Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl alpha-keto aldehydes (glyoxals).
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.
Lynas
J F
JF
Centre for Peptide and Protein Engineering, School of Biology and Biochemistry, Queen's University Belfast, Northern Ireland, U.K.
Harriott
P
P
Healy
A
A
McKervey
M A
MA
Walker
B
B
D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D003546:Cysteine Endopeptidases / Q000097:blood / Q000187:drug effects*; D006037:Glyoxal / Q000494:pharmacology*; D006801:Humans; D009097:Multienzyme Complexes / Q000097:blood / Q000187:drug effects*; D046988:Proteasome Endopeptidase Complex; D014361:Trypsin Inhibitors / Q000494:pharmacology*
D009097:Multienzyme Complexes; D014361:Trypsin Inhibitors; D006037:Glyoxal; D002918:Chymotrypsin; D003546:Cysteine Endopeptidases; D046988:Proteasome Endopeptidase Complex