Structural insights into G-protein-coupled receptor allostery

Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures

(2018) John A. Christopher et al.   JOURNAL OF MEDICINAL CHEMISTRY

Na+-mimicking ligands stabilize the inactive state of leukotriene B4 receptor BLT1

(2018) Tetsuya Hori et al.   Nature Chemical Biology

Biased signalling: from simple switches to allosteric microprocessors

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

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2muscarinic acetylcholine receptor

(2018) Magdalena Korczynska et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727

(2018) Nathan Robertson 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

Structure of CC Chemokine Receptor 5 with a Potent Chemokine Antagonist Reveals Mechanisms of Chemokine Recognition and Molecular Mimicry by HIV

(2017) Yi Zheng et al.   IMMUNITY

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

Mechanism of intracellular allosteric β2AR antagonist revealed by X-ray crystal structure

(2017) Xiangyu Liu et al.   NATURE

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

(2017) G. Glenn Gregorio 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

Structural insight into allosteric modulation of protease-activated receptor 2

(2017) Robert K. Y. Cheng et al.   NATURE

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

(2017) Yan Zhang et al.   NATURE

Crystal structures of agonist-bound human cannabinoid receptor CB1

(2017) Tian Hua et al.   NATURE

A kinetic view of GPCR allostery and biased agonism

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

Discovery of new GPCR ligands to illuminate new biology

(2017) Bryan L Roth et al.   Nature Chemical Biology

Opportunities for therapeutic antibodies directed at G-protein-coupled receptors

(2017) Catherine J. Hutchings et al.   NATURE REVIEWS DRUG DISCOVERY

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

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

Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

(2017) Jun Lu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

An update on the physiological and therapeutic relevance of GPCR oligomers

(2017) Batoul Farran   PHARMACOLOGICAL RESEARCH

Conformational equilibria of light-activated rhodopsin in nanodiscs

(2017) Ned Van Eps et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2

(2017) Zil E. Huma et al.   Science Signaling

Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs

(2017) Miles Congreve et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Structural basis for perception of diverse chemical substances by T1r taste receptors

(2017) Nipawan Nuemket et al.   Nature Communications

Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

(2017) Jun Lu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2

(2017) Zil E. Huma et al.   Science Signaling

Purification of family B G protein-coupled receptors using nanodiscs: Application to human glucagon-like peptide-1 receptor

(2017) Yingying Cai et al.   PLoS One

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

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

Biased Allostery

(2016) Stuart J. Edelstein et al.   BIOPHYSICAL JOURNAL

Cellular Cholesterol Directly Activates Smoothened in Hedgehog Signaling

(2016) Pengxiang Huang et al.   CELL

Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation

(2016) Jean-Pierre Changeux et al.   CELL

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

Interaction of G protein coupled receptors and cholesterol

(2016) Gerald Gimpl   CHEMISTRY AND PHYSICS OF LIPIDS

Structural basis of Smoothened regulation by its extracellular domains

(2016) Eamon F. X. Byrne et al.   NATURE

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

(2016) Yi Zheng et al.   NATURE

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

(2016) Mi-Hye Lee et al.   NATURE

Activation of the A2A adenosine G-protein-coupled receptor by conformational selection

(2016) Libin Ye 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

Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation

(2016) Dean P. Staus et al.   NATURE

Extra-helical binding site of a glucagon receptor antagonist

(2016) Ali Jazayeri et al.   NATURE

Activation mechanism of endothelin ETB receptor by endothelin-1

(2016) Wataru Shihoya et al.   NATURE

Organization and functions of mGlu and GABAB receptor complexes

(2016) Jean-Philippe Pin et al.   NATURE

Intracellular allosteric antagonism of the CCR9 receptor

(2016) Christine Oswald et al.   NATURE

Conformationally selective RNA aptamers allosterically modulate the β2-adrenoceptor

(2016) Alem W Kahsai et al.   Nature Chemical Biology

Hitchhiking on the heptahelical highway: structure and function of 7TM receptor complexes

(2016) John J. G. Tesmer   NATURE REVIEWS MOLECULAR CELL BIOLOGY

β 2 -Adrenergic Receptor Conformational Response to Fusion Protein in the Third Intracellular Loop

(2016) Matthew T. Eddy et al.   STRUCTURE

The role of kinetic context in apparent biased agonism at GPCRs

(2016) Carmen Klein Herenbrink et al.   Nature Communications

Cholesterol activates the G-protein coupled receptor Smoothened to promote Hedgehog signaling

(2016) Giovanni Luchetti et al.   eLife

Structural mechanism of ligand activation in human calcium-sensing receptor

(2016) Yong Geng et al.   eLife

Mechanism of allosteric regulation of β2-adrenergic receptor by cholesterol

(2016) Moutusi Manna et al.   eLife

Structural basis for regulation of human calcium-sensing receptor by magnesium ions and an unexpected tryptophan derivative co-agonist

(2016) C. Zhang et al.   Science Advances

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

(2015) Aashish Manglik et al.   CELL

Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile)

(2015) John A. Christopher et al.   JOURNAL OF MEDICINAL CHEMISTRY

Two disparate ligand-binding sites in the human P2Y1 receptor

(2015) Dandan Zhang et al.   NATURE

Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser

(2015) Yanyong Kang et al.   NATURE

Ligand occupancy in crystal structure of β1-adrenergic G protein–coupled receptor

(2015) Andrew G W Leslie et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Ligand occupancy in crystal structure of β1-adrenergic G protein–coupled receptor

(2015) Andrew G W Leslie et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

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

(2014) Arun K. Shukla et al.   NATURE

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

(2014) Ankita Srivastava et al.   NATURE

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

(2014) Andrew S. Doré et al.   NATURE

Agonist-bound structure of the human P2Y12 receptor

(2014) Jin Zhang et al.   NATURE

A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification

(2014) Whitney M Nolte et al.   Nature Chemical Biology

Unifying Family A GPCR Theories of Activation

(2014) Benjamin G. Tehan et al.   PHARMACOLOGY & THERAPEUTICS

The 2.1 Å Resolution Structure of Cyanopindolol-Bound β1-Adrenoceptor Identifies an Intramembrane Na+ Ion that Stabilises the Ligand-Free Receptor

(2014) Jennifer L. Miller-Gallacher et al.   PLoS One

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

(2014) H. Wu et al.   SCIENCE

Allosteric sodium in class A GPCR signaling

(2014) Vsevolod Katritch et al.   TRENDS IN BIOCHEMICAL SCIENCES

Crystal structure of pre-activated arrestin p44

(2013) Yong Ju Kim et al.   NATURE

Structure of active β-arrestin-1 bound to a G-protein-coupled receptor phosphopeptide

(2013) Arun K. Shukla et al.   NATURE

Structure of class B GPCR corticotropin-releasing factor receptor 1

(2013) Kaspar Hollenstein et al.   NATURE

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs

(2013) Ron O. Dror et al.   NATURE

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse 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

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

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

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

(2012) Tomoya Hino et al.   NATURE

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

Crystal structure of metarhodopsin II

(2011) Hui-Woog Choe et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

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

G protein-coupled receptor kinases: More than just kinases and not only for GPCRs

(2011) Eugenia V. Gurevich et al.   PHARMACOLOGY & THERAPEUTICS

Importance of lipid-exposed residues in transmembrane segment four for family B calcitonin receptor homo-dimerization

(2010) Kaleeckal G. Harikumar et al.   REGULATORY PEPTIDES

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