A cell-based beta-lactamase reporter gene assay for the identification of inhibitors of hepatitis C virus replication

Anal Biochem. 2004 Nov 15;334(2):344-55. doi: 10.1016/j.ab.2004.07.031.

Abstract

This report describes the development, optimization, and implementation of a cell-based assay for high-throughput screening (HTS) to identify inhibitors to hepatitis C virus (HCV) replication. The assay is based on a HCV subgenomic RNA replicon that expresses beta-lactamase as a reporter for viral replication in enhanced Huh-7 cells. The drug targets in this assay are viral and cellular enzymes required for HCV replication, which are monitored by fluorescence resonance energy transfer using cell-permeable CCF4-AM as a beta-lactamase substrate. Digital image processing was used to visualize cells that harbor viral RNA and to optimize key assay development parameters such as transfection and culturing conditions to obtain a cell line which produced a robust assay window. Formatting the assay for compound screening was problematic due to small signal-to-background ratio and reduced potency to known HCV inhibitors. These technical difficulties were solved by using clavulanic acid, an irreversible inhibitor of beta-lactamase, to eliminate residual beta-lactamase activity after HCV replication was terminated, thus resulting in an improved assay window. HTS was carried out in 384-well microplate format, and the signal-to-background ratio and Z factor for the assay plates during the screen were approximately 13-fold and 0.5, respectively.

MeSH terms

  • Antiviral Agents / pharmacology*
  • Cell Line
  • Clavulanic Acid / pharmacology
  • DNA Replication
  • Drug Evaluation, Preclinical / instrumentation
  • Drug Evaluation, Preclinical / methods*
  • Enzyme Inhibitors / pharmacology
  • Genes, Reporter / genetics*
  • Hepacivirus / drug effects*
  • Hepacivirus / genetics
  • Hepacivirus / physiology
  • Humans
  • Inhibitory Concentration 50
  • RNA, Viral / genetics
  • RNA, Viral / metabolism
  • Replicon / genetics
  • Sensitivity and Specificity
  • Transfection
  • Viral Nonstructural Proteins / antagonists & inhibitors
  • Viral Nonstructural Proteins / metabolism
  • Virus Replication / drug effects*
  • beta-Lactamases / biosynthesis
  • beta-Lactamases / genetics*
  • beta-Lactamases / metabolism*

Substances

  • Antiviral Agents
  • Enzyme Inhibitors
  • RNA, Viral
  • Viral Nonstructural Proteins
  • Clavulanic Acid
  • NS-5 protein, hepatitis C virus
  • beta-Lactamases