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. 2019 Jul 14;55(55):7914-7917.
doi: 10.1039/c9cc04022f. Epub 2019 Jun 21.

Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides

Jiraborrirak Charoenpattarapreeda  1 , Yaw Sing Tan  2 , Jessica Iegre  1 , Stephen J Walsh  1 , Elaine Fowler  1 , Rohan S Eapen  3 , Yuteng Wu  1 , Hannah F Sore  1 , Chandra S Verma  4 , Laura Itzhaki  3 , David R Spring  1
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Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides

Jiraborrirak Charoenpattarapreeda et al. Chem Commun (Camb). .

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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