• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

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.

DOI:10.1016/j.cellsig.2014.04.022
PMID:24793301
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4130774/
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。

相似文献

1
Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications.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
Cell Signal. 2014 Oct;26(10):2284-97. doi: 10.1016/j.cellsig.2014.04.022. Epub 2014 May 2.
2
Functional selectivity induced by mGlu₄ receptor positive allosteric modulation and concomitant activation of Gq coupled receptors.mGlu₄ 受体正变构调节和伴随激活 Gq 偶联受体诱导的功能选择性。
Neuropharmacology. 2013 Mar;66:122-32. doi: 10.1016/j.neuropharm.2012.03.003. Epub 2012 Mar 9.
3
Pharmacology of metabotropic glutamate receptor allosteric modulators: structural basis and therapeutic potential for CNS disorders.代谢型谷氨酸受体变构调节剂的药理学:中枢神经系统疾病的结构基础和治疗潜力。
Prog Mol Biol Transl Sci. 2013;115:61-121. doi: 10.1016/B978-0-12-394587-7.00002-6.
4
Allosteric modulation of metabotropic glutamate receptors.代谢型谷氨酸受体的变构调节
Adv Pharmacol. 2011;62:37-77. doi: 10.1016/B978-0-12-385952-5.00010-5.
5
International Union of Basic and Clinical Pharmacology. CXI. Pharmacology, Signaling, and Physiology of Metabotropic Glutamate Receptors.国际基础和临床药理学联合会. CXI. 代谢型谷氨酸受体的药理学、信号转导和生理学。
Pharmacol Rev. 2021 Jan;73(1):521-569. doi: 10.1124/pr.119.019133.
6
Allosteric Molecular Switches in Metabotropic Glutamate Receptors.变构分子开关在代谢型谷氨酸受体中的作用。
ChemMedChem. 2021 Jan 8;16(1):81-93. doi: 10.1002/cmdc.202000444. Epub 2020 Aug 25.
7
Photoswitchable allosteric modulators for metabotropic glutamate receptors.光致变色变构调节剂用于代谢型谷氨酸受体。
Curr Opin Pharmacol. 2022 Oct;66:102266. doi: 10.1016/j.coph.2022.102266. Epub 2022 Jul 20.
8
Neurobiological insights and novel therapeutic opportunities for CNS disorders from mGlu receptor allosteric and biased modulation.基于代谢型谷氨酸受体变构调节和偏向性调节的中枢神经系统疾病的神经生物学见解与新型治疗机遇
Curr Opin Pharmacol. 2017 Feb;32:49-55. doi: 10.1016/j.coph.2016.10.007. Epub 2016 Nov 11.
9
Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential.变构调节代谢型谷氨酸受体:结构见解与治疗潜力。
Neuropharmacology. 2011 Jan;60(1):66-81. doi: 10.1016/j.neuropharm.2010.07.007. Epub 2010 Jul 14.
10
Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders.G蛋白偶联受体的变构调节:治疗精神分裂症和其他中枢神经系统疾病的新见解及潜在应用
Neuron. 2017 May 3;94(3):431-446. doi: 10.1016/j.neuron.2017.03.016.

引用本文的文献

1
Unveiling the therapeutic potential of prenyl motif-containing derivatives: a key structural fragment for designing antidepressant compounds.揭示含异戊二烯基基序衍生物的治疗潜力:设计抗抑郁化合物的关键结构片段。
RSC Med Chem. 2025 Jul 3. doi: 10.1039/d5md00473j.
2
Role of mGluR7 in Alzheimer's disease: pathophysiological insights and therapeutic approaches.代谢型谷氨酸受体7在阿尔茨海默病中的作用:病理生理学见解与治疗方法
Inflammopharmacology. 2025 May 3. doi: 10.1007/s10787-025-01765-3.
3
Therapeutic Potential for Metabotropic Glutamate Receptor 7 Modulators in Cognitive Disorders.代谢型谷氨酸受体 7 调节剂在认知障碍中的治疗潜力。
Mol Pharmacol. 2024 Apr 17;105(5):348-358. doi: 10.1124/molpharm.124.000874.
4
Metabotropic Glutamate Receptor Subtype 5 Positron-Emission-Tomography Radioligands as a Tool for Central Nervous System Drug Development: Between Progress and Setbacks.代谢型谷氨酸受体5亚型正电子发射断层扫描放射性配体作为中枢神经系统药物开发工具:进展与挫折之间
Pharmaceuticals (Basel). 2023 Aug 10;16(8):1127. doi: 10.3390/ph16081127.
5
Genetic Downregulation of the Metabotropic Glutamate Receptor Type 5 Dampens the Reactive and Neurotoxic Phenotype of Adult ALS Astrocytes.代谢型谷氨酸受体 5 的遗传下调抑制成年 ALS 星形胶质细胞的反应性和神经毒性表型。
Cells. 2023 Jul 27;12(15):1952. doi: 10.3390/cells12151952.
6
Allosteric Modulators of Metabotropic Glutamate Receptors as Novel Therapeutics for Neuropsychiatric Disease.变构调节代谢型谷氨酸受体作为神经精神疾病治疗的新策略。
Pharmacol Rev. 2022 Jul;74(3):630-661. doi: 10.1124/pharmrev.121.000540.
7
Loss of retinoid X receptor gamma subunit impairs group 1 mGluR mediated electrophysiological responses and group 1 mGluR dependent behaviors.视黄酸 X 受体 γ 亚基缺失损害了 1 型 mGluR 介导的电生理反应和 1 型 mGluR 依赖的行为。
Sci Rep. 2021 Mar 10;11(1):5552. doi: 10.1038/s41598-021-84943-x.
8
Nonalcoholic Fatty Liver Disease and Non-Alcoholic Steatohepatitis: Current Issues and Future Perspectives in Preclinical and Clinical Research.非酒精性脂肪性肝病和非酒精性脂肪性肝炎:临床前和临床研究中的当前问题和未来展望。
Int J Mol Sci. 2020 Dec 17;21(24):9646. doi: 10.3390/ijms21249646.
9
Oligomeric Receptor Complexes and Their Allosteric Receptor-Receptor Interactions in the Plasma Membrane Represent a New Biological Principle for Integration of Signals in the CNS.寡聚受体复合物及其在质膜中的变构受体-受体相互作用代表了中枢神经系统中信号整合的一种新生物学原理。
Front Mol Neurosci. 2019 Sep 25;12:230. doi: 10.3389/fnmol.2019.00230. eCollection 2019.
10
Amygdala group II mGluRs mediate the inhibitory effects of systemic group II mGluR activation on behavior and spinal neurons in a rat model of arthritis pain.杏仁核群 II mGluRs 介导全身群 II mGluR 激活对关节炎疼痛大鼠模型中行为和脊髓神经元的抑制作用。
Neuropharmacology. 2019 Nov 1;158:107706. doi: 10.1016/j.neuropharm.2019.107706. Epub 2019 Jul 12.

本文引用的文献

1
Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator.结构的一类 C G 蛋白偶联受体代谢型谷氨酸受体 1 结合到一个变构调节剂。
Science. 2014 Apr 4;344(6179):58-64. doi: 10.1126/science.1249489. Epub 2014 Mar 6.
2
Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS.新型变构调节剂的选择性作用揭示了中枢神经系统代谢型谷氨酸受体的功能性异源二聚体。
J Neurosci. 2014 Jan 1;34(1):79-94. doi: 10.1523/JNEUROSCI.1129-13.2014.
3
Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM).(R)-(2-氟-4-((-4-甲氧基苯基)乙炔基)苯基)(3-羟基哌啶-1-基)甲酮(ML337)的发现,一种 mGlu3 选择性和中枢神经系统穿透性的负变构调节剂(NAM)。
J Med Chem. 2013 Jun 27;56(12):5208-12. doi: 10.1021/jm400439t. Epub 2013 Jun 13.
4
Regulation of metabotropic glutamate receptor 7 (mGluR7) internalization and surface expression by Ser/Thr protein phosphatase 1.丝氨酸/苏氨酸蛋白磷酸酶 1 对代谢型谷氨酸受体 7(mGluR7)内化和表面表达的调节。
J Biol Chem. 2013 Jun 14;288(24):17544-51. doi: 10.1074/jbc.M112.439513. Epub 2013 Apr 23.
5
Peripheral group II and III metabotropic glutamate receptors in the knee joint attenuate carrageenan-induced nociceptive behavior in rats.关节外周群 II 和 III 代谢型谷氨酸受体可减轻大鼠角叉菜胶诱导的痛觉行为。
Neurosci Lett. 2013 May 10;542:21-5. doi: 10.1016/j.neulet.2013.03.006. Epub 2013 Mar 15.
6
Glutamate acts as a partial inverse agonist to metabotropic glutamate receptor with a single amino acid mutation in the transmembrane domain.谷氨酸在跨膜结构域的单个氨基酸突变后,作为代谢型谷氨酸受体的部分反向激动剂起作用。
J Biol Chem. 2013 Apr 5;288(14):9593-9601. doi: 10.1074/jbc.M112.437780. Epub 2013 Feb 18.
7
Pharmacology of metabotropic glutamate receptor allosteric modulators: structural basis and therapeutic potential for CNS disorders.代谢型谷氨酸受体变构调节剂的药理学:中枢神经系统疾病的结构基础和治疗潜力。
Prog Mol Biol Transl Sci. 2013;115:61-121. doi: 10.1016/B978-0-12-394587-7.00002-6.
8
Role of metabotropic glutamate receptor 5 signaling and homer in oxygen glucose deprivation-mediated astrocyte apoptosis.代谢型谷氨酸受体 5 信号和 Homer 在氧葡萄糖剥夺介导的星形胶质细胞凋亡中的作用。
Mol Brain. 2013 Feb 14;6:9. doi: 10.1186/1756-6606-6-9.
9
A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.一种新型代谢型谷氨酸受体 5 正变构调节剂作用于独特的位点,并赋予 mGlu5 信号转导以刺激偏倚。
Mol Pharmacol. 2013 Apr;83(4):835-47. doi: 10.1124/mol.112.082891. Epub 2013 Jan 24.
10
The pathology roadmap in Parkinson disease.帕金森病的病理图谱。
Prion. 2013 Jan-Feb;7(1):85-91. doi: 10.4161/pri.23582. Epub 2013 Jan 1.