A new class of inhibitors of human leucocyte elastase.
Studies of the inhibition of elastases at a molecular level have resulted in the identification of protected dipeptides which are reversible and highly specific inhibitors of human leucocyte elastase (HLE). These have been further developed by increasing their hydrophilicity and potency to give a new family of elastase inhibitors, typically N alpha-(1-adamantanesulphonyl)-N epsilon-(4-carboxybenzoyl)-L-lysyl-L-alanyl-L-valinal. These compounds are active in pharmacological models designed to detect compounds of potential therapeutic value in the treatment of emphysema.
D000218:Adamantane / Q000031:analogs & derivatives* / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D006224:Cricetinae; D004646:Emphysema / Q000188:drug therapy; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007962:Leukocytes / Q000201:enzymology*; D008168:Lung / Q000187:drug effects; D008958:Models, Molecular; D009842:Oligopeptides; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D013379:Substrate Specificity
D004791:Enzyme Inhibitors; D009842:Oligopeptides; C045401:N(alpha)-(1-adamantanesulfonyl)-N(epsilon)-(4-carboxybenzoyl)lysyl-alanyl-valinal; D010196:Pancreatic Elastase; D000218:Adamantane