What is the natural ligand of GPR55?

被引:13
作者
Okuno, Toshiaki [1 ]
Yokomizo, Takehiko [1 ]
机构
[1] Kyushu Univ, Grad Sch Med, Dept Med Biochem, Higashi Ku, Fukuoka 81285823, Japan
关键词
GPR55; LPI; natural ligand; lipid; mass spectrometry; CANNABINOID RECEPTOR-LIGAND; ACTIVATED PROTEIN-KINASE; HL-60; CELLS; 2-ARACHIDONOYLGLYCEROL; LYSOPHOSPHATIDYLINOSITOL; ACID; GENERATION; CB1;
D O I
10.1093/jb/mvr022
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 G(12/13) and G(q/11) proteins, 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.
引用
收藏
页码:495 / 497
页数:3
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