targetinghsp90withfs108circumventsgefitinlbresistanceinegfrmutantnonsmallcelllungcancercells
文献类型：期刊论文
| 作者 | Wang Yueqin2; Shen Aijun3; Sun Jingya3; Wang Xin3; Liu Hongchun3; Zhang Minmin3; Chen Danqi4 ; Xiong Bing4; Shen Jingkang4; Geng Meiyu3
|
| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2016 |
| 卷号 | 37期号:12页码:1587 |
| 关键词 | non-small cell lung cancer gefitinlb resistance Hsp90 |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2016.85 |
| 英文摘要 | Aim: Inhibition of heat shock protein (Hsp90) has been proven to be effective in overriding primary and acquired resistance of kinase inhibitors. In this study, we investigated the role of FS-108, a newly developed Hsp90 Inhibitor, to overcome gefitinib resistance in EGFR mutant non-small cell lung cancer cells. Methods: Cell proliferation was assessed using the SRB assay. Cell cycle distribution and apoptosis were analyzed by flow cytometry. Protein expression was examined by Western blotting. The In vivo effectiveness of FS-108 was determined in an NCI-H1975 subcutaneous xenograft model. Results: FS-108 triggered obvious growth inhibition in gefitinib-resistant HCC827/GR6, NCI-H1650 and NCI-H1975 cells through inducing G_2/M phase arrest and apoptosis. FS-108 treatment resulted In a remarkable degradation of key client proteins involved in gefitinlb resistance and further abrogated their downstream signaling pathways. Interestingly, FS-108 alone exerted an identical or superior effect on circumventing gefitinlb resistance compared to combined kinase inhibition. Finally, the ability of FS-108 to overcome gefitinlb resistance In vivo was validated In an NCI-H1975 xenograft model. Conclusion: FS-108 is a powerful agent that impacts the survival of gefitinib-resistant cells In vitro and in vivo through targeting Hsp90. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/287540]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.Department of Thoracic Surgery, Shanghai Tongren Hospital, Shanghai Jlao Tong University School of Medicine 2.中国药科大学 3.中国科学院 4.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Wang Yueqin,Shen Aijun,Sun Jingya,et al. targetinghsp90withfs108circumventsgefitinlbresistanceinegfrmutantnonsmallcelllungcancercells[J]. actapharmacologicasinica,2016,37(12):1587. |
| APA | Wang Yueqin.,Shen Aijun.,Sun Jingya.,Wang Xin.,Liu Hongchun.,...&Ding Jian.(2016).targetinghsp90withfs108circumventsgefitinlbresistanceinegfrmutantnonsmallcelllungcancercells.actapharmacologicasinica,37(12),1587. |
| MLA | Wang Yueqin,et al."targetinghsp90withfs108circumventsgefitinlbresistanceinegfrmutantnonsmallcelllungcancercells".actapharmacologicasinica 37.12(2016):1587. |
入库方式： OAI收割
来源：上海药物研究所
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