Regulator of G protein signaling 4 (RGS4)

Regulator of G protein signaling 4 (RGS4) is a member of the RGS protein family that acts as a GTPase-activating protein (GAP) for G alpha subunits of heterotrimeric G proteins[1][4]. It accelerates GTP hydrolysis, thereby rapidly inactivating G proteins and turning off GPCR-mediated signaling cascades. RGS4 is localized predominantly in the cytoplasm and at neuronal plasma membranes, where it modulates signaling by a broad array of GPCRs including those for monoamines, opioids, and muscarinic ligands[1][7]. It is highly expressed in regions of the brain involved in mood, cognition, and movement, and has been implicated in psychiatric disorders like schizophrenia and bipolar disorder[4][6]. RGS4 also influences the pharmacological response to antidepressant and analgesic drugs and is under investigation as a therapeutic target in neuropsychiatric and pain-related conditions[7].

Other names

RGP4RGP-4SCZD9Regulator of G-protein signaling 4Schizophrenia disorder 9

Inhibition of RGS4 (e.g., by CCG-4986 or peptides): prolongs G protein signaling by preventing GTP hydrolysis. Many conventional drugs do not directly bind RGS4, but the protein modulates signaling responses to GPCR-targeting drugs