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

Article abstract of DOI:10.1016/S0960-894X(98)00030-4

A series of peptidyl α-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 K(i) values of approximately 3.0 nM. These are among the lowest values so far reported for (tri)peptide-based aldehyde-releated inhibitors.