Class III phosphatidylinositol 4-kinase alpha and beta are novel host factor regulators of hepatitis C virus replication

J Virol. 2009 Oct;83(19):10058-74. doi: 10.1128/JVI.02418-08. Epub 2009 Jul 15.

Abstract

Host factor pathways are known to be essential for hepatitis C virus (HCV) infection and replication in human liver cells. To search for novel host factor proteins required for HCV replication, we screened a subgenomic genotype 1b replicon cell line (Luc-1b) with a kinome and druggable collection of 20,779 siRNAs. We identified and validated several enzymes required for HCV replication, including class III phosphatidylinositol 4-kinases (PI4KA and PI4KB), carbamoyl-phosphate synthetase 2, aspartate transcarbamylase, and dihydroorotase (CAD), and mevalonate (diphospho) decarboxylase. Knockdown of PI4KA could inhibit the replication and/or HCV RNA levels of the two subgenomic genotype 1b clones (SG-1b and Luc-1b), two subgenomic genotype 1a clones (SG-1a and Luc-1a), JFH-1 genotype 2a infectious virus (JFH1-2a), and the genomic genotype 1a (FL-1a) replicon. In contrast, PI4KB knockdown inhibited replication and/or HCV RNA levels of Luc-1b, SG-1b, and Luc-1a replicons. The small molecule inhibitor, PIK93, was found to block subgenomic genotype 1b (Luc-1b), subgenomic genotype 1a (Luc-1a), and genomic genotype 2a (JFH1-2a) infectious virus replication in the nanomolar range. PIK93 was characterized by using quantitative chemical proteomics and in vitro biochemical assays to demonstrate PIK93 is a bone fide PI4KA and PI4KB inhibitor. Our data demonstrate that genetic or pharmacological modulation of PI4KA and PI4KB inhibits multiple genotypes of HCV and represents a novel druggable class of therapeutic targets for HCV infection.

MeSH terms

  • 1-Phosphatidylinositol 4-Kinase / chemistry
  • 1-Phosphatidylinositol 4-Kinase / metabolism*
  • Antiviral Agents / pharmacology
  • Binding, Competitive
  • Cell Line
  • Gene Silencing
  • Genotype
  • Hepacivirus / genetics*
  • Hepacivirus / metabolism*
  • Humans
  • Inhibitory Concentration 50
  • Liver / virology*
  • Mass Spectrometry / methods
  • Proteomics / methods
  • RNA, Small Interfering / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • Thiazoles / pharmacology
  • Virus Replication*

Substances

  • Antiviral Agents
  • RNA, Small Interfering
  • Thiazoles
  • 1-Phosphatidylinositol 4-Kinase