Abstract
Protease-activated receptors [PARs] are a family of G-protein-coupled seven-transmembrane domain receptors that are activated by proteolytic cleavage of their amino-terminal exodomain. To characterize the cleavage rate of human PAR-1 / 2 / 3 and 4 by trypsin and thrombin, four synthetic quenched-fluorescent peptide substrates have been synthesized. Each substrate consisted of a ten-residue peptide spanning the receptor activation cleavage site and using progress-curve kinetics, kcat / Km values were determined.
Keywords: Enzymology, serine proteases, progress-curve kinetics, fluorescence, 2-aminobenzoyl (Abz), 2,4-dinitrophenyl (Dnp), fluorescence resonance, G-protein-coupled, seven-transmembrane, domain receptor
Protein & Peptide Letters
Title: Kinetic Analysis of the Cleavage of Human Protease-Activated Receptor-1 / 2 / 3 and 4 Using Quenched-Fluorescent Peptide Substrates
Volume: 9 Issue: 5
Author(s): Mark T. Fox, Brett Greer, Jill Lawson, Adrienne Healy and Patrick Harriott
Affiliation:
Keywords: Enzymology, serine proteases, progress-curve kinetics, fluorescence, 2-aminobenzoyl (Abz), 2,4-dinitrophenyl (Dnp), fluorescence resonance, G-protein-coupled, seven-transmembrane, domain receptor
Abstract: Protease-activated receptors [PARs] are a family of G-protein-coupled seven-transmembrane domain receptors that are activated by proteolytic cleavage of their amino-terminal exodomain. To characterize the cleavage rate of human PAR-1 / 2 / 3 and 4 by trypsin and thrombin, four synthetic quenched-fluorescent peptide substrates have been synthesized. Each substrate consisted of a ten-residue peptide spanning the receptor activation cleavage site and using progress-curve kinetics, kcat / Km values were determined.
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Cite this article as:
Fox T. Mark, Greer Brett, Lawson Jill, Healy Adrienne and Harriott Patrick, Kinetic Analysis of the Cleavage of Human Protease-Activated Receptor-1 / 2 / 3 and 4 Using Quenched-Fluorescent Peptide Substrates, Protein & Peptide Letters 2002; 9 (5) . https://dx.doi.org/10.2174/0929866023408490
DOI https://dx.doi.org/10.2174/0929866023408490 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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