Review

Cellular and Molecular Life Sciences

, Volume 68, Issue 2, pp 195-203

First online:

Endothelin

  • Yoshifumi KawanabeAffiliated withDepartment of Neurosurgery, Otsu Municipal Hospital Email author 
  • , Surya M. NauliAffiliated withDepartment of Pharmacology, The University of Toledo

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Abstract

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.

Keywords

Endothelin Endothelin-converting enzymes Endothelin receptor Endothelin signal Pathophysiology