School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Kuopio, Finland.
Curr Top Med Chem. 2010;10(8):799-813. doi: 10.2174/156802610791164229.
Emerging data indicates the existence of novel molecular targets for cannabinoid ligands and recently it has been suggested that the orphan G-protein coupled receptor, GPR55 can be activated by a range of endogenous, plant and synthetic cannabinoids. However, to date, the most potent ligand identified for GPR55 is the endogenous phospholipid, lysophosphatidylinositol (LPI). GPR55 is thought to link predominantly G-protein alpha(13), where it promotes Rho-dependent signalling. Additional events downstream of GPR55 include activation of ERK-MAP kinase and Ca(2+) release from stores, as well as the induction of a number of transcription factors. Although GPR55 has only a low sequence identity with the CB1 or CB2 cannabinoid receptors, it clearly interacts with certain cannabinoid ligands. However, the nature and scope of these effects are presently unclear and they may be influenced by the assay and cellular background used for their study. This article reviews the current status of GPR55 pharmacology and its putative endogenous ligand, lysophosphatidylinositol LPI.
新兴数据表明，大麻素配体存在新的分子靶点，最近有人提出，孤儿 G 蛋白偶联受体 GPR55 可以被一系列内源性、植物和合成大麻素激活。然而，迄今为止，为 GPR55 鉴定的最有效配体是内源性磷脂，溶血磷脂酰肌醇（LPI）。GPR55 被认为主要与 G 蛋白 alpha(13)相连，在那里它促进 Rho 依赖性信号转导。GPR55 下游的其他事件包括 ERK-MAP 激酶的激活和储存中钙的释放，以及许多转录因子的诱导。尽管 GPR55 与 CB1 或 CB2 大麻素受体的序列同一性很低，但它显然与某些大麻素配体相互作用。然而，这些影响的性质和范围目前尚不清楚，它们可能受到用于研究的测定和细胞背景的影响。本文综述了 GPR55 药理学及其假定的内源性配体溶血磷脂酰肌醇 LPI 的现状。
