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

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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… Click to show full 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.

Keywords: covalent inhibitors; targeted covalent; electrophile bearing; mdm2 using; using electrophile; inhibitors mdm2

Journal Title: Chemical communications
Year Published: 2019

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