Mechanisms of signalling and biased agonism in G protein-coupled receptors

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy

(2018) Emma Dal Maso et al.   BIOCHEMICAL PHARMACOLOGY

Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor

(2018) Tao Che et al.   CELL

5-HT 2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology

(2018) Yao Peng et al.   CELL

Pharmacogenomics of GPCR Drug Targets

(2018) Alexander S. Hauser et al.   CELL

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

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

Biased Agonism in Drug Discovery—Is It Too Soon to Choose a Path?

(2018) Martin C. Michel et al.   MOLECULAR PHARMACOLOGY

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

(2018) Krishna Sriram et al.   MOLECULAR PHARMACOLOGY

Subcellular localization of MC4R with ADCY3 at neuronal primary cilia underlies a common pathway for genetic predisposition to obesity

(2018) Jacqueline E. Siljee et al.   NATURE GENETICS

Biased signalling: from simple switches to allosteric microprocessors

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

Understanding the diversity of membrane lipid composition

(2018) Takeshi Harayama et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The use of chemogenetic approaches to study the physiological roles of muscarinic acetylcholine receptors in the central nervous system

(2018) Sophie J. Bradley et al.   NEUROPHARMACOLOGY

Structural biology of GABA B receptor

(2018) Aurel Frangaj et al.   NEUROPHARMACOLOGY

Sortase ligation enables homogeneous GPCR phosphorylation to reveal diversity in β-arrestin coupling

(2018) Dean P. Staus et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Spatial Intensity Distribution Analysis: Studies of G Protein-Coupled Receptor Oligomerisation

(2018) John D. Pediani et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Phosphorylation-induced conformation of β2-adrenoceptor related to arrestin recruitment revealed by NMR

(2018) Yutaro Shiraishi et al.   Nature Communications

Evidence for functional pre-coupled complexes of receptor heteromers and adenylyl cyclase

(2018) Gemma Navarro et al.   Nature Communications

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

(2018) Manuel Grundmann et al.   Nature Communications

Structural insights into G-protein-coupled receptor allostery

(2018) David M. Thal et al.   NATURE

Structure of the glucagon receptor in complex with a glucagon analogue

(2018) Haonan Zhang et al.   NATURE

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

(2018) Yi-Lynn Liang et al.   NATURE

Type 2 diabetes–associated variants of the MT2melatonin receptor affect distinct modes of signaling

(2018) Angeliki Karamitri et al.   Science Signaling

Coexpressed Class B G Protein–Coupled Secretin and GLP-1 Receptors Self- and Cross-Associate: Impact on Pancreatic Islets

(2017) Kaleeckal G. Harikumar et al.   ENDOCRINOLOGY

The activity of the serotonin receptor 2C is regulated by alternative splicing

(2017) Stefan Stamm et al.   HUMAN GENETICS

Lipid stress inhibits endocytosis of melanocortin-4 receptor from modified clathrin-enriched sites and impairs receptor desensitization

(2017) Kimberly A. Cooney et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Heterologous phosphorylation–induced formation of a stability lock permits regulation of inactive receptors by β-arrestins

(2017) András D. Tóth et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The GPRC6A receptor displays constitutive internalization and sorting to the slow recycling pathway

(2017) Stine Engesgaard Jacobsen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Lymphoid differentiation of hematopoietic stem cells requires efficient Cxcr4 desensitization

(2017) Christelle Freitas et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Systematic protein–protein interaction mapping for clinically relevant human GPCRs

(2017) Kate Sokolina et al.   Molecular Systems Biology

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

(2017) Yi-Lynn Liang et al.   NATURE

Selectivity determinants of GPCR–G-protein binding

(2017) Tilman Flock et al.   NATURE

Single-molecule analysis of ligand efficacy in β2AR–G-protein activation

(2017) G. Glenn Gregorio et al.   NATURE

Crystal structure of the GLP-1 receptor bound to a peptide agonist

(2017) Ali Jazayeri et al.   NATURE

Structure of the full-length glucagon class B G-protein-coupled receptor

(2017) Haonan Zhang et al.   NATURE

Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators

(2017) Gaojie Song et al.   NATURE

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

(2017) Yan Zhang et al.   NATURE

Functional selectivity of GPCR-directed drug action through location bias

(2017) Roshanak Irannejad et al.   Nature Chemical Biology

A kinetic view of GPCR allostery and biased agonism

(2017) J Robert Lane et al.   Nature Chemical Biology

Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs

(2017) John D McCorvy et al.   Nature Chemical Biology

Membrane curvature regulates ligand-specific membrane sorting of GPCRs in living cells

