Cloning and expression of human endothelin-1 receptor cDNA

• Published in: FEBS letters Vol. 287; no. 1; pp. 23 - 26
• Main Authors: Hosoda, Kiminori, Nakao, Kazuwa, Hiroshi-Arai, Suga, Shin-ichi, Ogawa, Yoshihiro, Mukoyama, Masashi, Shirakami, Gotaro, Saito, Yoshihiko, Nakanishi, Shigetada, Imura, Hiroo
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 05.08.1991; Elsevier
• Subjects: 50% inhibitory concentration; Amino Acid Sequence; Animals; Base Sequence; Binding, Competitive; Biological and medical sciences; Blotting, Northern; cDNA cloning: G-protein; Cell Line; Cell receptors; Cell structures and functions; Cloning, Molecular; DNA - genetics; Electrophysiology; endothelin; Endothelin (ET); Endothelins - metabolism; Endothelins - pharmacology; Fundamental and applied biological sciences. Psychology; Gene Expression; genes; Humans; IC50; Miscellaneous; Molecular and cellular biology; Molecular Sequence Data; Northern blot hybridization analysis; Oocytes - physiology; Placenta - chemistry; Receptor; Receptors, Cell Surface - genetics; Receptors, Cell Surface - metabolism; Receptors, Endothelin; RNA, Messenger - analysis; RNA, Messenger - metabolism; Transfection; Xenopus; Xenopus oocyte; IC 50; Receptor; Northern blot hybridization analysis; cDNA cloning: G-protein; Endothelin (ET); Xenopus oocyte; ET; Human; Northern blotting; Membrane receptor; Binding capacity; Endothelin; Electrophysiology; Primary structure; Molecular cloning
• ISSN: 0014-5793; 1873-3468
• DOI: 10.1016/0014-5793(91)80007-P

We isolated a human endothelin-1 (ET-1) receptor cDNA from a human placenta cDNA library. The cDNA encodes a 427-amino acid protein with seven putative transmembrane domains. The rank order of the binding to the receptor expressed in COS-7 cells was: ET-1 ⩾ ET-2 ⪢ ET-3. The receptor expressed in Xenopus oocytes showed a potent electrophysiological response to 1 × 10 −7 M ET-1 under voltage clamp at −60 mV, while a much weaker response was produced by 1 × 10 −7 M ET-3. Northern blot analysis with RNA from human tissues revealed a single band with a size of 4.3 kb in a wide variety of human tissues, especially highly in the blood vessel.