Evidence map›Paper›PMID 30737440›Full record

ArticleScientific reports2019

Probing the Inhibition of Microtubule Affinity Regulating Kinase 4 by N-Substituted Acridones.

Maria Voura, Parvez Khan, Savvas Thysiadis, Sotiris Katsamakas, Aarfa Queen, Gulam Mustafa Hasan, Sher Ali, Vasiliki Sarli, Md Imtaiyaz Hassan

Abstract read
In one paragraph

Article in Scientific reports, 2019. 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.

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  17. Terpenoids, Cannabimimetic Ligands, beyond theMolecules (Basel, Switzerland) · 2020
    Review
  18. Article
  19. Genetically encoded FRET-based optical sensor for HgJournal of industrial microbiology & biotechnology · 2019
    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

9 authors.

Maria VouraDepartment of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
Parvez KhanCentre for interdisciplinary research in Basic Sciences, Jamia Millia Islamia, Jamia Nagar, New Delhi, 110025, India.ORCID 0000-0002-8566-0248
Savvas ThysiadisDepartment of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
Sotiris KatsamakasDepartment of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.ORCID 0000-0001-8715-0359
Aarfa QueenCentre for interdisciplinary research in Basic Sciences, Jamia Millia Islamia, Jamia Nagar, New Delhi, 110025, India.
Gulam Mustafa HasanDepartment of Biochemistry, College of Medicine, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj, 11942, Saudi Arabia.
Sher AliCentre for interdisciplinary research in Basic Sciences, Jamia Millia Islamia, Jamia Nagar, New Delhi, 110025, India.
Vasiliki SarliDepartment of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece. sarli@chem.auth.gr.
Md Imtaiyaz HassanCentre for interdisciplinary research in Basic Sciences, Jamia Millia Islamia, Jamia Nagar, New Delhi, 110025, India. mihassan@jmi.ac.in.ORCID 0000-0002-3663-4940

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Microtubule affinity regulating kinase 4 (MARK4) becomes a unique anti-cancer drug target as its overexpression is responsible for different types of cancers. In quest of novel, effective MARK4 inhibitors, some acridone derivatives were synthesized, characterized and evaluated for inhibitory activity against human MARK4. Among all the synthesized compounds, three (7b, 7d and 7f) were found to have better binding affinity and enzyme inhibition activity in µM range as shown by fluorescence binding, ITC and kinase assays. Here we used functional assays of selected potential lead molecules with commercially available panel of 26 kinases of same family. A distinctive kinase selectivity profile was observed for each compound. The selective compounds were identified with submicromolar cellular activity against MARK4. Furthermore, in vitro antitumor evaluation against cancerous cells (MCF-7 and HepG2) revealed that compounds 7b, 7d and 7f inhibit cell proliferation and predominantly induce apoptosis in MCF-7 cells, with IC

Indexed as

AcridonesBinding SitesCell ProliferationCell SurvivalHEK293 CellsHep G2 CellsHumansMCF-7 CellsModels, MolecularMolecular Docking SimulationMolecular StructureProtein ConformationProtein Kinase InhibitorsProtein Serine-Threonine KinasesAcridonesMARK4 protein, humanProtein Kinase InhibitorsProtein Serine-Threonine Kinases

Identifiers

PMID30737440
PMCPMC6368574

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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.