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IC261 inhibits the epithelial-mesenchymal transition induced by TGF-β in A549 lung cancer cells
Applied Biological Chemistry ( IF 3.2 ) Pub Date : 2022-03-27 , DOI: 10.1186/s13765-022-00690-1
Kim, Sung Jim, Shin, Myoung-Sook

Despite rapid advances in cancer diagnosis and therapy, lung cancer continues to be the primary cause of cancer-related mortality. Epithelial mesenchymal transition has been implicated in drug resistance and cancer metastasis. IC261 mediates various pathophysiological processes, including inflammation and tumorigenesis. Therefore, we analyzed the involvement of IC261 in epithelial mesenchymal transition. Pretreatment with IC261 significantly inhibited the expression of transforming growth factor (TGF)-β1-induced mesenchymal cell markers, including N-cadherin (N-cad), vimentin (Vim), and β-catenin (β-cat), at the mRNA and protein levels in A549 lung cancer cells, which was confirmed using immunofluorescence staining. A migration assay revealed that IC261 treatment strongly inhibited TGF-β1-induced migration activity at 24 and 48 h. Additionally, IC261 treatment suppressed the activation of the TGF-β1 signaling pathway in A549 cells and phosphorylation of Smad2 and Smad3. Our findings demonstrate that IC261, a selective inhibitor of casein kinase 1, inhibits the TGF-β1-induced migration of A549 cells by inhibiting Smad2/3 phosphorylation and downregulating the expression of N-cad, Vim, and β-cat.

中文翻译:

IC261抑制TGF-β诱导的A549肺癌细胞上皮间质转化

尽管癌症诊断和治疗取得了快速进展,但肺癌仍然是癌症相关死亡的主要原因。上皮间质转化与耐药性和癌症转移有关。IC261 介导各种病理生理过程,包括炎症和肿瘤发生。因此,我们分析了 IC261 在上皮间质转化中的作用。用 IC261 预处理显着抑制 mRNA 上转化生长因子 (TGF)-β1 诱导的间充质细胞标志物的表达,包括 N-钙粘蛋白 (N-cad)、波形蛋白 (Vim) 和 β-连环蛋白 (β-cat)和 A549 肺癌细胞中的蛋白质水平,使用免疫荧光染色证实。迁移测定显示,IC261 处理在 24 和 48 小时强烈抑制 TGF-β1 诱导的迁移活性。此外,IC261 处理抑制了 A549 细胞中 TGF-β1 信号通路的激活和 Smad2 和 Smad3 的磷酸化。我们的研究结果表明,酪蛋白激酶 1 的选择性抑制剂 IC261 通过抑制 Smad2/3 磷酸化和下调 N-cad、Vim 和 β-cat 的表达来抑制 TGF-β1 诱导的 A549 细胞迁移。
更新日期:2022-03-27
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