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Conformational biosensors delineate endosomal G protein regulation by GPCRs - PubMed

4 days ago
  • #endosomal signaling
  • #G protein regulation
  • #GPCR
  • Conformational biosensors reveal how GPCRs regulate G proteins in endosomes.
  • Three Gs-coupled GPCRs (β2-adrenergic receptor, VIP-1 receptor, adenosine 2B receptor) redistribute Gαs from plasma membrane to endosomes without receptor internalization.
  • Active-state Gαs production on endosomes depends on GPCR internalization.
  • GPCRs show location bias in coupling selectivity between Gs and Gq on endosomes vs. plasma membrane.
  • Endosomal Gs regulation involves two discrete coupling reactions: one at the plasma membrane controlling Gs concentration, another at endosomes controlling Gs activity.
  • GPCR endocytosis can switch signaling selectivity between G protein classes.