4.7 Article

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

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 47, Issue 8, Pages 1889-1892

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm049938j

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Funding

  1. NIAID NIH HHS [AI 053247] Funding Source: Medline
  2. NIGMS NIH HHS [GM 61964] Funding Source: Medline

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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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