Open AccessRegulators of G protein Signaling (RGS) proteins (version 2020.4) in the IUPHAR/BPS Guide to Pharmacology Database
Author(s) -
Katelin E. AhlersDannen,
Mohammed Alqinyah,
Christopher Bodle,
Josephine Bou Dagher,
Bandana Chakravarti,
Shreoshi Pal Choudhuri,
Kirk M. Druey,
Rory A. Fisher,
Kyle J. Gerber,
John R. Hepler,
Shelley B. Hooks,
Havish S. Kantheti,
Behirda Karaj,
Jaekyung Lee,
Zili Luo,
Kirill A. Martemyanov,
Luke D. Mascarenhas,
Hoa T.N. Phan,
David L. Roman,
Vincent Shaw,
Benita Sjögren,
Mackenzie M. Spicer,
Katherine E. Squires,
Laurie P. Sutton,
Thomas M. Wilkie,
Keqiang Xie,
Yalda Zolghadri
Publication year - 2020
Publication title -
iuphar/bps guide to pharmacology cite
Language(s) - English
Resource type - Journals
ISSN - 2633-1020
DOI - 10.2218/gtopdb/f891/2020.4
Subject(s) - heterotrimeric g protein , rgs2 , regulator of g protein signaling , gtpase activating protein , g protein , g protein coupled receptor , gtpase , gq alpha subunit , microbiology and biotechnology , gtp binding protein regulators , chemistry , g alpha subunit , gtp' , gi alpha subunit , g beta gamma complex , protein subunit , gs alpha subunit , biology , signal transduction , biochemistry , enzyme , gene
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. [160, 377, 411, 415, 416, 512, 519, 312, 6].