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对代谢型谷氨酸受体的深入理解进展:结构、信号传导及治疗适应症

Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications.

作者信息

Yin Shen, Niswender Colleen M

机构信息

Department of Pharmacology, Vanderbilt University Medical School, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical School, Nashville, TN 37232, USA.

Department of Pharmacology, Vanderbilt University Medical School, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical School, Nashville, TN 37232, USA.

出版信息

Cell Signal. 2014 Oct;26(10):2284-97. doi: 10.1016/j.cellsig.2014.04.022. Epub 2014 May 2.

Abstract

The metabotropic glutamate (mGlu) receptors are a group of Class C seven-transmembrane spanning/G protein-coupled receptors (7TMRs/GPCRs). These receptors are activated by glutamate, one of the standard amino acids and the major excitatory neurotransmitter. By activating G protein-dependent and non-G protein-dependent signaling pathways, mGlus modulate glutamatergic transmission both in the periphery and throughout the central nervous system. Since the discovery of the first mGlu receptor, and especially during the last decade, a great deal of progress has been made in understanding the signaling, structure, pharmacological manipulation and therapeutic indications of the 8 mGlu members.

摘要

代谢型谷氨酸(mGlu)受体是C类七跨膜/G蛋白偶联受体(7TMRs/GPCRs)中的一组受体。这些受体由谷氨酸激活,谷氨酸是标准氨基酸之一,也是主要的兴奋性神经递质。通过激活G蛋白依赖性和非G蛋白依赖性信号通路,mGlu受体在外周和整个中枢神经系统中调节谷氨酸能传递。自首个mGlu受体被发现以来,尤其是在过去十年间,在理解8种mGlu受体成员的信号传导、结构、药理操作和治疗适应症方面取得了很大进展。

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