Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 신윤용 | * |
dc.contributor.author | 김대기 | * |
dc.date.accessioned | 2016-08-28T12:08:26Z | - |
dc.date.available | 2016-08-28T12:08:26Z | - |
dc.date.issued | 2011 | * |
dc.identifier.issn | 1347-9032 | * |
dc.identifier.other | OAK-8822 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/222680 | - |
dc.description.abstract | Recently, small molecule inhibitors of transforming growth factorβ (TGF-β) type I receptor kinase/activin receptor-like kinase-5 (ALK5) have been developed to target TGF-β signalling as a therapeutic strategy for combating cancer. In the present study, the authors examined a novel small molecule inhibitor of ALK5, 3-((5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(6-methylpyridin-2-yl)thiazol-2-ylamino)methyl)benzonitrile (EW-7203) in breast cancer cells to determine if it has potential for cancer treatment. The inhibitory effects of EW-7203 on TGF-β-induced Smad signalling 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-7203 on mammary cancer metastasis to the lung were examined using a Balb/c xenograft model system. The novel ALK5 inhibitor, EW-7203, inhibited the TGF-β1-stimulated transcriptional activation of p3TP-Lux and pCAGA 12-Luc. In addition, EW-7203 decreased phosphorylated Smad2 levels and the nuclear translocation of Smad2 was increased by TGF-β1. In addition, EW-7203 inhibited TGF-β1-induced EMT and wound healing of NMuMG cells. Furthermore, in xenografted Balb/c mice, EW-7203 inhibited metastasis to the lung from breast tumors. The novel ALK5 inhibitor, EW-7203, efficiently inhibited TGF-β1-induced Smad signalling, EMT and breast tumor metastasis to the lung in vivo, demonstrating that EW-7203 has therapeutic potential for breast cancer metastasis to the lung. © 2011 Japanese Cancer Association. | * |
dc.language | English | * |
dc.title | EW-7203, a novel small molecule inhibitor of transforming growth factor-β (TGF-β) type I receptor/activin receptor-like kinase-5, blocks TGF-β1-mediated epithelial-to-mesenchymal transition in mammary epithelial cells | * |
dc.type | Article | * |
dc.relation.issue | 10 | * |
dc.relation.volume | 102 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 1889 | * |
dc.relation.lastpage | 1896 | * |
dc.relation.journaltitle | Cancer Science | * |
dc.identifier.doi | 10.1111/j.1349-7006.2011.02014.x | * |
dc.identifier.wosid | WOS:000304372700002 | * |
dc.identifier.scopusid | 2-s2.0-84863011208 | * |
dc.author.google | Park C.-Y. | * |
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 | * |