Identification of small molecules with type I interferon inducing properties by high-throughput screening

PLoS One. 2012;7(11):e49049. doi: 10.1371/journal.pone.0049049. Epub 2012 Nov 7.

Abstract

The continuous emergence of virus that are resistant to current anti-viral drugs, combined with the introduction of new viral pathogens for which no therapeutics are available, creates an urgent need for the development of novel broad spectrum antivirals. Type I interferon (IFN) can, by modulating the cellular expression profile, stimulate a non-specific antiviral state. The antiviral and adjuvant properties of IFN have been extensively demonstrated; however, its clinical application has been so far limited. We have developed a human cell-based assay that monitors IFN-β production for use in a high throughput screen. Using this assay we screened 94,398 small molecules and identified 18 compounds with IFN-inducing properties. Among these, 3 small molecules (C3, E51 and L56) showed activity not only in human but also in murine and canine derived cells. We further characterized C3 and showed that this molecule is capable of stimulating an anti-viral state in human-derived lung epithelial cells. Furthermore, the IFN-induction by C3 is not diminished by the presence of influenza A virus NS1 protein or hepatitis C virus NS3/4A protease, which make this molecule an interesting candidate for the development of a new type of broad-spectrum antiviral. In addition, the IFN-inducing properties of C3 also suggest its potential use as vaccine adjuvant.

Publication types

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

MeSH terms

  • Animals
  • Antiviral Agents / pharmacology*
  • Cell Line
  • Dogs
  • Epithelial Cells / drug effects
  • Epithelial Cells / metabolism
  • HEK293 Cells
  • High-Throughput Screening Assays / methods*
  • Humans
  • Interferon Type I / metabolism*
  • Lung / drug effects
  • Lung / metabolism
  • Mice
  • Small Molecule Libraries / pharmacology*
  • Vero Cells
  • Viral Nonstructural Proteins / metabolism

Substances

  • Antiviral Agents
  • INS1 protein, influenza virus
  • Interferon Type I
  • NS3 protein, hepatitis C virus
  • Small Molecule Libraries
  • Viral Nonstructural Proteins