A pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction

Nature. 2021 Oct;598(7881):504-509. doi: 10.1038/s41586-021-03990-6. Epub 2021 Oct 6.

Abstract

Dengue virus causes approximately 96 million symptomatic infections annually, manifesting as dengue fever or occasionally as severe dengue1,2. There are no antiviral agents available to prevent or treat dengue. Here, we describe a highly potent dengue virus inhibitor (JNJ-A07) that exerts nanomolar to picomolar activity against a panel of 21 clinical isolates that represent the natural genetic diversity of known genotypes and serotypes. The molecule has a high barrier to resistance and prevents the formation of the viral replication complex by blocking the interaction between two viral proteins (NS3 and NS4B), thus revealing a previously undescribed mechanism of antiviral action. JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models. Delaying start of treatment until peak viraemia results in a rapid and significant reduction in viral load. An analogue is currently in further development.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / pharmacokinetics
  • Antiviral Agents / pharmacology*
  • Antiviral Agents / therapeutic use
  • Dengue / drug therapy
  • Dengue / virology*
  • Dengue Virus / classification*
  • Dengue Virus / drug effects*
  • Dengue Virus / genetics
  • Dengue Virus / metabolism
  • Disease Models, Animal
  • Female
  • Male
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / metabolism*
  • Mice
  • RNA Helicases / antagonists & inhibitors
  • RNA Helicases / metabolism
  • Serine Endopeptidases / metabolism
  • Viral Load / drug effects
  • Viral Nonstructural Proteins / antagonists & inhibitors
  • Viral Nonstructural Proteins / metabolism*
  • Viremia / drug therapy
  • Viremia / virology
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • Membrane Proteins
  • NS3 protein, flavivirus
  • NS4B protein, Dengue virus
  • Viral Nonstructural Proteins
  • Serine Endopeptidases
  • RNA Helicases