Structural studies of G protein-coupled receptors

Extra-helical binding site of a glucagon receptor antagonist

(2016) Ali Jazayeri et al.   NATURE

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

(2016) David M. Thal et al.   NATURE

Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1

(2015) Jill E. Chrencik et al.   CELL

Structure of the Angiotensin Receptor Revealed by Serial Femtosecond Crystallography

(2015) Haitao Zhang et al.   CELL

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

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

(2015) Yanyong Kang et al.   NATURE

Crystal structure of the chemokine receptor CXCR4 in complex with a viral chemokine

(2015) L. Qin et al.   SCIENCE

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

Virtual fragment screening on GPCRs: A case study on dopamine D3 and histamine H4 receptors

(2014) Márton Vass et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2014) Ankita Srivastava et al.   NATURE

Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant

(2014) Jie Yin 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

Structure of the human P2Y12 receptor in complex with an antithrombotic drug

(2014) Kaihua Zhang et al.   NATURE

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

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

(2014) H. Wu et al.   SCIENCE

Structure-Based Discovery of Selective Serotonin 5-HT 1B Receptor Ligands

(2014) David Rodríguez et al.   STRUCTURE

Recent developments in biased agonism

(2013) James W Wisler et al.   CURRENT OPINION IN CELL BIOLOGY

Structure of class B GPCR corticotropin-releasing factor receptor 1

(2013) Kaspar Hollenstein et al.   NATURE

Structure of the human smoothened receptor bound to an antitumour agent

(2013) Chong Wang et al.   NATURE

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

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

(2013) Aaron M. Ring et al.   NATURE

Structure of the human glucagon class B G-protein-coupled receptor

(2013) Fai Yiu Siu et al.   NATURE

Molecular signatures of G-protein-coupled receptors

(2013) A. J. Venkatakrishnan et al.   NATURE

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

Serial Femtosecond Crystallography of G Protein-Coupled Receptors

(2013) W. Liu et al.   SCIENCE

Ice breaking in GPCR structural biology

(2012) Qiang Zhao et al.   ACTA PHARMACOLOGICA SINICA

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

High-resolution crystal structure of human protease-activated receptor 1

(2012) Cheng Zhang et al.   NATURE

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

Fusion Partner Toolchest for the Stabilization and Crystallization of G Protein-Coupled Receptors

(2012) Eugene Chun et al.   STRUCTURE

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

(2012) Tony Warne et al.   STRUCTURE

Structure-based drug screening for G-protein-coupled receptors

(2012) Brian K. Shoichet et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Pharmacological modulation of chemokine receptor function

(2011) DJ Scholten et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

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

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

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

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

GPCR oligomers in pharmacology and signaling

(2011) Javier González-Maeso   Molecular Brain

Structure-Based Discovery of Novel Chemotypes for Adenosine A2AReceptor Antagonists

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

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

(2010) Peter Keov et al.   NEUROPHARMACOLOGY

Structure–function analysis of helix 8 of human calcitonin receptor-like receptor within the adrenomedullin 1 receptor

(2010) Kenji Kuwasako et al.   PEPTIDES

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

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

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

(2008) Tony Warne et al.   NATURE

Crystal structure of squid rhodopsin

(2008) Midori Murakami 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

Conformational thermostabilization of the  1-adrenergic receptor in a detergent-resistant form

(2008) M. J. Serrano-Vega 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

Conformational changes involved in G-protein-coupled-receptor activation

(2008) Jürgen Wess et al.   TRENDS IN PHARMACOLOGICAL SCIENCES