Structure-Function of the G Protein–Coupled Receptor Superfamily

Lifting the lid on GPCRs: the role of extracellular loops

(2012) M Wheatley et al.   BRITISH JOURNAL OF PHARMACOLOGY

Oligomerization of G Protein-Coupled Receptors: Computational Methods

(2012) J. Selent et al.   CURRENT MEDICINAL CHEMISTRY

Oligomerization of G Protein-Coupled Receptors: Biochemical and Biophysical Methods

(2012) A.A. Kaczor et al.   CURRENT MEDICINAL CHEMISTRY

Optimization of Adenosine 5′-Carboxamide Derivatives as Adenosine Receptor Agonists Using Structure-Based Ligand Design and Fragment Screening

(2012) Dilip K. Tosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 1,2,4-Triazine Derivatives as Adenosine A2A Antagonists using Structure Based Drug Design

(2012) Miles Congreve et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

(2012) Tomoya Hino et al.   NATURE

Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy

(2012) R. Rahmeh et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure-based ligand discovery for the protein-protein interface of chemokine receptor CXCR4

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

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

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

(2012) J. J. 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

Strategies to Discover Unexpected Targets for Drugs Active at G Protein–Coupled Receptors

(2011) John A. Allen et al.   Annual Review of Pharmacology and Toxicology

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

Molecular Mechanism of β-Arrestin-Biased Agonism at Seven-Transmembrane Receptors

(2011) Eric Reiter et al.   Annual Review of Pharmacology and Toxicology

Progress in Structure Based Drug Design for G Protein-Coupled Receptors

(2011) Miles Congreve et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal Structure-Based Virtual Screening for Fragment-like Ligands of the Human Histamine H1Receptor

(2011) Chris de Graaf et al.   JOURNAL OF MEDICINAL CHEMISTRY

In silico analysis of the binding of agonists and blockers to the β2-adrenergic receptor

(2011) Santiago Vilar et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Conformational Dynamics of Single G Protein-Coupled Receptors in Solution

(2011) Samuel Bockenhauer et al.   JOURNAL OF PHYSICAL CHEMISTRY B

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

(2011) Ka Young Chung et al.   NATURE

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

The structural basis of agonist-induced activation in constitutively active rhodopsin

(2011) Jörg Standfuss 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

Ligand discovery from a dopamine D3 receptor homology model and crystal structure

(2011) Jens Carlsson et al.   Nature Chemical Biology

Dimers and beyond: The functional puzzles of class C GPCRs

(2011) Julie Kniazeff et al.   PHARMACOLOGY & THERAPEUTICS

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

Pathway and mechanism of drug binding to G-protein-coupled receptors

(2011) Ron O. Dror 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

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

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

(2011) Andrew S. Doré et al.   STRUCTURE

Status of GPCR Modeling and Docking as Reflected by Community-wide GPCR Dock 2010 Assessment

(2011) Irina Kufareva et al.   STRUCTURE

Ligand-Dependent Perturbation of the Conformational Ensemble for the GPCR β2 Adrenergic Receptor Revealed by HDX

(2011) Graham M. West et al.   STRUCTURE

Structural insights into RAMP modification of secretin family G protein-coupled receptors: implications for drug development

(2011) Julia K. Archbold et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Asymmetry of GPCR oligomers supports their functional relevance

(2011) Pascal Maurice et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Diversity and modularity of G protein-coupled receptor structures

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

Conformational Changes in the G Protein-Coupled Receptor Rhodopsin Revealed by Histidine Hydrogen−Deuterium Exchange

(2010) David T. Lodowski et al.   BIOCHEMISTRY

Allosteric modulation of adenosine receptors

(2010) Anikó Göblyös et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

GPCR-OKB: the G Protein Coupled Receptor Oligomer Knowledge Base

(2010) George Khelashvili et al.   BIOINFORMATICS

Structure-Based Discovery of Novel Chemotypes for Adenosine A2AReceptor Antagonists

(2010) Vsevolod Katritch et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Discovery of A2AAdenosine Receptor Ligands

