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. Author manuscript; available in PMC: 2022 Jul 1.
Published in final edited form as: Pharmacol Ther. 2021 Feb 15;223:107818. doi: 10.1016/j.pharmthera.2021.107818

Figure 3. Biochemical actions of RGS proteins.

Figure 3

Activated GPCRs promote exchange of guanosine-5’-diphosphate (GDP) for guanosine-5’-triphosphate (GTP) on the Gα subunit of heterotrimeric G-proteins, resulting in dissociation of Gα from Gβγ dimers and effector activation. Gα hydrolyzes GTP to GDP, which promotes re-association of the G-protein heterotrimer and termination of signaling. RGS proteins interact with Gα in its transition state between GTP- and GDP-bound forms, an interaction which catalyzes hydrolysis and limits the duration and magnitude of GPCR signaling.