Members of the “regulator of G-protein signaling” (RGS)-protein superfumily act as “GTPase-accelerating proteins” (GAP) for heterotrimeric G-protein alpha subunits, thereby attenuating GPCR signaling. Their selectivity for specific GPCRs and downstream signaling components and their tissue-specific expression makes them attractive as potential therapeutic targets, with the potential for modulating the effects of existing GPCR agonists.
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