Human A(2A) adenosine receptors: high-affinity agonist binding to receptor-G protein complexes containing Gbeta(4).

No abstract is available for this paper.

• Publication year

  2002

• Venue

  Molecular Pharmacology

• Publication date

  Unknown publication date

• Fields of study

  Medicine, Chemistry

• Identifiers
  PMID 11809871
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Design, synthesis, and evaluation of novel A2A adenosine receptor agonists.

  2001cited by this paper
• Molecular approach to adenosine receptors: receptor-mediated mechanisms of tissue protection.

  2001cited by this paper
• Cyclic AMP-dependent inhibition of human neutrophil oxidative activity by substituted 2-propynylcyclohexyl adenosine A(2A) receptor agonists.

  2001cited by this paper
• The G protein beta subunit is a determinant in the coupling of Gs to the beta 1-adrenergic and A2a adenosine receptors.

  2001cited by this paper
• G Protein beta subunit types differentially interact with a muscarinic receptor but not adenylyl cyclase type II or phospholipase C-beta 2/3.

  2001cited by this paper
• Neutrophil A2A adenosine receptor inhibits inflammation in a rat model of meningitis: synergy with the type IV phosphodiesterase inhibitor, rolipram.

  1999cited by this paper
• 2-Substituted N-ethylcarboxamidoadenosine derivatives as high-affinity agonists at human A3 adenosine receptors

  1999cited by this paper
• Purification of A1 adenosine receptor-G-protein complexes: effects of receptor down-regulation and phosphorylation on coupling.

  1999cited by this paper
• An agonist of adenosine A3 receptors decreases interleukin-12 and interferon-gamma production and prevents lethality in endotoxemic mice.

  1998cited by this paper
• Adenosine A3 receptors: novel ligands and paradoxical effects.

  1998cited by this paper
• Comparative pharmacology of human adenosine receptor subtypes – characterization of stably transfected receptors in CHO cells

  1997cited by this paper
• Reconstitution of bovine A1 adenosine receptors and G proteins in phospholipid vesicles: betagamma-subunit composition influences guanine nucleotide exchange and agonist binding.

  1997cited by this paper
• Adenosine A2a receptor activation delays apoptosis in human neutrophils.

  1997cited by this paper
• Inhibition of TNF-alpha expression by adenosine: role of A3 adenosine receptors.

  1996cited by this paper
• Double tagging recombinant A1- and A2A-adenosine receptors with hexahistidine and the FLAG epitope. Development of an efficient generic protein purification procedure.

  1996cited by this paper
• Adenosine receptor agonists differentially regulate IL-10, TNF-alpha, and nitric oxide production in RAW 264.7 macrophages and in endotoxemic mice.

  1996cited by this paper
• The in vitro pharmacology of ZM 241385, a potent, non‐xanthine, A2a selective adenosine receptor antagonist

  1995cited by this paper
• Characterization of two affinity states of adenosine A2a receptors with a new radioligand, 2-[2-(4-amino-3-[125I]iodophenyl)ethylamino]adenosine.

  1995cited by this paper
• A carboxyl-terminally truncated mutant and nonglycosylated A2a adenosine receptors retain ligand binding.

  1994cited by this paper
• Differential regulatory effects of adenosine on cytokine release by activated human monocytes.

  1994cited by this paper
• Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.

  1994cited by this paper
• Molecular cloning and functional expression of a sheep A3 adenosine receptor with widespread tissue distribution.

  1993cited by this paper
• A1 adenosine receptors of bovine brain couple to guanine nucleotide-binding proteins Gi1, Gi2, and Go.

  1991cited by this paper
• Effect of hypoxia on nerve-stimulation-induced release of noradrenaline from the rabbit heart.

  1988cited by this paper
• Fitting curves to data using nonlinear regression: a practical and nonmathematical review

  1987cited by this paper
• [125I]Aminobenzyladenosine, a new radioligand with improved specific binding to adenosine receptors in heart.

  1985cited by this paper
• Rapid agonist-induced decrease of 125I-pindolol binding to beta-adrenergic receptors. Relationship to desensitization of cyclic AMP accumulation in intact heart cells.

