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EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis.

Authors
 Ji Yeon Son  ;  So Yeon Park  ;  Sol Ji Kim  ;  Seon Joo Lee  ;  Sang A. Park  ;  Min Jin Kim  ;  Seung Won Kim  ;  Dae Kee Kim  ;  Jeong Seok Nam  ;  Yhun Yhong Sheen 
Citation
 Molecular Cancer Therapeutics, Vol.13(7) : 1704-1716, 2014 
Journal Title
 Molecular Cancer Therapeutics 
ISSN
 1535-7163 
Issue Date
2014
Abstract
Advanced tumors produce an excessive amount of transforming growth factor β (TGFβ), which promotes tumor progression at late stages of malignancy. The purpose of this study was to develop anti-TGFβ therapeutics for cancer. We synthesized a novel small-molecule TGFβ receptor I kinase (activin receptor-like kinase 5) inhibitor termed N-[[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl]methyl]-2-fluoroaniline (EW-7197), and we investigated its potential antimetastatic efficacy in mouse mammary tumor virus (MMTV)/c-Neu mice and 4T1 orthotopic-grafted mice. EW-7197 inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice and 4T1 orthotopic-grafted mice. EW-7197 also inhibited the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Furthermore, EW-7197 enhanced cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. In summary, EW-7197 showed potent in vivo antimetastatic activity, indicating its potential for use as an anticancer therapy.
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T201405551.pdf Download
DOI
10.1158/1535-7163.MCT-13-0903
Appears in Collections:
1. Journal Papers (연구논문) > 1. College of Medicine (의과대학) > BioMedical Science Institute (의생명과학부)
Yonsei Authors
김승원(Kim, Seung Won)
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URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/138745
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