Benjamin F. Cravatt

Tryptoline stereoprobe elaboration identifies inhibitors of the GRPEL1–HSPA9 complex

Abstract Activity-based protein profiling has identified hundreds of human proteins from diverse classes that react at cysteine residues with stereochemically defined electrophilic compounds (stereoprobes). The structure–activity relationships underlying these stereoprobe–protein...

An enantioselective covalent inhibitor of BAX confers cytoprotection in vivo

No therapies directly block apoptosis in tissue injury or the many diseases driven by cell loss. The BCL-2 family protein BAX is a central mediator of this pathway and C126 resides within a key regulatory region where physiologic or pharmacologic ligands can activate or inhibit i...