ArticleScience (New York, N.Y.)2008
The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist.
Article in Science (New York, N.Y.), 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 784 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
784 citing papers in PubMed, 1 synthesis or guideline pooled it, 1,741 citations in OpenAlex.
- Transactivation of receptor tyrosine kinases by purinergic P2Y and adenosine receptors.Purinergic signalling · 2023Pooled it
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- Molecular Docking of Natural Products: Critical Appraisal of Current Methodology and Practical Guidelines.Molecules (Basel, Switzerland) · 2026Review
- Molecular Insights into Caffeine Stacking, Partitioning, and Organization in DPPC Lipid Bilayers from Microseconds-Long Molecular Dynamics Simulations.International journal of molecular sciences · 2026Article
- Synthesis and Biological Activity of 2,6-Disubstituted and 2,6,9-Trisubstituted 7-Deazapurine Nucleobases.ChemMedChem · 2026Article
- Water Deficit and Methyl Jasmonate Enhance the Antiplatelet Potential of Blueberries Through Changes in Selected Phenolic Compounds.International journal of molecular sciences · 2026Article
- Article
- Atomistic insights into the magnetic-field modulation of the [Formula: see text] adenosine receptor.Scientific reports · 2026Article
- Glyceryl Trinitrate Enhances Caffeine Cytotoxicity Under Metabolic Stress in Cancer Cells.Molecules (Basel, Switzerland) · 2026Article
- A novel fusion tool to enable G protein-coupled receptor structure determination.Acta crystallographica. Section D, Structural biology · 2026Article
- Membrane protein structure and dynamics probed by MicroED.Biochemical Society transactions · 2026Review
- Evaluating 7‑Aminopyrazolo[4,3‑ACS omega · 2026Article
- Tool antibody fragments reveal multiple conformations of the rhodopsin-Gi signaling complex.Biophysical journal · 2026Article
- An integrated experimental and computational pipeline for crystallographic fragment screening of membrane protein in the lipid cubic phase.Communications chemistry · 2026Article
- Unraveling allosteric signaling of G protein-coupled receptors (GPCRs) by single-molecule fluorescence.Biophysical reviews · 2026Review
- Target-Centric Multiplexed Screening of an Herbal Extract Identifies a Novel Dual AACS central science · 2026Article
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- ABEL-FRET bridges the timescale gap in single-molecule measurements of the structural dynamics in the ACommunications chemistry · 2026Article
- Discovery of novel AMolecular diversity · 2025Article
724 more citing papers are in PubMed but not listed here.
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PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
The adenosine class of heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs) mediates the important role of extracellular adenosine in many physiological processes and is antagonized by caffeine. We have determined the crystal structure of the human A2A adenosine receptor, in complex with a high-affinity subtype-selective antagonist, ZM241385, to 2.6 angstrom resolution. Four disulfide bridges in the extracellular domain, combined with a subtle repacking of the transmembrane helices relative to the adrenergic and rhodopsin receptor structures, define a pocket distinct from that of other structurally determined GPCRs. The arrangement allows for the binding of the antagonist in an extended conformation, perpendicular to the membrane plane. The binding site highlights an integral role for the extracellular loops, together with the helical core, in ligand recognition by this class of GPCRs and suggests a role for ZM241385 in restricting the movement of a tryptophan residue important in the activation mechanism of the class A receptors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.