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GPR55:从孤儿受体到代谢调节剂?

GPR55: from orphan to metabolic regulator?

机构信息

Diabetes Research Group, Division of Diabetes & Nutritional Sciences, King's College London, London SE1 1UL, UK.

Diabetes Research Group, Division of Diabetes & Nutritional Sciences, King's College London, London SE1 1UL, UK.

出版信息

Pharmacol Ther. 2015 Jan;145:35-42. doi: 10.1016/j.pharmthera.2014.06.007. Epub 2014 Jun 24.

DOI:10.1016/j.pharmthera.2014.06.007
PMID:24972076
Abstract

GPR55 belongs to the class A family of G-protein coupled receptor (GPCRs) and its activity is regulated by a range of synthetic and endogenous cannabinoids, and by lipid-derived ligands. Cannabinoids are known to be important in controlling appetite and metabolic balance, and it is now emerging that GPR55 may have a role to play in energy homeostasis through the regulation of food intake, fuel storage in adipocytes, gut motility and insulin secretion. This review summarises our current knowledge of expression and function of GPR55 in tissues involved in metabolic regulation, the signalling cascades through which GPR55 is reported to act to exert its effects, and it comments on the difficulties in reaching firm conclusions when using GPR55 ligands of poor specificity. Understanding the role of GPR55 in energy homeostasis may provide a novel target for therapeutic intervention in obesity and type 2 diabetes mellitus.

摘要

GPR55 属于 A 类 G 蛋白偶联受体 (GPCR) 家族,其活性受一系列合成和内源性大麻素以及脂质衍生配体的调节。大麻素在控制食欲和代谢平衡方面的作用已众所周知,现在有研究表明,GPR55 可能通过调节食物摄入、脂肪细胞中燃料储存、肠道蠕动和胰岛素分泌在能量平衡中发挥作用。这篇综述总结了我们目前对 GPR55 在参与代谢调节的组织中的表达和功能的了解,以及据报道 GPR55 通过哪些信号通路发挥作用的信息,并评论了在使用特异性差的 GPR55 配体时难以得出明确结论的问题。了解 GPR55 在能量平衡中的作用可能为肥胖症和 2 型糖尿病的治疗干预提供新的靶点。

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