Ontology highlight
ABSTRACT:
SUBMITTER: O'Meara JA
PROVIDER: S-EPMC3581377 | biostudies-literature | 2013 Feb
REPOSITORIES: biostudies-literature
O'Meara Jeff A JA Lemke Christopher T CT Godbout Cédrickx C Kukolj George G Lagacé Lisette L Moreau Benoît B Thibeault Diane D White Peter W PW Llinàs-Brunet Montse M
The Journal of biological chemistry 20121227 8
Although optimizing the resistance profile of an inhibitor can be challenging, it is potentially important for improving the long term effectiveness of antiviral therapy. This work describes our rational approach toward the identification of a macrocyclic acylsulfonamide that is a potent inhibitor of the NS3-NS4A proteases of all hepatitis C virus genotypes and of a panel of genotype 1-resistant variants. The enhanced potency of this compound versus variants D168V and R155K facilitated x-ray det ...[more]