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Schematic illustration of the activating procedure of GPCR as well as the agonist-induced signaling event. a (Up) The heterotrimeric G protein complex interacts with the activated GPCRs, therefore triggers the dissociation of the Gα and Gβγ subunit, where the latter recruits GRKs to phosphorylate the C-terminal tail of GPCR. b (Down) The βarr tends to interact with activated and phosphorylated GPCRs than the phosphorylation-only GPCRs
