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Updated: Jan 23, 2026

Synthesis of Information-bearing Peptoids and their Sequence-directed Dynamic Covalent Self-assembly
Published on: February 6, 2020
Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides
Jiraborrirak Charoenpattarapreeda1, Yaw Sing Tan2, Jessica Iegre1
1Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, UK. spring@ch.cam.ac.uk.
Abstract:
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.
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