Abramovitz M, Boie Y, Nguyen T, Rushmore T H, Bayne M A, Metters K M, Slipetz D M, Grygorczyk R
Department of Molecular Biology, Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Quebec, Canada.
J Biol Chem. 1994 Jan 28;269(4):2632-6.
A cDNA clone coding for a functional human prostanoid FP receptor has been isolated from a uterus cDNA library. The human FP receptor consists of 359 amino acid residues with a predicted molecular mass of 40,060, and has the seven putative transmembrane domains characteristic of G-protein-coupled receptors. Challenge of Xenopus oocytes expressing the FP receptor with 10 nM of either prostaglandin (PG) F2 alpha or the selective FP-receptor agonist fluprostenol resulted in an elevation in intracellular Ca2+. Radioreceptor binding studies using membranes prepared from mammalian COS cells transfected with the FP receptor cDNA showed that the rank order of potency for prostaglandins and prostaglandin analogs in competition for [3H]PGF2 alpha specific binding sites was as predicted for the FP receptor, with PGF2 alpha approximately fluprostenol > PGD2 > PGE2 > U46619 > iloprost. In summary, we have cloned the human prostanoid FP receptor which is functionally coupled to the Ca2+ signalling pathway.
已从子宫cDNA文库中分离出编码功能性人前列腺素FP受体的cDNA克隆。人FP受体由359个氨基酸残基组成,预测分子量为40,060,具有G蛋白偶联受体特有的七个推定跨膜结构域。用10 nM前列腺素(PG)F2α或选择性FP受体激动剂氟前列醇刺激表达FP受体的非洲爪蟾卵母细胞,导致细胞内Ca2+升高。使用从转染了FP受体cDNA的哺乳动物COS细胞制备的膜进行的放射受体结合研究表明,前列腺素和前列腺素类似物竞争[3H]PGF2α特异性结合位点的效力顺序与FP受体预测的一致,即PGF2α≈氟前列醇>PGD2>PGE2>U46619>伊洛前列素。总之,我们克隆了与人Ca2+信号通路功能偶联的人前列腺素FP受体。