Discovery of hepatitis C virus NS3 helicase inhibitors by a multiplexed, high-throughput helicase activity assay based on graphene oxide

Angew Chem Int Ed Engl. 2013 Feb 18;52(8):2340-4. doi: 10.1002/anie.201209222. Epub 2013 Jan 25.

Abstract

A GO‐to solution: A simple graphene oxide (GO)‐based assay to screen for selective inhibitors of a hepatitis C virus (HCV) helicase along with inhibitors of a severe acute respiratory syndrome coronavirus (SARS CoV) helicase was tested (see scheme). A single screen found five inhibitors highly selective for the HCV helicase orthologous to the SARS CoV helicase. Some of these hits were validated using the same GO‐based assay.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Assay / methods*
  • Cells, Cultured
  • Drug Discovery*
  • Graphite / chemistry*
  • Hepacivirus
  • Humans
  • Inhibitory Concentration 50
  • Oxides / chemistry
  • Protease Inhibitors / chemistry*
  • Protease Inhibitors / pharmacology
  • Viral Nonstructural Proteins / antagonists & inhibitors*

Substances

  • NS3 protein, hepatitis C virus
  • Oxides
  • Protease Inhibitors
  • Viral Nonstructural Proteins
  • Graphite