Cloning and expression of a cDNA encoding an endothelin receptor

Abstract

Endothelins are a newly described peptide family consisting of three peptides (ET-1, ET-2 and ET-3) which are the most potent vasoconstrictive peptides known. They are crucial in the regulation of vascular smooth muscle tone. The diverse functions of endothelins are thought to be mediated by interaction with many different receptors coupled to the inositol phosphate/calcium ion messenger pathway. However, because of the structural resemblance of the three peptides, the presence and nature of multiple endothelin receptors remain to be elucidated. We report here the cloning of a complementary DNA encoding a bovine endothelin receptor, which has a transmembrane topology similar to that of other G protein-coupled receptors and shows specific binding, with the highest selectivity to ET-1 in animal cells transfected with the cloned cDNA. This receptor messenger RNA is widely distributed in the central nervous system and peripheral tissues, particularly in the heart and lung. Our results support the view that there are other receptor subtypes.

Drug Treatment of Hypertension: Focus on Vascular Health

“…ET-1 acts through ET A and ET B receptors. ET A receptors are found on vascular smooth muscle cells where they promote vasoconstriction, whilst ET B receptors are found on both endothelial and smooth muscle cells 17,18 . Activation of smooth muscle ET B receptors promotes vasoconstriction, whereas endothelial cell ET B receptors induce vasodilatation through production of substances such as NO and PGI 2 18-20 .…”

MEK1/2 inhibition attenuates vascular ETA and ETB receptor alterations after cerebral ischaemia

“…Two endothelin receptors have been identified in mammals, the endothelin type A (ET A ) and type B (ET B ) receptors (Arai et al 1990;Sakurai et al 1990). …”

Ultraviolet B irradiation increases endothelin‐1 and endothelin receptor expression in cultured human keratinocytes

“…ET consists of three isopeptides, termed ET-1, ET-2 and ET-3 (ETs), while their receptors are classified, both pharmacologically and molecularly, into ET A and ETB subtypes [2][3][4][5]. The ET A receptor has different affinities for the three ET isoforms in the order of ET-I>ET-2>>ET-3.…”