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

  • J Med Chem. 2004 Apr 8;47(8):1889-92. doi: 10.1021/jm049938j.
Ozlem Doğan Ekici  1 ,  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
Affiliations
  • 1. School of Chemistry and Biochemistry and the Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
PMID: 15055989 DOI: 10.1021/jm049938j
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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