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Article: Inhibition of human DNA topoisomerase IB by a Cyclometalated Gold III compound: Analysis on the different steps of the enzyme catalytic cycle

TitleInhibition of human DNA topoisomerase IB by a Cyclometalated Gold III compound: Analysis on the different steps of the enzyme catalytic cycle
Authors
Issue Date2011
PublisherAcademic Press. The Journal's web site is located at http://www.elsevier.com/locate/yabbi
Citation
Archives Of Biochemistry And Biophysics, 2011, v. 516 n. 2, p. 108-112 How to Cite?
AbstractA gold(III) compound [Au(CNC)(IMe)]CF 3SO 3 (Gold III) has been reported to have anticancer properties as it is able to reduce topoisomerase IB activity in vitro and suppress tumor growth in nude mice model. Here we have investigated the mechanism of inhibition of human topoisomerase IB activity by this compound, analyzing the various steps of the catalytic cycle. DNA supercoiled relaxation and the cleavage reaction are inhibited, but Gold III does not perturb the religation reaction, in contrast to what has been observed for camptothecin. Pre-incubation of enzyme with the inhibitor before adding DNA substrate increases the inhibitory effect. In addition, when Gold III is preincubated with the enzyme it prevents the stabilization of the cleavable complex by camptothecin. The analysis of the DNA-topoisomerase binding reaction indicates that the compound acts as a topoisomerase I inhibitor by preventing the enzyme-DNA interaction.
Persistent Identifierhttp://hdl.handle.net/10722/168590
ISSN
2015 Impact Factor: 2.807
2015 SCImago Journal Rankings: 1.478
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorCastelli, Sen_US
dc.contributor.authorVassallo, Oen_US
dc.contributor.authorKatkar, Pen_US
dc.contributor.authorChe, CMen_US
dc.contributor.authorSun, RWYen_US
dc.contributor.authorDesideri, Aen_US
dc.date.accessioned2012-10-08T03:21:14Z-
dc.date.available2012-10-08T03:21:14Z-
dc.date.issued2011en_US
dc.identifier.citationArchives Of Biochemistry And Biophysics, 2011, v. 516 n. 2, p. 108-112en_US
dc.identifier.issn0003-9861en_US
dc.identifier.urihttp://hdl.handle.net/10722/168590-
dc.description.abstractA gold(III) compound [Au(CNC)(IMe)]CF 3SO 3 (Gold III) has been reported to have anticancer properties as it is able to reduce topoisomerase IB activity in vitro and suppress tumor growth in nude mice model. Here we have investigated the mechanism of inhibition of human topoisomerase IB activity by this compound, analyzing the various steps of the catalytic cycle. DNA supercoiled relaxation and the cleavage reaction are inhibited, but Gold III does not perturb the religation reaction, in contrast to what has been observed for camptothecin. Pre-incubation of enzyme with the inhibitor before adding DNA substrate increases the inhibitory effect. In addition, when Gold III is preincubated with the enzyme it prevents the stabilization of the cleavable complex by camptothecin. The analysis of the DNA-topoisomerase binding reaction indicates that the compound acts as a topoisomerase I inhibitor by preventing the enzyme-DNA interaction.en_US
dc.languageengen_US
dc.publisherAcademic Press. The Journal's web site is located at http://www.elsevier.com/locate/yabbien_US
dc.relation.ispartofArchives of Biochemistry and Biophysicsen_US
dc.subject.meshAnimalsen_US
dc.subject.meshAntineoplastic Agents - Chemistry - Pharmacologyen_US
dc.subject.meshCatalysisen_US
dc.subject.meshDna - Metabolismen_US
dc.subject.meshDna Topoisomerases, Type I - Drug Effects - Metabolismen_US
dc.subject.meshElectrophoretic Mobility Shift Assayen_US
dc.subject.meshHumansen_US
dc.subject.meshKineticsen_US
dc.subject.meshMiceen_US
dc.subject.meshOrganogold Compounds - Chemistry - Pharmacologyen_US
dc.subject.meshRecombinant Proteins - Antagonists & Inhibitors - Metabolismen_US
dc.subject.meshSubstrate Specificityen_US
dc.subject.meshTopoisomerase I Inhibitors - Chemistry - Pharmacologyen_US
dc.titleInhibition of human DNA topoisomerase IB by a Cyclometalated Gold III compound: Analysis on the different steps of the enzyme catalytic cycleen_US
dc.typeArticleen_US
dc.identifier.emailChe, CM:cmche@hku.hken_US
dc.identifier.emailSun, RWY:rwysun@hku.hken_US
dc.identifier.authorityChe, CM=rp00670en_US
dc.identifier.authoritySun, RWY=rp00781en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1016/j.abb.2011.10.008en_US
dc.identifier.pmid22033340-
dc.identifier.scopuseid_2-s2.0-81755174145en_US
dc.identifier.hkuros205051-
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-81755174145&selection=ref&src=s&origin=recordpageen_US
dc.identifier.volume516en_US
dc.identifier.issue2en_US
dc.identifier.spage108en_US
dc.identifier.epage112en_US
dc.identifier.isiWOS:000297716700004-
dc.publisher.placeUnited Statesen_US
dc.identifier.scopusauthoridCastelli, S=35270975600en_US
dc.identifier.scopusauthoridVassallo, O=18435432000en_US
dc.identifier.scopusauthoridKatkar, P=54585391500en_US
dc.identifier.scopusauthoridChe, CM=7102442791en_US
dc.identifier.scopusauthoridSun, RWY=26325835800en_US
dc.identifier.scopusauthoridDesideri, A=35430278400en_US
dc.identifier.citeulike9933134-

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