title: Dynamics and modulation of metabotropic glutamate receptors.
abstract: The metabotropic glutamate receptors (mGluRs) are glutamate-activated G protein-coupled receptors widely expressed in the central nervous system. The eight mGluRs subtypes modulate transmission at many synapses, and are interesting therapeutic targets for the treatment of many neurological and psychiatric diseases. In particular, their organization in multiple domains and subunits offers various possibilities for the development of drugs that modulate mGluRs activity with different efficacies. Recent structural, biophysical and functional analyses have provided new insights into the mechanism of mGluR activation and dynamics. They also revealed the structural bases of ligand efficacy then providing possible mechanism of action of partial agonists and allosteric modulators. These new findings are of great interest for the development of novel mGluR subtype-selective compounds.
authors.affiliation: CNRS, UMR5203, Institut de Génomique Fonctionnelle, Montpellier, France; INSERM, U661, Montpellier, France; Université Montpellier 1 & 2, Montpellier F-34000, France. Electronic address: philippe.rondard@igf.cnrs.fr.
authors.forename: Philippe
authors.initials: P
authors.lastname: Rondard
authors.affiliation: CNRS, UMR5203, Institut de Génomique Fonctionnelle, Montpellier, France; INSERM, U661, Montpellier, France; Université Montpellier 1 & 2, Montpellier F-34000, France.
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Pin
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D002490:Central Nervous System / Q000378:metabolism; D015195:Drug Design; D018698:Glutamic Acid / Q000378:metabolism; D006801:Humans; D008024:Ligands; D001523:Mental Disorders / Q000188:drug therapy* / Q000503:physiopathology; D058990:Molecular Targeted Therapy; D009422:Nervous System Diseases / Q000188:drug therapy* / Q000503:physiopathology; D018094:Receptors, Metabotropic Glutamate / Q000187:drug effects* / Q000378:metabolism; D009435:Synaptic Transmission / Q000502:physiology
chemical_list: D008024:Ligands; D018094:Receptors, Metabotropic Glutamate; D018698:Glutamic Acid