What is the natural ligand of GPR55?
What is the natural ligand of GPR55?
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GPR55 的天然配体是什么？
DOI：
10.1093/jb/mvr022
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发表时间：
2011
期刊：
影响因子：
--
通讯作者：
Yokomizo T
中科院分区：
文献类型：
--
作者：
Okuno T;Yokomizo T
GPR55 是一种七跨膜 G 蛋白偶联受体，最初被鉴定为假定的第三种大麻素受体。最近，据报道溶血磷脂酰肌醇（LPI）是 GPR55 的配体。 LPI 刺激 GPR55 会激活 G12/13 和 Gq/11 蛋白，诱导细胞外信号调节激酶磷酸化并增加细胞内钙离子浓度。溶血磷脂在不同物种和组织中的分子结构非常不同。最近的一份报告表明，大鼠脑中 LPI 的主要脂肪酰基部分是硬脂酸，其次是花生四烯酸。含花生四烯酸的 LPI 物种对 GPR55 的生物活性明显高于含有其他脂肪酰基的 LPI 物种，表明 2-花生四烯酸 LPI 是最有可能的 GPR55 天然配体。
GPR55 is a seven transmembrane G protein-coupled receptor and was originally identified as a putative third cannabinoid receptor. Recently, lysophosphatidylinositol (LPI) was reported to be a GPR55 ligand. Stimulation of GPR55 by LPI activates G12/13and Gq/11proteins, induces phosphorylation of the extracellular signal-regulated kinase and increases intracellular calcium concentration. Lysophospholipids are molecularly quite diverse across species and tissues. A recent report showed that the predominant fatty acyl moiety of LPI in rat brain is stearic acid followed by arachidonic acid. The biological activity of arachidonic acid-containing LPI species towards GPR55 was shown to be markedly higher than that of LPI species containing other fatty acyl groups, suggesting that 2-arachidonolyl LPI is the most likely natural ligand of GPR55.