Human UCN1 derivative	Treating Autoimmune disease	N.A.	1 mg/kg	17	C57Bl/6J mice plasma protease	Laser capture/mass spectrometry	C57BL/6J mice plasma	In Vivo	None	None	At the CRHR2 receptor, the PEG-hUCN1 peptide was also less potent than UCN2 or UCN1 peptides with EC50 values of 80, 10, and 6.6 nM, respectively
4655	35150805	2022	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSIEGR	Exenatide-4aa-ABNF	43	Free	Albumin binding Nanofitins (ABNF) linked at C terminus by 4 aa	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection	400 nmol/kg	19.6 (Terminal Half Life)	Male CDR1 mice plasma protease	ELISA	Male CDR1 mice plasma	In Vivo	PDB id: 7MLL	None	EC50 = 1.387 nM ( in the classical in vitro GLP1R cell based assay based on cAMP)
4657	35150805	2022	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSGGGGSGG	Exenatide-7aa-ABNF	46	Free	Albumin binding Nanofitins (ABNF) linked at C terminus by 7 aa	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection	400 nmol/kg	19.3 (Terminal Half Life)	Male CDR1 mice plasma protease	ELISA	Male CDR1 mice plasma	In Vivo	PDB id: 7MLL	None	EC50 = 0.7459 nM ( in the classical in vitro GLP1R cell based assay based on cAMP)
4659	35150805	2022	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSGGS(GGGGS)4GG	Exenatide-25aa-ABNF	64	Free	Albumin binding Nanofitins (ABNF) linked at C terminus by 25 aa	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection	370 nmol/kg	18.7 (Terminal Half Life)	Male CDR1 mice plasma protease	ELISA	Male CDR1 mice plasma	In Vivo	PDB id: 7MLL	None	EC50 = 0.4903 nM ( in the classical in vitro GLP1R cell based assay based on cAMP)
4666	35046019	2022	MSKGPG-(VPGGGVPGAGVPG(pAzF-FA)GVPGGGVPGAGVPGYG)5-PGGGG-SKGEELFTGVVPILVELDGDVNGHKFSVRGEGEGDATNGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKRHDFFKSAMPEGYVQERTISFKDDGTYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNFNSHNVYITADKQKNGIKANFKIRHNVEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSVLSKDPNEKRDHMVLLEFVTAAGITHGMDELYKGS	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
4668	35046019	2022	MSKGPG-(VPGGGVPGAGVPG(pAzF-FA)G)1(VPGGGVPGAGVPGYG)9-PGGGG-SKGEELFTGVVPILVELDGDVNGHKFSVRGEGEGDATNGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKRHDFFKSAMPEGYVQERTISFKDDGTYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNFNSHNVYITADKQKNGIKANFKIRHNVEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSVLSKDPNEKRDHMVLLEFVTAAGITHGMDELYKGS	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
4683	34807760	2022	RRWVRRVRRVWRRVVRVVRRWVRR	PLG0206	24	Free	Free	Linear	L	None	Synthetic	Antimicrobial	Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion	0.25 mg/kg	19.94 (Median Terminal Half Life)	Human plasma protease	HPLC-MS	Human plasma	In Vivo	Pubchem CID : 16152467	None	N.A.
4685	34807760	2022	RRWVRRVRRVWRRVVRVVRRWVRR	PLG0206	24	Free	Free	Linear	L	None	Synthetic	Antimicrobial	Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion	0.5 mg/kg	16.2 (Median Terminal Half Life)	Human plasma protease	HPLC-MS	Human plasma	In Vivo	Pubchem CID : 16152467	None	N.A.
4686	34807760	2022	RRWVRRVRRVWRRVVRVVRRWVRR	PLG0206	24	Free	Free	Linear	L	None	Synthetic	Antimicrobial	Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion	1 mg/kg	19.97 (Median Terminal Half Life)	Human plasma protease	HPLC-MS	Human plasma	In Vivo	Pubchem CID : 16152467	None	N.A.
