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Selection of cancer chemopreventive agents based on inhibition of topoisomerase II activity

dc.contributor.authorCho, K. H.en
dc.contributor.authorPezzuto, J. M.en
dc.contributor.authorBolton, J. L.en
dc.contributor.authorSteele, V. E.en
dc.contributor.authorKelloff, G. J.en
dc.contributor.authorLee, S. K.en
dc.contributor.authorConstantinou, Andreas I.en
dc.creatorCho, K. H.en
dc.creatorPezzuto, J. M.en
dc.creatorBolton, J. L.en
dc.creatorSteele, V. E.en
dc.creatorKelloff, G. J.en
dc.creatorLee, S. K.en
dc.creatorConstantinou, Andreas I.en
dc.date.accessioned2019-11-04T12:50:20Z
dc.date.available2019-11-04T12:50:20Z
dc.date.issued2000
dc.identifier.urihttp://gnosis.library.ucy.ac.cy/handle/7/52977
dc.description.abstractThe present study was undertaken to determine if in vitro inhibition of one or both of the two most dominant mammalian DNA topoisomerases (topos) is common among chemopreventive agents. To determine if an agent was a topo I inhibitor, we employed the DNA relaxation and nicking assays. For potential topo II inhibitors, we used the DNA unknotting and linearisation assays. 14 of 30 agents (47%) were ineffective in all four assays (IC50 >100 μg/ml), and 11 (37%) inhibited topo II catalytic activity. The sensitivity of the topo II assay was 63%, selectivity 93%, positive predictive value 91%, and total accuracy 77%. For chemopreventive efficacy, the positive predictive value of the unknotting assay was 92%, and the total accuracy was 60%. These data suggest that reduced topo II activity is a desirable property of many known chemopreventive agents. We conclude that the unknotting assay could be a valuable addition to the in vitro tests presently used to select chemopreventive agents. Copyright (C) 2000 Elsevier Science Ltd.en
dc.sourceEuropean journal of canceren
dc.source.urihttps://www.scopus.com/inward/record.uri?eid=2-s2.0-0033810964&doi=10.1016%2fS0959-8049%2800%2900300-2&partnerID=40&md5=e9fd0e2e76dfd25bbf5d89e49b498baa
dc.subjectarticleen
dc.subjectantineoplastic agenten
dc.subjecthumanen
dc.subjectNeoplasmsen
dc.subjectcontrolled studyen
dc.subjectfemaleen
dc.subjectpredictionen
dc.subjectpriority journalen
dc.subjectmaleen
dc.subjectunclassified drugen
dc.subjectAnticarcinogenic Agentsen
dc.subjectChemopreventionen
dc.subjectnonhumanen
dc.subjectDNA topoisomerase inhibitoren
dc.subjectdrug selectivityen
dc.subjectdrug screeningen
dc.subjectMiceen
dc.subjectAnimalen
dc.subjectanimal modelen
dc.subjectmouseen
dc.subjectDNAen
dc.subjectDNA topoisomerase (ATP hydrolysing)en
dc.subjectTopoisomerase Ien
dc.subjectchemoprophylaxisen
dc.subjectSensitivity and Specificityen
dc.subjectPredictive valueen
dc.subjectaccuracyen
dc.subjectenzyme inhibitionen
dc.subjectcatalysisen
dc.subjectSupport, Non-U.S. Gov'ten
dc.subjectDNA Topoisomerases, Type IIen
dc.subjectSupport, U.S. Gov't, P.H.S.en
dc.subjectgenisteinen
dc.subjectcaffeic acid derivativeen
dc.subjectgallic aciden
dc.subjectraten
dc.subjectRatsen
dc.subject1,2 dithiole 3 thione derivativeen
dc.subject1,4 phenylene bis(methylene)selenocyanateen
dc.subject3 indolemethanolen
dc.subject4 aminobutyric aciden
dc.subject4 hydroxy 2 ethyl 5 methyl 3(2h) furanoneen
dc.subjectanethole trithioneen
dc.subjectascorbigenen
dc.subjectassayen
dc.subjectastaxanthinen
dc.subjectcaffeic acid phenethyl esteren
dc.subjectCarcinogenesisen
dc.subjectchalconeen
dc.subjectchemical carcinogenesisen
dc.subjectdiflunisalen
dc.subjectDNA topoisomeraseen
dc.subjectDNA Topoisomerases, Type Ien
dc.subjectDrug Screening Assays, Antitumoren
dc.subjectdrug specificityen
dc.subjectellagic aciden
dc.subjectgalaninen
dc.subjectHamstersen
dc.subjecthederageninen
dc.subjectmadecassosideen
dc.subjectmaltolen
dc.subjectnifedipineen
dc.subjectoleanolic aciden
dc.subjectOrganoseleniumen
dc.subjectpiroxicamen
dc.subjectprotamine sulfateen
dc.subjectprotocatechuic aciden
dc.subjectquercetinen
dc.subjectRelaxation assayen
dc.subjectresveratrolen
dc.subjects allylcysteineen
dc.subjectSelectivityen
dc.subjectSpecificityen
dc.subjectsphingomyelinen
dc.subjectsulphoraphaneen
dc.subjectthiaprolineen
dc.subjectTopoisomerase IIen
dc.subjectUnknotting assayen
dc.subjectursolic aciden
dc.titleSelection of cancer chemopreventive agents based on inhibition of topoisomerase II activityen
dc.typeinfo:eu-repo/semantics/article
dc.identifier.doi10.1016/S0959-8049(00)00300-2
dc.description.volume36
dc.description.startingpage2146
dc.description.endingpage2156
dc.author.facultyΣχολή Θετικών και Εφαρμοσμένων Επιστημών / Faculty of Pure and Applied Sciences
dc.author.departmentΤμήμα Βιολογικών Επιστημών / Department of Biological Sciences
dc.type.uhtypeArticleen
dc.description.notes<p>Manufacturers: Sigma, United Statesen
dc.description.notesCited By :39</p>en
dc.source.abbreviationEur.J.Canceren
dc.contributor.orcidConstantinou, Andreas I. [0000-0003-0365-1821]
dc.gnosis.orcid0000-0003-0365-1821


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