Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides

Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides
Title:
Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides
Other Titles:
Chemical Communications
Keywords:
Publication Date:
17 June 2019
Citation:
Chem. Commun., 2019,55, 7914-7917
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.
License type:
PublisherCopyrights
Funding Info:
YST and CSV would like to thank A*STAR (IAF-PP H17/01/a0/010) for support.
Description:
ISSN:
1359-7345
1364-548X
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