ErbB2过表达激活Akt/雷帕霉素哺乳动物靶蛋白/4E-BP1信号通路预示着乳腺癌的肿瘤进展。
Activation of the Akt/mammalian target of rapamycin/4E-BP1 pathway by ErbB2 overexpression predicts tumor progression in breast cancers.
作者信息
Zhou Xiaoyan, Tan Ming, Stone Hawthorne Valerie, Klos Kristine S, Lan Keng-Hsueh, Yang Ying, Yang Wentao, Smith Terry L, Shi Daren, Yu Dihua
机构信息
Department of Surgical Oncology, The University of Texas M. D. Anderson Cancer Center, Houston, Texas 77030, USA.
出版信息
Clin Cancer Res. 2004 Oct 15;10(20):6779-88. doi: 10.1158/1078-0432.CCR-04-0112.
The Akt/mammalian target of rapamycin (mTOR)/4E-BP1 pathway is considered to be a central regulator of protein synthesis, involving the regulation of cell proliferation, differentiation, and survival. The inhibitors of mTOR as anticancer reagents are undergoing active evaluation in various malignancies including breast cancer. However, the activation status of the Akt/mTOR/4E-BP1 pathway and its potential roles in breast cancers remain unknown. Thus, we examined 165 invasive breast cancers with specific antibodies for the phosphorylation of Akt, mTOR, and 4E-BP1 by immunohistochemistry and compared them with normal breast epithelium, fibroadenoma, intraductal hyperplasia, and ductal carcinoma in situ. We discovered that the phosphorylation of Akt, mTOR, and 4E-BP1 increased progressively from normal breast epithelium to hyperplasia and abnormal hyperplasia to tumor invasion. Phosphorylated Akt, mTOR, and 4E-BP1 were positively associated with ErbB2 overexpression. Survival analysis showed that phosphorylation of each of these three markers was associated with poor disease-free survival independently. In vitro, we further confirmed the causal relationship between ErbB2 overexpression and mTOR activation, which was associated with enhanced invasive ability and sensitivity to a mTOR inhibitor, rapamycin. Our results, for the first time, demonstrate the following: (a) high levels of phosphorylation of Akt, mTOR, and 4E-BP1 in breast cancers, indicating activation of the Akt/mTOR/4E-BP1 pathway in breast cancer development and progression; (b) a link between ErbB2 and the Akt/mTOR/4E-BP1 pathway in breast cancers in vitro and in vivo, indicating the possible role of Akt/mTOR activation in ErbB2-mediated breast cancer progression; and (c) a potential role for this pathway in predicting the prognosis of patients with breast cancer, especially those treated with mTOR inhibitors.
Akt/雷帕霉素哺乳动物靶蛋白(mTOR)/4E-结合蛋白1(4E-BP1)信号通路被认为是蛋白质合成的核心调节因子,参与细胞增殖、分化和存活的调控。mTOR抑制剂作为抗癌试剂正在包括乳腺癌在内的各种恶性肿瘤中进行积极评估。然而,Akt/mTOR/4E-BP1信号通路的激活状态及其在乳腺癌中的潜在作用仍不清楚。因此,我们通过免疫组织化学法,使用针对Akt、mTOR和4E-BP1磷酸化的特异性抗体,检测了165例浸润性乳腺癌,并将其与正常乳腺上皮、纤维腺瘤、导管内增生和导管原位癌进行比较。我们发现,从正常乳腺上皮到增生、异常增生再到肿瘤浸润,Akt、mTOR和4E-BP1的磷酸化逐渐增加。磷酸化的Akt、mTOR和4E-BP1与ErbB2过表达呈正相关。生存分析表明,这三种标志物各自的磷酸化均与无病生存期差独立相关。在体外,我们进一步证实了ErbB2过表达与mTOR激活之间的因果关系,这与侵袭能力增强和对mTOR抑制剂雷帕霉素的敏感性相关。我们的结果首次证明了以下几点:(a)乳腺癌中Akt、mTOR和4E-BP1的高水平磷酸化,表明Akt/mTOR/4E-BP1信号通路在乳腺癌发生发展中被激活;(b)体外和体内乳腺癌中ErbB2与Akt/mTOR/4E-BP1信号通路之间的联系,表明Akt/mTOR激活在ErbB2介导的乳腺癌进展中可能发挥的作用;(c)该信号通路在预测乳腺癌患者,尤其是接受mTOR抑制剂治疗患者的预后方面的潜在作用。