Targeting G protein-coupled receptor signalling by blocking G proteins

4-Hydroxynonenal-induced GPR109A (HCA2 receptor) activation elicits bipolar responses, Gαi -mediated anti-inflammatory effects and Gβγ -mediated cell death

(2018) Jaya Gautam et al.   BRITISH JOURNAL OF PHARMACOLOGY

G protein-coupled receptor kinases: Past, present and future

(2018) Konstantin E. Komolov et al.   CELLULAR SIGNALLING

Biased signalling: from simple switches to allosteric microprocessors

(2018) Jeffrey S. Smith et al.   NATURE REVIEWS DRUG DISCOVERY

APP/Go protein Gβγ-complex signaling mediates Aβ degeneration and cognitive impairment in Alzheimer's disease models

(2018) Elena Anahi Bignante et al.   NEUROBIOLOGY OF AGING

Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor

(2018) Sahil Gulati et al.   Nature Communications

Lack of beta-arrestin signaling in the absence of active G proteins

(2018) Manuel Grundmann et al.   Nature Communications

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex

(2018) Yi-Lynn Liang et al.   NATURE

Targeting nucleotide exchange to inhibit constitutively active G protein α subunits in cancer cells

(2018) Michael D. Onken et al.   Science Signaling

Signaling bias in drug discovery

(2017) Terry Kenakin   Expert Opinion on Drug Discovery

A disease-associated mutation in the adhesion GPCR BAI2 (ADGRB2 ) increases receptor signaling activity

(2017) Ryan H. Purcell et al.   HUMAN MUTATION

Involvement of Gβγ subunits of Giprotein coupled with S1P receptor on multivesicular endosomes in F-actin formation and cargo sorting into exosomes

(2017) Taketoshi Kajimoto et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

TRV0109101, a G Protein-Biased Agonist of the µ -Opioid Receptor, Does Not Promote Opioid-Induced Mechanical Allodynia following Chronic Administration

(2017) Michael Koblish et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Pharmacological and Activated Fibroblast Targeting of Gβγ-GRK2 After Myocardial Ischemia Attenuates Heart Failure Progression

(2017) Joshua G. Travers et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Gβγ subunit activation promotes dopamine efflux through the dopamine transporter

(2017) J Garcia-Olivares et al.   MOLECULAR PSYCHIATRY

Phase-plate cryo-EM structure of a class B GPCR–G-protein complex

(2017) Yi-Lynn Liang et al.   NATURE

Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein

(2017) Yan Zhang et al.   NATURE

WD40 repeat domain proteins: a novel target class?

(2017) Matthieu Schapira et al.   NATURE REVIEWS DRUG DISCOVERY

The Diverse Roles of Arrestin Scaffolds in G Protein–Coupled Receptor Signaling

(2017) Yuri K. Peterson et al.   PHARMACOLOGICAL REVIEWS

Genetic evidence that β-arrestins are dispensable for the initiation of β2-adrenergic receptor signaling to ERK

(2017) Morgan O’Hayre et al.   Science Signaling

Targeted inhibition of G q signaling induces airway relaxation in mouse models of asthma

(2017) Michaela Matthey et al.   Science Translational Medicine

Inhibiting G protein βγ signaling blocks prostate cancer progression and enhances the efficacy of paclitaxel

(2017) Prakash Paudyal et al.   Oncotarget

Sonic Hedgehog Activates Phospholipase A2 to Enhance Smoothened Ciliary Translocation

(2017) Angela M. Arensdorf et al.   Cell Reports

Genetic evidence that β-arrestins are dispensable for the initiation of β2-adrenergic receptor signaling to ERK

(2017) Morgan O’Hayre et al.   Science Signaling

A randomized, Phase IIb study investigating oliceridine (TRV130), a novel µ-receptor G-protein pathway selective (µ-GPS) modulator, for the management of moderate to severe acute pain following abdominoplasty

(2017) Neil Singla et al.   Journal of Pain Research

On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin

(2016) Zhan-Guo Gao et al.   BIOCHEMICAL PHARMACOLOGY

Potent and Selective Peptide-based Inhibition of the G Protein Gαq

(2016) Thomas H. Charpentier et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeted Elimination of G Proteins and Arrestins Defines Their Specific Contributions to Both Intensity and Duration of G Protein-coupled Receptor Signaling

(2016) Elisa Alvarez-Curto et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Protein Kinase D and Gβγ Subunits Mediate Agonist-evoked Translocation of Protease-activated Receptor-2 from the Golgi Apparatus to the Plasma Membrane

(2016) Dane D. Jensen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

G Protein–Coupled Receptor-G–Proteinβγ–Subunit Signaling Mediates Renal Dysfunction and Fibrosis in Heart Failure

(2016) Fadia A. Kamal et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

β-Arrestin drives MAP kinase signalling from clathrin-coated structures after GPCR dissociation

