Reversible, slow, tight-binding inhibition of human leukocyte elastase.
CBz-Ala-Ala-Pro-ambo-Val-CF3 (1) was synthesized. The compound inhibits human Leucocyte elastase with Ki = 1.0 x 10(-9) M. This inhibitor is reversible, slow, tight-binding inhibitor with k on = 2 x 10(4) M-1 s-1 k off = 1.9 x 10(-5) s-1. For the solubilization of elastin by HLE by 1 I.C. 50 = 110 nM. This inhibitor is the most effective aldehyde or ketone inhibitor of a serine proteinase yet described.
D001667:Binding, Competitive; D006801:Humans; D007700:Kinetics; D007962:Leukocytes / Q000201:enzymology*; D009842:Oligopeptides / Q000494:pharmacology*; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors / Q000097:blood*
D009842:Oligopeptides; C052802:benzyloxycarbonylalanyl-alanyl-prolyl-valine-trifluoromethyl ketone; D010196:Pancreatic Elastase