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Peptide-based inhibitors of the hepatitis C virus serine protease. 1998
M Llinàs-Brunet, and
M Bailey, and
G Fazal, and
S Goulet, and
T Halmos, and
S Laplante, and
R Maurice, and
M Poirier, and
M A Poupart, and
D Thibeault, and
D Wernic, and
D Lamarre
Bio-Méga Research Division, Boehringer Ingelheim (Canada) Ltd., Laval, Québec, Canada.
Hexapeptide DDIVPC-OH is a competitive inhibitor of the hepatitis C virus (HCV) NS3 protease complexed with NS4A cofactor peptide. This hexapeptide corresponds to the N-terminal cleavage product of an HCV dodecapeptide substrate derived from the NS5A/5B cleavage site. Structure-activity studies on Ac-DDIVPC-OH revealed that side chains of the P4, P3 and P1 residues contribute the most to binding and that the introduction of a D-amino acid at the P5 position improves potency considerably. Furthermore, there is a strong preference for cysteine at the P1 position and conservative replacements, such as serine, are not well tolerated.
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G Fazal, and
S Goulet, and
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M A Poupart, and
D Thibeault, and
D Wernic, and
D Lamarre
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G Fazal, and
S Goulet, and
T Halmos, and
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M A Poupart, and
D Thibeault, and
D Wernic, and
D Lamarre
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