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

Guolin Wu Bao Cheng Hui Qian Shengming Ma Qin Chen

Published in: Organic & biomolecular chemistry (2020)

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).

Keyphrases

heat shock protein
nitric oxide
heat shock
plasmodium falciparum
hiv infected
mass spectrometry
antiretroviral therapy
high resolution
nitric oxide synthase
label free
signaling pathway
hydrogen peroxide
single cell
oxidative stress
drug induced