Structure and function of G protein-coupled receptor oligomers: implications for drug discovery

High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875

(2014) Ankita Srivastava et al.   NATURE

Agonist-bound structure of the human P2Y12 receptor

(2014) Jin Zhang et al.   NATURE

Structure of the human P2Y12 receptor in complex with an antithrombotic drug

(2014) Kaihua Zhang et al.   NATURE

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

Differential Stability of the Crystallographic Interfaces of Mu- and Kappa-Opioid Receptors

(2014) Jennifer M. Johnston et al.   PLoS One

Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution inEscherichia coli

(2014) Pascal Egloff et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

(2014) H. Wu et al.   SCIENCE

Determining the Oligomeric Structure of Proteorhodopsin by Gd3+-Based Pulsed Dipolar Spectroscopy of Multiple Distances

(2014) Devin T. Edwards et al.   STRUCTURE

Transmembrane Protein Activation Refined by Site-Specific Hydration Dynamics

(2013) Sunyia Hussain et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Druggable Genome: Evaluation of Drug Targets in Clinical Trials Suggests Major Shifts in Molecular Class and Indication

(2013) Mathias Rask-Andersen et al.   Annual Review of Pharmacology and Toxicology

Double Electron–Electron Resonance Probes Ca2+-Induced Conformational Changes and Dimerization of Recoverin

(2013) William K. Myers et al.   BIOCHEMISTRY

Structural features of the apelin receptor N-terminal tail and first transmembrane segment implicated in ligand binding and receptor trafficking

(2013) David N. Langelaan et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Structural Insight into Proteorhodopsin Oligomers

(2013) Katherine M. Stone et al.   BIOPHYSICAL JOURNAL

Simultaneous method for analyzing dimerization and signaling of G-protein-coupled receptor in yeast by dual-color reporter system

(2013) Yasuyuki Nakamura et al.   BIOTECHNOLOGY AND BIOENGINEERING

Mutations in G protein-coupled receptors that impact receptor trafficking and reproductive function

(2013) Alfredo Ulloa-Aguirre et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

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 smoothened receptor bound to an antitumour agent

(2013) Chong Wang et al.   NATURE

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

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

(2013) Fai Yiu Siu et al.   NATURE

Crystal structure of oligomeric β1-adrenergic G protein–coupled receptors in ligand-free basal state

(2013) Jianyun Huang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Dependence of Micelle Size and Shape on Detergent Alkyl Chain Length and Head Group

(2013) Ryan C. Oliver et al.   PLoS One

Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors

(2013) E. Doumazane et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Solution NMR resonance assignment strategies for β-barrel membrane proteins

(2013) Daniel A. Fox et al.   PROTEIN SCIENCE

Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex

(2013) Q. Tan et al.   SCIENCE

Structural Basis for Molecular Recognition at Serotonin Receptors

(2013) C. Wang et al.   SCIENCE

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

Serial Femtosecond Crystallography of G Protein-Coupled Receptors

(2013) W. Liu et al.   SCIENCE

Functional Homomers and Heteromers of Dopamine D2Land D3Receptors Co-exist at the Cell Surface

(2012) Chantevy Pou et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Determinants of the Supramolecular Organization of G Protein-Coupled Receptors in Bilayers

(2012) Xavier Periole et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Platform for the rapid construction and evaluation of GPCRs for crystallography in Saccharomyces cerevisiae

(2012) Mitsunori Shiroishi et al.   Microbial Cell Factories

Structure of the δ-opioid receptor bound to naltrindole

(2012) Sébastien Granier et al.   NATURE

Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist

(2012) Kazuko Haga et al.   NATURE

Structure of the human κ-opioid receptor in complex with JDTic

(2012) Huixian Wu et al.   NATURE

Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic

(2012) Aaron A. Thompson et al.   NATURE

Structure of the agonist-bound neurotensin receptor

(2012) Jim F. White et al.   NATURE

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

(2012) Aashish Manglik et al.   NATURE

Structure and dynamics of the M3 muscarinic acetylcholine receptor

(2012) Andrew C. Kruse et al.   NATURE

Structure of the chemokine receptor CXCR1 in phospholipid bilayers

(2012) Sang Ho Park et al.   NATURE

G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody

(2012) Tomoya Hino et al.   NATURE

High-resolution crystal structure of human protease-activated receptor 1

(2012) Cheng Zhang et al.   NATURE

Crystal Structure of a Lipid G Protein-Coupled Receptor

(2012) M. A. Hanson et al.   SCIENCE

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

(2012) W. Liu et al.   SCIENCE

Crystal Structures of a Stabilized β1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol

(2012) Tony Warne et al.   STRUCTURE

Assessing the Relative Stability of Dimer Interfaces in G Protein-Coupled Receptors

