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Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides.

Jiraborrirak CharoenpattarapreedaYaw Sing TanJessica IegreStephen J WalshElaine FowlerRohan S EapenYuteng WuHannah F SoreChandra Shekhar VermaLaura S ItzhakiDavid R Spring
Published in: Chemical communications (Cambridge, England) (2019)
Herein, we describe the development of a novel staple with an electrophilic warhead to enable the generation of stapled peptide covalent inhibitors of the p53-MDM2 protein-protein interaction (PPI). The peptide developed showed complete and selective covalent binding resulting in potent inhibition of p53-MDM2 PPI.
Keyphrases
  • protein protein
  • small molecule
  • cancer therapy
  • amino acid
  • dna binding
  • drug delivery