Document Report Card

ID: ALA1149135

Journal: J Med Chem

Title: Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases.

Authors: Ekici OD, Götz MG, James KE, Li ZZ, Rukamp BJ, Asgian JL, Caffrey CR, Hansell E, Dvorák J, McKerrow JH, Potempa J, Travis J, Mikolajczyk J, Salvesen GS, Powers JC.

Abstract: Aza-peptide Michael acceptors are a new class of irreversible inhibitors that are highly potent and specific for clan CD cysteine proteases. The aza-Asp derivatives were specific for caspases, while aza-Asn derivatives were effective legumain inhibitors. Aza-Lys and aza-Orn derivatives were potent inhibitors of gingipain K and clostripain. Aza-peptide Michael acceptors showed no cross reactivity toward papain, cathepsin B, and calpain.

CiteXplore: 15055989

DOI: 10.1021/jm049938j