Evidence map›Paper›PMID 21393508›Full record

ArticleScience (New York, N.Y.)2011

Structure of an agonist-bound human A2A adenosine receptor.

Fei Xu, Huixian Wu, Vsevolod Katritch, Gye Won Han, Kenneth A Jacobson, Zhan-Guo Gao, Vadim Cherezov, Raymond C Stevens

Abstract read
In one paragraph

Article in Science (New York, N.Y.), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 404 papers.

0numbers the graph read from it
0cells of the map it votes in
404citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

The trial behind it

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

404 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Placental SNV rs8192446 in theFrontiers in physiology · 2026
    Article
  5. Adenosine in the Brain: Recent Progress on Detection, Function, and Translation.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2025
    Review
  6. Review
  7. Article
  8. Article
  9. Unlocking GPCR-ligand interactions: Measuring binding affinities with thermal shift assay.Protein science : a publication of the Protein Society · 2025
    Article
  10. Review
  11. Article
  12. Article
  13. Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024
    Article
  19. Membrane mimetic-dependence of GPCR energy landscapes.Structure (London, England : 1993) · 2024
    Article
  20. G protein βResearch square · 2024
    Article

344 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Fei XuDepartment of Molecular Biology, Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Huixian Wu
Vsevolod Katritch
Gye Won Han
Kenneth A Jacobson
Zhan-Guo Gao
Vadim Cherezov
Raymond C Stevens

Funding

JCSG Center:Innovative Membrane Protein Technology (RMI)P50GM073197 · NIGMS · SCRIPPS RESEARCH INSTITUTE, THE · PI STEVENS, RAYMOND C · 2004 to 2013
$26.8M
Project 3U54GM094618 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI STEVENS, RAYMOND C · 2010 to 2014
$17.1M
Development Of Drugs Acting At Adenosine ReceptorsZIADK031117 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$10.4M
Molecular Mechanism of Allosteric Modulation of the Oxytocin Receptor by SterolsR01GM089857 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI CHEREZOV, VADIM · 2010 to 2014
$1.7M
Membrane Proteins. Crystallogenesis/X-ray Structure(RMI)R01GM075915 · NIGMS · UNIVERSITY OF LIMERICK · PI CAFFREY, MARTIN D. · 2005 to 2009
$984k
Intramural NIH HHSNCI NIH HHS Y1-CO-1020NIGMS NIH HHS GM075915NIGMS NIH HHS P50 GM073197NIGMS NIH HHS R01 GM075915NIGMS NIH HHS R01 GM089857NIGMS NIH HHS U54 GM094618NIGMS NIH HHS Y1-GM-1104
6 · The paper itself

Abstract

Activation of G protein-coupled receptors upon agonist binding is a critical step in the signaling cascade for this family of cell surface proteins. We report the crystal structure of the A(2A) adenosine receptor (A(2A)AR) bound to an agonist UK-432097 at 2.7 angstrom resolution. Relative to inactive, antagonist-bound A(2A)AR, the agonist-bound structure displays an outward tilt and rotation of the cytoplasmic half of helix VI, a movement of helix V, and an axial shift of helix III, resembling the changes associated with the active-state opsin structure. Additionally, a seesaw movement of helix VII and a shift of extracellular loop 3 are likely specific to A(2A)AR and its ligand. The results define the molecule UK-432097 as a "conformationally selective agonist" capable of receptor stabilization in a specific active-state configuration.

Indexed as

AdenosineAdenosine A2 Receptor AgonistsBinding SitesCrystallography, X-RayHumansHydrogen BondingLigandsModels, MolecularOpsinsProtein ConformationProtein Structure, SecondaryReceptor, Adenosine A2ARhodopsinTriazinesTriazolesAdenosineAdenosine A2 Receptor AgonistsLigandsOpsinsReceptor, Adenosine A2ARhodopsinTriazinesTriazolesUK-432097ZM 241385

Identifiers

PMID21393508
PMCPMC3086811

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

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.