Department of Molecular Pharmacology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA.
Cancer Lett. 2011 Dec 1;311(1):20-8. doi: 10.1016/j.canlet.2011.06.005. Epub 2011 Jun 29.
The present study was performed to investigate the possible role of mTOR inhibitors in restoring chemosensitivity to adriamycin/cisplatin and elucidate the underlying mechanism. Combining adriamycin/cisplatin with torisel synergistically inhibited the cell proliferation in human oropharyngeal carcinoma cell line KB and its multidrug-resistant subclone KB/7D. Combining adriamycin and torisel inhibited the phosphorylation of 4EBP-1 and p70S6K, the proteins involved in mTOR pathway, increased expression of γH2AX indicative of DNA damage, triggered cell cycle arrest at G2/M and apoptosis. We conclude that chromatin decondensation by DNA damage provided an easy access for torisel to block the translation of proteins essential for DNA repair thereby restoring the chemosensitivity.
本研究旨在探讨 mTOR 抑制剂在恢复阿霉素/顺铂化疗敏感性中的可能作用,并阐明其潜在机制。Torisel 联合阿霉素和顺铂协同抑制人咽癌细胞系 KB 及其多药耐药亚系 KB/7D 的细胞增殖。Torisel 联合阿霉素抑制 mTOR 通路相关蛋白 4EBP-1 和 p70S6K 的磷酸化,增加 DNA 损伤标志物 γH2AX 的表达,导致细胞周期阻滞在 G2/M 期和凋亡。我们的结论是,DNA 损伤导致的染色质解凝聚为 torisel 阻断修复 DNA 所必需的蛋白质的翻译提供了便利,从而恢复了化疗敏感性。