Mechanistic Insights into Light-Driven Allosteric Control of GPCR Biological Activity.

ABSTRACT: G protein-coupled receptors (GPCR), including the metabotrobic glutamate 5 receptor (mGlu₅), are important therapeutic targets and the development of allosteric ligands for targeting GPCRs has become a desirable approach toward modulating receptor activity. Traditional pharmacological approaches toward modulating GPCR activity are still limited since precise spatiotemporal control of a ligand is lost as soon as it is administered. Photopharmacology proposes the use of photoswitchable ligands to overcome this limitation, since their activity can be reversibly controlled by light with high precision. As this is still a growing field, our understanding of the molecular mechanisms underlying the light-induced changes of different photoswitchable ligand pharmacology is suboptimal. Fo

SUBMITTER: Ricart-Ortega M 

PROVIDER: S-EPMC7551736 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature