GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

Determinants of Ligand Subtype-Selectivity at α1A-Adrenoceptor Revealed Using Saturation Transfer Difference (STD) NMR

(2018) Kelvin J. Yong et al.   ACS Chemical Biology

Structure and Dynamics of Membrane Proteins from Solid-State NMR

(2018) Venkata S. Mandala et al.   Annual Review of Biophysics

Illuminating the Energy Landscape of GPCRs: The Key Contribution of Solution-State NMR Associated with Escherichia coli as an Expression Host

(2018) Marina Casiraghi et al.   BIOCHEMISTRY

Solution NMR views of dynamical ordering of biomacromolecules

(2018) Teppei Ikeya et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Allosteric Coupling of Drug Binding and Intracellular Signaling in the A 2A Adenosine Receptor

(2018) Matthew T. Eddy et al.   CELL

Pharmacogenomics of GPCR Drug Targets

(2018) Alexander S. Hauser et al.   CELL

Deuteration and selective labeling of alanine methyl groups of β2-adrenergic receptor expressed in a baculovirus-insect cell expression system

(2018) Yutaka Kofuku et al.   JOURNAL OF BIOMOLECULAR NMR

Ligand-Based NMR Study of C-X-C Chemokine Receptor Type 4 (CXCR4)–Ligand Interactions on Living Cancer Cells

(2018) Diego Brancaccio et al.   JOURNAL OF MEDICINAL CHEMISTRY

Expanding the Paradigm: Intrinsically Disordered Proteins and Allosteric Regulation

(2018) Rebecca B. Berlow et al.   JOURNAL OF MOLECULAR BIOLOGY

Primary Transfer Step in the Light-Driven Ion Pump Bacteriorhodopsin: An Irreversible U-Turn Revealed by Dynamic Nuclear Polarization-Enhanced Magic Angle Spinning NMR

(2018) Qing Zhe Ni et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Extrinsic Tryptophans as NMR Probes of Allosteric Coupling in Membrane Proteins: Application to the A2A Adenosine Receptor

(2018) Matthew T. Eddy et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Applications of dissolution dynamic nuclear polarization in chemistry and biochemistry

(2018) Guannan Zhang et al.   MAGNETIC RESONANCE IN CHEMISTRY

Strategy for making safer opioids bolstered

(2018) Susruta Majumdar et al.   NATURE

Structural basis of ligand binding modes at the neuropeptide Y Y1 receptor

(2018) Zhenlin Yang et al.   NATURE

The molecular basis of subtype selectivity of human kinin G-protein-coupled receptors

(2018) Lisa Joedicke et al.   Nature Chemical Biology

Cryo-EM in drug discovery: achievements, limitations and prospects

(2018) Jean-Paul Renaud et al.   NATURE REVIEWS DRUG DISCOVERY

Biased signalling: from simple switches to allosteric microprocessors

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

Structure and dynamics of GPCR signaling complexes

(2018) Daniel Hilger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

GPCRs and Signal Transducers: Interaction Stoichiometry

(2018) Vsevolod V. Gurevich et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Mechanistic insights into allosteric regulation of the A2A adenosine G protein-coupled receptor by physiological cations

(2018) Libin Ye et al.   Nature Communications

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

(2018) Yutaro Shiraishi et al.   Nature Communications

Structure and dynamics of GPCR signaling complexes

(2018) Daniel Hilger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Enabling STD-NMR fragment screening using stabilized native GPCR: A case study of adenosine receptor

(2018) Sébastien Igonet et al.   Scientific Reports

Cryo-EM structure of human rhodopsin bound to an inhibitory G protein

(2018) Yanyong Kang et al.   NATURE

Structure of the adenosine-bound human adenosine A1 receptor–Gi complex

(2018) Christopher J. Draper-Joyce et al.   NATURE

Cryo-EM structure of the serotonin 5-HT1B receptor coupled to heterotrimeric Go

(2018) Javier García-Nafría et al.   NATURE

Structure of the µ-opioid receptor–Gi protein complex

(2018) Antoine Koehl et al.   NATURE

Solvent-accessibility of discrete residue positions in the polypeptide hormone glucagon by 19F-NMR observation of 4-fluorophenylalanine

(2017) Yaguang Hou et al.   JOURNAL OF BIOMOLECULAR NMR

Structure of monomeric Interleukin-8 and its interactions with the N-terminal Binding Site-I of CXCR1 by solution NMR spectroscopy

(2017) Sabrina Berkamp et al.   JOURNAL OF BIOMOLECULAR NMR

Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor

(2017) Zhong Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure and Function of Peptide-Binding G Protein-Coupled Receptors

(2017) Fan Wu et al.   JOURNAL OF MOLECULAR BIOLOGY

An Adaptable Phospholipid Membrane Mimetic System for Solution NMR Studies of Membrane Proteins

(2017) Chih-Ta Henry Chien et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Spontaneous Lipid Nanodisc Fomation by Amphiphilic Polymethacrylate Copolymers

(2017) Kazuma Yasuhara et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

β-arrestin signalling and bias in hormone-responsive GPCRs

(2017) Eric Reiter et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

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

(2017) Yi-Lynn Liang 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

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

(2017) Yan Zhang et al.   NATURE

A kinetic view of GPCR allostery and biased agonism

(2017) J Robert Lane 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

Competitive association binding kinetic assays: a new tool to detect two different binding orientations of a ligand to its target protein under distinct conditions?

(2017) Hans-Joachim Wittmann et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

The Role of Science in Addressing the Opioid Crisis

(2017) Nora D. Volkow et al.   NEW ENGLAND JOURNAL OF MEDICINE

GPCRdb in 2018: adding GPCR structure models and ligands

(2017) Gáspár Pándy-Szekeres et al.   NUCLEIC ACIDS 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

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

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

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

Insight into partial agonism by observing multiple equilibria for ligand-bound and Gs-mimetic nanobody-bound β1-adrenergic receptor

(2017) Andras S. Solt et al.   Nature Communications

Dynamic regulation of GDP binding to G proteins revealed by magnetic field-dependent NMR relaxation analyses

(2017) Yuki Toyama et al.   Nature Communications

Crystal structure of a multi-domain human smoothened receptor in complex with a super stabilizing ligand

(2017) Xianjun Zhang et al.   Nature Communications

Ligand modulation of sidechain dynamics in a wild-type human GPCR

(2017) Lindsay D Clark et al.   eLife

Improvement of Ligand Affinity and Thermodynamic Properties by NMR-Based Evaluation of Local Dynamics and Surface Complementarity in the Receptor-Bound State

(2016) Yumiko Mizukoshi et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

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

Biased agonism: An emerging paradigm in GPCR drug discovery

(2016) Zoran Rankovic et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Co-inhibition of CD73 and A2AR Adenosine Signaling Improves Anti-tumor Immune Responses

(2016) Arabella Young et al.   CANCER CELL

Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation

(2016) Jean-Pierre Changeux et al.   CELL

Structurally Enabled Discovery of Adenosine A2A Receptor Antagonists

(2016) Ali Jazayeri et al.   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

The expanding repertoire of receptor activity modifying protein (RAMP) function

(2016) Klara R. Klein et al.   CRITICAL REVIEWS IN BIOCHEMISTRY AND MOLECULAR BIOLOGY

A2A adenosine receptor antagonists to weaken the hypoxia-HIF-1α driven immunosuppression and improve immunotherapies of cancer

(2016) Stephen M Hatfield et al.   CURRENT OPINION IN PHARMACOLOGY

Ring current shifts in 19F-NMR of membrane proteins

(2016) Dongsheng Liu et al.   JOURNAL OF BIOMOLECULAR NMR

Functional Modulation of a G Protein-Coupled Receptor Conformational Landscape in a Lipid Bilayer

(2016) Marina Casiraghi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Advances in solid-state NMR of membrane proteins

(2016) Benjamin J. Wylie et al.   MOLECULAR PHYSICS

Structure of the adenosine A2A receptor bound to an engineered G protein

(2016) Byron Carpenter et al.   NATURE

Backbone NMR reveals allosteric signal transduction networks in the β1-adrenergic receptor

