Class B1 GPCR activation by an intracellular agonist.

ABSTRACT: G protein-coupled receptors (GPCRs) generally accommodate specific ligands in the orthosteric-binding pockets. Ligand binding triggers a receptor allosteric conformational change that leads to the activation of intracellular transducers, G proteins and β-arrestins. Because these signals often induce adverse effects, the selective activation mechanism for each transducer must be elucidated. Thus, many orthosteric-biased agonists have been developed, and intracellular-biased agonists have recently attracted broad interest. These agonists bind within the receptor intracellular cavity and preferentially tune the specific signalling pathway over other signalling pathways, without allosteric rearrangement of the receptor from the extracellular side^1-3. However, only antagonist-bound s

SUBMITTER: Kobayashi K 

PROVIDER: S-EPMC10307627 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature