2. Academic Validation
  3. 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

  • 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

Affiliation

  • 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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