Literature DB >> 15055989

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

Ozlem Doğan Ekici1, 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.   

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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Year:  2004        PMID： 15055989     DOI： 10.1021/jm049938j

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  18 in total

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