The orphan GPCR GPR87 was deorphanized and shown to be a lysophosphatidic acid receptor
The orphan GPCR GPR87 was deorphanized and shown to be a lysophosphatidic acid receptor
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DOI：
10.1016/j.bbrc.2007.09.063
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发表时间：
2007-11-23
影响因子：
3.1
通讯作者：
Fujita, Norihisa
中科院分区：
文献类型：
--
作者：
Tabata, Ken-Ichi;Baba, Kiyoshi;Fujita, Norihisa
在稳定表达GPR87与G（16 α）蛋白融合的CHO细胞中，溶血磷脂酸（LPA）以高亲和力的方式引起细胞内Ca2+的增加。Ca2+的增加被LPA受体拮抗剂可逆地阻断，并被gpr87特异性sirna预处理的细胞抑制。ClustalW分析显示GPR87比LPA受体更接近P2Y和P2Y-rektted受体。然而，没有核链及其衍生物激活GPR87。人类gpr87位于包含p2y的染色体簇中的3q25染色体上（12,13,14）。RT-PCR分析显示，GPR87在小鼠胎盘、卵巢、睾丸、前列腺、脑、骨骼肌中均有表达。GPR87- lpa复合物的3D模型表明，该配体与GPR87的r115和K296相互作用，在P2Y受体中具有良好的保守性。这些结果表明GPR87是由P2Y受体的共同祖先进化而来的LPA受体。(C) 2007爱思唯尔公司版权所有。
In CHO cells stably expressing the GPR87 fused with a G(16 alpha) protein, lysophosphatidic acid (LPA) evoked an intracellular Ca2+ increase in a high affinity manner. The Ca2+ increase was reversibly blocked by the LPA receptor antagonists and inhibited by pretreatment of the cells with GPR87-specific siRNAs. GPR87 was shown to be closer to the P2Y and P2Y-rektted receptors than LPA receptors by ClustalW analyses. However, none of nucleoticles and their derivatives activated GPR87. The human gpr87 is located on the chromosome 3q25 in a cluster containing p2y(12,13,14). RT-PCR analysis showed that the mouse GPR87 was expressed in placenta, ovary, testis, prostate, brain, and skeletal muscle. The 3D model of GPR87-LPA complex indicated that the ligand interacted with R 115 and K296 of GPR87, which are well conserved in the P2Y receptors. These results suggest that the GPR87 is a LPA receptor which evolved from a common ancestor of P2Y receptors. (C) 2007 Elsevier Inc. All rights reserved.