(2016) Shin Isogai et al.   NATURE

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

(2016) Libin Ye 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

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

Self-assembly of size-controlled liposomes on DNA nanotemplates

(2016) Yang Yang et al.   Nature Chemistry

Covalently circularized nanodiscs for studying membrane proteins and viral entry

(2016) Mahmoud L Nasr et al.   NATURE METHODS

A saposin-lipoprotein nanoparticle system for membrane proteins

(2016) Jens Frauenfeld et al.   NATURE METHODS

G protein-coupled receptors as targets for anti-diabetic therapeutics

(2016) Da Young Oh et al.   NATURE REVIEWS DRUG DISCOVERY

Biophysics in drug discovery: impact, challenges and opportunities

(2016) Jean-Paul Renaud et al.   NATURE REVIEWS DRUG DISCOVERY

Twenty years on: the impact of fragments on drug discovery

(2016) Daniel A. Erlanson et al.   NATURE REVIEWS DRUG DISCOVERY

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

Recent updates on GPCR biased agonism

(2016) André S. Pupo et al.   PHARMACOLOGICAL RESEARCH

Conductance of P2X4purinergic receptor is determined by conformational equilibrium in the transmembrane region

(2016) Yuichi Minato et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Conformational dynamics of a G-protein α subunit is tightly regulated by nucleotide binding

(2016) David Goricanec et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

β-arrestin–biased signaling through the β2-adrenergic receptor promotes cardiomyocyte contraction

(2016) Richard Carr et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Nuclear magnetic resonance (NMR) applied to membrane–protein complexes

(2016) Mohammed Kaplan et al.   QUARTERLY REVIEWS OF BIOPHYSICS

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

(2016) Matthew T. Eddy et al.   STRUCTURE

New Technologies for Elucidating Opioid Receptor Function

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

Utilization of paramagnetic relaxation enhancements for structural analysis of actin-binding proteins in complex with actin

(2016) Shuxian Huang et al.   Scientific Reports

In-Membrane Chemical Modification (IMCM) for Site-Specific Chromophore Labeling of GPCRs

(2015) Lukas Sušac et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Identification of a Conformational Equilibrium That Determines the Efficacy and Functional Selectivity of the μ-Opioid Receptor

(2015) Junya Okude et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Structural analysis of CXCR4 – Antagonist interactions using saturation-transfer double-difference NMR

(2015) Bryan D. Cox et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Real-time monitoring of binding events on a thermostabilized human A2A receptor embedded in a lipid bilayer by surface plasmon resonance

(2015) Nicolas Bocquet et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Lipid modulation of early G protein-coupled receptor signalling events

(2015) Patricia M. Dijkman et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

HN, N, Cα, Cβ and C′ assignments of the intrinsically disordered C-terminus of human adenosine A2A receptor

(2015) Helena Tossavainen et al.   Biomolecular NMR Assignments

Human Adenosine A2A Receptor Binds Calmodulin with High Affinity in a Calcium-Dependent Manner

(2015) Henni Piirainen et al.   BIOPHYSICAL JOURNAL

Optical probes based on G protein-coupled receptors - added work or added value?

(2015) A D Stumpf et al.   BRITISH JOURNAL OF PHARMACOLOGY

Sensitivity-Enhanced NMR Reveals Alterations in Protein Structure by Cellular Milieus

(2015) Kendra K. Frederick et al.   CELL

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

(2015) Aashish Manglik et al.   CELL

Role of post-translational modifications on structure, function and pharmacology of class C G protein-coupled receptors

(2015) Lenea Nørskov-Lauritsen et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Dopamine receptor partial agonists and addiction

(2015) Fabricio A. Moreira et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Pharmacological targeting of dopamine D3 receptors: Possible clinical applications of selective drugs

(2015) Emilio Merlo Pich et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

Partial adenosine A1 receptor agonism: a potential new therapeutic strategy for heart failure

(2015) Stephen J. Greene et al.   HEART FAILURE REVIEWS

From G Protein-coupled Receptor Structure Resolution to Rational Drug Design

(2015) Ali Jazayeri et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Elucidation of the CCR1- and CCR5-binding modes of MIP-1α by application of an NMR spectra reconstruction method to the transferred cross-saturation experiments

