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小型综述:溶血磷脂酰肌醇敏感受体GPR55的生理学和病理学最新进展

Minireview: recent developments in the physiology and pathology of the lysophosphatidylinositol-sensitive receptor GPR55.

作者信息

Henstridge Christopher M, Balenga Nariman A B, Kargl Julia, Andradas Clara, Brown Andrew J, Irving Andrew, Sanchez Cristina, Waldhoer Maria

机构信息

Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest.

出版信息

Mol Endocrinol. 2011 Nov;25(11):1835-48. doi: 10.1210/me.2011-1197. Epub 2011 Sep 29.

DOI:10.1210/me.2011-1197
PMID:21964594
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5417173/
Abstract

Emerging data suggest that off-target cannabinoid effects may be mediated via novel seven-transmembrane spanning/G protein-coupled receptors. Due to its cannabinoid sensitivity, the G protein-coupled receptor 55 (GPR55) was recently proposed as a candidate; however, GPR55 is phylogenetically distinct from the traditional cannabinoid receptors, and the conflicting pharmacology, signaling, and functional data have prevented its classification as a novel cannabinoid receptor. Indeed, the most consistent and potent agonist to date is the noncannabinoid lysophospholipid, lysophosphatidylinositol. Here we present new human GPR55 mRNA expression data, providing supportive evidence of GPR55 expression in a vast array of tissues and cell types. Moreover, we summarize major recent developments in GPR55 research and aim to update the reader in the rapidly expanding fields of GPR55 pharmacology, physiology, and pathology.

摘要

新出现的数据表明,脱靶大麻素效应可能通过新型七跨膜/G蛋白偶联受体介导。由于其对大麻素的敏感性,G蛋白偶联受体55(GPR55)最近被提议作为一个候选者;然而,GPR55在系统发育上与传统大麻素受体不同,相互矛盾的药理学、信号传导和功能数据使其无法被归类为新型大麻素受体。事实上,迄今为止最一致且有效的激动剂是非大麻素溶血磷脂,溶血磷脂酰肌醇。在此,我们展示了新的人类GPR55 mRNA表达数据,为GPR55在大量组织和细胞类型中的表达提供了支持性证据。此外,我们总结了GPR55研究的主要最新进展,旨在让读者了解GPR55药理学、生理学和病理学快速发展的领域。

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2
The GPCR-associated sorting protein 1 regulates ligand-induced down-regulation of GPR55.G 蛋白偶联受体相关分拣蛋白 1 调节 GPR55 配体诱导的下调。
Br J Pharmacol. 2012 Apr;165(8):2611-9. doi: 10.1111/j.1476-5381.2011.01562.x.
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The abnormal cannabidiol analogue O-1602 reduces nociception in a rat model of acute arthritis via the putative cannabinoid receptor GPR55.异常的大麻二酚类似物 O-1602 通过假定的大麻素受体 GPR55 减少急性关节炎大鼠模型中的痛觉。
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The GPR55 agonist lysophosphatidylinositol directly activates intermediate-conductance Ca2+ -activated K+ channels.GPR55 激动剂溶血磷脂酰肌醇直接激活中间电导钙激活钾通道。
Pflugers Arch. 2011 Aug;462(2):245-55. doi: 10.1007/s00424-011-0977-7. Epub 2011 May 21.
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Endocannabinoids inhibit release of nerve growth factor by inflammation-activated mast cells.内源性大麻素抑制炎症激活的肥大细胞释放神经生长因子。
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