喹唑啉类PAK4小分子抑制剂CWS1抑制肺癌细胞迁移侵袭  

Quinazoline PAK4 small molecule inhibitor CWS1 inhibits lung cancer cell migration and invasion

作　　者：冯晓琳 李晓东[1] 宋培鲁 王健[1] 李丰[1] FENG Xiao-lin;LI Xiao-dong;SONG Pei-lu;WANG Jian;LI Feng(Department of Molecular Cell Biology,College of Life Sciences,China Medical University,Shenyang 110122;Department of Pharmaceutical Chemistry,College of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Benxi 117004,China)

机构地区：[1]中国医科大学生命科学学院细胞生物学教研室,辽宁沈阳110122 [2]沈阳药科大学制药工程学院药物化学教研室,辽宁本溪117004

出　　处：《解剖科学进展》2024年第3期314-316,共3页Progress of Anatomical Sciences

基　　金：国家自然科学基金(31970741)。

摘　　要：目的探讨喹唑啉类PAK4小分子抑制剂CWS1对肺癌细胞迁移的作用。方法划痕实验实验检测不同浓度CWS1对肺癌细胞迁移的作用;Transwell实验检测不同浓度CWS1对肺癌细胞侵袭的作用;Western blot实验检测CWS1对肺癌细胞PAK4激酶的活化作用的影响。结果CWS1对肺癌细胞的迁移有较明显抑制作用,2μmol/L CWS1对肺癌细胞的迁移及侵袭能力有抑制作用;CWS1对PAK4激酶的磷酸化活性有抑制作用,且呈剂量时间效应关系。结论CWS1通过抑制PAK4激酶活性抑制肺癌细胞的迁移及侵袭能力。Objective To investigate the effect of quinazoline PAK4 small molecule inhibitor CWS1 on migration of lung cancer cells.Methods The effects of different concentrations of CWS1 on lung cancer cell migration were detected by scratch test.Transwell assay was used to detect the effects of CWS1 on the invasion of lung cancer cells.The effect of CWS1 on the activation of PAK4 kinase in lung cancer cells was detected by Western blot assay.Results CWS1 significantly inhibited the migration of lung cancer cells,and 2μmol/L CWS1 obviously inhibited the migration and invasion ability of lung cancer cells.CWS1 could inhibit the phosphorylation activity of PAK4 kinase in a dose-time effect relationship.Conclusion CWS1 inhibits the migration and invasion of lung cancer cells by inhibiting PAK4 kinase activity.

关 键 词：PAK4 肺癌 小分子抑制剂 迁移 侵袭 

分 类 号：R734.2[医药卫生—肿瘤]