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.


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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chymotrypsin / antagonists & inhibitors*
  • Cysteine Endopeptidases / blood
  • Cysteine Endopeptidases / drug effects*
  • Glyoxal / pharmacology*
  • Humans
  • Multienzyme Complexes / blood
  • Multienzyme Complexes / drug effects*
  • Proteasome Endopeptidase Complex
  • Trypsin Inhibitors / pharmacology*


  • Multienzyme Complexes
  • Trypsin Inhibitors
  • Glyoxal
  • Chymotrypsin
  • Cysteine Endopeptidases
  • Proteasome Endopeptidase Complex