(2016) K. Eichel et al.   NATURE CELL BIOLOGY

Total synthesis and structure–activity relationship studies of a series of selective G protein inhibitors

(2016) Xiao-Feng Xiong et al.   Nature Chemistry

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

Loss of epithelial Gq and G11 signaling inhibits TGF  production but promotes IL-33-mediated macrophage polarization and emphysema

(2016) A. E. John et al.   Science Signaling

Dynamic regulation of neutrophil polarity and migration by the heterotrimeric G protein subunits Gαi-GTP and Gβγ

(2016) Chinmay R. Surve et al.   Science Signaling

PREX1 integrates G protein-coupled receptor and phosphoinositide 3-kinase signaling to promote glioblastoma invasion

(2016) Alexander Gont et al.   Oncotarget

Loss of epithelial Gq and G11 signaling inhibits TGF  production but promotes IL-33-mediated macrophage polarization and emphysema

(2016) A. E. John et al.   Science Signaling

Dynamic regulation of neutrophil polarity and migration by the heterotrimeric G protein subunits Gαi-GTP and Gβγ

(2016) Chinmay R. Surve et al.   Science Signaling

Inhibition of G Protein βγ Subunit Signaling Abrogates Nephritis in Lupus-Prone Mice

(2016) Javier Rangel-Moreno et al.   Arthritis & Rheumatology

Endothelial Gαq/11is required for VEGF-induced vascular permeability and angiogenesis

(2015) Kishor K. Sivaraj et al.   CARDIOVASCULAR RESEARCH

P2Y2 and Gq/G11 control blood pressure by mediating endothelial mechanotransduction

(2015) ShengPeng Wang et al.   JOURNAL OF CLINICAL INVESTIGATION

Repeated Mu-Opioid Exposure Induces a Novel Form of the Hyperalgesic Priming Model for Transition to Chronic Pain

(2015) D. Araldi et al.   JOURNAL OF NEUROSCIENCE

G protein βγ subunits regulate cardiomyocyte hypertrophy through a perinuclear Golgi phosphatidylinositol 4-phosphate hydrolysis pathway

(2015) S. Malik et al.   MOLECULAR BIOLOGY OF THE CELL

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia

(2015) Florian Grebien et al.   Nature Chemical Biology

Toward the Selective Inhibition of G Proteins: Total Synthesis of a Simplified YM-254890 Analog

(2015) Derek T. Rensing et al.   ORGANIC LETTERS

Structural basis for nucleotide exchange in heterotrimeric G proteins

(2015) R. O. Dror et al.   SCIENCE

The experimental power of FR900359 to study Gq-regulated biological processes

(2015) Ramona Schrage et al.   Nature Communications

Inhibition of G-Protein βγ Signaling Enhances T Cell Receptor-Stimulated Interleukin 2 Transcription in CD4+ T Helper Cells

(2015) Evan A. Yost et al.   PLoS One

Gαq signalling: The new and the old

(2014) Guzmán Sánchez-Fernández et al.   CELLULAR SIGNALLING

Simultaneous Adrenal and Cardiac G-Protein–Coupled Receptor-G βγ Inhibition Halts Heart Failure Progression

(2014) Fadia A. Kamal et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

G-protein stimulatory subunit alpha and Gq/11α G-proteins are both required to maintain quiescent stem-like chondrocytes

(2014) Andrei S. Chagin et al.   Nature Communications

Inhibition of Gβγ-subunit signaling potentiates morphine-induced antinociception but not respiratory depression, constipation, locomotion, and reward

(2013) Michelle R. Hoot et al.   BEHAVIOURAL PHARMACOLOGY

Phospholipase Cε Hydrolyzes Perinuclear Phosphatidylinositol 4-Phosphate to Regulate Cardiac Hypertrophy

(2013) Lianghui Zhang et al.   CELL

Structural insights into G protein-coupled receptor kinase function

(2013) Kristoff T Homan et al.   CURRENT OPINION IN CELL BIOLOGY

Gq Rather than G11 Preferentially Mediates Nociceptor Sensitization

(2013) Laura Nikita Wirotanseng et al.   Molecular Pain

X-ray structure of the mammalian GIRK2–βγ G-protein complex

(2013) Matthew R. Whorton et al.   NATURE

Conformational biosensors reveal GPCR signalling from endosomes

(2013) Roshanak Irannejad et al.   NATURE

Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction

(2013) Yuri Bolshan et al.   ACS Medicinal Chemistry Letters

Mammalian Phospholipase C

(2012) Ganesh Kadamur et al.   Annual Review of Physiology

All G protein βγ complexes are capable of translocation on receptor activation

(2012) W.K. Ajith Karunarathne et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Protein Kinase C (PKC)ζ-mediated GαqStimulation of ERK5 Protein Pathway in Cardiomyocytes and Cardiac Fibroblasts

