Utility of endothelin-converting enzyme inhibitors for the treatment of cardiovascular diseases.
Endothelins (ETs) are a family of potent peptidic vasoconstrictors that have been implicated in the pathogenesis of many cardiovascular disorders such as hypertension, myocardial infarction, congestive heart failure, atherosclerosis and restenosis. Suppression of the production of these peptides by inhibitors of endothelin-converting enzyme-1 (ECE-1), which is involved in the final step of post-translational processing of ETs, may therefore have beneficial effects for the treatment of these disorders. A number of non-selective and selective ECE-1 inhibitors have been identified, and this article reviews the pharmacological effects of these agents in animal models of cardiovascular diseases and presents available clinical data.
Novartis Institute for Biomedical Research, Novartis Pharmaceuticals Corporation, Building 435, Room 2191, 1 Health Plaza, East Hanover, NJ 07936, USA. arco.jeng@pharma.novartis.com
Arco Y
AY
Jeng
D000818:Animals; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000201:enzymology; D002986:Clinical Trials as Topic; D000072396:Endothelin-Converting Enzymes; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D008666:Metalloendopeptidases; D015394:Molecular Structure; D016896:Treatment Outcome
D004791:Enzyme Inhibitors; D016282:Aspartic Acid Endopeptidases; D008666:Metalloendopeptidases; C000606923:ECE1 protein, human; D000072396:Endothelin-Converting Enzymes