Peptide Inhibitors of Hepatitis C Virus NS3 Protease-Reference-Cited by-同舟云学术

Peptide Inhibitors of Hepatitis C Virus NS3 Protease

Published:2003-10 Issue:5 Volume:14 Page:225-233
ISSN:2040-2066
Container-title:Antiviral Chemistry and Chemotherapy
language:en
Short-container-title:Antivir Chem Chemother

Author:

Portal-Núñez Sergio¹,González-Navarro Carlos J¹,García-Delgado Marina¹,Vizmanos José Luis¹,Lasarte Juan José²,Borrás-Cuesta Francisco²

Affiliation:

1. Department of Genetics, Faculty of Science, University of Navarra, Pamplona, Spain

2. FIMA, Division of Hepatology & Gene Therapy, University of Navarra, Pamplona, Spain

Abstract

Hepatitis C virus (HCV) is a highly prevalent virus and one of the major agents of chronic hepatitis. Since HCV NS3 protease is essential for the processing of HCV polyprotein, this protease is a target of choice to control HCV replication. Peptide inhibitors of NS3 were developed by selective amino acid replacement of six leader sequences, corresponding to regions of HCV polyprotein that are cleaved by NS3. The large numbers of potential 14-mer and 16-mer peptide inhibitors thus obtained were tested against NS3 using the fluorescent probe RETS1 and peptide cofactor SVVIVGRIILSGRA from NS4A protein. This afforded several peptide inhibitors with an IC50 of around 2 μM. These peptides may be good leading compounds for the development of peptidomimetics to control HCV replication in the treatment of chronic hepatitis C.

Publisher

SAGE Publications

Link

http://journals.sagepub.com/doi/pdf/10.1177/095632020301400501

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