4717	N.A.	2022	(eeeeeeeeeXPLGLAXrrrrrrrrrk)2-(PEG)126	G5-PAMAM4-[e9-XPLGLAX-r9-k(cy5)]2[PEG]126	48	G5-PAMAM4	Cy5 linked with Lys side chain at C terminus, PEGylation	Linear	Mix	e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Strep=Streptavidin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker	Synthetic	Transport molecule	Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points	3 nmol	20	Mice blood plasma protease	N.A.	Mice blood plasma	In Vivo	None	US 201916457763 A	N.A.
4735	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGSHLVEALYLVCGERGFFETPR-OH)	Example 45	51	Free	B29R, desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	1 nmol/kg	987	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	N.A.
4807	35259149	2022	(HPN-Mal-C11-GIVEQCCTSICSLYQLENYCN)-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C3-Mal-HPN)	CH-/HPN-Conjugated Insulins (GlyA1/LysB29)	50	Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN]	K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN]	Cyclic (C6-C11 disulfide bond in A chain)	L	C7-C7 and C20-C19 disulfide bond between A and B chain	Human insulin analog	Antidiabetes	Blood samples were collected immediately before injection and at various time points up to 48 h after injection	100 nmol/kg	16.9	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50(nM) = 24.16
4839	35807558	2022	IKPEAPGEDASPEELNRYYASLRHYLNLVTR-βhGln-RY	[β-homoGln34]PYY3−36	34	Free	β-homoGln34 at C terminus	Linear	L	β-homoGln34 modification	PYY analogue	Antidiabetes, Antiobesity	The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)	1 μM	1200	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vitro	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	Ki(nM) = 160 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
4841	35807558	2022	IKPEAPGEDASPEELNRYYASLRHYLNWVTRQ-MeArg-RY	[Trp30, MeArg35]PYY3−36	34	Free	MeArg35 at C terminus	Linear	L	Trp30 modification, Methylated Arg35	PYY analogue	Antidiabetes, Antiobesity	The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)	1 μM	980	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vitro	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	Ki(nM) = 2500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
4857	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 1	34	Free	Amidation	Linear	L	None	Derived from PYY	Antiobesity	Blood samples (0.8 ml) were taken either from the jugular vein using vacutainer or from the IV catheter not used for dosing according to one of the following schedules: Predose, and 5, 15, 30, 45 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 192 h, 216 h, 240 h, 264 h and 288 h post dosing; or Predose, and 5, 30 min, 1 h, 2 h, 4 h, 7 h, 11 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 216 h, 264 h post dosing	15 nmol/kg	17	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 0.6 for Y2 receptor
4865	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 21	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 23	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	19	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 2 for Y2 receptor
4876	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 40	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	20	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4902	34450223	2021	HGEGTFTSNVSSYLEGQAAKEFIAWLVKGRG	GLP-DARPin	31	Genetic fusion of modified GLP-1 to the N-terminal of DARPins through a flexible linke (GGGGS)3	Free	Linear	L	FITC labeled	GLP-1 analogs	Antidiabetes	At 0.5, 2, 4, 7, 10, 24, 36, 48 and 72 h after injection, 20 μL of blood was collected	2 mg/mL	18.0 ± 2.8	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	Glucose-lowering effect of GLP-DARPin was more potent than that of GLP-2DARPin, EC50 of GLP-2DARPin was 9.06 ± 0.15 nM
4925	34064291	2021	RGDfK	111In-DOTA-cRGDfK	5	Radiolabelled with 111ln, DOTA	Free	Cyclic	L	None	Synthetic	For Spect imaging and potential theranostic	Blood samples (10 μL) were collected by heart puncture under 2% isoflurane anesthesia at 0.083, 0.5, 2, 4, 24, 48, 72, 96, and 168 h	1.85 MBq	17.2 (Terminal Half Life)	U-87 mg tumor bearing mice plasma protease	Radioactivity assay	U-87 mg tumor-bearing mice plasma	In Vivo	None	None	IC50(nM) =35.2
4937	33918853	2021	TSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIKKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLG-GGGSGGGTGGGSGGG-GFLG-ASPAAPAPAPAAPAPSAPAASPAAPAPASPAAPAPSAPA-GGSGG-RGDK	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
4938	33918853	2021	TSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIKKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLG-GGGSGGGTGGGSGGG-PLGLAG-ASPAAPAPAPAAPAPSAPAASPAAPAPASPAAPAPSAPA-GGSGG-RGDK	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
5037	32078672	2020	KTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	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
5043	33374407	2020	SDAAVDTSSEITTKDLKEKKEVVEEAEN	Tα1-PAS	28	Free	PAS#1(600)	Linear	L	None	Synthetic	Antiviral, Anticancer	Blood samples (100 µL) were taken from 5 animals each at various time points	3.4 mg/kg	15.7 ± 0.8 (Τ1/2a)	Rats plasma protease	sandwich ELISA	Rats plasma	In Vivo	UniprotKb ID: P06454	None	N.A.
5044	33374407	2020	SDAAVDTSSEITTKDLKEKKEVVEEAEN	Tα1-PAS	28	Free	PAS#1(600)	Linear	L	None	Synthetic	Antiviral, Anticancer	Blood samples (100 µL) were taken from 5 animals each at various time points	3.4 mg/kg	15.9 ± 0.9 (Τ1/2b )	Rats plasma protease	sandwich ELISA	Rats plasma	In Vivo	UniprotKb ID: P06454	None	N.A.
5077	32888078	2020	QHTQITKV	Human Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	18.5	50% W/V liver homogenate protease	HPLC	50% w/v liver homogenate	In Vitro	None	None	N.A.
5093	32858124	2020	(C18-diacid)-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip	Cmpd# 23	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C18-diacid	Free	Linear	Mix	hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid	Derived from pyr-apelin-13	Treatment of Chronic Hepatic Failure	N.A.	0.1 mg/kg	19.7	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE = 117 ± 23.3
5141	32582624	2020	Kψ(CH2NH)K-Sip-YI	Entry 8	5	Kψ[CH2NH]K substiuition	TMSAla conjugation	Linear	L	Sip amino acid substiution, TMSAla substuition	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	20 ± 4	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 610 ± 30 for hNTS1
5147	32582624	2020	Kψ(CH2NH)KPwI	Entry 14	5	Kψ[CH2NH]K substiuition	TMSAla-OH conjugation	Linear	L	Substiution of Y amino acid with d-W	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	19 ± 0.3	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 55 ± 3 for hNTS1
5190	35496622	2020	HGEGTFTSDLSQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK	Lixisenatide 1b	44	Free	Amidation	Linear	L	(X2) MPAs modification on Lys12	lixisenatide analogues	Antidiabetes	incubated at 37 °C for 6, 12, 24, and 48 h	1000 ng/mL	19.1	Rats blood plasma protease	LC-MS/MS	Rats blood plasma	In Vitro	None	None	EC50(nM) = 0.49 ± 0.11 for Lixisenatide 1b (in vitro GLP-1 receptor activation potency)
5196	35496622	2020	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKK	Lixisenatide 1h	44	Free	Amidation	Linear	L	(X2) MPAs modification on Lys12	lixisenatide analogues	Antidiabetes	incubated at 37 °C for 6, 12, 24, and 48 h	1000 ng/mL	17.8	Rats blood plasma protease	LC-MS/MS	Rats blood plasma	In Vitro	None	None	EC50(nM) = 1.97 ± 0.53 for Lixisenatide 1h (in vitro GLP-1 receptor activation potency)
5210	32082972	2020	PHWSYGLRPGGGGGSGGGGSGGGGSESKYGPPCPSCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSGGGGSGGGGSGGGGSIVRRADRAAVPGGGGACDCRGDCFC	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
5270	N.A.	2020	CSWPA-NMeArg-CLHQDLC	Ac-(06-34-18) (NMeArg5)	12	Acetylation	Free	Linear	L	NMeArg6 replaces Arg (R)	Synthetic	Targets plasma kallikrein	N.A.	5 uM	>20	Rats plasma protease	Waters Xevo TQ-MS	Rats plasma	In Vitro	None	US 201214350192 A	IC50(nM)(rat kallikrein) = 98
5277	N.A.	2020	CSFPY-NMeArg-CLHQDLC	Ac-(06-34-18) Phe2 Tyr4 NMeArg5	12	Acetylation	Free	Linear	L	NMeArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr	Synthetic	Targets plasma kallikrein	N.A.	5 uM	>20	Rats plasma protease	Waters Xevo TQ-MS	Rats plasma	In Vitro	None	US 201214350192 A	IC50(nM)(rat kallikrein) = 60.2
5365	31194563	2019	CARSKNKDC	Fasudil in CAR-liposome	9	Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys	Amidation	Linear	L	None	Synthetic	Treatment of Pulmonary Arterial Hypertension	N.A.	3 mg/kg	16.1 ± 4.1	PAH rats plasma protease	LC–MS/MS	PAH rats plasma	In Vivo	None	None	N.A.
