Evidence map›Paper›PMID 23597047›Full record

ReviewJournal of medicinal chemistry2013

Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates.

Kenneth A Jacobson

Abstract readReview
In one paragraph

Review in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing 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

16 citing papers in PubMed.

  1. Review
  2. Review
  3. P2YMolecules (Basel, Switzerland) · 2021
    Review
  4. Synthetic Strategies for Dinucleotides Synthesis.Molecules (Basel, Switzerland) · 2019
    Review
  5. Article
  6. Review
  7. Article
  8. Purinergic regulation of the immune system.Nature reviews. Immunology · 2016
    Review
  9. Article
  10. Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System.Evidence-based complementary and alternative medicine : eCAM · 2016
    Article
  11. New paradigms in GPCR drug discovery.Biochemical pharmacology · 2015
    Review
  12. Review
  13. Article
  14. Article
  15. Review
  16. Review
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

1 author.

Kenneth A JacobsonMolecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892, USA. kajacobs@helix.nih.gov

Funding

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
Development Of P2Y Receptor LigandsZIADK031116 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$8.9M
Computer Modeling of G Protein-Coupled ReceptorsZIADK031126 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$6.6M
Functionalized Congeners Of Bioactive CompoundsZIADK031115 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$5.3M
Intramural NIH HHS Z99 DA999999Intramural NIH HHS Z99 DK999999Intramural NIH HHS Z99 OD999999Intramural NIH HHS ZIA DK031116Intramural NIH HHS ZIA DK031117Intramural NIH HHS ZIA DK031126
6 · The paper itself

Abstract

Adenosine receptor (ARs) and P2Y receptors (P2YRs) that respond to extracellular nucleosides/nucleotides are associated with new directions for therapeutics. The X-ray structures of the A2AAR complexes with agonists and antagonists are examined in relationship to the G-protein-coupled receptor (GPCR) superfamily and applied to drug discovery. Much of the data on AR ligand structure from early SAR studies now are explainable from the A2AAR X-ray crystallography. The ligand-receptor interactions in related GPCR complexes can be identified by means of modeling approaches, e.g., molecular docking. Thus, molecular recognition in binding and activation processes has been studied effectively using homology modeling and applied to ligand design. Virtual screening has yielded new nonnucleoside AR antagonists, and existing ligands have been improved with knowledge of the receptor interactions. New agonists are being explored for central nervous system and peripheral therapeutics based on in vivo activity, such as chronic neuropathic pain. Ligands for receptors more distantly related to the X-ray template, i.e., P2YRs, have been introduced and are mainly used as pharmacological tools for elucidating the physiological role of extracellular nucleotides. Other ligand tools for drug discovery include fluorescent probes, radioactive probes, multivalent probes, and functionalized nanoparticles.

Indexed as

Adenosine A2 Receptor AgonistsAdenosine A2 Receptor AntagonistsAnimalsDrug DesignDrug DiscoveryFluorescent DyesHigh-Throughput Screening AssaysHumansIndicators and ReagentsLigandsNanoconjugatesRadiopharmaceuticalsReceptor, Adenosine A2AReceptors, G-Protein-CoupledReceptors, Purinergic P1Receptors, Purinergic P2YAdenosine A2 Receptor AgonistsAdenosine A2 Receptor AntagonistsFluorescent DyesIndicators and ReagentsLigandsNanoconjugatesRadiopharmaceuticalsReceptor, Adenosine A2AReceptors, G-Protein-CoupledReceptors, Purinergic P1Receptors, Purinergic P2YSmall Molecule Libraries

Identifiers

PMID23597047
PMCPMC3701956

What Socratic holds

Textmetadata
LicenceTDM
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 Socratic graph.