(2015) Chie Yoshiura et al.   JOURNAL OF BIOMOLECULAR NMR

An economic approach to efficient isotope labeling in insect cells using homemade 15N-, 13C- and 2H-labeled yeast extracts

(2015) Christian Opitz et al.   JOURNAL OF BIOMOLECULAR NMR

Methyl labeling and TROSY NMR spectroscopy of proteins expressed in the eukaryote Pichia pastoris

(2015) Lindsay Clark et al.   JOURNAL OF BIOMOLECULAR NMR

The power of mass spectrometry in structural characterization of GPCR signaling

(2015) Kunhong Xiao et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Two disparate ligand-binding sites in the human P2Y1 receptor

(2015) Dandan Zhang et al.   NATURE

Structural insights into µ-opioid receptor activation

(2015) Weijiao Huang et al.   NATURE

Propagation of conformational changes during μ-opioid receptor activation

(2015) Rémy Sounier et al.   NATURE

Allosteric regulation of G protein–coupled receptor activity by phospholipids

(2015) Rosie Dawaliby et al.   Nature Chemical Biology

Methodological advances: the unsung heroes of the GPCR structural revolution

(2015) Eshan Ghosh et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Substrate-modulated ADP/ATP-transporter dynamics revealed by NMR relaxation dispersion

(2015) Sven Brüschweiler et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The energy landscape of adenylate kinase during catalysis

(2015) S Jordan Kerns et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Single-molecule view of basal activity and activation mechanisms of the G protein-coupled receptor β2AR

(2015) Rajan Lamichhane et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

NMR structure and dynamics of the agonist dynorphin peptide bound to the human kappa opioid receptor

(2015) Casey O’Connor et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Membrane proteins in their native habitat as seen by solid-state NMR spectroscopy

(2015) Leonid S. Brown et al.   PROTEIN SCIENCE

On the relationship between NMR-derived amide order parameters and protein backbone entropy changes

(2015) Kim A. Sharp et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

The importance of ligands for G protein-coupled receptor stability

(2015) Xianjun Zhang et al.   TRENDS IN BIOCHEMICAL SCIENCES

Emerging Approaches to GPCR Ligand Screening for Drug Discovery

(2015) Punita Kumari et al.   TRENDS IN MOLECULAR MEDICINE

Substrate-modulated ADP/ATP-transporter dynamics revealed by NMR relaxation dispersion

(2015) Sven Brüschweiler et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The energy landscape of adenylate kinase during catalysis

(2015) S Jordan Kerns et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

A2aR antagonists: Next generation checkpoint blockade for cancer immunotherapy

(2015) Robert D. Leone et al.   Computational and Structural Biotechnology Journal

Functional Dynamics of Deuterated β2-Adrenergic Receptor in Lipid Bilayers Revealed by NMR Spectroscopy

(2014) Yutaka Kofuku et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

GPCR structures in drug design, emerging opportunities with new structures

(2014) Christofer S. Tautermann   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Antimetastatic Effects of Blocking PD-1 and the Adenosine A2A Receptor

(2014) D. Mittal et al.   CANCER RESEARCH

SnapShot: GPCR-Ligand Interactions

(2014) Eshan Ghosh et al.   CELL

Structured and disordered facets of the GPCR fold

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

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

(2014) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers

(2014) David G. Soergel et al.   PAIN

Unifying Family A GPCR Theories of Activation

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

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

Membranes, peptides, and disease: Unraveling the mechanisms of viral proteins with solid state nuclear magnetic resonance spectroscopy

(2014) Matthew T. Eddy et al.   SOLID STATE NUCLEAR MAGNETIC RESONANCE

Biased ligands at G-protein-coupled receptors: promise and progress

(2014) Jonathan D. Violin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

β2-Adrenergic Receptor Activation by Agonists Studied with19F NMR Spectroscopy

(2013) Reto Horst et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Functionally biased signalling properties of 7TM receptors - opportunities for drug development for the ghrelin receptor

