Evidence map›Paper›PMID 28724198›Full record

ArticleChemMedChem2017

Direct and Topoisomerase II Mediated DNA Damage by Bis-3-chloropiperidines: The Importance of Being an Earnest G.

Alice Sosic, Ivonne Zuravka, Nina-Katharina Schmitt, Angelica Miola, Richard Göttlich, Dan Fabris, Barbara Gatto

Abstract read
In one paragraph

Article in ChemMedChem, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
0.6field-weighted citation impact, top 34% 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

8 citing papers in PubMed, 15 citations in OpenAlex.

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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

7 authors at 3 institutions in 3 countries.

Alice SosicDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Francesco Marzolo 5, 35131, Padova, Italy.ORCID 0000-0002-1070-1869
Ivonne ZuravkaDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Francesco Marzolo 5, 35131, Padova, Italy.
Nina-Katharina SchmittDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Francesco Marzolo 5, 35131, Padova, Italy.
Angelica MiolaDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Francesco Marzolo 5, 35131, Padova, Italy.
Richard GöttlichInstitute of Organic Chemistry, Justus Liebig University Giessen, Heinrich-Buff-Ring 17, 35392, Giessen, Germany.
Dan FabrisDepartments of Chemistry and Biological Sciences, University at Albany - SUNY, 1400 Washington Avenue, Albany, NY, 12222, USA.
Barbara GattoDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Francesco Marzolo 5, 35131, Padova, Italy.ORCID 0000-0001-9465-6913
University of Padua · ITJustus-Liebig-Universität Gießen · DEUniversity at Albany, State University of New York · US

Funding

Structural determinants of HIV-1 5'-UTR riboswitch and NC actuation by MS3DR01GM064328 · NIGMS · UNIVERSITY OF MARYLAND BALTIMORE COUNTY · PI FABRIS, DANIELE · 2001 to 2013
$3.8M
NIGMS NIH HHS R01 GM064328
6 · The paper itself

Abstract

Bis-3-chloropiperidines are a new class of DNA-active compounds capable of alkylating nucleobases and inducing strand cleavage. In this study, we investigated the reactivity of these mustard-based agents with both single- and double-stranded DNA constructs. Polyacrylamide gel electrophoresis (PAGE) and electrospray ionization mass spectrometry (ESI-MS) were used to obtain valuable insight into their mechanism at the molecular level and to investigate their time- and concentration-dependent activity. The results revealed the preferential formation of mono- and bifunctional adducts at nucleophilic guanine sites. In a stepwise fashion, alkylation was followed by depurination and subsequent strand scission at the ensuing apurinic site. We demonstrated that the covalent modifications introduced by this new class of compounds can inhibit the activity of essential DNA-processing proteins, such as topoisomerase IIα, thereby suggesting that bis-3-chloropiperidines may have excellent anticancer potential.

Indexed as

Antigens, NeoplasmDNADNA AdductsDNA-Binding ProteinsDNA DamageDNA Topoisomerases, Type IIHumansPiperidinesTopoisomerase II InhibitorsAntigens, Neoplasmbis-3-chloropiperidineDNADNA AdductsDNA-Binding ProteinsDNA Topoisomerases, Type IIPiperidinesTopoisomerase II Inhibitorsanticancer agentsbis-3-chloropiperidinesDNA alkylationDNA depurinationtopoisomerase IIα inhibition

Identifiers

PMID28724198
PMCPMC7054790
OpenAlexW2738126261

What OpenQuestion holds

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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.