Human Adenosine A2A Receptor: Molecular Mechanism of Ligand Binding and Activation

Crystal structure of the adenosine A2Areceptor bound to an antagonist reveals a potential allosteric pocket

(2017) Bingfa Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structures of Human A 1 and A 2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity

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

Serial millisecond crystallography for routine room-temperature structure determination at synchrotrons

(2017) Tobias Weinert et al.   Nature Communications

Serial millisecond crystallography of membrane and soluble protein microcrystals using synchrotron radiation

(2017) Jose M. Martin-Garcia et al.   IUCrJ

Fast iodide-SAD phasing for high-throughput membrane protein structure determination

(2017) Igor Melnikov et al.   Science Advances

Mini-G proteins: Novel tools for studying GPCRs in their active conformation

(2017) Rony Nehmé et al.   PLoS One

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength

(2016) Elena Segala et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2016) Byron Carpenter et al.   NATURE

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

(2016) Libin Ye et al.   NATURE

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

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

A mutagenesis and screening strategy to generate optimally thermostabilized membrane proteins for structural studies

(2016) Francesca Magnani et al.   Nature Protocols

Adenosine receptor targets for pain

(2016) J. Sawynok   NEUROSCIENCE

Engineering a minimal G protein to facilitate crystallisation of G protein-coupled receptors in their active conformation

(2016) Byron Carpenter et al.   PROTEIN ENGINEERING DESIGN & SELECTION

Native phasing of x-ray free-electron laser data for a G protein-coupled receptor

(2016) A. Batyuk et al.   Science Advances

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

(2015) Aashish Manglik et al.   CELL

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

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

Novel Allosteric Modulators of G Protein-coupled Receptors

(2015) Patrick R. Gentry et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Universal allosteric mechanism for Gα activation by GPCRs

(2015) Tilman Flock et al.   NATURE

A comprehensive review of the lipid cubic phase orin mesomethod for crystallizing membrane and soluble proteins and complexes

(2015) Martin Caffrey   Acta Crystallographica Section F-Structural Biology Communications

Probing biased/partial agonism at the G protein-coupled A2B adenosine receptor

(2014) Zhan-Guo Gao et al.   BIOCHEMICAL PHARMACOLOGY

Allosteric sodium in class A GPCR signaling

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

Adenosine—a physiological or pathophysiological agent?

(2013) Bertil B. Fredholm   JOURNAL OF MOLECULAR MEDICINE-JMM

Molecular signatures of G-protein-coupled receptors

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

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

Adenosine receptors as drug targets — what are the challenges?

(2013) Jiang-Fan Chen et al.   NATURE REVIEWS DRUG DISCOVERY

The Role of a Sodium Ion Binding Site in the Allosteric Modulation of the A2A Adenosine G Protein-Coupled Receptor

(2013) Hugo Gutiérrez-de-Terán et al.   STRUCTURE

Agonist-bound structures of G protein-coupled receptors

(2012) Guillaume Lebon et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Discovery of 1,2,4-Triazine Derivatives as Adenosine A2A Antagonists using Structure Based Drug Design

(2012) Miles Congreve et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of the agonist-bound neurotensin receptor

(2012) Jim F. White et al.   NATURE

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

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

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

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

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors--An Update

(2011) B. B. Fredholm et al.   PHARMACOLOGICAL REVIEWS

Structural flexibility of the G s  -helical domain in the  2-adrenoceptor Gs complex

(2011) G. H. Westfield et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Functional selectivity of adenosine receptor ligands

(2011) Dennis Verzijl et al.   Purinergic Signalling

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu 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

Recent developments in adenosine receptor ligands and their potential as novel drugs

(2010) Christa E. Müller et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Engineering G protein-coupled receptors to facilitate their structure determination

(2009) Christopher G Tate et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Thermostabilization of the Neurotensin Receptor NTS1

(2009) Yoko Shibata et al.   JOURNAL OF MOLECULAR BIOLOGY

The structure and function of G-protein-coupled receptors

(2009) Daniel M. Rosenbaum et al.   NATURE

Protein crystallography with a micrometre-sized synchrotron-radiation beam

(2008) Rouslan Moukhametzianov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

(2008) Tony Warne et al.   NATURE

Co-evolving stability and conformational homogeneity of the human adenosine A2a receptor

(2008) F. Magnani et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Adenosine A2A receptors in Parkinson’s disease treatment

(2008) Marek Cieślak et al.   Purinergic Signalling

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

Purinergic signalling

(2006) Geoffrey Burnstock   BRITISH JOURNAL OF PHARMACOLOGY