Literature summary for 3.4.21.1 extracted from

Mazur-Marzec, H.; Fidor, A.; Ceglowska, M.; Wieczerzak, E.; Kropidlowska, M.; Goua, M.; Macaskill, J.; Edwards, C.
Cyanopeptolins with trypsin and chymotrypsin inhibitory activity from the cyanobacterium Nostoc edaphicum CCNP1411 (2018), Mar. Drugs, 16, E220 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
cyanopeptolin	Arg-containing cyanopeptolins inhibit trypsin at low IC50 values (0.00024-0.00026 mM)and show mild activity against chymotrypsin (IC50 0.0031-0.0038 mM), while Tyr-containing cyanopeptolins are selectively and potently active against chymotrypsin (IC50 0.00026 mM). Neither of the cyanopeptolins are active against thrombin, elastase or protein phosphatase 1. Two cyanopeptolins (CP962 and CP985) have no cytotoxic effects on MCF-7 breast cancer cells. Strong and selective activity of the new cyanopeptolin variants makes them potential candidates for the development of drugs against metabolic disorders and other diseases	Bos taurus
cyanopeptolin 1020	isolated from Nostoc edaphicum CCNP1411	Bos taurus
cyanopeptolin 1027	isolated from Nostoc edaphicum CCNP1411	Bos taurus
cyanopeptolin 978	isolated from Nostoc edaphicum CCNP1411	Bos taurus
cyanopeptolin 985	isolated from Nostoc edaphicum CCNP1411	Bos taurus
cyanopeptolin 992	isolated from Nostoc edaphicum CCNP1411	Bos taurus

Organism

Organism	UniProt	Comment	Textmining
Bos taurus	P00766	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
pancreas	-	Bos taurus	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
N-succinyl-Gly-Gly-4-nitroanilide + H2O	-	Bos taurus	N-succinyl-Gly-Gly + 4-nitroaniline	-	?

Synonyms

Synonyms	Comment	Organism
alpha-chymotrypsin	-	Bos taurus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00026	-	pH 7.5, 37°C	Bos taurus	cyanopeptolin 1027
0.00026	-	pH 7.5, 37°C	Bos taurus	cyanopeptolin 985
0.0031	-	pH 7.5, 37°C	Bos taurus	cyanopeptolin 1020
0.0035	-	pH 7.5, 37°C	Bos taurus	cyanopeptolin 992
0.0038	-	pH 7.5, 37°C	Bos taurus	cyanopeptolin 978

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Release 2023.1 (January 2023)