In vitro activity of BMS-790052 on hepatitis C virus genotype 4 NS5A

Antimicrob Agents Chemother. 2012 Mar;56(3):1588-90. doi: 10.1128/AAC.06169-11. Epub 2011 Dec 27.

Abstract

The antiviral profile of BMS-790052, a potent hepatitis C virus (HCV) replication complex inhibitor targeting nonstructural protein NS5A, is well characterized for HCV genotype-1. Here, we report that BMS-790052 inhibits hybrid replicons containing HCV genotype-4 NS5A genes with 50% effective concentrations (EC(50)s) ranging from 7 to 13 pM. NS5A residue 30 was an important site for BMS-790052-selected resistance in the hybrid replicons. Our results support the potential of BMS-790052 as a valuable component of combination therapy for HCV genotype-4 chronic infection.

MeSH terms

  • Amino Acid Sequence
  • Antiviral Agents / pharmacology*
  • Carbamates
  • Cell Line
  • Drug Resistance, Viral
  • Genes, Reporter
  • Genotype
  • Hepacivirus / drug effects*
  • Hepacivirus / physiology
  • Humans
  • Imidazoles / pharmacology*
  • Inhibitory Concentration 50
  • Luciferases / genetics
  • Molecular Sequence Data
  • Pyrrolidines
  • Replicon / genetics
  • Valine / analogs & derivatives
  • Viral Nonstructural Proteins / antagonists & inhibitors*
  • Viral Nonstructural Proteins / genetics
  • Viral Nonstructural Proteins / metabolism
  • Virus Replication / drug effects
  • Virus Replication / genetics

Substances

  • Antiviral Agents
  • Carbamates
  • Imidazoles
  • Pyrrolidines
  • Viral Nonstructural Proteins
  • Luciferases
  • NS-5 protein, hepatitis C virus
  • Valine
  • daclatasvir

Associated data

  • GENBANK/JQ347513
  • GENBANK/JQ347514
  • GENBANK/JQ347515