Arrestin recognizes GPCRs independently of the receptor state.

ABSTRACT: Only two nonvisual arrestins recognize many hundreds of different, intracellularly phosphorylated G protein-coupled receptors (GPCRs). Due to the highly dynamic nature of GPCR•arrestin complexes, the critical determinants of GPCR-arrestin recognition have remained largely unclear. We show here that arrestin2 recruitment to the β₁-adrenergic receptor (β₁AR) can be induced by an arrestin-activating phosphopeptide that is not covalently linked to the receptor and that the recruitment is independent of the presence and type of the orthosteric receptor ligand. Apparently, the arrestin-receptor interaction is driven by the conformational switch within arrestin induced by the phosphopeptide, whereas the electrostatic attraction toward the receptor phosphosites may only play

SUBMITTER: Petrovic I 

PROVIDER: S-EPMC12107136 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature