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

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.

Keywords: 7TMR; Allosteric modulation; Drug discovery; Heterodimer; Pharmacology; mGlu.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Allosteric Regulation
  • Antipsychotic Agents / therapeutic use
  • Central Nervous System Diseases / drug therapy
  • Central Nervous System Diseases / metabolism
  • Humans
  • Ligands
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, Metabotropic Glutamate / agonists
  • Receptors, Metabotropic Glutamate / metabolism*
  • Signal Transduction

Substances

  • Antipsychotic Agents
  • Ligands
  • Receptors, G-Protein-Coupled
  • Receptors, Metabotropic Glutamate