(2012) Jennifer M. Johnston et al.   PLoS Computational Biology

Solution NMR Structure of Proteorhodopsin

(2011) Sina Reckel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Lipid–protein nanodiscs for cell-free production of integral membrane proteins in a soluble and folded state: Comparison with detergent micelles, bicelles and liposomes

(2011) E.N. Lyukmanova et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Artificial membrane-like environments for in vitro studies of purified G-protein coupled receptors

(2011) Eugene Serebryany et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Toward Rational Design of Protein Detergent Complexes: Determinants of Mixed Micelles That Are Critical for the In Vitro Stabilization of a G-Protein Coupled Receptor

(2011) Michelle A. O'Malley et al.   BIOPHYSICAL JOURNAL

The Morphology and Composition of Cholesterol-Rich Micellar Nanostructures Determine Transmembrane Protein (GPCR) Activity

(2011) Michelle A. O'Malley et al.   BIOPHYSICAL JOURNAL

Update 1 of: Computational Modeling Approaches to Structure–Function Analysis of G Protein-Coupled Receptors

(2011) Francesca Fanelli et al.   CHEMICAL REVIEWS

Recombinant Cannabinoid Type 2 Receptor in Liposome Model Activates G Protein in Response to Anionic Lipid Constituents

(2011) Tomohiro Kimura et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Bivalent Dopamine D2Receptor Ligands: Synthesis and Binding Properties

(2011) Julia Kühhorn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystallographic Analysis of the Primary Photochemical Reaction of Squid Rhodopsin

(2011) Midori Murakami et al.   JOURNAL OF MOLECULAR BIOLOGY

Evaluation of the Pichia pastoris expression system for the production of GPCRs for structural analysis

(2011) Hidetsugu Asada et al.   Microbial Cell Factories

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

(2011) Guillaume Lebon et al.   NATURE

Structure of the human histamine H1 receptor complex with doxepin

(2011) Tatsuro Shimamura et al.   NATURE

Crystal structure of metarhodopsin II

(2011) Hui-Woog Choe et al.   NATURE

The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

(2011) Tony Warne et al.   NATURE

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

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

Structure and function of an irreversible agonist-β2 adrenoceptor complex

(2011) Daniel M. Rosenbaum et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

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

Functional crosstalk and heteromerization of serotonin 5-HT2A and dopamine D2 receptors

(2011) Laura Albizu et al.   NEUROPHARMACOLOGY

The Physiology, Signaling, and Pharmacology of Dopamine Receptors

(2011) J.-M. Beaulieu et al.   PHARMACOLOGICAL REVIEWS

Two distinct conformations of helix 6 observed in antagonist-bound structures of a  1-adrenergic receptor

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

Stabilized G protein binding site in the structure of constitutively active metarhodopsin-II

(2011) X. Deupi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine

(2011) Andrew S. Doré et al.   STRUCTURE

Toward the Fourth Dimension of Membrane Protein Structure: Insight into Dynamics from Spin-Labeling EPR Spectroscopy

(2011) Hassane S. Mchaourab et al.   STRUCTURE

Dopamine D1-D2 receptor heteromer signaling pathway in the brain: emerging physiological relevance

(2011) Ahmed Hasbi et al.   Molecular Brain

Analysis of Adenosine A2a Receptor Stability: Effects of Ligands and Disulfide Bonds

(2010) Michelle A. O’Malley et al.   BIOCHEMISTRY

Dimerization and ligand binding affect the structure network of A2A adenosine receptor

(2010) Francesca Fanelli et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Principles of early drug discovery

(2010) JP Hughes et al.   BRITISH JOURNAL OF PHARMACOLOGY

Dopamine Receptor Homooligomers and Heterooligomers in Schizophrenia

(2010) Melissa L. Perreault et al.   CNS Neuroscience & Therapeutics

Trans-activation between 7TM domains: implication in heterodimeric GABABreceptor activation

(2010) Carine Monnier et al.   EMBO JOURNAL

Conserved Binding Mode of Human β2Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography

(2010) Daniel Wacker et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor

(2010) Michael P. Bokoch et al.   NATURE

Rescue of defective G protein-coupled receptor function in vivo by intermolecular cooperation

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

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

Lighting up multiprotein complexes: lessons from GPCR oligomerization

(2010) Francisco Ciruela et al.   TRENDS IN BIOTECHNOLOGY

Schizophrenia, amphetamine-induced sensitized state and acute amphetamine exposure all show a common alteration: increased dopamine D2 receptor dimerization

(2010) Min Wang et al.   Molecular Brain

Coreceptors and HIV-1 Pathogenesis

(2010) Paul R. Gorry et al.   Current HIV/AIDS Reports

The role of dimerisation in the cellular trafficking of G-protein-coupled receptors

