Regulators of G protein Signaling (RGS) proteins (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database

Katelin E. Ahlers-Dannen; Mohammed Alqinyah; Christopher Bodle; Josephine Bou Dagher; Bandana Chakravarti; Shreoshi P. Choudhuri; Kirk M. Druey; Rory A. Fisher; Kyle J. Gerber; John R. Hepler; Shelley B. Hooks; Havish S. Kantheti; Behirda Karaj; Jae-Kyung Lee; Zili Luo; Kirill Martemyanov; Luke D. Mascarenhas; Carolina Montañez-Miranda; Hoa Phan Thi Nhu; David L. Roman; Vincent Shaw; Benita Sjögren; Mackenzie M. Spicer; Katherine E. Squires; Laurie Sutton; Menbere Wendimu; Thomas M. Wilkie; Keqiang Xie; Yalda Zolghadri

doi:10.2218/gtopdb/F891/2020.5

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Regulators of G protein Signaling (RGS) proteins (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database

Journal article

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Regulators of G protein Signaling (RGS) proteins (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database

Katelin E. Ahlers-Dannen, Mohammed Alqinyah, Christopher Bodle, Josephine Bou Dagher, Bandana Chakravarti, Shreoshi P. Choudhuri, Kirk M. Druey, Rory A. Fisher, Kyle J. Gerber, John R. Hepler, …

IUPHAR/BPS Guide to Pharmacology CITE, Vol.2020(5)

11/12/2020

DOI: 10.2218/gtopdb/F891/2020.5

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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. [183, 411, 446, 450, 451, 558, 566, 345, 9].

Details

Title: Subtitle: Regulators of G protein Signaling (RGS) proteins (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database
Creators: Katelin E. Ahlers-Dannen
Mohammed Alqinyah
Christopher Bodle
Josephine Bou Dagher
Bandana Chakravarti
Shreoshi P. Choudhuri
Kirk M. Druey
Rory A. Fisher
Kyle J. Gerber
John R. Hepler
Shelley B. Hooks
Havish S. Kantheti
Behirda Karaj
Jae-Kyung Lee
Zili Luo
Kirill Martemyanov
Luke D. Mascarenhas
Carolina Montañez-Miranda
Hoa Phan Thi Nhu
David L. Roman
Vincent Shaw
Benita Sjögren
Mackenzie M. Spicer
Katherine E. Squires
Laurie Sutton
Menbere Wendimu
Thomas M. Wilkie
Keqiang Xie
Yalda Zolghadri
Resource Type: Journal article
Publication Details: IUPHAR/BPS Guide to Pharmacology CITE, Vol.2020(5)
DOI: 10.2218/gtopdb/F891/2020.5
ISSN: 2633-1020
eISSN: 2633-1020
Language: English
Date published: 11/12/2020
Academic Unit: 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: 9984274650102771

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