Article
Preclinical characterization of BMS-791325, an allosteric inhibitor of hepatitis C Virus NS5B polymerase.
Antimicrobial agents and chemotherapy - 1 Jun 2014
Lemm Julie A, Liu Mengping, Gentles Robert G, Ding Min, Voss Stacey, Pelosi Lenore A, Wang Ying-Kai, Rigat Karen L, Mosure Kathleen W, Bender John A, Knipe Jay O, Colonno Richard, Meanwell Nicholas A, Kadow John F, Santone Kenneth S, Roberts Susan B, Gao Min
Abstract excerpt
BMS-791325 is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. BMS-791325 inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 at 50% inhibitory concentrations (IC50) below 28 nM. In cell culture, BMS-791325 inhibited replication of HCV subgenomic replicons representing genotypes 1a and 1b at 50% effective concentrations (EC50s)...
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