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dc.contributor.author신윤용-
dc.contributor.author김대기-
dc.date.accessioned2016-08-28T12:08:36Z-
dc.date.available2016-08-28T12:08:36Z-
dc.date.issued2011-
dc.identifier.issn0959-8049-
dc.identifier.otherOAK-8234-
dc.identifier.urihttps://dspace.ewha.ac.kr/handle/2015.oak/222160-
dc.description.abstractRecently, researchers are actively pursuing efforts to develop potent and selective ALK5 (TβRI) kinase inhibitors for clinical development. In this study, the authors examined a novel small molecule inhibitor of ALK5, 3-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl) -1H-imidazol-2-yl)methylamino)benzonitrile (EW-7195) to determine if it has potential for cancer treatment. The inhibitory effects of EW-7195 on TGF-β-induced Smad signaling and epithelial-to-mesenchymal transition (EMT) were investigated in mammary epithelial cells using luciferase reporter assays, immunoblotting, confocal microscopy and wound healing assays. In addition, the suppressive effects of EW-7195 on mammary cancer metastasis to lung were examined using a Balb/c xenograft and MMTV/cNeu transgenic mice model system. The novel ALK5 inhibitor, EW-7195, inhibited the TGF-β 1- stimulated transcriptional activations of p3TP-Lux and pCAGA 12-Luc. In addition, EW-7195 decreased phosphorylated Smad2 levels and the nuclear translocation of Smad2 increased by TGF-β 1. In addition, EW-7195 inhibited TGF-β 1-induced EMT and wound healing of NMuMG cells. Furthermore, in xenografted Balb/c and MMTV/cNeu mice, EW-7195 inhibited metastasis to lung from breast tumours. The novel ALK5 inhibitor, EW-7195, efficiently inhibited TGF-β 1-induced Smad signaling, EMT and breast tumour metastasis to the lung in vivo, demonstrating that EW-7195 has therapeutic potential for the breast cancer metastasis to the lung. © 2011 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.titleEW-7195, a novel inhibitor of ALK5 kinase inhibits EMT and breast cancer metastasis to lung-
dc.typeArticle-
dc.relation.issue17-
dc.relation.volume47-
dc.relation.indexSCI-
dc.relation.indexSCIE-
dc.relation.indexSCOPUS-
dc.relation.startpage2642-
dc.relation.lastpage2653-
dc.relation.journaltitleEuropean Journal of Cancer-
dc.identifier.doi10.1016/j.ejca.2011.07.007-
dc.identifier.wosidWOS:000297874900018-
dc.identifier.scopusid2-s2.0-80755163620-
dc.author.googlePark C.-Y.-
dc.author.googleSon J.-Y.-
dc.author.googleJin C.H.-
dc.author.googleNam J.-S.-
dc.author.googleKim D.-K.-
dc.author.googleSheen Y.Y.-
dc.contributor.scopusid신윤용(6603872711)-
dc.contributor.scopusid김대기(35083694200)-
dc.date.modifydate20210301081004-
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약학대학 > 약학과 > Journal papers
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