Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs

Common coupling map advances GPCR-G protein selectivity

(2022) Alexander S Hauser et al.   eLife

Development of conformational BRET biosensors that monitor ezrin, radixin and moesin activation in real-time

(2021) Kévin Leguay et al.   JOURNAL OF CELL SCIENCE

The G protein database, GproteinDb

(2021) Gáspár Pándy-Szekeres et al.   NUCLEIC ACIDS RESEARCH

TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome

(2020) Reid H. J. Olsen et al.   Nature Chemical Biology

Revealing the Activity of Trimeric G-proteins in Live Cells with a Versatile Biosensor Design

(2020) Marcin Maziarz et al.   CELL

Agonist-induced formation of unproductive receptor-G12complexes

(2020) Najeah Okashah et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The PAR2 inhibitor I-287 selectively targets Gαq and Gα12/13 signaling and has anti-inflammatory effects

(2020) Charlotte Avet et al.   Communications Biology

Biased Receptor Signaling in Drug Discovery

(2019) Terry Kenakin   PHARMACOLOGICAL REVIEWS

Bioluminescence resonance energy transfer–based imaging of protein–protein interactions in living cells

(2019) Hiroyuki Kobayashi et al.   Nature Protocols

Illuminating G-Protein-Coupling Selectivity of GPCRs

(2019) Asuka Inoue et al.   CELL

A dynamic and screening-compatible nanoluciferase-based complementation assay enables profiling of individual GPCR-G protein interactions

(2018) Céline Laschet et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Translating biased signaling in the ghrelin receptor system into differential in vivo functions

(2018) Franziska Mende et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Functional selectivity profiling of the angiotensin II type 1 receptor using pathway-wide BRET signaling sensors

(2018) Yoon Namkung et al.   Science Signaling

Conformational Profiling of the AT1 Angiotensin II Receptor Reflects Biased Agonism, G Protein Coupling, and Cellular Context

(2017) Dominic Devost et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Purinergic Receptor Transactivation by the β 2 -Adrenergic Receptor Increases Intracellular Ca 2+ in Nonexcitable Cells

(2017) Wayne Stallaert et al.   MOLECULAR PHARMACOLOGY

Trends in GPCR drug discovery: new agents, targets and indications

(2017) Alexander S. Hauser et al.   NATURE REVIEWS DRUG DISCOVERY

Activated G Protein GαsSamples Multiple Endomembrane Compartments

(2016) Brent R. Martin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET

(2016) Yoon Namkung et al.   Nature Communications

Exploring the Technology Landscape of 7TMR Drug Signaling Profiling

(2015) Arturo Mancini et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors

(2015) Ikuo Masuho et al.   Science Signaling

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

(2015) Ramona Schrage et al.   Nature Communications

Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors

(2015) Ikuo Masuho et al.   Science Signaling

The chemokine CXC4 and CC2 receptors form homo- and heterooligomers that can engage their signaling G-protein effectors and βarrestin

(2014) Sylvain Armando et al.   FASEB JOURNAL

Development and Characterization of Pepducins as Gs-biased Allosteric Agonists

(2014) Richard Carr et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Angiotensin II Type I and Prostaglandin F2α Receptors Cooperatively Modulate Signaling in Vascular Smooth Muscle Cells

(2014) Eugénie Goupil et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

PQ-69, a novel and selective adenosine A1 receptor antagonist with inverse agonist activity

(2014) Min Lu et al.   Purinergic Signalling

Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein

(2013) J. Quoyer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Reducing safety-related drug attrition: the use of in vitro pharmacological profiling

(2012) Joanne Bowes et al.   NATURE REVIEWS DRUG DISCOVERY

Differential  -Arrestin-Dependent Conformational Signaling and Cellular Responses Revealed by Angiotensin Analogs

(2012) B. Zimmerman et al.   Science Signaling

Expression of G protein-coupled receptors and related proteins in HEK293, AtT20, BV2, and N18 cell lines as revealed by microarray analysis

(2011) Brady K Atwood et al.   BMC GENOMICS

Plasma Membrane Association of p63 Rho Guanine Nucleotide Exchange Factor (p63RhoGEF) Is Mediated by Palmitoylation and Is Required for Basal Activity in Cells

(2011) Mohamed Aittaleb et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Multiplexing of Multicolor Bioluminescence Resonance Energy Transfer

(2010) Billy Breton et al.   BIOPHYSICAL JOURNAL

Functional Selectivity of Natural and Synthetic Prostaglandin EP4 Receptor Ligands

(2009) M. Leduc et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

(2009) M. Aittaleb et al.   MOLECULAR PHARMACOLOGY

Phosphorylation of Rap1GAP, a striatally enriched protein, by protein kinase A controls Rap1 activity and dendritic spine morphology

(2009) T. McAvoy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Heterotrimeric G protein activation by G-protein-coupled receptors

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