(2017) Kadla R Rosholm et al.   Nature Chemical Biology

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

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

Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders

(2017) Daniel J. Foster et al.   NEURON

Molecular insights into allosteric modulation of Class C G protein-coupled receptors

(2017) Katie Leach et al.   PHARMACOLOGICAL RESEARCH

An update on the physiological and therapeutic relevance of GPCR oligomers

(2017) Batoul Farran   PHARMACOLOGICAL RESEARCH

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

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

Priming GPCR signaling through the synergistic effect of two G proteins

(2017) Tejas M. Gupte et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

GPCRs globally coevolved with receptor activity-modifying proteins, RAMPs

(2017) Shahar Barbash et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Endosomal signaling of the receptor for calcitonin gene-related peptide mediates pain transmission

(2017) Rebecca E. Yarwood et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Distinct conformations of GPCR–β-arrestin complexes mediate desensitization, signaling, and endocytosis

(2017) Thomas J. Cahill et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dual role of mitochondria in producing melatonin and driving GPCR signaling to block cytochrome c release

(2017) Yalikun Suofu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief

(2017) Dane D. Jensen et al.   Science Translational Medicine

Extending the Structural View of Class B GPCRs

(2017) Chris de Graaf et al.   TRENDS IN BIOCHEMICAL SCIENCES

Novel Structural Insights into GPCR–β-Arrestin Interaction and Signaling

(2017) Ravi Ranjan et al.   TRENDS IN CELL BIOLOGY

Evolutionary action and structural basis of the allosteric switch controlling β2AR functional selectivity

(2017) Anne-Marie Schönegge et al.   Nature Communications

A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling

(2017) Alexandre Beautrait et al.   Nature Communications

Amino acid metabolites that regulate G protein signaling during osmotic stress

(2017) James P. Shellhammer et al.   PLoS Genetics

Intracellular Angiotensin‐II Interacts With Nuclear Angiotensin Receptors in Cardiac Fibroblasts and Regulates RNA Synthesis, Cell Proliferation, and Collagen Secretion

(2017) Artavazd Tadevosyan et al.   Journal of the American Heart Association

Receptor Activity-Modifying Proteins (RAMPs): New Insights and Roles

(2016) Debbie L. Hay et al.   Annual Review of Pharmacology and Toxicology

G Protein–Coupled Receptor Heteromers

(2016) Ivone Gomes et al.   Annual Review of Pharmacology and Toxicology

Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor

(2016) Denise Wootten et al.   BIOCHEMICAL PHARMACOLOGY

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor

(2016) Georgina L. Thompson et al.   BIOCHEMICAL PHARMACOLOGY

Compartmentalization of GPCR signalling controls unique cellular responses

(2016) Andrew M. Ellisdon et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

White matter integrity in individuals at ultra-high risk for psychosis: a systematic review and discussion of the role of polyunsaturated fatty acids

(2016) Nandita Vijayakumar et al.   BMC Psychiatry

GPCR-G Protein-β-Arrestin Super-Complex Mediates Sustained G Protein Signaling

(2016) Alex R.B. Thomsen et al.   CELL

Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy

(2016) Sebastian George Barton Furness et al.   CELL

The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

(2016) Denise Wootten et al.   CELL

Theoretical Aspects of GPCR–Ligand Complex Pharmacology

(2016) Terry Kenakin   CHEMICAL REVIEWS

GPCR Dynamics: Structures in Motion

(2016) Naomi R. Latorraca et al.   CHEMICAL REVIEWS

Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

(2016) Denise Wootten et al.   CHEMICAL REVIEWS

Beneficial effects of β-sitosterol on type 1 cholecystokinin receptor dysfunction induced by elevated membrane cholesterol

(2016) Aditya J. Desai et al.   CLINICAL NUTRITION

Membrane potentials regulating GPCRs: insights from experiments and molecular dynamics simulations

(2016) Owen N Vickery et al.   CURRENT OPINION IN PHARMACOLOGY

Newly synthesized cAMP is integrated at a membrane protein complex signalosome to ensure receptor response specificity

(2016) Raquel Guinzberg et al.   FEBS Journal

The conformational signature of β-arrestin2 predicts its trafficking and signalling functions

