Discovery of cisplatin-binding proteins by competitive cysteinome profiling

RSC Chem Biol. 2023 Aug 1;4(9):670-674. doi: 10.1039/d3cb00042g. eCollection 2023 Aug 30.

Abstract

Cisplatin is a widely used cancer metallodrug that induces cytotoxicity by targeting DNA and chelating cysteines in proteins. Here we applied a competitive activity-based protein profiling strategy to identify cisplatin-binding cysteines in cancer proteomes. A novel cisplatin target, MetAP1, was identified and functionally validated to contribute to cisplatin's cytotoxicity.