Journal article
Regulators of G protein Signaling (RGS) proteins in GtoPdb v.2025.3
IUPHAR/BPS Guide to Pharmacology CITE, Vol.2025(3)
09/10/2025
DOI: 10.2218/gtopdb/F891/2025.3
Abstract
Regulator of G protein Signaling, or RGS, proteins serve an important regulatory role in signaling mediated by G protein-coupled receptors (GPCRs). They all share a common RGS domain that directly interacts with active, GTP-bound Gα subunits of heterotrimeric G proteins. RGS proteins stabilize the transition state for GTP hydrolysis on Gα and thus induce a conformational change in the Gα subunit that accelerates GTP hydrolysis, thereby effectively turning off signaling cascades mediated by GPCRs. This GTPase accelerating protein (GAP) activity is the canonical mechanism of action for RGS proteins, although many also possess additional functions and domains. RGS proteins are divided into four families, R4, R7, R12 and RZ based on sequence homology, domain structure as well as specificity towards Gα subunits. For reviews on RGS proteins and their potential as therapeutic targets, see e.g. [226, 530, 579, 584, 585, 744, 755, 445, 11].
Details
- Title: Subtitle
- Regulators of G protein Signaling (RGS) proteins in GtoPdb v.2025.3
- Creators
- Katelin E. Ahlers-DannenHarrison J. McNabbCarolina Montañez-MirandaOsita W. OgujioforHoa Phan Thi NhuDavid L. RomanVincent ShawBenita SjögrenMackenzie M. SpicerKatherine E. SquiresLaurie SuttonMenbere WendimuThomas M. WilkieKeqiang XieQian ZhangLuke D. MascarenhasKirill MartemyanovZili LuoMohammed AlqinyahChristopher BodleJosephine Bou DagherBandana ChakravartiShreoshi P. ChoudhuriKirk M. DrueyRory A. FisherKyle J. GerberJohn R. HeplerShelley B. HooksHavish S. KanthetiBehirda KarajSomayeh Layeghi-GhalehsoukhtehJae-Kyung LeeYalda Zolghadri
- Resource Type
- Journal article
- Publication Details
- IUPHAR/BPS Guide to Pharmacology CITE, Vol.2025(3)
- DOI
- 10.2218/gtopdb/F891/2025.3
- ISSN
- 2633-1020
- eISSN
- 2633-1020
- Language
- English
- Date published
- 09/10/2025
- Academic Unit
- Neurology; Pharmacy; Critical Care; Stead Family Department of Pediatrics; Iowa Neuroscience Institute; Pharmaceutical Sciences and Experimental Therapeutics; Neuroscience and Pharmacology; Medicinal and Natural Products Chemistry; Internal Medicine
- Record Identifier
- 9985019032702771
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