Metabotropic glutamate receptors: physiology, pharmacology, and disease.
Metabotropic glutamate receptors: physiology, pharmacology, and disease.
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DOI：
10.1146/annurev.pharmtox.011008.145533
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发表时间：
2010
影响因子：
12.5
通讯作者：
Conn PJ
中科院分区：
文献类型：
--
作者：
Niswender CM;Conn PJ
代谢型谷氨酸受体（metabotropic glutamate receptor，mGluRs）是一类参与中枢神经系统突触传递和神经元兴奋性调节的G蛋白偶联受体。mGluR在大的细胞外结构域内结合谷氨酸，并通过受体蛋白将信号传递到细胞内信号传导伴侣。在确定mGluRs被激活的机制、与它们相互作用的蛋白质以及可以调节受体活性的正构和变构配体方面已经取得了很大进展。mGluR的广泛表达使得这些受体成为特别有吸引力的药物靶标，并且最近的研究继续验证mGluR配体在神经和精神障碍如阿尔茨海默病、帕金森病、焦虑症、抑郁症和精神分裂症中的治疗效用。
The metabotropic glutamate receptors (mGluRs) are family C G-protein-coupled receptors that participate in the modulation of synaptic transmission and neuronal excitability throughout the central nervous system. The mGluRs bind glutamate within a large extracellular domain and transmit signals through the receptor protein to intracellular signaling partners. A great deal of progress has been made in determining the mechanisms by which mGluRs are activated, proteins with which they interact, and orthosteric and allosteric ligands that can modulate receptor activity. The widespread expression of mGluRs makes these receptors particularly attractive drug targets, and recent studies continue to validate the therapeutic utility of mGluR ligands in neurological and psychiatric disorders such as Alzheimer’s disease, Parkinson’s disease, anxiety, depression, and schizophrenia.
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