  1984cited by this paper
• Calculating the dissociation constant of an unlabeled compound from the concentration required to displace radiolabel binding by 50%.

  1982cited by this paper

• Structural Insights into Partial Activation of the Prototypic G Protein-Coupled Adenosine A2A Receptor.

  2024cites this paper
• G protein β4 as a structural determinant of enhanced nucleotide exchange in the A2AAR-Gs complex

  2024cites this paper
• Intracellular VHHs to monitor and modulate GPCR signaling

  2022cites this paper
• Yeast-based directed-evolution for high-throughput structural stabilization of G protein-coupled receptors (GPCRs)

  2022cites this paper
• Nucleoside transporters and immunosuppressive adenosine signaling in the tumor microenvironment: Potential therapeutic opportunities.

  2022cites this paper
• Agonist Binding and G Protein Coupling in Histamine H2 Receptor: A Molecular Dynamics Study

  2020cites this paper
• Adenosine A2A receptor agonist (regadenoson) in human lung transplantation.

  2020cites this paper
• Reconstruction of apo A2A receptor activation pathways reveal ligand-competent intermediates and state-dependent cholesterol hotspots

  2019cites this paper
• Molecular Basis of Modulating Adenosine Receptors Activities.

  2019cites this paper
• Dynamic Role of the G Protein in Stabilizing the Active State of the Adenosine A2A Receptor

  2019cites this paper
• Species differences and mechanism of action of A3 adenosine receptor allosteric modulators

  2018cites this paper
• AquaMMapS: An Alternative Tool to Monitor the Role of Water Molecules During Protein–Ligand Association

  2018cites this paper
• Activation of adenosine A2A or A2B receptors causes hypothermia in mice

  2018cites this paper
• Active state structures of G protein-coupled receptors highlight the similarities and differences in the G protein and arrestin coupling interfaces.

  2017cites this paper
• A2AR Binding Kinetics in the Ligand Depletion Regime

  2017cites this paper
• Nanobodies to Study G Protein-Coupled Receptor Structure and Function.

  2017cites this paper
• Human Adenosine A2A Receptor: Molecular Mechanism of Ligand Binding and Activation

  2017cites this paper
• Mechanisms of modulation of cytokine release by human cord blood monocytes exposed to high concentrations of caffeine

  2016cites this paper
• Role of extracellular cysteine residues in the adenosine A2A receptor

  2016cites this paper
• Structure of the adenosine A2A receptor bound to an engineered G protein

  2016cites this paper
• Studies of interactions of STIM1 and GPCRs with their binding partners

  2015cites this paper
• Novel approaches for targeting the adenosine A2A receptor

  2015cites this paper
• The infarct-sparing effect of IB-MECA against myocardial ischemia/reperfusion injury in mice is mediated by sequential activation of adenosine A3 and A2A receptors

  2015cites this paper
• Selectivity is species-dependent: Characterization of standard agonists and antagonists at human, rat, and mouse adenosine receptors

  2015cites this paper
• Programmable Nanoscaffolds That Control Ligand Display to a G-Protein-Coupled Receptor in Membranes To Allow Dissection of Multivalent Effects

  2014cites this paper
• Adenosine A2A receptor as a drug discovery target.

  2014cites this paper
• Protection from Myocardial Ischemia/Reperfusion Injury by a Positive Allosteric Modulator of the A3 Adenosine Receptor

  2012cites this paper
• Agonist-bound structures of G protein-coupled receptors.

  2012cites this paper
• Adenosine A2A receptor activation reduces recurrence and mortality from Clostridium difficile infection in mice following vancomycin treatment

  2012cites this paper
• Activity of LUF6000 and LUF6096 as positive allosteric modulators (PAMs) for the A3 adenosine receptor (AR) is species‐dependent

  2012cites this paper
• The importance of alkynyl chain presence for the activity of adenine nucleosides/nucleotides on purinergic receptors.

