Communications Chemistry (Jun 2022)

Controlling oncogenic KRAS signaling pathways with a Palladium-responsive peptide

  • Soraya Learte-Aymamí,
  • Pau Martin-Malpartida,
  • Lorena Roldán-Martín,
  • Giuseppe Sciortino,
  • José R. Couceiro,
  • Jean-Didier Maréchal,
  • Maria J. Macias,
  • José L. Mascareñas,
  • M. Eugenio Vázquez

DOI
https://doi.org/10.1038/s42004-022-00691-7
Journal volume & issue
Vol. 5, no. 1
pp. 1 – 9

Abstract

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Mutations to oncogenic protein KRAS are responsible for some of the deadliest cancers, and KRAS is thus a key target for new antitumour agents. Here, a short bis-histidine peptide derived from the αH helix of the cofactor SOS1 is designed and shown to reversibly bind to KRAS with high affinity upon coordination to Pd(II), inhibiting KRAS-activated pathways in live cells.