Conformational inhibition of the hepatitis C virus internal ribosome entry site RNA

Nat Chem Biol. 2009 Nov;5(11):823-5. doi: 10.1038/nchembio.217. Epub 2009 Sep 20.

Abstract

The internal ribosome entry site (IRES), a highly conserved structured element of the hepatitis C virus (HCV) genomic RNA, is an attractive target for antiviral drugs. Here we show that benzimidazole inhibitors of the HCV replicon act by conformational induction of a widened interhelical angle in the IRES subdomain IIa, which facilitates the undocking of subdomain IIb from the ribosome and ultimately leads to inhibition of IRES-driven translation in HCV-infected cells.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antiviral Agents / pharmacology
  • Antiviral Agents / therapeutic use
  • Base Sequence
  • Benzimidazoles / pharmacology
  • Cytosine / chemistry
  • Genome, Viral / drug effects
  • Genotype
  • Hepacivirus / chemistry
  • Hepacivirus / drug effects
  • Hepacivirus / genetics
  • Hepacivirus / metabolism*
  • Magnesium / pharmacology
  • Models, Molecular
  • Nucleic Acid Conformation
  • RNA, Viral / chemistry
  • RNA, Viral / genetics
  • RNA, Viral / metabolism
  • Replicon / drug effects
  • Replicon / genetics
  • Ribosomes / genetics
  • Ribosomes / metabolism*
  • Ribosomes / virology
  • Signal Transduction

Substances

  • Antiviral Agents
  • Benzimidazoles
  • RNA, Viral
  • Cytosine
  • Magnesium

Associated data

  • PubChem-Substance/85182175
  • PubChem-Substance/85182176
  • PubChem-Substance/85182177
  • PubChem-Substance/85182178
  • PubChem-Substance/85182179