Evidence map›Paper›PMID 32193613›Full record

ArticleJournal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry2020

Biological evaluation of novel thiomaltol-based organometallic complexes as topoisomerase IIα inhibitors.

Maria S Legina, Juan J Nogueira, Wolfgang Kandioller, Michael A Jakupec, Leticia González, Bernhard K Keppler

Open access · hybridAbstract read
In one paragraph

Article in Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.3field-weighted citation impact, top 21% 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

12 citing papers in PubMed, 19 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Review
  5. Article
  6. Article
  7. Review
  8. Article
  9. Review
  10. Article
  11. Cosolvent and Dynamic Effects in Binding Pocket Search by Docking Simulations.Journal of chemical information and modeling · 2021
    Article
  12. 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

6 authors at 2 institutions in 2 countries.

Maria S LeginaFaculty of Chemistry, Institute of Inorganic Chemistry, University of Vienna, Vienna, Austria.
Juan J NogueiraIADCHEM, Institute for Advanced Research in Chemistry, Universidad Autónoma de Madrid, Madrid, Spain.ORCID 0000-0001-7419-5670
Wolfgang KandiollerFaculty of Chemistry, Institute of Inorganic Chemistry, University of Vienna, Vienna, Austria.ORCID 0000-0002-5630-712X
Michael A JakupecFaculty of Chemistry, Institute of Inorganic Chemistry, University of Vienna, Vienna, Austria. michael.jakupec@univie.ac.at.ORCID 0000-0001-7945-1426
Leticia GonzálezFaculty of Chemistry, Institute of Theoretical Chemistry, University of Vienna, Vienna, Austria.ORCID 0000-0001-5112-794X
Bernhard K KepplerFaculty of Chemistry, Institute of Inorganic Chemistry, University of Vienna, Vienna, Austria.ORCID 0000-0003-0877-1822
University of Vienna · ATUniversidad Autónoma de Madrid · ES

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Topoisomerase IIα (topo2α) is an essential nuclear enzyme involved in DNA replication, transcription, recombination, chromosome condensation, and highly expressed in many tumors. Thus, topo2α-targeting has become a very efficient and well-established anticancer strategy. Herein, we investigate the cytotoxic and DNA-damaging activity of thiomaltol-containing ruthenium-, osmium-, rhodium- and iridium-based organometallic complexes in human mammary carcinoma cell lines by means of several biological assays, including knockdown of topo2α expression levels by RNA interference. Results suggest that inhibition of topo2α is a key process in the cytotoxic mechanism for some of the compounds, whereas direct induction of DNA double-strand breaks or other DNA damage is mostly rather minor. In addition, molecular modeling studies performed for two of the compounds (with Ru(II) as the metal center) evinces that these complexes are able to access the DNA-binding pocket of the enzyme, where the hydrophilic environment favors the interaction with highly polar complexes. These findings substantiate the potential of these compounds for application as antitumor metallopharmaceuticals.

Indexed as

Antineoplastic AgentsApoptosisCell ProliferationDNA DamageDNA Topoisomerases, Type IIDrug Screening Assays, AntitumorFemaleHumansMetals, HeavyMolecular Dynamics SimulationMolecular StructureOrganometallic CompoundsPoly-ADP-Ribose Binding ProteinsPyransThionesTopoisomerase II Inhibitors3-hydroxy-2-methyl-4H-pyran-4-thioneAntineoplastic AgentsDNA Topoisomerases, Type IIMetals, HeavyOrganometallic CompoundsPoly-ADP-Ribose Binding ProteinsPyransThionesTOP2A protein, humanTopoisomerase II InhibitorsAnticancer drugMetal complexMolecular dynamicsMonte Carlo simulationRNA interferenceTopoisomerase IIα

Identifiers

PMID32193613
PMCPMC7186247
OpenAlexW3010660161

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.