Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides†
Jiraborrirak
Charoenpattarapreeda, 
a
Jessica
Iegre,
a
Stephen J.
Walsh,
a
Elaine
Fowler,
a
Rohan S.
Eapen,
c
Hannah F.
Sore,
a
Chandra S.
Verma,
bde
Laura
Itzhaki
c
and
David R.
Spring
*a
a
Jessica
Iegre,
a
Stephen J.
Walsh,
a
Elaine
Fowler,
a
Rohan S.
Eapen,
c
Hannah F.
Sore,
a
Chandra S.
Verma,
bde
Laura
Itzhaki
c
and
David R.
Spring
*a
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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