Rules and mechanisms governing G protein coupling selectivity of GPCRs.

ABSTRACT: G protein-coupled receptors (GPCRs) convert extracellular stimuli into intracellular signaling by coupling to heterotrimeric G proteins of four classes: G_i/o, G_q, G_s, and G_12/13. However, our understanding of the G protein selectivity of GPCRs is incomplete. Here, we quantitatively measure the enzymatic activity of GPCRs in living cells and reveal the G protein selectivity of 124 GPCRs with the exact rank order of their G protein preference. Using this information, we establish a classification of GPCRs by functional selectivity, discover the existence of a G_12/13-coupled receptor, G₁₅-coupled receptors, and a variety of subclasses for G_i/o-, G_q-, and G_s-coupled receptors, culminating in deve

SUBMITTER: Masuho I 

PROVIDER: S-EPMC10842385 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature