Evidence map›Paper›PMID 30895781›Full record

ArticleJournal of medicinal chemistry2019

Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors.

Anna Junker, Christian Renn, Clemens Dobelmann, Vigneshwaran Namasivayam, Shanu Jain, Karolina Losenkova, Heikki Irjala, Sierra Duca, Ramachandran Balasubramanian, Saibal Chakraborty and 5 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.

0numbers the graph read from it
0cells of the map it votes in
29citing papers in PubMed
6.8field-weighted citation impact, top 3% 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

29 citing papers in PubMed, 68 citations in OpenAlex.

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  18. Purinergic signaling in diabetes and metabolism.Biochemical pharmacology · 2021
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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

15 authors at 6 institutions in 3 countries.

Anna JunkerMolecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases , National Institutes of Health , Bethesda , Maryland 20892 , United States.
Christian RennPharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I , University of Bonn , An der Immenburg 4 , D-53121 Bonn , Germany.
Clemens DobelmannEuropean Institute for Molecular Imaging (EIMI) , University of Münster , Waldeyerstr. 15 , D-48149 Münster , Germany.
Vigneshwaran NamasivayamPharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I , University of Bonn , An der Immenburg 4 , D-53121 Bonn , Germany.ORCID 0000-0003-3031-3377
Shanu JainMolecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases , National Institutes of Health , Bethesda , Maryland 20892 , United States.
Karolina LosenkovaMedicity Research Laboratory , University of Turku , 20520 Turku , Finland.
Heikki IrjalaDepartment of Otorhinolaryngology-Head and Neck Surgery , Turku University Hospital and Turku University , 20520 Turku , Finland.
Sierra DucaMolecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases , National Institutes of Health , Bethesda , Maryland 20892 , United States.
Ramachandran BalasubramanianMolecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases , National Institutes of Health , Bethesda , Maryland 20892 , United States.
Saibal ChakrabortyMolecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases , National Institutes of Health , Bethesda , Maryland 20892 , United States.
Frederik BörgelInstitute for Pharmaceutical and Medicinal Chemistry , University of Münster , Correnstr. 48 , D-48149 Münster , Germany.
Herbert ZimmermannInstitute of Cell Biology and Neuroscience , Goethe-University , D-60438 Frankfurt am Main , Germany.
Gennady G YegutkinMedicity Research Laboratory , University of Turku , 20520 Turku , Finland.ORCID 0000-0001-6684-7982
Christa E MüllerPharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I , University of Bonn , An der Immenburg 4 , D-53121 Bonn , Germany.ORCID 0000-0002-0013-6624
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 , United States.ORCID 0000-0001-8104-1493
National Institutes of Health · USUniversity of Bonn · DEUniversity of Münster · DEUniversity of Turku · FIGoethe University Frankfurt · DETurku University Hospital · FI

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
Intramural NIH HHS ZIA DK031116Intramural NIH HHS ZIA DK031117
6 · The paper itself

Abstract

Cluster of differentiation 73 (CD73) converts adenosine 5'-monophosphate to immunosuppressive adenosine, and its inhibition was proposed as a new strategy for cancer treatment. We synthesized 5'- O-[(phosphonomethyl)phosphonic acid] derivatives of purine and pyrimidine nucleosides, which represent nucleoside diphosphate analogues, and compared their CD73 inhibitory potencies. In the adenine series, most ribose modifications and 1-deaza and 3-deaza were detrimental, but 7-deaza was tolerated. Uracil substitution with N

Indexed as

5'-NucleotidaseAnimalsEnzyme InhibitorsGPI-Linked ProteinsHumansPurine NucleotidesPyrimidine NucleotidesRatsStructure-Activity Relationship5'-NucleotidaseEnzyme InhibitorsGPI-Linked ProteinsNT5E protein, humanPurine NucleotidesPyrimidine Nucleotides

Identifiers

PMID30895781
PMCPMC6526958
OpenAlexW2923915955

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.