  2011cites this paper
• Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

  2011cites this paper
• Technology development for the over-expression, purification and crystallisation of human membrane proteins

  2011cites this paper
• Binding of β4γ5 by adenosine A1 and A2A receptors determined by stable isotope labeling with amino acids in cell culture and mass spectrometry.

  2011cites this paper
• Thermostabilisation of an Agonist-Bound Conformation of the Human Adenosine A2A Receptor

  2011cites this paper
• A Role for the Low-Affinity A2B Adenosine Receptor in Regulating Superoxide Generation by Murine Neutrophils

  2011cites this paper
• Detection of novel functional selectivity at M3 muscarinic acetylcholine receptors using a Saccharomyces cerevisiae platform.

  2010cites this paper
• Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists.

  2010cites this paper
• Sf9 cells: a versatile model system to investigate the pharmacological properties of G protein-coupled receptors.

  2010cites this paper
• Adenosine A2A Receptor Signaling and Golf Assembly Show a Specific Requirement for the γ7 Subtype in the Striatum*

  2010cites this paper
• Characterization of the A2B Adenosine Receptor from Mouse, Rabbit, and Dog

  2009cites this paper
• Structural Determinants Involved in the Formation and Activation of G Protein βγ Dimers

  2009cites this paper
• The A3 Adenosine Receptor Agonist CP-532,903 [N6-(2,5-Dichlorobenzyl)-3′-aminoadenosine-5′-N-methylcarboxamide] Protects against Myocardial Ischemia/Reperfusion Injury via the Sarcolemmal ATP-Sensitive Potassium Channel

  2008cites this paper
• Adenosine A2A receptor activation reduces infarct size in the isolated, perfused mouse heart by inhibiting resident cardiac mast cell degranulation.

  2008cites this paper
• A2A receptors in inflammation and injury: lessons learned from transgenic animals

  2008cites this paper
• A2A adenosine receptor and its modulators: overview on a druggable GPCR and on structure-activity relationship analysis and binding requirements of agonists and antagonists.

  2008cites this paper
• Pharmacological characterisation and inhibitory effects of (2R,3R,4S,5R)-2-(6-amino-2-{[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino}-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydro-3,4-furandiol, a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor

  2007cites this paper
• THE ADENOSINE 2A RECEPTOR AGONIST ATL‐146E ATTENUATES EXPERIMENTAL POSTHEMORRHAGIC VASOSPASM

  2007influential citation
• Influence of differential stability of G protein βγ dimers containing the γ11 subunit on functional activity at the M1 muscarinic receptor, A1 adenosine receptor, and phospholipase C-β.

  2006cites this paper
• Functional Coupling of the Gαolf Variant XLGαolf with the Human Adenosine A2A Receptor

  2006cites this paper
• Adenosine Inhibits Matrix Metalloproteinase-9 Secretion By Neutrophils: Implication of A2a Receptor and cAMP/PKA/Ca2+ Pathway

  2006cites this paper
• Attenuation of gastric mucosal inflammation induced by aspirin through activation of A2A adenosine receptor in rats.

  2006cites this paper
• Adenosine A2A receptors are expressed in human atrial myocytes and modulate spontaneous sarcoplasmic reticulum calcium release.

  2006cites this paper
• A selective adenosine A2A receptor agonist, ATL-146e, prevents concanavalin A-induced acute liver injury in mice.

  2006cites this paper
• Cl-IB-MECA [2-Chloro-N6-(3-iodobenzyl)adenosine-5′-N-methylcarboxamide] Reduces Ischemia/Reperfusion Injury in Mice by Activating the A Adenosine Receptor

  2006cites this paper
• Characterization of [125I]ZM 241385 binding to adenosine A2A receptors in the pineal of sheep brain.

  2006cites this paper
• Modulation of signal transduction of heptahelical receptors by other receptors and G proteins

  2006cites this paper
• The allosteric enhancer PD81,723 increases chimaeric A1/A2A adenosine receptor coupling with Gs.

  2006cites this paper
• Characterization of human and rodent native and recombinant adenosine A2B receptors by radioligand binding studies

  2006cites this paper
• Lipopolysaccharide rapidly modifies adenosine receptor transcripts in murine and human macrophages: role of NF-kappaB in A(2A) adenosine receptor induction.

