Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl alpha-keto aldehydes (glyoxals)

  • Bioorg Med Chem Lett. 1998 Feb 17;8(4):373-8. doi: 10.1016/s0960-894x(98)00030-4.
J F Lynas  1 ,  P Harriott ,  A Healy ,  M A McKervey ,  B Walker
Affiliations
  • 1. Centre for Peptide and Protein Engineering, School of Biology and Biochemistry, Queen's University Belfast, Northern Ireland, U.K.
PMID: 9871688 DOI: 10.1016/s0960-894x(98)00030-4
Abstract

A series of peptidyl alpha-keto aldehydes (glyoxals) have been synthesised as putative inhibitors of the chymotryptic-like activity of Proteasome. The most potent peptides, Cbz-Leu-Leu-Tyr-COCHO and Bz-Leu-Leu-Leu-COCHO, function as slow-binding reversible inhibitors, exhibiting final Ki values of approximately 3.0 nM. These are among the lowest values so far reported for (tri)peptide-based aldehyde-related inhibitors.

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