(2013) B Sivertsen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth

(2013) Melanie Mediavilla-Varela et al.   CANCER BIOLOGY & THERAPY

The Dynamic Process of β2-Adrenergic Receptor Activation

(2013) Rie Nygaard et al.   CELL

Structure-Based and Fragment-Based GPCR Drug Discovery

(2013) Stephen P. Andrews et al.   ChemMedChem

Fluorine-19 NMR of integral membrane proteins illustrated with studies of GPCRs

(2013) Tatiana Didenko et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

First Clinical Experience With TRV130: Pharmacokinetics and Pharmacodynamics in Healthy Volunteers

(2013) David G. Soergel et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Functional dynamics of cell surface membrane proteins

(2013) Noritaka Nishida et al.   JOURNAL OF MAGNETIC RESONANCE

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

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

Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain

(2013) Xiao-Tao Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Dynamic ligand binding dictates partial agonism at a G protein–coupled receptor

(2013) Andreas Bock et al.   Nature Chemical Biology

50 years of allosteric interactions: the twists and turns of the models

(2013) Jean-Pierre Changeux   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Involvement of distinct arrestin-1 elements in binding to different functional forms of rhodopsin

(2013) T. Zhuang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

Fragment Screening of GPCRs Using Biophysical Methods: Identification of Ligands of the Adenosine A2A Receptor with Novel Biological Activity

(2012) Dan Chen et al.   ACS Chemical Biology

Calcium-Dependent Ligand Binding and G-protein Signaling of Family B GPCR Parathyroid Hormone 1 Receptor Purified in Nanodiscs

(2012) Nivedita Mitra et al.   ACS Chemical Biology

Detergent-Free Formation and Physicochemical Characterization of Nanosized Lipid-Polymer Complexes: Lipodisq

(2012) Marcella C. Orwick et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Restructuring G-Protein- Coupled Receptor Activation

(2012) Martin Audet et al.   CELL

Functional dynamics of proteins revealed by solution NMR

(2012) Masanori Osawa et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Non-Analgesic Effects of Opioids: Opioid-induced Respiratory Depression

(2012) Merel Boom et al.   CURRENT PHARMACEUTICAL DESIGN

Functional Equilibrium of the KcsA Structure Revealed by NMR

(2012) Shunsuke Imai et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Role of Detergents in Conformational Exchange of a G Protein-coupled Receptor

(2012) Ka Young Chung et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Translational research: A UK tissue bank for breast tumours

(2012) Alastair M. Thompson   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

N-Terminal T4 Lysozyme Fusion Facilitates Crystallization of a G Protein Coupled Receptor

(2012) Yaozhong Zou et al.   PLoS One

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

Distinct roles of metabotropic glutamate receptor dimerization in agonist activation and G-protein coupling

(2012) D. El Moustaine 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

Expression, purification and preliminary NMR characterization of isotopically labeled wild-type human heterotrimeric G protein αi1

(2012) Jan Maly et al.   PROTEIN EXPRESSION AND PURIFICATION

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

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

(2012) Yutaka Kofuku et al.   Nature Communications

Solution NMR of Polypeptides Hyperpolarized by Dynamic Nuclear Polarization

(2011) Mukundan Ragavan et al.   ANALYTICAL CHEMISTRY

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

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

Mapping the Ligand-Binding Site on a G Protein-Coupled Receptor (GPCR) Using Genetically Encoded Photocrosslinkers

(2011) Amy Grunbeck et al.   BIOCHEMISTRY

Recent contributions from solid-state NMR to the understanding of membrane protein structure and function

(2011) Peter J Judge et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Site-specific in vitro and in vivo incorporation of molecular probes to study G-protein-coupled receptors

(2011) Kelly A Daggett et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Nanobody stabilization of G protein-coupled receptor conformational states

(2011) Jan Steyaert et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Thermostabilisation of an Agonist-Bound Conformation of the Human Adenosine A2A Receptor

(2011) Guillaume Lebon et al.   JOURNAL OF MOLECULAR BIOLOGY

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 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

