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Int. J. Mol. Sci. 2017, 18(3), 672; doi:10.3390/ijms18030672

Molecular Basis for Modulation of Metabotropic Glutamate Receptors and Their Drug Actions by Extracellular Ca2+

Department of Chemistry, Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA
These authors contributed equally to this work.
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Academic Editor: ChulHee Kang
Received: 8 February 2017 / Revised: 13 March 2017 / Accepted: 17 March 2017 / Published: 21 March 2017
(This article belongs to the Special Issue Calcium Regulation and Sensing)
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Abstract

Metabotropic glutamate receptors (mGluRs) associated with the slow phase of the glutamatergic signaling pathway in neurons of the central nervous system have gained importance as drug targets for chronic neurodegenerative diseases. While extracellular Ca2+ was reported to exhibit direct activation and modulation via an allosteric site, the identification of those binding sites was challenged by weak binding. Herein, we review the discovery of extracellular Ca2+ in regulation of mGluRs, summarize the recent developments in probing Ca2+ binding and its co-regulation of the receptor based on structural and biochemical analysis, and discuss the molecular basis for Ca2+ to regulate various classes of drug action as well as its importance as an allosteric modulator in mGluRs. View Full-Text
Keywords: extracellular Ca2+; metabotropic glutamate receptor (mGluR); regulation; family C of G-protein coupled receptor (cGPCR) extracellular Ca2+; metabotropic glutamate receptor (mGluR); regulation; family C of G-protein coupled receptor (cGPCR)
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Zou, J.; Jiang, J.Y.; Yang, J.J. Molecular Basis for Modulation of Metabotropic Glutamate Receptors and Their Drug Actions by Extracellular Ca2+. Int. J. Mol. Sci. 2017, 18, 672.

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