Solid-Phase Synthesis of Peptidomimetic Inhibitors for the Hepatitis C Virus NS3 Protease

The NS3 serine protease enzyme of the hepatitis C virus (HCV) is essential for viral replication. Short peptides mimicking the N-terminal substrate cleavage products of the NS3 protease are known to act as weak inhibitors of the enzyme and have been used as templates for the design of peptidomimetic...

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Bibliographic Details
Published in:Journal of organic chemistry 2001-07, Vol.66 (14), p.4743-4751
Main Authors: Poupart, Marc-André, Cameron, Dale R, Chabot, Catherine, Ghiro, Elise, Goudreau, Nathalie, Goulet, Sylvie, Poirier, Martin, Tsantrizos, Youla S
Format: Article
Language:English
Subjects:
Combinatorial Chemistry Techniques
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - pharmacology
Humans
Molecular Mimicry
Oligopeptides - chemical synthesis
Oligopeptides - pharmacology
Peptide Library
Structure-Activity Relationship
Viral Nonstructural Proteins - antagonists & inhibitors
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Summary:The NS3 serine protease enzyme of the hepatitis C virus (HCV) is essential for viral replication. Short peptides mimicking the N-terminal substrate cleavage products of the NS3 protease are known to act as weak inhibitors of the enzyme and have been used as templates for the design of peptidomimetic inhibitors. Automated solid-phase synthesis of a small library of compounds based on such a peptidomimetic scaffold has led to the identification of potent and highly selective inhibitors of the NS3 protease enzyme.
ISSN:0022-3263
1520-6904
DOI:10.1021/jo010164d