Endothelin.
Endothelin-1 is the most potent vasoconstrictor agent currently identified, and it was originally isolated and characterized from the culture media of aortic endothelial cells. Two other isoforms, termed endothelin-2 and endothelin-3, were subsequently identified, along with structural homologues isolated from the venom of Actractapis engaddensis known as the sarafotoxins. In this review, we will discuss the basic science of endothelins, endothelin-converting enzymes, and endothelin receptors. Only concise background information pertinent to clinical physician is provided. Next we will describe the pathophysiological roles of endothelin-1 in pulmonary arterial hypertension, heart failure, systemic hypertension, and female malignancies, with emphasis on ovarian cancer. The potential intervention with pharmacological therapeutics will be succinctly summarized to highlight the exciting pre-clinical and clinical studies within the endothelin field. Of note is the rapid development of selective endothelin receptor antagonists, which has led to an explosion of research in the field.
Kawanabe
Yoshifumi
Y
Department of Neurosurgery, Otsu Municipal Hospital, Shiga, Japan. bwh5255725@yahoo.co.jp
Nauli
Surya M
SM
D016282:Aspartic Acid Endopeptidases / Q000378:metabolism; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000378:metabolism / Q000503:physiopathology; D002986:Clinical Trials as Topic; D065128:Endothelin Receptor Antagonists; D000072396:Endothelin-Converting Enzymes; D016232:Endothelins / Q000737:chemistry / Q000502:physiology; D065627:Familial Primary Pulmonary Hypertension; D005260:Female; D006333:Heart Failure / Q000378:metabolism / Q000503:physiopathology; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy / Q000378:metabolism / Q000503:physiopathology; D008666:Metalloendopeptidases / Q000378:metabolism; D010051:Ovarian Neoplasms / Q000378:metabolism / Q000503:physiopathology; D017466:Receptors, Endothelin / Q000502:physiology; D014661:Vasoconstriction
D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D017466:Receptors, Endothelin; D016282:Aspartic Acid Endopeptidases; D008666:Metalloendopeptidases; D000072396:Endothelin-Converting Enzymes