Identification of HSP90 as a direct target of artemisinin for its anti-inflammatory activity via quantitative chemical proteomics

Org Biomol Chem. 2019 Jul 17;17(28):6854-6859. doi: 10.1039/c9ob01264h.

Abstract

The anti-malarial drug artemisinin (ART) possesses potent anti-inflammatory activity, yet its underlying mechanism of action has remained elusive. Here we employed quantitative chemical proteomics to in situ profile the cellular targets of ART and identified heat shock protein 90 (HSP90) as a direct target. Further study revealed that ART suppressed the production of nitric oxide (NO) in macrophages via inhibiting the interaction between HSP90 and inducible NO synthase (iNOS).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Artemisinins / chemistry
  • Artemisinins / pharmacology*
  • Cells, Cultured
  • HSP90 Heat-Shock Proteins / analysis
  • HSP90 Heat-Shock Proteins / antagonists & inhibitors*
  • In Situ Hybridization, Fluorescence
  • Mice
  • Proteomics*
  • RAW 264.7 Cells

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Artemisinins
  • HSP90 Heat-Shock Proteins