Explanipedia

Systematic analysis of the RGS2 degron reveals characteristics of substrate recognition by the F-box protein FBXO44 Open

Harrison J. McNabb, Eugene Cho, Mary Pitman, Phillip S Rushton, David Mobley , et al. · 2025

Regulator of G protein signaling 2 (RGS2) negatively modulates signaling downstream of G protein-coupled receptors by accelerating GTP hydrolysis at Gα subunits of heterotrimeric G proteins. Decreased RGS2 levels are implicated in numerous…

Regulators of G protein Signaling (RGS) proteins in GtoPdb v.2025.3 Open

Katelin E. Ahlers‐Dannen, Harrison J. McNabb, Carolina Montañez‐Miranda, Osita W. Ogujiofor, H. T. Phan , et al. · 2025

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 subuni…

Discovery of RGS2-FBXO44 interaction inhibitors using a cell-based NanoBit assay Open

Sadikshya Aryal, C. Wong, Harrison J. McNabb, Junaid Ahmad, Ryan A. Altman , et al. · 2025

Regulators of G protein signaling (RGS) proteins negatively regulate signaling through G protein-coupled receptors, and reduced RGS protein function is involved in numerous pathologies. However, therapeutic intervention is challenging, as …

G protein regulation by RGS proteins in the pathophysiology of dilated cardiomyopathy Open

Yadhira E. Garcia, Benita Sjögren, Patrick Osei‐Owusu · 2025

Regulators of G protein signaling (RGS) proteins fine-tune signaling via heterotrimeric G proteins to maintain physiologic homeostasis in various organ systems of the human body including the brain, kidney, heart, and vasculature. Impaired…

A Phenotypic High-Throughput Screen Identifies Small Molecule Modulators of Endogenous RGS10 in BV-2 Cells Open

Shwetal Talele, Stephanie González, Julia Trudeau, Junaid Ahmad, Cody A. Loy , et al. · 2024

Chronic dysregulation of microglial phenotypic balance contributes to prolonged neuroinflammation and neurotoxicity, which is a hallmark of neurodegenerative diseases. Thus, targeting microglial inflammatory signaling represents a promisin…

The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets Open

S P H Alexander, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale , et al. · 2023

The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 600…

Identification of Small Molecule RGS10 Modulators in a Microglial Cell Model of Neuroinflammation Open

Stephanie González, Benita Sjögren · 2023

Discovery and Validation of RGS2-FBXO44 Protein-Protein Interaction Inhibitors Open

Sadikshya Aryal, Harrison J. McNabb, Benita Sjögren · 2023

Transcriptional Analysis of RGS10 Function in Microglia Open

Shwetal Talele, Stephanie González, Violeta Saldarriaga, Shelley B. Hooks, Benita Sjögren · 2023

Regulator of G protein signaling 2 inhibits Gαq-dependent uveal melanoma cell growth Open

Qian Zhang, Andrew J. Haak, Benita Sjögren · 2022

Activating mutations in Gα_q/11 are a major driver of uveal melanoma (UM), the most common intraocular cancer in adults. While progress has recently been made in targeting Gα_q/11 for UM therapy, the crucial role for th…

Roles of Cullin-RING Ubiquitin Ligases in Cardiovascular Diseases Open

Stephanie Diaz, Kankan Wang, Benita Sjögren, Xing Liu · 2022

Maintenance of protein homeostasis is crucial for virtually every aspect of eukaryotic biology. The ubiquitin-proteasome system (UPS) represents a highly regulated quality control machinery that protects cells from a variety of stress cond…

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Introduction and Other Protein Targets Open

S P H Alexander, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale , et al. · 2021

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasi…

Regulators of G protein Signaling (RGS) proteins in GtoPdb v.2021.2 Open

Katelin E. Ahlers‐Dannen, Mohammed Alqinyah, Christopher Bodle, Josephine Bou Dagher, Bandana Chakravarti , et al. · 2021

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 subuni…

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

Katelin E. Ahlers‐Dannen, Mohammed Alqinyah, Christopher Bodle, Josephine Bou Dagher, Bandana Chakravarti , et al. · 2020

