Departments of Pharmacology and Toxicology, Geisel School of Medicine at Dartmouth, Hanover, NH, USA.
Mol Cancer Ther. 2013 Aug;12(8):1545-55. doi: 10.1158/1535-7163.MCT-12-0933. Epub 2013 May 16.
Histone deacetylase inhibitor (HDACi; vorinostat) responses were studied in murine and human lung cancer cell lines and genetically engineered mouse lung cancer models. Findings were compared with a window of opportunity trial in aerodigestive tract cancers. In human (HOP62, H522, and H23) and murine transgenic (ED-1, ED-2, LKR-13, and 393P, driven, respectively, by cyclin E, degradation-resistant cyclin E, KRAS, or KRAS/p53) lung cancer cell lines, vorinostat reduced growth, cyclin D1, and cyclin E levels, but induced p27, histone acetylation, and apoptosis. Other biomarkers also changed. Findings from transgenic murine lung cancer models were integrated with those from a window of opportunity trial that measured vorinostat pharmacodynamic responses in pre- versus posttreatment tumor biopsies. Vorinostat repressed cyclin D1 and cyclin E expression in murine transgenic lung cancers and significantly reduced lung cancers in syngeneic mice. Vorinostat also reduced cyclin D1 and cyclin E expression, but increased p27 levels in post- versus pretreatment human lung cancer biopsies. Notably, necrotic and inflammatory responses appeared in posttreatment biopsies. These depended on intratumoral HDACi levels. Therefore, HDACi treatments of murine genetically engineered lung cancer models exert similar responses (growth inhibition and changes in gene expression) as observed in lung cancer cell lines. Moreover, enhanced pharmacodynamic responses occurred in the window of opportunity trial, providing additional markers of response that can be evaluated in subsequent HDACi trials. Thus, combining murine and human HDACi trials is a strategy to translate preclinical HDACi treatment outcomes into the clinic. This study uncovered clinically tractable mechanisms to engage in future HDACi trials.
组蛋白去乙酰化酶抑制剂(HDACi;伏立诺他)在鼠类和人类肺癌细胞系以及基因工程小鼠肺癌模型中的反应进行了研究。研究结果与一项呼吸道癌症的治疗窗试验进行了比较。在人类(HOP62、H522 和 H23)和鼠类转基因(ED-1、ED-2、LKR-13 和 393P,分别由细胞周期蛋白 E、抗降解的细胞周期蛋白 E、KRAS 或 KRAS/p53 驱动)肺癌细胞系中,伏立诺他降低了细胞生长、细胞周期蛋白 D1 和 E 水平,但诱导了 p27、组蛋白乙酰化和细胞凋亡。其他生物标志物也发生了变化。转基因鼠类肺癌模型的研究结果与一项治疗窗试验的结果相结合,该试验测量了伏立诺他在治疗前和治疗后肿瘤活检中的药效反应。伏立诺他抑制了鼠类转基因肺癌中的细胞周期蛋白 D1 和 E 表达,并显著减少了同基因小鼠中的肺癌。伏立诺他还降低了人类肺癌活检中的细胞周期蛋白 D1 和 E 表达,但增加了 p27 水平。值得注意的是,在治疗后的活检中出现了坏死和炎症反应。这些反应依赖于肿瘤内的 HDACi 水平。因此,HDACi 治疗鼠类基因工程肺癌模型产生的反应(生长抑制和基因表达变化)与在肺癌细胞系中观察到的反应相似。此外,在治疗窗试验中观察到增强的药效反应,提供了可在随后的 HDACi 试验中评估的额外反应标志物。因此,结合鼠类和人类的 HDACi 试验是将临床前 HDACi 治疗结果转化为临床的一种策略。本研究揭示了可行的临床机制,以参与未来的 HDACi 试验。