Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 신윤용 | * |
dc.contributor.author | 김대기 | * |
dc.date.accessioned | 2016-08-28T12:08:36Z | - |
dc.date.available | 2016-08-28T12:08:36Z | - |
dc.date.issued | 2011 | * |
dc.identifier.issn | 0959-8049 | * |
dc.identifier.other | OAK-8234 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/222160 | - |
dc.description.abstract | Recently, 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.language | English | * |
dc.title | EW-7195, a novel inhibitor of ALK5 kinase inhibits EMT and breast cancer metastasis to lung | * |
dc.type | Article | * |
dc.relation.issue | 17 | * |
dc.relation.volume | 47 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 2642 | * |
dc.relation.lastpage | 2653 | * |
dc.relation.journaltitle | European Journal of Cancer | * |
dc.identifier.doi | 10.1016/j.ejca.2011.07.007 | * |
dc.identifier.wosid | WOS:000297874900018 | * |
dc.identifier.scopusid | 2-s2.0-80755163620 | * |
dc.author.google | Park C.-Y. | * |
dc.author.google | Son J.-Y. | * |
dc.author.google | Jin C.H. | * |
dc.author.google | Nam J.-S. | * |
dc.author.google | Kim D.-K. | * |
dc.author.google | Sheen Y.Y. | * |
dc.contributor.scopusid | 신윤용(6603872711) | * |
dc.contributor.scopusid | 김대기(35083694200) | * |
dc.date.modifydate | 20240118164500 | * |