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Regulator of G protein signaling 8 (RGS8) is a member of the RGS protein family, which acts as a GTPase-activating protein (GAP) for the alpha subunits of heterotrimeric G proteins. RGS8 accelerates the hydrolysis of GTP to GDP by G protein alpha subunits, thereby terminating GPCR-mediated signaling events and ensuring timely signal desensitization. RGS8 has a single RGS domain, is part of the R4 subfamily, and regulates signaling via muscarinic acetylcholine and dopamine receptors, as well as the activity of potassium channels. It is predominantly expressed in the brain and is implicated in neurological diseases, including spinocerebellar ataxia and night blindness. Experimental inhibitors of RGS8 are used in research to unravel G protein pathway dynamics, but there are currently no clinically approved drugs directly targeting this protein.
Inhibition of GTPase accelerating activity (by small molecules or peptides that block the interaction between RGS8 and G protein alpha subunits)
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