  2005cites this paper
• A2A Adenosine Receptors on Bone Marrow-Derived Cells Protect Liver from Ischemia-Reperfusion Injury1

  2005cites this paper
• Selective adenosine A receptor agonist, ATL-146e, attenuates stress-induced gastric lesions in rats.

  2005cites this paper
• Characterization of 16 human G protein-coupled receptors expressed in baculovirus-infected insect cells.

  2005cites this paper
• Optimisation of insect cell growth in deep-well blocks: development of a high-throughput insect cell expression screen.

  2005cites this paper
• Selective A2A adenosine agonist ATL-146e attenuates acute lethal liver injury in mice

  2005cites this paper
• Selective adenosine A2A receptor agonist, ATL‐146e, attenuates stress‐induced gastric lesions in rats

  2005cites this paper
• Adenosine Inhibits Tumor Necrosis Factor-α Release from Mouse Peritoneal Macrophages via A2A and A2B but Not the A3 Adenosine Receptor

  2005cites this paper
• Regulation of Adenosine Receptor Subtypes during Cultivation of Human Monocytes: Role of Receptors in Preventing Lipopolysaccharide-Triggered Respiratory Burst

  2004cites this paper
• Activation of A2A adenosine receptors inhibits expression of alpha 4/beta 1 integrin (very late antigen-4) on stimulated human neutrophils.

  2004cites this paper
• Building a better fluid for emergency resuscitation of traumatic brain injury.

  2004cites this paper
• Regulation of receptor-coupling to (multiple) G proteins. A challenge for basic research and drug discovery.

  2004cites this paper
• Development of a Sensitive and HTS-Compatible Reporter Gene Assay for Functional Analysis of Human Adenosine A2a Receptors in CHO-K1 Cells

  2004cites this paper
• Inhibition of sequestration of human B2 bradykinin receptor by phenylarsine oxide or sucrose allows determination of a receptor affinity shift and ligand dissociation in intact cells

  2004cites this paper
• Physiological control of immune response and inflammatory tissue damage by hypoxia-inducible factors and adenosine A2A receptors.

  2004cites this paper
• New potent and selective A1 adenosine receptor agonists.

  2004cites this paper
• Activation of A2A adenosine receptors inhibits expression of α4/β1 integrin (very late antigen‐4) on stimulated human neutrophils

  2004cites this paper
• Expression of A3 adenosine receptors in human lymphocytes: up-regulation in T cell activation.

  2004cites this paper
• Protection from ischemic liver injury by activation of A2A adenosine receptors during reperfusion: inhibition of chemokine induction.

  2004cites this paper
• A2A adenosine receptor activation improves survival in mouse models of endotoxemia and sepsis.

  2004cites this paper
• Expression of A 3 Adenosine Receptors in Human Lymphocytes : Up-Regulation in T Cell Activation

  2004cites this paper
• Pharmacological analysis of calcium responses mediated by the human A3 adenosine receptor in monocyte-derived dendritic cells and recombinant cells.

  2003cites this paper
• G protein-coupled receptor overexpression with the baculovirus-insect cell system: a tool for structural and functional studies.

  2003cites this paper
• Protection from myocardial stunning by ischaemia and hypoxia with the adenosine A3 receptor agonist, IB-MECA.

  2003cites this paper
• Use of the A(2A) adenosine receptor as a physiological immunosuppressor and to engineer inflammation in vivo.

  2003cites this paper
• A3 adenosine receptor agonist IB-MECA reduces myocardial ischemia-reperfusion injury in dogs.

  2003cites this paper
• The C-terminal Tail Preceding the CAAX Box of a Yeast G Protein γ Subunit Is Dispensable for Receptor-mediated G Protein Activation in Vivo*

  2003cites this paper
• Adenosine receptor agonists: from basic medicinal chemistry to clinical development

  2003cites this paper
• Pharmacologic stress testing: New methods and new agents

  2003cites this paper