(2016) Mi-Hye Lee et al.   NATURE

Allosteric coupling from G protein to the agonist-binding pocket in GPCRs

(2016) Brian T. DeVree et al.   NATURE

β-Arrestin biosensors reveal a rapid, receptor-dependent activation/deactivation cycle

(2016) Susanne Nuber et al.   NATURE

Extra-helical binding site of a glucagon receptor antagonist

(2016) Ali Jazayeri et al.   NATURE

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

β2-adrenergic receptor control of endosomal PTH receptor signaling via Gβγ

(2016) Frédéric G Jean-Alphonse et al.   Nature Chemical Biology

DREADDs for Neuroscientists

(2016) Bryan L. Roth   NEURON

Gβγ subunits—Different spaces, different faces

(2016) Shahriar M. Khan et al.   PHARMACOLOGICAL RESEARCH

Plasma membrane localization of the μ-opioid receptor controls spatiotemporal signaling

(2016) Michelle L. Halls et al.   Science Signaling

Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria

(2016) Tarsis F. Brust et al.   Science Signaling

New Technologies for Elucidating Opioid Receptor Function

(2016) Michael R. Bruchas et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

The role of kinetic context in apparent biased agonism at GPCRs

(2016) Carmen Klein Herenbrink et al.   Nature Communications

Structural mechanism of ligand activation in human calcium-sensing receptor

(2016) Yong Geng et al.   eLife

Plasma membrane localization of the μ-opioid receptor controls spatiotemporal signaling

(2016) Michelle L. Halls et al.   Science Signaling

Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria

(2016) Tarsis F. Brust et al.   Science Signaling

Basic Pharmacological and Structural Evidence for Class A G-Protein-Coupled Receptor Heteromerization

(2016) Rafael Franco et al.   Frontiers in Pharmacology

Cardiac myosin light chain phosphorylation and inotropic effects of a biased ligand, TRV120023, in a dilated cardiomyopathy model

(2015) Madhusudhan Tarigopula et al.   CARDIOVASCULAR RESEARCH

Structural Insights into the Dynamic Process of β 2 -Adrenergic Receptor Signaling

(2015) Aashish Manglik et al.   CELL

Effects of endocytosis on receptor-mediated signaling

(2015) Roshanak Irannejad et al.   CURRENT OPINION IN CELL BIOLOGY

G Protein-coupled Receptor (GPCR) Signaling via Heterotrimeric G Proteins from Endosomes

(2015) Nikoleta G. Tsvetanova et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Universal allosteric mechanism for Gα activation by GPCRs

(2015) Tilman Flock et al.   NATURE

PTH receptor-1 signalling—mechanistic insights and therapeutic prospects

(2015) Ross W. Cheloha et al.   Nature Reviews Endocrinology

Convergent evidence for mGluR5 in synaptic and neuroinflammatory pathways implicated in ASD

(2015) Daniela Zantomio et al.   NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS

Buried ionizable networks are an ancient hallmark of G protein-coupled receptor activation

(2015) Daniel G. Isom et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural basis for nucleotide exchange in heterotrimeric G proteins

(2015) R. O. Dror et al.   SCIENCE

Structural basis for chemokine recognition and activation of a viral G protein-coupled receptor

(2015) J. S. Burg et al.   SCIENCE

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics

(2014) A E Cook et al.   BRITISH JOURNAL OF PHARMACOLOGY

Structured and disordered facets of the GPCR fold

(2014) AJ Venkatakrishnan et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Endothelin-converting Enzyme 1 and β-Arrestins Exert Spatiotemporal Control of Substance P-induced Inflammatory Signals

(2014) Dane D. Jensen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Visualization of arrestin recruitment by a G-protein-coupled receptor

(2014) Arun K. Shukla et al.   NATURE

Endosomal generation of cAMP in GPCR signaling

(2014) Jean-Pierre Vilardaga et al.   Nature Chemical Biology

Major ligand-induced rearrangement of the heptahelical domain interface in a GPCR dimer

(2014) Li Xue et al.   Nature Chemical Biology

Spatial encoding of cyclic AMP signaling specificity by GPCR endocytosis

(2014) Nikoleta G Tsvetanova et al.   Nature Chemical Biology

The Dynamic Process of β2-Adrenergic Receptor Activation

(2013) Rie Nygaard et al.   CELL

Inhibitory Mechanism of an Allosteric Antibody Targeting the Glucagon Receptor

(2013) Susmith Mukund et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Regulation of cardiac nitric oxide signaling by nuclear β-adrenergic and endothelin receptors

