FS-108, an Hsp90 inhibitor,impairs survival and motility of oncogene addicted cancer cells
10.3969/j.issn.1001-1978.2016.10.007
- VernacularTitle: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
- Author:
Fangfang PING
;
Yueqin WANG
;
Minmin ZHANG
;
Feng SHI
;
Danqi CHEN
;
Jian DING
- Publication Type:Journal Article
- Keywords:
Hsp90;
EBC-1 and A375 cells;
G2/M ar-rest;
apoptosis;
Caspase-3;
migration
- From:
Chinese Pharmacological Bulletin
2016;32(10):1357-1363
- CountryChina
- Language:Chinese
-
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.
