A New Staple: Peptide-Targeted Covalent Inhibitors.
In this issue of Cell Chemical Biology, Huhn et al. (2016) unveil a clever strategy for selectively and irreversibly inhibiting an anti-apoptotic protein, BFL-1. The authors describe stapled peptides bearing carefully placed electrophiles that target a unique cysteine residue in BFL-1 via covalent modification, thus representing an extension of the stapled peptide concept into the covalent inhibitor space.
Oncology Development, AbbVie, Inc., 1 Waukegan Road, North Chicago, IL 60064, USA. Electronic address: joel.leverson@abbvie.com.
Joel D
JD
Leverson
D017209:Apoptosis; D003545:Cysteine; D008747:Methylcellulose; D010455:Peptides; D011506:Proteins
D010455:Peptides; D011506:Proteins; D008747:Methylcellulose; D003545:Cysteine