Cloning and expression of a cDNA for the human prostacyclin receptor

FEBS Letters

Negishi, Manabu²  Ichikawa, Atsushi²  Sugimoto, Yukihiko²  Katsuyama, Masato²  Irie, Atsushi²  Namba, Tsunehisa¹  Narumiya, Shuh¹ 

[1] Department of Pharmacology, Faculty of Medicine, Kyoto University, Kyoto 606, Japan;Department of Physiological Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Yoshida, Sakyo-Ku, Kyoto 606, Japan

关键词: Prostaglandin;    Prostacyclin;    Prostanoid receptor;    Signal transduction;   

DOI  :  10.1016/0014-5793(94)00355-6

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

A functional cDNA for the human prostacyclin receptor was isolated from a cDNA library of CMK cells, a human megakaryocytic leukaemia cell line. The cDNA encodes a protein consisting of 386 amino acid residues with seven putative transmembrane domains and a deduced molecular weight of 40,956. [³H]Iloprost specifically bound to the membrane of CHO cells stably expressing the cDNA with a Kd of 3.3 nM. This binding was displaced by unlabelled prostanoids in the order of iloprost = cicaprost ⪢ carbacyclin ⪢ prostaglandin E₁ (PGE₁) > STA₂. PGE₂, PGD₂ and PGF_2α did not inhibit it. Iloprost in a concentration-dependent manner increased the cAMP level and generated inositol trisphosphate in these cells, indicating that this human receptor can couple to multiple signal transduction pathways.

【 授权许可】

Unknown