(2009) Graeme Milligan   CURRENT OPINION IN PHARMACOLOGY

Bioinformatics and molecular modelling approaches to GPCR oligomerization

(2009) Lisa M Simpson et al.   CURRENT OPINION IN PHARMACOLOGY

Dimerization in GPCR mobility and signaling

(2009) Martin J Lohse   CURRENT OPINION IN PHARMACOLOGY

Ligand-regulated oligomerization of β2-adrenoceptors in a model lipid bilayer

(2009) Juan José Fung et al.   EMBO JOURNAL

Metabotropic glutamate type 5, dopamine D2and adenosine A2areceptors form higher-order oligomers in living cells

(2009) Nuria Cabello et al.   JOURNAL OF NEUROCHEMISTRY

Calcium Signaling by Dopamine D5 Receptor and D5-D2 Receptor Hetero-Oligomers Occurs by a Mechanism Distinct from That for Dopamine D1-D2 Receptor Hetero-Oligomers

(2009) C. H. So et al.   MOLECULAR PHARMACOLOGY

Instability of a Class A G Protein-Coupled Receptor Oligomer Interface

(2009) J. M. Fonseca et al.   MOLECULAR PHARMACOLOGY

The structure and function of G-protein-coupled receptors

(2009) Daniel M. Rosenbaum et al.   NATURE

Analysis of receptor oligomerization by FRAP microscopy

(2009) Sandra Dorsch et al.   NATURE METHODS

Progress toward heterologous expression of active G-protein-coupled receptors inSaccharomyces cerevisiae: Linking cellular stress response with translocation and trafficking

(2009) Michelle A. O'Malley et al.   PROTEIN SCIENCE

Functional Rescue of β1-Adrenoceptor Dimerization and Trafficking by Pharmacological Chaperones

(2009) Hiroyuki Kobayashi et al.   TRAFFIC

The asymmetric/symmetric activation of GPCR dimers as a possible mechanistic rationale for multiple signalling pathways

(2009) Xavier Rovira et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

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

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

Over-Expression, Solubilization, and Purification of G Protein-Coupled Receptors for Structural Biology

(2008) Mark Chiu et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

An Update on Adenosine A2A-Dopamine D2 Receptor Interactions: Implications for the Function of G Protein-Coupled Receptors

(2008) S. Ferre et al.   CURRENT PHARMACEUTICAL DESIGN

Physiological relevance of GPCR oligomerization and its impact on drug discovery

(2008) Rosemarie Panetta et al.   DRUG DISCOVERY TODAY

Dopamine D2 receptors form higher order oligomers at physiological expression levels

(2008) Wen Guo et al.   EMBO JOURNAL

Ligand sensitivity in dimeric associations of the serotonin 5HT2c receptor

(2008) Filippo Mancia et al.   EMBO REPORTS

The ocular albinism type 1 protein, an intracellular G protein-coupled receptor, regulates melanosome transport in pigment cells

(2008) Ilaria Palmisano et al.   HUMAN MOLECULAR GENETICS

Crystal Structure of Squid Rhodopsin with Intracellularly Extended Cytoplasmic Region

(2008) Tatsuro Shimamura et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lipid−Rhodopsin Hydrophobic Mismatch Alters Rhodopsin Helical Content

(2008) Olivier Soubias et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Static light scattering to characterize membrane proteins in detergent solution

(2008) Dirk Jan Slotboom et al.   METHODS

Ligand-Dependent Oligomerization of Dopamine D2 and Adenosine A2A Receptors in Living Neuronal Cells

(2008) P.-A. Vidi et al.   MOLECULAR PHARMACOLOGY

Structure of a β1-adrenergic G-protein-coupled receptor

(2008) Tony Warne et al.   NATURE

Crystal structure of opsin in its G-protein-interacting conformation

(2008) Patrick Scheerer et al.   NATURE

Crystal structure of squid rhodopsin

(2008) Midori Murakami et al.   NATURE

Crystal structure of the ligand-free G-protein-coupled receptor opsin

(2008) Jung Hee Park et al.   NATURE

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

(2008) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

Biochemical approaches for discovering protein-protein interactions

(2008) Jan A. Miernyk et al.   PLANT JOURNAL

High-resolution distance mapping in rhodopsin reveals the pattern of helix movement due to activation

(2008) C. Altenbach et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

A Specific Cholesterol Binding Site Is Established by the 2.8 Å Structure of the Human β2-Adrenergic Receptor

(2008) Michael A. Hanson et al.   STRUCTURE

Heterologous GPCR Expression: A Bottleneck to Obtaining Crystal Structures

(2007) Emily C. McCusker et al.   BIOTECHNOLOGY PROGRESS