- Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases.
Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases.
Journal of medicinal chemistry (2004-04-02)
Ozlem Doğan Ekici, Marion G Götz, Karen Ellis James, Zhao Zhao Li, Brian J Rukamp, Juliana L Asgian, Conor R Caffrey, Elizabeth Hansell, Jan Dvorák, James H McKerrow, Jan Potempa, James Travis, Jowita Mikolajczyk, Guy S Salvesen, James C Powers
PMID15055989
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.
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