(2012) Carlota García-Hoz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Genome-wide RNAi Screen Reveals a Trio-Regulated Rho GTPase Circuitry Transducing Mitogenic Signals Initiated by G Protein-Coupled Receptors

(2012) Jose P. Vaqué et al.   MOLECULAR CELL

G-protein signaling leverages subunit-dependent membrane affinity to differentially control    translocation to intracellular membranes

(2012) P. R. O'Neill et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

P2Y12 receptors in platelets and other hematopoietic and non-hematopoietic cells

(2012) Christian Gachet   Purinergic Signalling

p63RhoGEF: A New Switch for Gq-Mediated Activation of Smooth Muscle

(2012) Ko Momotani et al.   TRENDS IN CARDIOVASCULAR MEDICINE

Direct-reversible binding of small molecules to G protein βγ subunits

(2011) A.M.P.B. Seneviratne et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

G-protein βγ subunits in vasorelaxing and anti-endothelinergic effects of calcitonin gene-related peptide

(2011) MJPMT Meens et al.   BRITISH JOURNAL OF PHARMACOLOGY

Alteration of Golgi structure in senescent cells and its regulation by a G protein γ subunit

(2011) Joon-Ho Cho et al.   CELLULAR SIGNALLING

Mechanism of Activation and Inactivation of Gq/Phospholipase C-β Signaling Nodes

(2011) T. Kendall Harden et al.   CHEMICAL REVIEWS

p63RhoGEF Couples G αq/11 -Mediated Signaling to Ca 2+ Sensitization of Vascular Smooth Muscle Contractility

(2011) Ko Momotani et al.   CIRCULATION RESEARCH

A Critical Role of Gβγ in Tumorigenesis and Metastasis of Breast Cancer

(2011) Xiaoyun Tang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synergistic Roles for G-protein γ3and γ7Subtypes in Seizure Susceptibility as Revealed in Double Knock-out Mice

(2011) William F. Schwindinger et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Understanding Molecular Recognition by G protein    Subunits on the Path to Pharmacological Targeting

(2011) Y. Lin et al.   MOLECULAR PHARMACOLOGY

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Small Molecule Disruption of Gβγ Signaling Inhibits the Progression of Heart Failure

(2010) Liam M. Casey et al.   CIRCULATION RESEARCH

Synergistic Activation of Phospholipase C-β3 by Gαq and Gβγ Describes a Simple Two-State Coincidence Detector

(2010) Finly Philip et al.   CURRENT BIOLOGY

Regulation of Constitutive Cargo Transport from thetrans-Golgi Network to Plasma Membrane by Golgi-localized G Protein βγ Subunits

(2010) Roshanak Irannejad et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synergistic Ca2+Responses by Gαi- and Gαq-coupled G-protein-coupled Receptors Require a Single PLCβ Isoform That Is Sensitive to Both Gβγ and Gαq

(2010) Robert A. Rebres et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

GαqActs as an Adaptor Protein in Protein Kinase Cζ (PKCζ)-mediated ERK5 Activation by G Protein-coupled Receptors (GPCR)

(2010) Carlota García-Hoz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

GRK2 as a novel gene therapy target in heart failure

(2010) Giuseppe Rengo et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

G   Signaling Promotes Breast Cancer Cell Migration and Invasion

(2010) J. K. Kirui et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Mutations inGNA11in Uveal Melanoma

(2010) Catherine D. Van Raamsdonk et al.   NEW ENGLAND JOURNAL OF MEDICINE

Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule

(2010) A. Nishimura et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Supraspinal Gβγ-dependent stimulation of PLCβ3originating from G inhibitory protein-μ opioid receptor-coupling is necessary for morphine induced acute hyperalgesia

(2009) Enrica Bianchi et al.   JOURNAL OF NEUROCHEMISTRY

Structure and Function of Heterotrimeric G Protein-Regulated Rho Guanine Nucleotide Exchange Factors

(2009) M. Aittaleb et al.   MOLECULAR PHARMACOLOGY

Sustained cyclic AMP production by parathyroid hormone receptor endocytosis

(2009) Sébastien Ferrandon et al.   Nature Chemical Biology

G protein βγ subunits: Central mediators of G protein-coupled receptor signaling

(2008) A. V. Smrcka   CELLULAR AND MOLECULAR LIFE SCIENCES

A Novel G  -Subunit Inhibitor Selectively Modulates  -Opioid-Dependent Antinociception and Attenuates Acute Morphine-Induced Antinociceptive Tolerance and Dependence

(2008) J. L. Mathews et al.   JOURNAL OF NEUROSCIENCE

Frequent somatic mutations of GNAQ in uveal melanoma and blue naevi

(2008) Catherine D. Van Raamsdonk et al.   NATURE

A new type of ERK1/2 autophosphorylation causes cardiac hypertrophy

(2008) Kristina Lorenz et al.   NATURE MEDICINE

Heterotrimeric G protein activation by G-protein-coupled receptors

(2007) William M. Oldham et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY