Evidence map›Paper›PMID 33130128›Full record

ReviewBiochemical pharmacology2021

Medicinal chemistry of P2 and adenosine receptors: Common scaffolds adapted for multiple targets.

Kenneth A Jacobson, Adriaan P IJzerman, Christa E Müller

Open access · greenAbstract readReview
In one paragraph

Review in Biochemical pharmacology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
4.3field-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

20 citing papers in PubMed, 43 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Ligand-Directed Labeling of the Adenosine AJournal of medicinal chemistry · 2024
    Article
  5. DualACS medicinal chemistry letters · 2024
    Article
  6. Fluorescent APurinergic signalling · 2023
    Article
  7. Review
  8. Review
  9. Review
  10. "Dual Anta-Inhibitors" of the APharmaceuticals (Basel, Switzerland) · 2023
    Article
  11. Review
  12. AMolecules (Basel, Switzerland) · 2022
    Article
  13. Review
  14. Review
  15. ACurrent medicinal chemistry · 2022
    Review
  16. Article
  17. Review
  18. TNAP as a New Player in Chronic Inflammatory Conditions and Metabolism.International journal of molecular sciences · 2021
    Review
  19. Review
  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

3 authors at 3 institutions in 3 countries.

Kenneth A JacobsonMolecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, United States. Electronic address: kennethj@niddk.nih.gov.
Adriaan P IJzermanDivision of Drug Discovery and Safety, LACDR, Leiden University, the Netherlands.
Christa E MüllerPharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.
Centre for Human Drug Research · NLNational Institute of Diabetes and Digestive and Kidney Diseases · USUniversity of Bonn · DE

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
Intramural NIH HHS ZIA DK031116Intramural NIH HHS ZIA DK031117Intramural NIH HHS ZIA DK031126
6 · The paper itself

Abstract

Prof. Geoffrey Burnstock originated the concept of purinergic signaling. He demonstrated the interactions and biological roles of ionotropic P2X and metabotropic P2Y receptors. This review paper traces the historical origins of many currently used antagonists and agonists for P2 receptors, as well as adenosine receptors, in early attempts to identify ligands for these receptors - prior to the use of chemical libraries for screening. Rather than presenting a general review of current purinergic ligands, we focus on common chemical scaffolds (privileged scaffolds) that can be adapted for multiple receptor targets. By carefully analyzing the structure activity relationships, one can direct the selectivity of these scaffolds toward different receptor subtypes. For example, the weak and non-selective P2 antagonist reactive blue 2 (RB-2) was derivatized using combinatorial synthetic approaches, leading to the identification of selective P2Y

Indexed as

AnimalsArthritis, RheumatoidChemistry, PharmaceuticalChronic PainDrug Delivery SystemsHumansPurinergic P1 Receptor AgonistsPurinergic P1 Receptor AntagonistsPurinergic P2 Receptor AgonistsPurinergic P2 Receptor AntagonistsPyridinesReceptors, Purinergic P1Receptors, Purinergic P2TriazolesJNJ-54175446Purinergic P1 Receptor AgonistsPurinergic P1 Receptor AntagonistsPurinergic P2 Receptor AgonistsPurinergic P2 Receptor AntagonistsPyridinesReceptors, Purinergic P1Receptors, Purinergic P2TriazolesAdenosine receptorP2X receptorP2Y receptorPurinergic agonistPurinergic antagonistScaffold

Identifiers

PMID33130128
PMCPMC8081756
OpenAlexW3095533779

What OpenQuestion 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 OpenQuestion graph.