Advances in receptor conformation research: the quest for functionally selective conformations focusing on the β2-adrenoceptor

Biased β2-adrenoceptor signalling in heart failure: pathophysiology and drug discovery

(2014) Anthony Yiu-Ho Woo et al.   BRITISH JOURNAL OF PHARMACOLOGY

Tyrosine 308 Is Necessary for Ligand-directed GsProtein-biased Signaling of β2-Adrenoceptor

(2014) Anthony Yiu-Ho Woo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2014) Arun K. Shukla et al.   NATURE

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

Biased ligand bonds to make right calls—laboratory of signal transduction reveals molecular mechanism for functional selectivity of GPCR

(2014) Jue Wang   Science China-Life Sciences

The Concise Guide to PHARMACOLOGY 2013/14: Enzymes

(2013) Stephen P.H. Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors

(2013) Stephen P.H. Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Dynamic Process of β2-Adrenergic Receptor Activation

(2013) Rie Nygaard et al.   CELL

Detection of G Protein-selective G Protein-coupled Receptor (GPCR) Conformations in Live Cells

(2013) Rabia U. Malik et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Structure–Activity Analysis of Biased Agonism at the Dopamine D2 Receptor

(2013) Jeremy Shonberg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular interactions between fenoterol stereoisomers and derivatives and the β2-adrenergic receptor binding site studied by docking and molecular dynamics simulations

(2013) Anita Plazinska et al.   JOURNAL OF MOLECULAR MODELING

The Role of Ligands on the Equilibria Between Functional States of a G Protein-Coupled Receptor

(2013) Tae Hun Kim et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Adrenaline-activated structure of β2-adrenoceptor stabilized by an engineered nanobody

(2013) Aaron M. Ring et al.   NATURE

The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands

(2013) Adam J. Pawson et al.   NUCLEIC ACIDS RESEARCH

Ligand-specific conformational change of the G-protein-coupled receptor ALX/FPR2 determines proresolving functional responses

(2013) S. N. Cooray et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Kinetic, Energetic, and Mechanical Differences between Dark-State Rhodopsin and Opsin

(2013) Shiho Kawamura et al.   STRUCTURE

β-Adrenergic receptor subtype signaling in heart: From bench to bedside

(2012) Anthony Yiu Ho Woo et al.   ACTA PHARMACOLOGICA SINICA

Structure–Functional Selectivity Relationship Studies of β-Arrestin-Biased Dopamine D2 Receptor Agonists

(2012) Xin Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ligands and signaling proteins govern the conformational landscape explored by a G protein-coupled receptor

(2012) S. Mary et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Single-molecule analysis of fluorescently labeled G-protein-coupled receptors reveals complexes with distinct dynamics and organization

(2012) D. Calebiro 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

Ligand-Specific Interactions Modulate Kinetic, Energetic, and Mechanical Properties of the Human β2 Adrenergic Receptor

(2012) Michael Zocher et al.   STRUCTURE

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

(2012) Tony Warne et al.   STRUCTURE

The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling

(2012) Andreas Bock et al.   Nature Communications

Efficacy of the β2-adrenergic receptor is determined by conformational equilibrium in the transmembrane region

(2012) Yutaka Kofuku et al.   Nature Communications

Biased Ligands for Better Cardiovascular Drugs

(2011) Scott M. DeWire et al.   CIRCULATION RESEARCH

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

Multiple ligand-specific conformations of the β2-adrenergic receptor

(2011) Alem W Kahsai et al.   Nature Chemical Biology

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

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

G s-Biased  2-Adrenergic Receptor Signaling from Restoring Synchronous Contraction in the Failing Heart

(2011) K. Chakir et al.   Science Translational Medicine

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

(2011) Graham M. West et al.   STRUCTURE

Ligand-directed signalling at β-adrenoceptors

(2010) Bronwyn A. Evans et al.   BRITISH JOURNAL OF PHARMACOLOGY

Differential Signaling of the Endogenous Agonists at the β2-Adrenergic Receptor

(2010) Susanne Reiner et al.   JOURNAL OF BIOLOGICAL 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

Histidine 6.55 Is a Major Determinant of Ligand-Biased Signaling in Dopamine D2L Receptor

(2010) N. Tschammer et al.   MOLECULAR PHARMACOLOGY

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

(2010) Michael P. Bokoch et al.   NATURE

Teaching old receptors new tricks: biasing seven-transmembrane receptors

(2010) Sudarshan Rajagopal et al.   NATURE REVIEWS DRUG DISCOVERY

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

Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective β2-adrenergic receptor agonists

(2009) Krzysztof Jozwiak et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Therapeutic Efficacy of a Combination of a  1-Adrenoreceptor (AR) Blocker and  2-AR Agonist in a Rat Model of Postmyocardial Infarction Dilated Heart Failure Exceeds That of a  1-AR Blocker plus Angiotensin-Converting Enzyme Inhibitor

(2009) I. Ahmet et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

Bioluminescence Resonance Energy Transfer Assays Reveal Ligand-specific Conformational Changes within Preformed Signaling Complexes Containing δ-Opioid Receptors and Heterotrimeric G Proteins

(2008) Nicolas Audet et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cardioprotective and Survival Benefits of Long-Term Combined Therapy with  2 Adrenoreceptor (AR) Agonist and  1 AR Blocker in Dilated Cardiomyopathy Postmyocardial Infarction

(2008) I. Ahmet et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

(2008) A. Zurn et al.   MOLECULAR PHARMACOLOGY

Conformational Rearrangements and Signaling Cascades Involved in Ligand-Biased Mitogen-Activated Protein Kinase Signaling through the  1-Adrenergic Receptor

(2008) S. Galandrin et al.   MOLECULAR PHARMACOLOGY

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

(2008) Tony Warne et al.   NATURE

 -Blockers alprenolol and carvedilol stimulate  -arrestin-mediated EGFR transactivation

(2008) I.-M. Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA