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Endothelin Kawanabe Y; Nauli SMCell Mol Life Sci 2011[Jan]; 68 (2): 195-203Endothelin-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.|*Aspartic Acid Endopeptidases/metabolism[MESH]|*Endothelins/chemistry/physiology[MESH]|*Hypertension, Pulmonary/drug therapy/metabolism/physiopathology[MESH]|*Metalloendopeptidases/metabolism[MESH]|*Receptors, Endothelin/physiology[MESH]|Cardiovascular Diseases/drug therapy/metabolism/physiopathology[MESH]|Clinical Trials as Topic[MESH]|Endothelin Receptor Antagonists[MESH]|Endothelin-Converting Enzymes[MESH]|Familial Primary Pulmonary Hypertension[MESH]|Female[MESH]|Heart Failure/metabolism/physiopathology[MESH]|Humans[MESH]|Ovarian Neoplasms/metabolism/physiopathology[MESH]|Vasoconstriction[MESH] |
