Selective Photoswitchable Allosteric Agonist of a G Protein-Coupled Receptor.

ABSTRACT: G protein-coupled receptors (GPCRs) are the most common targets of drug discovery. However, the similarity between related GPCRs combined with the complex spatiotemporal dynamics of receptor activation in vivo has hindered drug development. Photopharmacology offers the possibility of using light to control the location and timing of drug action by incorporating a photoisomerizable azobenzene into a GPCR ligand, enabling rapid and reversible switching between an inactive and active configuration. Recent advances in this area include (i) photoagonists and photoantagonists that directly control receptor activity but are nonselective because they bind conserved sites, and (ii) photoallosteric modulators that bind selectively to nonconserved sites but indirectly control receptor activity

SUBMITTER: Donthamsetti P 

PROVIDER: S-EPMC8227462 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature