Evidence map›Paper›PMID 29747534›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2018

Binding investigation and preliminary optimisation of the 3-amino-1,2,4-triazin-5(2H)-one core for the development of new Fyn inhibitors.

Giulio Poli, Margherita Lapillo, Carlotta Granchi, Jessica Caciolla, Nayla Mouawad, Isabella Caligiuri, Flavio Rizzolio, Thierry Langer, Filippo Minutolo, Tiziano Tuccinardi

Abstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.

0numbers the graph read from it
0cells of the map it votes in
21citing 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

21 citing papers in PubMed.

  1. Zebrafish frk Gene Knockout Shows Social Impairments Relevant to Autism and Delays Brain Development by Increasing Cell Proliferation.Autism research : official journal of the International Society for Autism Research · 2026
    Article
  2. Article
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  12. GSK-3β, FYN, and DYRK1A: Master Regulators in Neurodegenerative Pathways.International journal of molecular sciences · 2021
    Review
  13. Review
  14. Article
  15. Application of MM-PBSA Methods in Virtual Screening.Molecules (Basel, Switzerland) · 2020
    Review
  16. The Journal of biological chemistry · 2020
    Article
  17. Article
  18. Article
  19. First-of-its-kind STARDACS medicinal chemistry letters · 2019
    Article
  20. Extensive Reliability Evaluation of Docking-Based Target-Fishing Strategies.International journal of molecular sciences · 2019
    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

10 authors.

Giulio Polia Department of Pharmacy , University of Pisa , Pisa , Italy.
Margherita Lapilloa Department of Pharmacy , University of Pisa , Pisa , Italy.
Carlotta Granchia Department of Pharmacy , University of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0002-5849-0722
Jessica Caciollaa Department of Pharmacy , University of Pisa , Pisa , Italy.
Nayla Mouawada Department of Pharmacy , University of Pisa , Pisa , Italy.
Isabella Caligiurib Pathology Unit, Department of Molecular Biology and Translational Research , National Cancer Institute and Center for Molecular Biomedicine , Aviano (PN) , Italy.
Flavio Rizzoliob Pathology Unit, Department of Molecular Biology and Translational Research , National Cancer Institute and Center for Molecular Biomedicine , Aviano (PN) , Italy.ORCID http://orcid.org/0000-0002-3400-4363
Thierry Langerd Department of Pharmaceutical Chemistry, Faculty of Life Sciences , University of Vienna , Vienna , Austria.
Filippo Minutoloa Department of Pharmacy , University of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0002-3312-104X
Tiziano Tuccinardia Department of Pharmacy , University of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0002-6205-4069

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Fyn tyrosine kinase inhibitors are considered potential therapeutic agents for a variety of human cancers. Furthermore, the involvement of Fyn kinase in signalling pathways that lead to severe pathologies, such as Alzheimer's and Parkinson's diseases, has also been demonstrated. In this study, starting from 3-(benzo[d][1,3]dioxol-5-ylamino)-6-methyl-1,2,4-triazin-5(2H)-one (VS6), a hit compound that showed a micromolar inhibition of Fyn (IC

Indexed as

Antineoplastic AgentsBinding SitesCell Line, TumorCell ProliferationCell SurvivalCytosineDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansModels, MolecularMolecular StructureProtein Kinase InhibitorsProto-Oncogene Proteins c-fynStructure-Activity Relationship6-azacytosineAntineoplastic AgentsCytosineProtein Kinase InhibitorsProto-Oncogene Proteins c-fyndrug designFyn kinasekinase inhibitorsmolecular modelling

Identifiers

PMID29747534
PMCPMC6009924

What OpenQuestion holds

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LicenceCC BY
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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.