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PMID: 3863616 Published · ppublish English Journal Article

Specificity of activated human protein C.

The Biochemical journal ·Vol. 230 ·No. 2 ·1985-09-01 ·Pages 497-502

Stone SR, Hofsteenge J

Abstract

Peptide p-nitroanilide substrates and peptidylchloromethane inhibitors were used to examine the specificity of activated human Protein C. Substrates with arginine in the P1 position had the highest activity. The best substrates and inhibitors, as judged by the second-order rate constant for their interaction with the enzyme, had an apolar residue in the P2 position. In contrast with thrombin [Kettner & Shaw (1981) Methods Enzymol. 80, 826-842], activated Protein C was able to accommodate large hydrophobic residues such as phenylalanine and leucine in the P2 position. In the P3 position, the enzyme preferred an apolar D-amino acid residue. The results of the present study have also indicated a suitable substrate and inhibitor to be used in the assay of functional protein C and of thrombomodulin.

MeSH Terms
Anilides/metabolism Blood Coagulation Factors/metabolism Enzyme Activation/drug effects Glycoproteins/antagonists & inhibitors,metabolism Humans Hydrocarbons, Chlorinated/pharmacology Kinetics Peptides/pharmacology Protein C Substrate Specificity
Chemicals
Anilides Blood Coagulation Factors Glycoproteins Hydrocarbons, Chlorinated Peptides Protein C
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Stone S R
Hofsteenge J
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27 references, click to expand
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Article Info
Journal
The Biochemical journal
Abbr.
Biochem J
ISSN
0264-6021
DOI
10.1042/bj2300497
Published
1985-09-01
Pages
497-502
Language
English
Region
England
NLM ID
2984726R
PMCID
PMC1152642
Subset
IM
External Links
PubMed source DOI: 10.1042/bj2300497 PMC Full Text View journal details
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