Characterization of V36C, a novel amino acid substitution conferring hepatitis C virus (HCV) resistance to telaprevir, a potent peptidomimetic inhibitor of HCV protease.
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ABSTRACT:
SUBMITTER: Barbotte L
PROVIDER: S-EPMC2876365 | biostudies-literature | 2010 Jun
REPOSITORIES: biostudies-literature
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Characterization of V36C, a novel amino acid substitution conferring hepatitis C virus (HCV) resistance to telaprevir, a potent peptidomimetic inhibitor of HCV protease.
Barbotte Laetitia L Ahmed-Belkacem Abdelhakim A Chevaliez Stéphane S Soulier Alexandre A Hézode Christophe C Wajcman Henri H Bartels Doug J DJ Zhou Yi Y Ardzinski Andrzej A Mani Nagraj N Rao B Govinda BG George Shelley S Kwong Ann A Pawlotsky Jean-Michel JM
Antimicrobial agents and chemotherapy 20100405 6
We characterized a novel substitution conferring moderate resistance to telaprevir, a peptidomimetic inhibitor of hepatitis C virus protease. V36C conferred a 4.0-fold increase in the telaprevir 50% inhibitory concentration in an enzyme assay and a 9.5-fold increase in the replicon model. The replication capacity of a replicon harboring V36C was close to that of the wild-type protease. This case emphasizes the complexity of hepatitis C virus resistance to protease inhibitors. ...[more]
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