Crystal structure of the β2 adrenergic receptor–Gs protein complex

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

Antiparallel EmrE exports drugs by exchanging between asymmetric structures

(2011) Emma A. Morrison et al.   NATURE

Multiple ligand-specific conformations of the β2-adrenergic receptor

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

Trends in the exploitation of novel drug targets

(2011) Mathias Rask-Andersen et al.   NATURE REVIEWS DRUG DISCOVERY

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

A Dynamic Knockout Reveals That Conformational Fluctuations Influence the Chemical Step of Enzyme Catalysis

(2011) G. Bhabha 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

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

(2011) Graham M. West et al.   STRUCTURE

Drug Design for G-Protein-Coupled Receptors by a Ligand-Based NMR Method

(2010) Stefan Bartoschek et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Protein NMR Using Paramagnetic Ions

(2010) Gottfried Otting   Annual Review of Biophysics

Monomeric Rhodopsin Is Sufficient for Normal Rhodopsin Kinase (GRK1) Phosphorylation and Arrestin-1 Binding

(2010) Timothy H. Bayburt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Conformational dependence of 13C shielding and coupling constants for methionine methyl groups

(2010) Glenn L. Butterfoss et al.   JOURNAL OF BIOMOLECULAR NMR

Functional Selectivity and Biased Receptor Signaling

(2010) T. Kenakin   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Structure of a GPCR Ligand in Its Receptor-Bound State: Leukotriene B4 Adopts a Highly Constrained Conformation When Associated to Human BLT2

(2010) Laurent J. Catoire et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

NMR Analyses of the Interaction between CCR5 and Its Ligand Using Functional Reconstitution of CCR5 in Lipid Bilayers

(2010) Chie Yoshiura et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Tracking G-protein-coupled receptor activation using genetically encoded infrared probes

(2010) Shixin Ye et al.   NATURE

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

(2010) Michael P. Bokoch et al.   NATURE

Comparison of functional non-glycosylated GPCRs expression in Pichia pastoris

(2009) Takami Yurugi-Kobayashi et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Theory, Practice, and Applications of Paramagnetic Relaxation Enhancement for the Characterization of Transient Low-Population States of Biological Macromolecules and Their Complexes

(2009) G. Marius Clore et al.   CHEMICAL REVIEWS

Clinical implications of the intrinsic efficacy of beta-adrenoceptor drugs in asthma: full, partial and inverse agonism

(2009) Nicola A Hanania et al.   CURRENT OPINION IN PULMONARY MEDICINE

Opioid dependence treatment: options in pharmacotherapy

(2009) Angela L Stotts et al.   EXPERT OPINION ON PHARMACOTHERAPY

Structural Basis of the Interaction between Chemokine Stromal Cell-derived Factor-1/CXCL12 and Its G-protein-coupled Receptor CXCR4

(2009) Yutaka Kofuku et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Paramagnetic labelling of proteins and oligonucleotides for NMR

(2009) Xun-Cheng Su et al.   JOURNAL OF BIOMOLECULAR NMR

The structure and function of G-protein-coupled receptors

(2009) Daniel M. Rosenbaum et al.   NATURE

Functional and shunt states of bacteriorhodopsin resolved by 250 GHz dynamic nuclear polarization-enhanced solid-state NMR

(2009) V. S. Bajaj 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

Observing biological dynamics at atomic resolution using NMR

(2009) Anthony K. Mittermaier et al.   TRENDS IN BIOCHEMICAL SCIENCES

Dependence of Amino Acid Side Chain13C Shifts on Dihedral Angle: Application to Conformational Analysis

(2008) Robert E. London et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Direct NMR Detection of the Binding of Functional Ligands to the Human Sweet Receptor, a Heterodimeric Family 3 GPCR

(2008) Fariba M. Assadi-Porter et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2008) Jung Hee Park et al.   NATURE

Energy transformations early in the bacteriorhodopsin photocycle revealed by DNP-enhanced solid-state NMR

(2008) M. L. Mak-Jurkauskas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Recognition Dynamics Up to Microseconds Revealed from an RDC-Derived Ubiquitin Ensemble in Solution

(2008) O. F. Lange et al.   SCIENCE

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