Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias.

ABSTRACT: The metabotropic glutamate receptor subtype 5 (mGlu5 ) is a family C GPCR that has been implicated in various neuronal processes and, consequently, in several CNS disorders. Over the past few decades, GPCR-based drug discovery, including that for mGlu5 receptors, has turned considerable attention to targeting allosteric binding sites. Modulation of endogenous agonists by allosteric ligands offers the advantages of spatial and temporal fine-tuning of receptor activity, increased selectivity and reduced adverse effects with the potential to elicit improved clinical outcomes. Further, with greater appreciation of the multifaceted nature of the transduction of mGlu5 receptor signalling, it is increasingly apparent that drug discovery must take into consideration unique receptor conformations a

SUBMITTER: Sengmany K 

PROVIDER: S-EPMC5341252 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature