Bioorganic and Medicinal Chemistry Letters p. 373 - 378 (1998)
Update date:2022-08-04
Topics:
Lynas, John F.
Harriott, Patrick
Healy, Adrienne
McKervey, M. Anthony
Walker, Brian
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.
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