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Molecular Biology of the Endothelin Receptors

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Endothelin

Part of the book series: Contemporary Biomedicine ((CB))

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Abstract

Since the initial discovery of the endothelium-derived constricting factor, endothelin-1 (ET-1) (1) and determination of its peptidic nature (2), elucidation of the molecular details of the endothelin (ET) system has progressed rapidly via a multidisciplinary approach using the tools of biochemistry, chemistry, pharmacology, and molecular biology. Milestones in the development of this area include the isolation (3) and three-dimensional structure determination (4,5) of ET-1 and related peptides, the pharmacological characterization and molecular cloning of ET-receptor subtypes (6,7) which was followed by the development of potent peptide and nonpeptide antagonists (8–13), and, more recently, the disruption of the genes encoding ET-1, ET-3, and the ETB receptor subtype (14–16). Thus elucidation of the intricacies of the endothelin system has been the product of a truly molecular approach to pharmacology.

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Lee, J.A., Ohlstein, E.H., Peishoff, C.E., Elliott, J.D. (1998). Molecular Biology of the Endothelin Receptors. In: Highsmith, R.F. (eds) Endothelin. Contemporary Biomedicine. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-4757-2783-8_2

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