A Small-Molecule Oligosaccharyltransferase Inhibitor with Pan-flaviviral Activity

Cell Rep. 2017 Dec 12;21(11):3032-3039. doi: 10.1016/j.celrep.2017.11.054.

Abstract

The mosquito-borne flaviviruses include important human pathogens such as dengue, Zika, West Nile, and yellow fever viruses, which pose a serious threat for global health. Recent genetic screens identified endoplasmic reticulum (ER)-membrane multiprotein complexes, including the oligosaccharyltransferase (OST) complex, as critical flavivirus host factors. Here, we show that a chemical modulator of the OST complex termed NGI-1 has promising antiviral activity against flavivirus infections. We demonstrate that NGI-1 blocks viral RNA replication and that antiviral activity does not depend on inhibition of the N-glycosylation function of the OST. Viral mutants adapted to replicate in cells deficient of the OST complex showed resistance to NGI-1 treatment, reinforcing the on-target activity of NGI-1. Lastly, we show that NGI-1 also has strong antiviral activity in primary and disease-relevant cell types. This study provides an example for advancing from the identification of genetic determinants of infection to a host-directed antiviral compound with broad activity against flaviviruses.

Keywords: West Nile virus; Zika virus; antiviral; dengue virus; flaviviruses; host-directed therapy; oligosaccharyltransferase; yellow fever virus.

MeSH terms

  • Antiviral Agents / pharmacology*
  • Benzamides / pharmacology*
  • Dengue Virus / drug effects*
  • Dengue Virus / genetics
  • Dengue Virus / growth & development
  • Gene Expression
  • Gene Expression Regulation
  • Genes, Reporter
  • HEK293 Cells
  • Hexosyltransferases / antagonists & inhibitors
  • Hexosyltransferases / deficiency
  • Hexosyltransferases / genetics*
  • Host-Pathogen Interactions / drug effects*
  • Humans
  • Luciferases
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / deficiency
  • Membrane Proteins / genetics*
  • Microbial Sensitivity Tests
  • Signal Transduction
  • Sulfonamides / pharmacology*
  • Virus Replication / drug effects*
  • West Nile virus / drug effects
  • West Nile virus / genetics
  • West Nile virus / growth & development
  • Yellow fever virus / drug effects
  • Yellow fever virus / genetics
  • Yellow fever virus / growth & development
  • Zika Virus / drug effects
  • Zika Virus / genetics
  • Zika Virus / growth & development

Substances

  • Antiviral Agents
  • Benzamides
  • CID2519269
  • Membrane Proteins
  • Sulfonamides
  • Luciferases
  • Hexosyltransferases
  • STT3A protein, human
  • STT3B protein, human