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dc.contributor.author김대기*
dc.contributor.author권영주*
dc.contributor.author전규연*
dc.date.accessioned2016-08-28T10:08:45Z-
dc.date.available2016-08-28T10:08:45Z-
dc.date.issued2012*
dc.identifier.issn0304-3835*
dc.identifier.otherOAK-9213*
dc.identifier.urihttps://dspace.ewha.ac.kr/handle/2015.oak/223006-
dc.description.abstractHER2 overexpression is observed in ∼6-35% of all gastric cancers, while co-amplification of topoisomerase IIα occurs in ∼32-90% of all cancers with HER2 amplification. The present study reports that HER2 expression is down-regulated by A-62176, a fluoroquinophenoxazine derivative that we previously demonstrated to inhibit topoisomerase I and IIα. The results suggest that A-62176 inhibits the interaction between the ESX, an ets transcription factor, and its co-activator Sur2, leading to the attenuation of HER2-mediated phosphorylation of MAPK/Akt. A-62176 arrests the cell cycle in the G1 phase via the down-regulation of cyclin D1 and the up-regulation of p27Kip1 in NCI-N87 gastric cancer cells. The combination of A-62176 with doxorubicin provides a strong synergistic activity. We propose that A-62176 is a dual inhibitor that impairs the expression of HER2 and restrains the activity of topoisomerase IIα. Our results may lead to the rational design of anticancer molecules targeting a subgroup of gastric cancer cells overexpressing both HER2 and topoisomerase IIα. © 2012 Elsevier Ireland Ltd.*
dc.languageEnglish*
dc.titleA-62176, a potent topoisomerase inhibitor, inhibits the expression of human epidermal growth factor receptor 2*
dc.typeArticle*
dc.relation.issue1*
dc.relation.volume325*
dc.relation.indexSCI*
dc.relation.indexSCIE*
dc.relation.indexSCOPUS*
dc.relation.startpage72*
dc.relation.lastpage79*
dc.relation.journaltitleCancer Letters*
dc.identifier.doi10.1016/j.canlet.2012.06.004*
dc.identifier.wosidWOS:000308781600009*
dc.identifier.scopusid2-s2.0-84865304154*
dc.author.googleKim H.-L.*
dc.author.googleJeon K.-H.*
dc.author.googleJun K.-Y.*
dc.author.googleChoi Y.*
dc.author.googleKim D.-K.*
dc.author.googleNa Y.*
dc.author.googleKwon Y.*
dc.contributor.scopusid김대기(35083694200)*
dc.contributor.scopusid권영주(12446435600)*
dc.contributor.scopusid전규연(25632526500)*
dc.date.modifydate20240422124907*
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약학대학 > 약학과 > Journal papers
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