Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 김대기 | * |
dc.contributor.author | 권영주 | * |
dc.contributor.author | 전규연 | * |
dc.date.accessioned | 2016-08-28T10:08:45Z | - |
dc.date.available | 2016-08-28T10:08:45Z | - |
dc.date.issued | 2012 | * |
dc.identifier.issn | 0304-3835 | * |
dc.identifier.other | OAK-9213 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/223006 | - |
dc.description.abstract | HER2 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.language | English | * |
dc.title | A-62176, a potent topoisomerase inhibitor, inhibits the expression of human epidermal growth factor receptor 2 | * |
dc.type | Article | * |
dc.relation.issue | 1 | * |
dc.relation.volume | 325 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 72 | * |
dc.relation.lastpage | 79 | * |
dc.relation.journaltitle | Cancer Letters | * |
dc.identifier.doi | 10.1016/j.canlet.2012.06.004 | * |
dc.identifier.wosid | WOS:000308781600009 | * |
dc.identifier.scopusid | 2-s2.0-84865304154 | * |
dc.author.google | Kim H.-L. | * |
dc.author.google | Jeon K.-H. | * |
dc.author.google | Jun K.-Y. | * |
dc.author.google | Choi Y. | * |
dc.author.google | Kim D.-K. | * |
dc.author.google | Na Y. | * |
dc.author.google | Kwon Y. | * |
dc.contributor.scopusid | 김대기(35083694200) | * |
dc.contributor.scopusid | 권영주(12446435600) | * |
dc.contributor.scopusid | 전규연(25632526500) | * |
dc.date.modifydate | 20240422124907 | * |