(2010) Jens Carlsson et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Evolution of GPCR: Change and continuity

(2010) Rainer Strotmann et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

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

(2010) Michael P. Bokoch et al.   NATURE

G protein-coupled receptors: novel targets for drug discovery in cancer

(2010) Rosamaria Lappano et al.   NATURE REVIEWS DRUG DISCOVERY

Transmembrane signaling by GPCRs: Insight from rhodopsin and opsin structures

(2010) Hui-Woog Choe et al.   NEUROPHARMACOLOGY

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

(2010) Peter Keov et al.   NEUROPHARMACOLOGY

Structure based prediction of subtype-selectivity for adenosine receptor antagonists

(2010) Vsevolod Katritch et al.   NEUROPHARMACOLOGY

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

(2010) T. Kenakin et al.   PHARMACOLOGICAL REVIEWS

Energy Landscapes as a Tool to Integrate GPCR Structure, Dynamics, and Function

(2010) Xavier Deupi et al.   PHYSIOLOGY

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

Therapeutic potential of β-arrestin- and G protein-biased agonists

(2010) Erin J. Whalen et al.   TRENDS IN MOLECULAR MEDICINE

Induced Effects of Sodium Ions on Dopaminergic G-Protein Coupled Receptors

(2010) Jana Selent et al.   PLoS Computational Biology

Observation of “Ionic Lock” Formation in Molecular Dynamics Simulations of Wild-Type β1and β2Adrenergic Receptors

(2009) Stefano Vanni et al.   BIOCHEMISTRY

Monitoring the Interaction of a Single G-Protein Key Binding Site with Rhodopsin Disk Membranes upon Light Activation

(2009) Tai-Yang Kim et al.   BIOCHEMISTRY

G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function

(2009) Graeme Milligan   BRITISH JOURNAL OF PHARMACOLOGY

G-protein-coupled receptors, cholesterol and palmitoylation: facts about fats

(2009) Bice Chini et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

Analysis of full and partial agonists binding to β2-adrenergic receptor suggests a role of transmembrane helix V in agonist-specific conformational changes

(2009) Vsevolod Katritch et al.   JOURNAL OF MOLECULAR RECOGNITION

Rastering strategy for screening and centring of microcrystal samples of human membrane proteins with a sub-10  m size X-ray synchrotron beam

(2009) V. Cherezov et al.   Journal of the Royal Society Interface

Crystallizing membrane proteins using lipidic mesophases

(2009) Martin Caffrey et al.   Nature Protocols

Fine-tuning of GPCR activity by receptor-interacting proteins

(2009) Stefanie L. Ritter et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Structure-based discovery of  2-adrenergic receptor ligands

(2009) P. Kolb et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex

(2009) X. J. Yao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Development and crystallization of a minimal thermostabilised G protein-coupled receptor

(2009) Tony Warne et al.   PROTEIN EXPRESSION AND PURIFICATION

Ligand binding and micro-switches in 7TM receptor structures

(2009) Rie Nygaard et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

An ion-responsive motif in the second transmembrane segment of rhodopsin-like receptors

(2008) M. S. Parker et al.   AMINO ACIDS

Mutations Affecting the Oligomerization Interface of G-Protein-Coupled Receptors Revealed by a Novel De Novo Protein Design Framework

(2008) Martin S. Taylor et al.   BIOPHYSICAL JOURNAL

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

Functional Role of the “Ionic Lock”—An Interhelical Hydrogen-Bond Network in Family A Heptahelical Receptors

(2008) Reiner Vogel et al.   JOURNAL OF MOLECULAR BIOLOGY

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 the ligand-free G-protein-coupled receptor opsin

(2008) Jung Hee Park et al.   NATURE

Structural diversity of G protein-coupled receptors and significance for drug discovery

(2008) Malin C. Lagerström et al.   NATURE REVIEWS DRUG DISCOVERY

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

Activation of G Protein–Coupled Receptors: Beyond Two-State Models and Tertiary Conformational Changes

(2007) Paul S.-H. Park et al.   Annual Review of Pharmacology and Toxicology