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 subuni…

N-Terminal Targeting of Regulator of G Protein Signaling Protein 2 for F-Box Only Protein 44–Mediated Proteasomal Degradation Open

Harrison J. McNabb, Stephanie González, Christine S. Muli, Benita Sjögren · 2020

Regulators of G protein Signaling (RGS) proteins (version 2020.4) in the IUPHAR/BPS Guide to Pharmacology Database Open

Katelin E. Ahlers‐Dannen, Mohammed Alqinyah, Christopher Bodle, Josephine Bou Dagher, Bandana Chakravarti , et al. · 2020

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 subuni…

Emerging Roles for Regulator of G Protein Signaling 2 in (Patho)physiology Open

Harrison J. McNabb, Qian Zhang, Benita Sjögren · 2020

Regulators of G protein Signaling (RGS) proteins (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database Open

Mohammed Alqinyah, Christopher Bodle, Josephine Bou Dagher, Bandana Chakravarti, Shreoshi Pal Choudhuri , et al. · 2019

Regulators of G protein signalling (RGS) proteins display a common RGS domain that interacts with the GTP-bound Gα subunits of heterotrimeric G proteins, enhancing GTP hydrolysis by stabilising the transition state [29, 419, 418], leading …

FBXO44-mediated RGS2 protein degradation uniquely depends on a novel Cullin 4B/DDB1 E3 ligase complex Open

Benita Sjögren · 2018

Hypertension and heart failure are major health issues with a need to identify more effective treatments. Regulator of G protein Signaling 2 (RGS2) is highly expressed throughout the cardiovascular system and negatively regulates signaling…

Movement disorder in<i>GNAO1</i>encephalopathy associated with gain-of-function mutations Open

Huijie Feng, Benita Sjögren, Behirda Karaj, Vincent Shaw, Aysegul Gezer , et al. · 2017

Both LOF and GOF mutations in Gα_o (encoded by GNAO1) are associated with neurologic pathophysiology. There appears to be a strong predictive correlation between the in vitro biochemical phenotype and the clinical pattern …

Small Molecule Enhancement of 20S Proteasome Activity Targets Intrinsically Disordered Proteins Open

Corey L. Jones, Evert Njomen, Benita Sjögren, Thomas S. Dexheimer, Jetze J. Tepe · 2017

The 20S proteasome is the main protease for the degradation of oxidatively damaged and intrinsically disordered proteins. When accumulation of disordered or oxidatively damaged proteins exceeds proper clearance in neurons, imbalanced pathw…

Regulator of G protein signaling 2 is a key regulator of pancreatic β-cell mass and function Open

Huansheng Dong, Y Zhang, J Wang, D S Kim, Hongju Wu , et al. · 2017

Pancreatic β -cell death and dysfunction contributes to the pathogenesis of both type 1 and type 2 diabetes. We aimed to examine whether the regulator of G protein signaling protein 2 (RGS2), a multifunctional inhibitor of G protein-couple…

The evolution of regulators of G protein signalling proteins as drug targets – 20 years in the making: IUPHAR Review 21 Open

Benita Sjögren · 2017

Regulators of G protein signalling (RGS) proteins are celebrating the 20th anniversary of their discovery. The unveiling of this new family of negative regulators of G protein signalling in the mid‐1990s solved a persistent conundrum in th…

Chemerin-induced arterial contraction is Gi- and calcium-dependent Open

David J. Ferland, Emma S. Darios, Richard R. Neubig, Benita Sjögren, Nguyen Truong , et al. · 2016

Digoxin-Mediated Upregulation of RGS2 Protein Protects against Cardiac Injury Open

Benita Sjögren, Sergio Parra, Kevin B. Atkins, Behirda Karaj, Richard R. Neubig · 2016

FBXO44-Mediated Degradation of RGS2 Protein Uniquely Depends on a Cullin 4B/DDB1 Complex Open

Benita Sjögren, Steven Swaney, Richard R. Neubig · 2015

The ubiquitin-proteasome system for protein degradation plays a major role in regulating cell function and many signaling proteins are tightly controlled by this mechanism. Among these, Regulator of G Protein Signaling 2 (RGS2) is a target…

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