ABSTRACT Endothelin-1 (ET-1), the most potent vasoconstrictor yet identified, is a 21 amino acid peptide originally isolated from the culture medium of endothelial cells. This peptide mediates its biological responses by binding to specific cell surface receptors that are located on a number of tissues and cell lines. These receptors belong to the superfamily of seven transmembrane G protein-coupled receptors. Soon after the identification of ET-1, two other closely related peptides (ET-2 and ET-3) were also identified. Based on the different biological effects of these agonists, subtypes of ET receptors (ETA and ETB) have been identified, cloned and characterized. This review briefly explains the tissue localization, molecular cloning and regulation of these ET receptors.
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