Journal
CELLULAR AND MOLECULAR LIFE SCIENCES
Volume 68, Issue 2, Pages 195-203Publisher
SPRINGER BASEL AG
DOI: 10.1007/s00018-010-0518-0
Keywords
Endothelin; Endothelin-converting enzymes; Endothelin receptor; Endothelin signal; Pathophysiology
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Funding
- Merck Company Foundation
- National Institutes of Health [NIH: DK080640]
- Japan Society for the Promotion of Science [JSPS: S-10707]
- Banyu fellowship awards in cardiovascular medicine
- Banyu Fellowship in Cardiovascular Medicine
- NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES [R01DK080640] Funding Source: NIH RePORTER
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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.
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