1. Academic Validation
  2. A masked zinger to block GPX4

A masked zinger to block GPX4

  • Nat Chem Biol. 2020 May;16(5):482-483. doi: 10.1038/s41589-020-0511-3.
Stefan G Kathman 1 Benjamin F Cravatt 2
Affiliations

Affiliations

  • 1 Department of Chemistry, The Scripps Research Institute, La Jolla, CA, USA. [email protected].
  • 2 Department of Chemistry, The Scripps Research Institute, La Jolla, CA, USA. [email protected].
Abstract

Ferroptosis induced by GPX4 inhibition offers promise for killing drug-resistant Cancer cells, yet current GPX4 inhibitors lack selectivity. The discovery of masked nitrile oxide electrophiles as selective prodrug inhibitors of GPX4 points to an attractive path for chemically inducing Ferroptosis.

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