5373	31156041	2019	LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK	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
5396	31083740	2019	HSEGTFTSDVSSYLEGQAAKEFIAWLVKGGVKALIDEILAA	SKL-18287	41	Free	Amidation	Linear	L	3H labeling at Tyr, Ser8 modification	GLP-1 analogs	Antidiabetes	Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration	17.4 µ/kg	15.4 ± 0.3 (Elimination Half Life)	Göttingen minipigs plasma protease	LC-MS/MS	Göttingen minipigs plasma	In Vivo	None	None	N.A.
5421	30973007	2019	QNSPNIFGQWM	GBAP 12	11	Free	Free	Linear	L	None	GBAP analogs	Antibacterial	Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, and 24 hr	0.28 mM	>20	N.A.	HPLC	pH 7.2 buffer	In Vitro	None	None	EC50 (nM) = 1.15 for GBAP
5483	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin7	20	R1 = PEG-Lys-Phe-Arg	Free	Linear	L	None	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	18	hplasma protease	LC-MS	hplasma	In Vitro	None	None	EC50(nM) = 6.3 ± 1.0
5486	30658804	2019	IVRRADRAAVP	ES2	11	Free	FITC	Linear	L	None	derived from the C-terminus of endostatin	Antiangiogenic	Immediately, 0.5, 1, 2, 4, 6, 8, 12, 24, and 36 h after injection, blood was collected	20 mg/kg	18.04 ± 2.38	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	Antitumor activity = 35.31%
5548	30504081	2019	(VPKEG)120	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
5656	30170067	2018	IVRRADRAAVPIVRRADRAAVPGGGGGGNQWFI	HA-ES2-AF	33	ES2-AF peptide was conjugated with HA by the formation of an amide linkage between the amino group of the ES2-AF peptide and the activated carboxyl of HA	Free	Linear	L	None	Synthetic	Treatment of diseases caused by Diabetic Eye Disease, Rheumatoid Arthritis And Other Neo-Vascularization, Anti-Angiogenesis Activity	Blood samples were collected through the jugular vein at 5 min, 15 min, 30 min, 1 h, 2 h, 6 h, 12 h, 24 h, and 48 h after administration	25 mg/kg	18.07	Wistar rats plasma protease	Fluorescence spectrometry	Wistar rats plasma	In Vivo	None	None	KD (mol· L−1) = 4.779 × 10−10
5689	30023916	2018	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	CH10-conjugated peptides	31	Free	CH10 linked by linker	Linear	L	Substituition of G for A at position 2	Synthetic	Antidiabetes	37 °C for 2 h	N.A.	16 (T1/2 Elimination Half life)	0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii	HPLC	N.A.	In Vitro	None	None	N.A.
5691	30023916	2018	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	PEG30k-conjugated GLP-1C peptide	31	PEG30K	Free	Linear	L	Substituition of G for A at position 2	Synthetic	Antidiabetes	37 °C for 2 h	N.A.	17.5 (T1/2 Elimination Half life)	0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii	HPLC	N.A.	In Vitro	None	None	EC50 = 5.2 nM
5694	30012756	2018	L-threonyl-L-tryptophanyl-L-isoleucyl-L-2,4-diaminobutyryl-L-ornithyl-D-2,4-diaminobutyryl-L-2,4-diaminobutyryl-L-tryptophanyl-L-2,4-diaminobutyryl-L-2,4-diaminobutyryl-L-alanyl-L-seryl,D-prolyl-L-prolyl	Murepavadin	14	Free	Free	Cyclic (N-C terminal end)	Mix	Acetate	Synthetic	Antimicrobial	Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment	2.2 mg/kg	15.9	Human plasma protease	LC-MS with electrospray ionization assay	Human plasma (Moderate Renal impairment group)	In Vivo	https://sci-hub.st/10.1080/14787210.2018.1441024	None	MIC50 = 0.12 mg/L against P. aeruginosa
5707	29799205	2018	HGEGTYTNDVTEYLEEEAA-X1-EFIEWLIKGK	4a	29	Free	Free	Linear	L	X1 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	17.4	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.29 ± 0.04
5719	29799205	2018	HGEGTYTNDVTEYLEEEAA-X1-EFIEWLIKGKPSSGAPPSKKKKKK	4m	43	Free	Free	Linear	L	X1 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	18.8	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.18 ± 0.06
5722	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X1-GKPSSGAPPSKKKKKK	4p	43	Free	Free	Linear	L	X1 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	16.9	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.14 ± 0.02
5737	29738954	2018	FGrKKRrQrRr-βAla	γTatM4	12	Acetylation	Amidation	Linear	L	None	Tat peptide analogue	Antibacterial and Anti-Tb	N.A.	10 mM	16	Trypsin	RP-HPLC	Tris-EDTA buffer	In Vitro	None	None	MIC(micrmolar) = 1.12 ± 0.01 for E.coli
5755	29673717	2018	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Liraglutide	32	Free	Free	Linear	L	Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu	GLP-1 analogs	Antidiabetes	At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points	1000 ng/mL	15.4	Rats plasma protease	LC-MS/MS	Rats plasma	In Vitro	None	None	N.A.
5780	29602308	2018	HSTPSSP	P4-Chlorambucil-PEG-AuNP	7	Free	Chlorambucil	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	20	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5782	29602308	2018	HSTPSSP	P4-Melphalan-PEG-AuNP	7	Free	Melphalan	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	18.3	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5784	29602308	2018	HSTPSSP	P4-Bendamustine-PEG-AuNP	7	Free	Bendamustine	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	18.3	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5853	29436835	2018	(hpcdypewqwlcelGk)3	CPT31	48	Chol-Maleimide joined by linker PEG31	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	Plasma samples were collected pre-dose and 0.25, 0.5, 1, 2, 4, 8, 16, 24, 48 and 72 h post-dose	3 mg/kg	18.8	Male cynomolgus monkeys plasma protease	LC-MS	Male cynomolgus monkeys plasma	In Vivo	None	None	JRFL(nM) = 0.015 ± 0.0062 (antiviral potency)
5883	29329072	2018	YFLNGRPRN	Compound 38	8	Acetylation	Amidation	Linear	L	N(4-OH-Phenethyl)Gly at position 4	NMU-analogs	Regulation Of Feeding Behavior, The Stress Response And Nociception	37 °C	112 µM	1096.1 ± 56.1	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 216.6, IC50(nM) = 3.9 for hNMUR1 and EC50(nM) = 339.2, IC50(nM) = 206.9 for hNMUR2
5965	28741871	2017	Y-Aib-EGTFTSDYSIYLDKQAA-Aib-EFVNWLLAGGPSSGAPPPSK	RG7697	40	Free	Acylated at a C-terminal lysine with a saturated C16 lipid	Cyclic (L14-E21, Q17-N24 Lactam Bridge)	L	Aib modification at position 2, 20	chimera of GLP-1 and GIP peptides	Antidiabetes	RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted	0.2 mg	19.3 (T1/2b- Appearant Terminal Half Life)	Human plasma protease	LC-MS	Human plasma	In Vivo	None	None	for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors
