中国药理学通报2016，Vol.32Issue(10)：1357-1363,7.DOI:10.3969/j.issn.1001-1978.2016.10.007
Hsp90抑制剂FS-108抑制癌基因依赖肿瘤细胞增殖及运动的机制研究
FS-108, an Hsp90 inhibitor,impairs survival and motility of oncogene addicted cancer cells
摘要
Abstract
Aim To investigate the anti-tumor effects of FS-108 an Hsp90 inhibitor, on oncogene addicted EBC-1 and A375 cells. Methods SRB assay was performed to investigate cell proliferation. Immunoblot was conducted to investigate the specific proteins. FACS was conducted to test cell cycle distribution and apoptosis. Transwell assay was conducted to investigate cell motility. Results FS-108 significantly suppressed cell proliferation of EBC-1 and A375 cancer cells with IC50 at 25. 53 nmol · L-1 and 30. 02 nmol · L-1 re-spectively. FS-108 treatment triggered the degradation of key client proteins such as c-Met and B-Raf and thereby reduced their downstream AKT and ERK signa-ling pathways. The FACS analysis results demonstrated that FS-108 treatment induced G2/M phase arrest and apoptosis significantly. Furthermore, FS-108 inhibited the migration of EBC-1 and A375 cells. Conclusion As a potent Hsp90 inhibitor, FS-108 can inhibit onco-gene addicted cancer cells proliferation through induc-tion of G2/M phase arrest and apoptosis.关键词
Hsp90/EBC-1和A375细胞/周期阻滞/细胞凋亡/caspase-3/迁移Key words
Hsp90/EBC-1 and A375 cells/G2/M ar-rest/apoptosis/Caspase-3/migration分类
医药卫生引用本文复制引用
平芳芳,王月琴,张敏敏,石峰,陈丹琦,丁健..Hsp90抑制剂FS-108抑制癌基因依赖肿瘤细胞增殖及运动的机制研究[J].中国药理学通报,2016,32(10):1357-1363,7.基金项目
国家自然科学基金资助项目(No 9122920) （No 9122920）
