β-arrestin recruitment facilitates a direct association with G proteins.

ABSTRACT: G protein-coupled receptors (GPCRs) are targets for almost a third of all FDA-approved drugs. GPCRs are known to signal through both heterotrimeric G proteins and β-arrestins. Traditionally these pathways were viewed as largely separable, with G proteins primarily initiating downstream signaling while β-arrestins modulate receptor trafficking and desensitization in addition to regulating their own signaling events. Recent studies suggest an integrated role of G proteins and β-arrestins in GPCR signaling, however the cellular and biochemical requirements for G protein: β-arrestin interactions remain unclear. Here we show that G proteins and β-arrestins can directly interact. Through utilization of β-arrestin-biased receptors and artificially enforced β-arrestin relocalization, we demonstrat

SUBMITTER: Lee CY 

PROVIDER: S-EPMC12236855 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature