Evidence map›Paper›PMID 15078212›Full record

ReviewCurrent topics in medicinal chemistry2004

Molecular recognition at purine and pyrimidine nucleotide (P2) receptors.

Kenneth A Jacobson, Stefano Costanzi, Michihiro Ohno, Bhalchandra V Joshi, Pedro Besada, Bin Xu, Susanna Tchilibon

Abstract readReview
In one paragraph

Review in Current topics in medicinal chemistry, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.

0numbers the graph read from it
0cells of the map it votes in
31citing papers in PubMed
4.6field-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

31 citing papers in PubMed, 53 citations in OpenAlex.

  1. Purinergic system in cancer stem cells.Purinergic signalling · 2025
    Review
  2. Review
  3. Role of the Purinergic P2Y2 Receptor in Pulmonary Hypertension.International journal of environmental research and public health · 2021
    Review
  4. Article
  5. Review
  6. Quality Evaluation ofMolecules (Basel, Switzerland) · 2018
    Article
  7. Article
  8. Article
  9. Article
  10. Review
  11. Review
  12. Review
  13. Article
  14. Article
  15. Article
  16. Directed molecular screening for RecA ATPase inhibitors.Bioorganic & medicinal chemistry letters · 2007
    Article
  17. Article
  18. 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

7 authors at 1 institution in 1 country.

Kenneth A JacobsonMolecular Recognition Section, Laboratory of Biorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Disease, Bethesda, MD 20892-0810, USA. E-mail: kajacobs@helix.nih.gov
Stefano Costanzi
Michihiro Ohno
Bhalchandra V Joshi
Pedro Besada
Bin Xu
Susanna Tchilibon
National Institute of Diabetes and Digestive and Kidney Diseases · US

Funding

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
Intramural NIH HHS Z01 DK031116
6 · The paper itself

Abstract

In comparison to other classes of cell surface receptors, the medicinal chemistry at P2X (ligand-gated ion channels) and P2Y (G protein-coupled) nucleotide receptors has been relatively slow to develop. Recent effort to design selective agonists and antagonists based on a combination of library screening, empirical modification of known ligands, and rational design have led to the introduction of potent antagonists of the P2X(1) (derivatives of pyridoxal phosphates and suramin), P2X(3)(A-317491), P2X(7) (derivatives of the isoquinoline KN-62), P2Y(1)(nucleotide analogues MRS 2179 and MRS 2279), P2Y(2)(thiouracil derivatives such as AR-C126313), and P2Y(12)(nucleotide/nucleoside analogues AR-C69931X and AZD6140) receptors. A variety of native agonist ligands (ATP, ADP, UTP, UDP, and UDP-glucose) are currently the subject of structural modification efforts to improve selectivity. MRS2365 is a selective agonist for P2Y(1)receptors. The dinucleotide INS 37217 potently activates the P2Y(2)receptor. UTP-gamma-S and UDP-beta-S are selective agonists for P2Y(2)/P2Y(4)and P2Y(6)receptors, respectively. The current knowledge of the structures of P2X and P2Y receptors, is derived mainly from mutagenesis studies. Site-directed mutagenesis has shown that ligand recognition in the human P2Y(1)receptor involves individual residues of both the TMs (3, 5, 6, and 7), as well as EL 2 and 3. The binding of the negatively-charged phosphate moiety is dependent on positively charged lysine and arginine residues near the exofacial side of TMs 3 and 7.

Indexed as

Adenine NucleotidesAnimalsHumansIon Channel GatingLigandsMutagenesis, Site-DirectedPurine NucleotidesPurinergic P2 Receptor AgonistsPurinergic P2 Receptor AntagonistsReceptors, Purinergic P2Uracil NucleotidesAdenine NucleotidesLigandsPurine NucleotidesPurinergic P2 Receptor AgonistsPurinergic P2 Receptor AntagonistsReceptors, Purinergic P2Uracil Nucleotides

Identifiers

PMID15078212
PMCPMC4428617
OpenAlexW1998079322

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.