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The Endothelin Receptor

The Endothelin Receptor Endothelin-1 (ET-1), a potent vasoconstrictor, was discovered in 1988. Its role in cardiovascular and pulmonary diseases has been widely investigated. Recent investigations of the pleiotropic actions of the endothelins, such as mitogenesis and inhibition of apoptosis, provide evidence for their potential role in cancer. Available data suggest that ET-1 plays a significant role in the growth and progression of such neoplasms as prostate and ovarian cancer, melanoma, bone malignancies, and other tumors. Development of endothelin receptor antagonists has allowed a better understanding of the role of ET-1 in cancer pathogenesis, and provided the possibility of therapeutic intervention. ET-1 exerts its action via the endothelin receptors A (ETA) and B (ETB); however, it appears that most of the mitogenic activity of ET-1 is mediated through the ETa receptor. Preliminary data from clinical trials investigating the ETa receptor antagonist, atrasentan, in patients with prostate cancer, were encouraging. The role of the endothelin axis in other malignancies is discussed as well. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png American Journal of Cancer Springer Journals

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Publisher
Springer Journals
Copyright
Copyright © 2002 by Adis International Limited
Subject
Pharmacy; Pharmacy
ISSN
1175-6357
DOI
10.2165/00024669-200201020-00001
Publisher site
See Article on Publisher Site

Abstract

Endothelin-1 (ET-1), a potent vasoconstrictor, was discovered in 1988. Its role in cardiovascular and pulmonary diseases has been widely investigated. Recent investigations of the pleiotropic actions of the endothelins, such as mitogenesis and inhibition of apoptosis, provide evidence for their potential role in cancer. Available data suggest that ET-1 plays a significant role in the growth and progression of such neoplasms as prostate and ovarian cancer, melanoma, bone malignancies, and other tumors. Development of endothelin receptor antagonists has allowed a better understanding of the role of ET-1 in cancer pathogenesis, and provided the possibility of therapeutic intervention. ET-1 exerts its action via the endothelin receptors A (ETA) and B (ETB); however, it appears that most of the mitogenic activity of ET-1 is mediated through the ETa receptor. Preliminary data from clinical trials investigating the ETa receptor antagonist, atrasentan, in patients with prostate cancer, were encouraging. The role of the endothelin axis in other malignancies is discussed as well.

Journal

American Journal of CancerSpringer Journals

Published: Aug 9, 2012

References