(2013) George Vaniotis et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

Caveolin-3 regulates compartmentation of cardiomyocyte beta2-adrenergic receptor-mediated cAMP signaling

(2013) Peter T. Wright et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

Structure of class B GPCR corticotropin-releasing factor receptor 1

(2013) Kaspar Hollenstein et al.   NATURE

Structural mechanism of ligand activation in human GABAB receptor

(2013) Yong Geng et al.   NATURE

Structure of the human glucagon class B G-protein-coupled receptor

(2013) Fai Yiu Siu et al.   NATURE

Molecular signatures of G-protein-coupled receptors

(2013) A. J. Venkatakrishnan et al.   NATURE

Caveolae as plasma membrane sensors, protectors and organizers

(2013) Robert G. Parton et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations

(2013) D. Wootten et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Noncanonical GPCR signaling arising from a PTH receptor–arrestin–Gβγ complex

(2013) Vanessa L. Wehbi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

TRV120027, a Novel β-Arrestin Biased Ligand at the Angiotensin II Type I Receptor, Unloads the Heart and Maintains Renal Function When Added to Furosemide in Experimental Heart Failure

(2012) Guido Boerrigter et al.   Circulation-Heart Failure

Plasticity of Surface Structures and β 2 -Adrenergic Receptor Localization in Failing Ventricular Cardiomyocytes During Recovery From Heart Failure

(2012) Alexander R. Lyon et al.   Circulation-Heart Failure

Agonist-bound structures of G protein-coupled receptors

(2012) Guillaume Lebon et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Adenylyl cyclase AC8 directly controls its micro-environment by recruiting the actin cytoskeleton in a cholesterol-rich milieu

(2012) Laura J. Ayling et al.   JOURNAL OF CELL SCIENCE

Modulation of the Interaction between Neurotensin Receptor NTS1 and Gq Protein by Lipid

(2012) Sayaka Inagaki et al.   JOURNAL OF MOLECULAR BIOLOGY

Cholesterol increases kinetic, energetic, and mechanical stability of the human  2-adrenergic receptor

(2012) M. Zocher et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Molecular basis for negative regulation of the glucagon receptor

(2012) C. M. Koth et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery

(2012) K. G. Harikumar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Biased Signaling Pathways in  2-Adrenergic Receptor Characterized by 19F-NMR

(2012) J. J. Liu et al.   SCIENCE

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

(2011) Celine Valant et al.   Annual Review of Pharmacology and Toxicology

Activation mechanism of the  2-adrenergic receptor

(2011) R. O. Dror et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Distinct Phosphorylation Sites on the  2-Adrenergic Receptor Establish a Barcode That Encodes Differential Functions of  -Arrestin

(2011) K. N. Nobles et al.   Science Signaling

Diversity and modularity of G protein-coupled receptor structures

(2011) Vsevolod Katritch et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Sub-picomolar relaxin signalling by a pre-assembled RXFP1, AKAP79, AC2, β-arrestin 2, PDE4D3 complex

(2010) Michelle L Halls et al.   EMBO JOURNAL

Site-specific Phosphorylation of CXCR4 Is Dynamically Regulated by Multiple Kinases and Results in Differential Modulation of CXCR4 Signaling

(2010) John M. Busillo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Differential G-protein-coupled Receptor Phosphorylation Provides Evidence for a Signaling Bar Code

(2010) Adrian J. Butcher et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Fluorescence Resonance Energy Transfer-based M2Muscarinic Receptor Sensor Reveals Rapid Kinetics of Allosteric Modulation

(2010) Monika Maier-Peuschel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

 2-Adrenergic Receptor Redistribution in Heart Failure Changes cAMP Compartmentation

(2010) V. O. Nikolaev et al.   SCIENCE

Selective engagement of G protein coupled receptor kinases (GRKs) encodes distinct functions of biased ligands

(2009) D. A. Zidar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Fluorescence Resonance Energy Transfer Analysis of  2a-Adrenergic Receptor Activation Reveals Distinct Agonist-Specific Conformational Changes

(2008) A. Zurn et al.   MOLECULAR PHARMACOLOGY