Quantitative assessment of constitutive G protein–coupled receptor activity with BRET-based G protein biosensors

Cryo-EM structure of constitutively active human Frizzled 7 in complex with heterotrimeric Gs

(2021) Lu Xu et al.   CELL RESEARCH

Residue 6.43 defines receptor function in class F GPCRs

(2021) Ainoleena Turku et al.   Nature Communications

Constitutive activity of a G protein-coupled receptor, DRD1, contributes to human cerebral organoid formation

(2020) Qinying Wang et al.   STEM CELLS

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

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

Development of a Conformational Histamine H3 Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists

(2020) Hannes Schihada et al.   ACS Sensors

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

(2020) Marcin Maziarz et al.   CELL

Re‐examining the ‘Dissociation Model’ of G protein activation from the perspective of Gβγ signaling

(2020) Yin Kwan Chung et al.   FEBS Journal

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

Illuminating G-Protein-Coupling Selectivity of GPCRs

(2019) Asuka Inoue et al.   CELL

Probing thermostability of detergent-solubilized CB2 receptor by parallel G protein-activation and ligand-binding assays

(2019) Ryan L Beckner et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The constitutive activity of melanocortin‐4 receptors in cAMP pathway is allosterically modulated by zinc and copper ions

(2019) Reet Link et al.   JOURNAL OF NEUROCHEMISTRY

β-Arrestin-2 BRET Biosensors Detect Different β-Arrestin-2 Conformations in Interaction with GPCRs

(2019) Atsuro Oishi et al.   ACS Sensors

Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor

(2018) Maarten L.J. Doornbos et al.   BIOCHEMICAL PHARMACOLOGY

Towards a better understanding of the cannabinoid-related orphan receptors GPR3, GPR6, and GPR12

(2018) Paula Morales et al.   DRUG METABOLISM REVIEWS

Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

(2018) Qingwen Wan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

G Protein-Coupled Receptors as Targets for Approved Drugs: How Many Targets and How Many Drugs?

(2018) Krishna Sriram et al.   MOLECULAR PHARMACOLOGY

A FRET-based biosensor for measuring Gα13 activation in single cells

(2018) Marieke Mastop et al.   PLoS One

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

(2018) Yoon Namkung et al.   Science Signaling

Development of novel biosensors to study receptor-mediated activation of the G-protein α subunits Gsand Golf

(2017) Hideaki Yano et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A subcellular map of the human proteome

(2017) Peter J. Thul et al.   SCIENCE

The HCMV US28 vGPCR induces potent Gαq/PLC-β signaling in monocytes leading to increased adhesion to endothelial cells

(2016) Shu-en Wu et al.   VIROLOGY

A New Generation of FRET Sensors for Robust Measurement of Gαi1, Gαi2 and Gαi3 Activation Kinetics in Single Cells

(2016) Jakobus van Unen et al.   PLoS One

Probing Gαi1 protein activation at single–amino acid resolution

(2015) Dawei Sun et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structural basis for nucleotide exchange in heterotrimeric G proteins

(2015) R. O. Dror et al.   SCIENCE

Probing Gαi1 protein activation at single–amino acid resolution

(2015) Dawei Sun et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Fourth-Generation Epac-Based FRET Sensors for cAMP Feature Exceptional Brightness, Photostability and Dynamic Range: Characterization of Dedicated Sensors for FLIM, for Ratiometry and with High Affinity

(2015) Jeffrey Klarenbeek et al.   PLoS One

Constitutive Activity among Orphan Class-A G Protein Coupled Receptors

(2015) Adam L. Martin et al.   PLoS One

Inverse Agonism of SQ 29,548 and Ramatroban on Thromboxane A2 Receptor

(2014) Raja Chakraborty et al.   PLoS One

The vital role of constitutive GPCR activity in the mesolimbic dopamine system

(2014) F J Meye et al.   Translational Psychiatry

Engineered Luciferase Reporter from a Deep Sea Shrimp Utilizing a Novel Imidazopyrazinone Substrate

(2012) Mary P. Hall et al.   ACS Chemical Biology

Deciphering biased-agonism complexity reveals a new active AT1 receptor entity

(2012) Aude Saulière et al.   Nature Chemical Biology

Site-Directed Mutations and the Polymorphic Variant Ala160Thr in the Human Thromboxane Receptor Uncover a Structural Role for Transmembrane Helix 4

(2012) Raja Chakraborty et al.   PLoS One

Real-time visualization of heterotrimeric G protein Gq activation in living cells

(2011) Merel JW Adjobo-Hermans et al.   BMC BIOLOGY

Functional Selective Oxytocin-derived Agonists Discriminate between Individual G Protein Family Subtypes

(2011) Marta Busnelli et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Conformational changes in the G protein Gs induced by the β2 adrenergic receptor

(2011) Ka Young Chung et al.   NATURE

Structural and Functional Analysis of the C-Terminus of Gαq in Complex with the Human Thromboxane A2Receptor Provides Evidence of Constitutive Activity

(2010) Annirudha Chillar et al.   BIOCHEMISTRY

On the roles of Mg in the activation of G proteins

(2010) Lutz Birnbaumer et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Constitutive Activity of the Cannabinoid CB1 Receptor Regulates the Function of Co-expressed Mu Opioid Receptors

(2008) Meritxell Canals et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Constitutive Activity at the Cannabinoid CB1 Receptor Is Required for Behavioral Response to Noxious Chemical Stimulation of TRPV1: Antinociceptive Actions of CB1 Inverse Agonists

(2008) B. Fioravanti et al.   JOURNAL OF NEUROSCIENCE

Dissociation of Heterotrimeric G Proteins in Cells

(2008) N. A. Lambert   Science Signaling