5968	28741871	2017	Y-Aib-EGTFTSDYSIYLDKQAA-Aib-EFVNWLLAGGPSSGAPPPSK	RG7697	40	Free	Acylated at a C-terminal lysine with a saturated C16 lipid	Cyclic (L14-E21, Q17-N24 Lactam Bridge)	L	Aib modification at position 2, 20	chimera of GLP-1 and GIP peptides	Antidiabetes	RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted	3.6 mg	19.9 (T1/2b- Appearant Terminal Half Life)	Human plasma protease	LC-MS	Human plasma	In Vivo	None	None	for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors
5969	28741871	2017	Y-Aib-EGTFTSDYSIYLDKQAA-Aib-EFVNWLLAGGPSSGAPPPSK	RG7697	40	Free	Acylated at a C-terminal lysine with a saturated C16 lipid	Cyclic (L14-E21, Q17-N24 Lactam Bridge)	L	Aib modification at position 2, 20	chimera of GLP-1 and GIP peptides	Antidiabetes	RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted	5 mg	15.3 / 15.7 (T1/2b- Appearant Terminal Half Life)	Human plasma protease	LC-MS	Human plasma	In Vivo	None	None	for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors
6032	28323965	2017	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGFSSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)
6047	28068664	2017	N.A.	scFv57R	N.A.	Free	Free	Linear	L	None	Synthetic	Antiviral (against Rabies Virus)	37o C for 0-72 hours	0.5 mg/ml	14.1	N.A.	ELISA	PBS	In Vitro	None	None	Neutralizing potency (IU/ml) = 83.8 ± 9.4 for monomer
6049	28068664	2017	DPDNEAYEMPSEEGYQDYEPEA	scFv57R-ATS	N.A.	Free	(ATS) was fused to the C-terminus of the anti-RV scFv57R	Linear	L	None	scFv57R-ATS fusion protein	Antiviral (against Rabies Virus)	37o C	0.5 mg/ml	15.6	Mouse serum protease	ELISA	Mouse serum	In Vitro	None	None	Neutralizing potency (IU/ml) = 2.9 ± 0.5 for polymer
6127	27240277	2016	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	PEG2k-ENF	36	mPEG(2KDa)-Maleimide	Free	Linear	L	None	Synthetic	Antiviral (against HIV infection)	N.A.	1.7 μmol/kg	16.1 ± 3.8 (Elimination Half Life)	SD rats plasma protease	HPLC	SD rats plasma	In Vivo	None	None	EC50(nM) = 4 ± 0
6142	27115755	2016	MKWVTFISLLFLFSSAYSRGVFRRHHHHHH-IEGPTLRQWLAARAGGGGSIEGPTLRQWLAARA	HSA-dTMP	63	HSA joined using a linker	Free	Linear	L	None	Fusion protein of dTMP and HSA	Treatment of Thrombocytopenia	Serum was sampled from mice eyes at 5 min, 30 min, 1 h,1.5 h, 2 h, 4 h, 12 h, 24 h, and 48 h after dosing	300 μg/kg	17.1	Mice serum protease	Immunoenzymetric assay	Mice serum	In Vivo	None	None	both HSA-dTMP and dTMP-HSA could significantly increase peripheral platelet counts in a dose-dependent manner in normal mice
6143	27115755	2016	IEGPTLRQWLAARA-GGGGS-IEGPTLRQWLAARA-MKWVTFISLLFLFSSAYSRGVFRRHHHHHH	dTMP-HSA	63	Free	HSA joined using a linker	Linear	L	None	Fusion protein of dTMP and HSA	Treatment of Thrombocytopenia	Serum was sampled from mice eyes at 5 min, 30 min, 1 h,1.5 h, 2 h, 4 h, 12 h, 24 h, and 48 h after dosing	300 μg/kg	16.1	Mice serum protease	Immunoenzymetric assay	Mice serum	In Vivo	None	None	both HSA-dTMP and dTMP-HSA could significantly increase peripheral platelet counts in a dose-dependent manner in normal mice
6151	26905040	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	WT-EX4	39	Free	Amidation	Linear	L	None	GLP-1 analogs	Antidiabetes	37 °C	200 μg/mL	16.9	Mice plasma protease	RP-HPLC	CLP-induced septic mice plasma	In Vitro	None	None	WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM
6168	26808199	2016	LRHYLNLLTRQRY	PYY24–36-Leu31 conjugates 2	13	R2( structure given in paper) at NH terminal	Amidation	Linear	L	Leu31 substituitions	PYY analog	Antiobesity	An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point	1000 ng/mL	>20	SD rats plasma protease	LC–MS/MS	SD rats plasma	In Vitro	None	None	HSA binding correlated well with plasma stability
6212	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)
6213	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)
6214	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)
6215	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)
6216	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)
6217	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)
6219	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)
6220	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	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)