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G蛋白偶联受体作为2型糖尿病的新治疗靶点。

G protein-coupled receptors as new therapeutic targets for type 2 diabetes.

作者信息

Reimann Frank, Gribble Fiona M

机构信息

Wellcome Trust-MRC Institute of Metabolic Science, Metabolic Research Laboratories, University of Cambridge, Addenbrooke's Hospital Box 289, Hills Road, Cambridge, CB2 0QQ, UK.

出版信息

Diabetologia. 2016 Feb;59(2):229-33. doi: 10.1007/s00125-015-3825-z. Epub 2015 Dec 12.

Abstract

G protein-coupled receptors (GPCRs) in the gut-brain-pancreatic axis are key players in the postprandial control of metabolism and food intake. A number of intestinally located receptors have been implicated in the chemo-detection of ingested nutrients, and in the pancreatic islets and nervous system GPCRs play essential roles in the detection of many hormones and neurotransmitters. Because of the diversity, cell-specific expression and 'druggability' of the GPCR superfamily, these receptors are popular targets for therapeutic development. This review will outline current and potential future approaches to develop GPCR agonists for the treatment of type 2 diabetes. This review summarises a presentation given at the 'Novel approaches to treating type 2 diabetes' symposium at the 2015 annual meeting of the EASD. It is accompanied by a commentary by the Session Chair, Michael Nauck (DOI: 10.1007/s00125-015-3823-1 ).

摘要

肠-脑-胰腺轴中的G蛋白偶联受体(GPCRs)是餐后代谢和食物摄入控制的关键参与者。许多位于肠道的受体参与了对摄入营养物质的化学检测,并且在胰岛和神经系统中,GPCRs在许多激素和神经递质的检测中发挥着重要作用。由于GPCR超家族的多样性、细胞特异性表达以及“可成药性”,这些受体是治疗开发的热门靶点。本综述将概述目前以及未来开发用于治疗2型糖尿病的GPCR激动剂的方法。本综述总结了在2015年欧洲糖尿病研究协会(EASD)年会“治疗2型糖尿病的新方法”研讨会上的一次演讲内容。同时还附有会议主席迈克尔·瑙克的评论(DOI: 10.1007/s00125-015-3823-1 )。

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