Evidence map›Paper›PMID 18600475›Full record

ArticlePurinergic signalling2009

Development of selective agonists and antagonists of P2Y receptors.

Kenneth A Jacobson, Andrei A Ivanov, Sonia de Castro, T Kendall Harden, Hyojin Ko

Open access · hybridAbstract read
In one paragraph

Article in Purinergic signalling, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers.

0numbers the graph read from it
0cells of the map it votes in
58citing papers in PubMed
4.8field-weighted citation impact, top 5% of its field
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

58 citing papers in PubMed, 117 citations in OpenAlex.

  1. Investigation of reported small molecule P2Y6 receptor antagonists.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026
    Article
  2. Article
  3. Inhibition of (interstitial) P2YPflugers Archiv : European journal of physiology · 2026
    Article
  4. Inhibition of (interstitial) P2YResearch square · 2026
    Article
  5. Inhibition of (interstitial) P2YbioRxiv : the preprint server for biology · 2026
    Article
  6. Article
  7. Review
  8. Purinergic agonists increase [CaAmerican journal of physiology. Cell physiology · 2024
    Article
  9. Review
  10. Involvement of P2YCells · 2023
    Article
  11. Review
  12. Review
  13. Article
  14. Article
  15. Article
  16. Article
  17. Purinergic Receptors Crosstalk with CCR5 to Amplify CaCellular and molecular neurobiology · 2021
    Article
  18. Purinergic P2YCellular and molecular life sciences : CMLS · 2020
    Article
  19. Article
  20. Article
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

5 authors at 3 institutions in 1 country.

Kenneth A JacobsonMolecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bldg. 8A, Rm. B1A-19, Bethesda, MD, USA, kajacobs@helix.nih.gov.
Andrei A Ivanov
Sonia de Castro
T Kendall Harden
Hyojin Ko
National Institute of Diabetes and Digestive and Kidney Diseases · USNational Institutes of Health · USUniversity of North Carolina at Chapel Hill · US

Funding

Development Of P2Y Receptor LigandsZIADK031116 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$8.9M
PROSTHETIC GROUPS FOR RADIOLABELING OF FUNCTIONALIZED DRUGS AND PEPTIDESZ01DK031116 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 1991 to 2008
$769k
6 · The paper itself

Abstract

Although elucidation of the medicinal chemistry of agonists and antagonists of the P2Y receptors has lagged behind that of many other members of group A G protein-coupled receptors, detailed qualitative and quantitative structure-activity relationships (SARs) were recently constructed for several of the subtypes. Agonists selective for P2Y(1), P2Y(2), and P2Y(6) receptors and nucleotide antagonists selective for P2Y(1) and P2Y(12) receptors are now known. Selective nonnucleotide antagonists were reported for P2Y(1), P2Y(2), P2Y(6), P2Y(11), P2Y(12), and P2Y(13) receptors. At the P2Y(1) and P2Y(12) receptors, nucleotide agonists (5'-diphosphate derivatives) were converted into antagonists of nanomolar affinity by altering the phosphate moieties, with a focus particularly on the ribose conformation and substitution pattern. Nucleotide analogues with conformationally constrained ribose-like rings were introduced as selective receptor probes for P2Y(1) and P2Y(6) receptors. Screening chemically diverse compound libraries has begun to yield new lead compounds for the development of P2Y receptor antagonists, such as competitive P2Y(12) receptor antagonists with antithrombotic activity. Selective agonists for the P2Y(4), P2Y(11), and P2Y(13) receptors and selective antagonists for P2Y(4) and P2Y(14) receptors have not yet been identified. The P2Y(14) receptor appears to be the most restrictive of the class with respect to modification of the nucleobase, ribose, and phosphate moieties. The continuing process of ligand design for the P2Y receptors will aid in the identification of new clinical targets.

Identifiers

PMID18600475
PMCPMC2721770
OpenAlexW1979393217

What OpenQuestion holds

Textmetadata
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.