Conformational selection guides β-arrestin recruitment at a biased G protein–coupled receptor

Structure of the neurotensin receptor 1 in complex with β-arrestin 1

(2020) Weijiao Huang et al.   NATURE

Structure of the M2 muscarinic receptor–β-arrestin complex in a lipid nanodisc

(2020) Dean P. Staus et al.   NATURE

Molecular mechanism of biased signaling in a prototypical G protein–coupled receptor

(2020) Carl-Mikael Suomivuori et al.   SCIENCE

Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR

(2020) Laura M. Wingler et al.   SCIENCE

β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors

(2020) Lauren M. Slosky et al.   CELL

Molecular basis of β-arrestin coupling to formoterol-bound β1-adrenoceptor

(2020) Yang Lee et al.   NATURE

Conformational Basis of G Protein-Coupled Receptor Signaling Versatility

(2020) Laura M. Wingler et al.   TRENDS IN CELL BIOLOGY

The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides

(2020) Max Meyrath et al.   Nature Communications

Structure of the class D GPCR Ste2 dimer coupled to two G proteins

(2020) Vaithish Velazhahan et al.   NATURE

Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations

(2019) Laura M. Wingler et al.   CELL

APOLLO ‐2: A Randomized, Placebo and Active‐Controlled Phase III Study Investigating Oliceridine ( TRV 130), a G Protein‐Biased Ligand at the μ‐Opioid Receptor, for Management of Moderate to Severe Acute Pain Following Abdominoplasty

(2019) Neil K. Singla et al.   Pain Practice

A complex structure of arrestin-2 bound to a G protein-coupled receptor

(2019) Wanchao Yin et al.   CELL RESEARCH

Different contributions of chemokine N-terminal features attest to a different ligand binding mode and a bias towards activation of ACKR3/CXCR7 compared with CXCR4 and CXCR3

(2018) Martyna Szpakowska et al.   BRITISH JOURNAL OF PHARMACOLOGY

Visualization and analysis of non-covalent contacts using the Protein Contacts Atlas

(2018) Melis Kayikci et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Molecular mechanism of modulating arrestin conformation by GPCR phosphorylation

(2018) Andrija Sente et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Visualization and analysis of non-covalent contacts using the Protein Contacts Atlas

(2018) Melis Kayikci et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Molecular mechanism of modulating arrestin conformation by GPCR phosphorylation

(2018) Andrija Sente et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Mechanisms of signalling and biased agonism in G protein-coupled receptors

(2018) Denise Wootten et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Structural determinants of 5-HT2B receptor activation and biased agonism

(2018) John D. McCorvy et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

CXCR4-targeting nanobodies differentially inhibit CXCR4 function and HIV entry

(2018) Anneleen Van Hout et al.   BIOCHEMICAL PHARMACOLOGY

Nanobody-Fc constructs targeting chemokine receptor CXCR4 potently inhibit signaling and CXCR4-mediated HIV-entry and induce antibody effector functions

(2018) Vladimir Bobkov et al.   BIOCHEMICAL PHARMACOLOGY

Ligand-specific conformational transitions and intracellular transport are required for atypical chemokine receptor 3–mediated chemokine scavenging

(2017) Nicolas Montpas et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2017) Xiangyu Liu et al.   NATURE

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

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

GPCRdb in 2018: adding GPCR structure models and ligands

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

The Diverse Roles of Arrestin Scaffolds in G Protein–Coupled Receptor Signaling

(2017) Yuri K. Peterson et al.   PHARMACOLOGICAL REVIEWS

Distinct conformations of GPCR–β-arrestin complexes mediate desensitization, signaling, and endocytosis

(2017) Thomas J. Cahill et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Structural basis of ligand interaction with atypical chemokine receptor 3

(2017) Martin Gustavsson et al.   Nature Communications

A randomized, Phase IIb study investigating oliceridine (TRV130), a novel µ-receptor G-protein pathway selective (µ-GPS) modulator, for the management of moderate to severe acute pain following abdominoplasty

(2017) Neil Singla et al.   Journal of Pain Research

Protocols for Molecular Modeling with Rosetta3 and RosettaScripts

(2016) Brian J. Bender et al.   BIOCHEMISTRY

DNA immunization combined with scFv phage display identifies antagonistic GCGR specific antibodies and reveals new epitopes on the small extracellular loops

(2016) Bas van der Woning et al.   mAbs

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

(2016) Libin Ye et al.   NATURE

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

Diverse activation pathways in class A GPCRs converge near the G-protein-coupling region

(2016) A. J. Venkatakrishnan et al.   NATURE

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

(2015) Aashish Manglik et al.   CELL

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

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

(2015) Yanyong Kang et al.   NATURE

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

(2015) Wesley K Kroeze et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The importance of ligands for G protein-coupled receptor stability

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

Generic GPCR residue numbers – aligning topology maps while minding the gaps

(2015) Vignir Isberg et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

(2015) Wesley K Kroeze et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Divergent Transducer-specific Molecular Efficacies Generate Biased Agonism at a G Protein-coupled Receptor (GPCR)

(2014) Ryan T. Strachan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

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

Conformational selection in protein binding and function

(2014) Thomas R. Weikl et al.   PROTEIN SCIENCE

Allosteric sodium in class A GPCR signaling

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

The importance of interactions with helix 5 in determining the efficacy of β-adrenoceptor ligands

(2013) Tony Warne et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Protein and ligand preparation: parameters, protocols, and influence on virtual screening enrichments

(2013) G. Madhavi Sastry et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

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

High-Resolution Comparative Modeling with RosettaCM

(2013) Yifan Song et al.   STRUCTURE

Optimization of the Additive CHARMM All-Atom Protein Force Field Targeting Improved Sampling of the Backbone ϕ, ψ and Side-Chain χ1 and χ2 Dihedral Angles

(2012) Robert B. Best et al.   Journal of Chemical Theory and Computation

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

(2012) Kazuko Haga et al.   NATURE

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

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

Fast, scalable generation of high-quality protein multiple sequence alignments using Clustal Omega

(2011) F. Sievers et al.   Molecular Systems Biology

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

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

OPM database and PPM web server: resources for positioning of proteins in membranes

(2011) Mikhail A. Lomize et al.   NUCLEIC ACIDS RESEARCH

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

An introduction to NMR-based approaches for measuring protein dynamics

(2010) Ian R. Kleckner et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

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

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

Alternate States of Proteins Revealed by Detailed Energy Landscape Mapping

(2010) Michael D. Tyka et al.   JOURNAL OF MOLECULAR BIOLOGY

 -arrestin- but not G protein-mediated signaling by the "decoy" receptor CXCR7

(2009) S. Rajagopal et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ligand binding and micro-switches in 7TM receptor structures

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

OCTOPUS: improving topology prediction by two-track ANN-based preference scores and an extended topological grammar

(2008) Håkan Viklund et al.   BIOINFORMATICS

Noncompetitive Antagonism and Inverse Agonism as Mechanism of Action of Nonpeptidergic Antagonists at Primate and Rodent CXCR3 Chemokine Receptors

(2008) D. Verzijl et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

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

 -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