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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YST and CSV would like to thank A*STAR (IAF-PP H17/01/a0/010) for support.