BIX02189 inhibits TGF-β1-induced lung cancer cell metastasis by directly targeting TGF-β type I receptor
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- 作者：Seong Ji Parka ; Yu Sun Choia ; Seungkoo Leeb ; Young Jae Leec ; Suntaek Hongc ; Sanghwa Hana ; Byung-Chul Kima ; bckim@kangwon.ac.kr" class="auth_mail" title="E-mail the corresponding author
- 关键词：BLI ; bioluminescent imaging ; EGF ; epidermal growth factor ; EMT ; epithelial-to-mesenchymal transition ; ERK ; extracellular-signal-regulated kinase ; Fluc ; firefly luciferase ; MAPK ; mitogen-activated protein kinase ; MEK5 ; mitogen-activated protein kinase/extracellular-signal-regulated kinase5 ; MMP ; matrix metalloproteinase ; PBS ; phosphate buffered saline ; siRNA ; small interfering RNA ; TβRI ; transforming growth factor-β1 receptor type I ; TGF-β1 ; transforming growth factor-β1
- 刊名：Cancer Letters
- 出版年：2016
- 出版时间：28 October 2016
- 年：2016
- 卷：381
- 期：2
- 页码：314-322
- 全文大小：2578 K
文摘
- 10">
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10">BIX02189 inhibits TGF-β1-induced EMT and cell migration in A549 lung cancer cells.
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15">The inhibitory effect of BIX02189 is independent of its action as a MEK5 inhibitor.
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BIX02189 directly binds to TβRI and suppresses its kinase activity.
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BIX02189 blocks the metastatic spread of A549 cells in a xenograft mouse model.
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BIX02189 may have use as a potential therapeutic agent for human lung cancer.