Discovery of treatment for nerve agents targeting a new metabolic pathway

Arch Toxicol. 2020 Sep;94(9):3249-3264. doi: 10.1007/s00204-020-02820-4. Epub 2020 Jul 27.

Abstract

The inhibition of acetylcholinesterase is regarded as the primary toxic mechanism of action for chemical warfare agents. Recently, there have been numerous reports suggesting that metabolic processes could significantly contribute to toxicity. As such, we applied a multi-omics pipeline to generate a detailed cascade of molecular events temporally occurring in guinea pigs exposed to VX. Proteomic and metabolomic profiling resulted in the identification of several enzymes and metabolic precursors involved in glycolysis and the TCA cycle. All lines of experimental evidence indicated that there was a blockade of the TCA cycle at isocitrate dehydrogenase 2, which converts isocitrate to α-ketoglutarate. Using a primary beating cardiomyocyte cell model, we were able to determine that the supplementation of α-ketoglutarate subsequently rescued cells from the acute effects of VX poisoning. This study highlights the broad impacts that VX has and how understanding these mechanisms could result in new therapeutics such as α-ketoglutarate.

Keywords: Cardiomyocytes; Glycolysis; Metabolomics; Proteomics; VX poisoning; a-Ketoglutarate.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Acetylcholinesterase / metabolism*
  • Animals
  • Chemical Warfare Agents / toxicity
  • Guinea Pigs
  • Metabolic Networks and Pathways
  • Metabolomics
  • Nerve Agents / toxicity*
  • Poisoning / drug therapy*
  • Poisoning / metabolism
  • Proteome / drug effects*
  • Proteomics

Substances

  • Chemical Warfare Agents
  • Nerve Agents
  • Proteome
  • Acetylcholinesterase