Henstridge Christopher M, Balenga Nariman A B, Kargl Julia, Andradas Clara, Brown Andrew J, Irving Andrew, Sanchez Cristina, Waldhoer Maria
Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest.
Mol Endocrinol. 2011 Nov;25(11):1835-48. doi: 10.1210/me.2011-1197. Epub 2011 Sep 29.
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.
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。