Title : Inhibition of trypsin-like serine proteinases by tripeptide arginyl and lysyl chloromethylketones.

Pub. Date : 1984 Jun 1

PMID : 6234678






2 Functional Relationships(s)
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Protein Name
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1 Tripeptide derivatives of lysyl or arginyl chloromethylketone inhibit the trypsin-like serine proteases trypsin, thrombin, plasmin, Factor Xa, urokinase, tissue-type plasminogen activator and protein Ca following the reaction scheme: (formula; see text) Extremely potent tripeptide inhibitors were obtained for thrombin and trypsin (k2/Ki greater than 10(6) M-1s-1), moderate inhibitors for plasmin and Factor Xa (10(6) M-1s-1 greater than k2/Ki greater than 10(4) M-1s-1) and only weak inhibitors for urokinase, tissue-type plasminogen activator and protein Ca (k2/Ki less than 10(4) M-1s-1). tripeptide K-26 plasminogen Homo sapiens
2 Tripeptide derivatives of lysyl or arginyl chloromethylketone inhibit the trypsin-like serine proteases trypsin, thrombin, plasmin, Factor Xa, urokinase, tissue-type plasminogen activator and protein Ca following the reaction scheme: (formula; see text) Extremely potent tripeptide inhibitors were obtained for thrombin and trypsin (k2/Ki greater than 10(6) M-1s-1), moderate inhibitors for plasmin and Factor Xa (10(6) M-1s-1 greater than k2/Ki greater than 10(4) M-1s-1) and only weak inhibitors for urokinase, tissue-type plasminogen activator and protein Ca (k2/Ki less than 10(4) M-1s-1). tripeptide K-26 plasminogen Homo sapiens