Jiang Weiqin, Zhu Zongjian, Thompson Henry J
Cancer Prevention Laboratory, Colorado State University, Fort Collins, Colorado 80523, USA.
Cancer Res. 2008 Jul 1;68(13):5492-9. doi: 10.1158/0008-5472.CAN-07-6721.
Dietary energy restriction (DER) inhibits mammary carcinogenesis, yet mechanisms accounting for its protective activity have not been fully elucidated. In this study, we tested the hypothesis that DER exerts effects on intracellular energy sensing pathways, resulting in alterations of phosphorylated proteins that play a key role in the regulation of cancer. Experiments were conducted using the 1-methyl-1-nitrosourea-induced mammary cancer model in which rats were 0%, 20%, or 40% energy restricted during the postinitiation stage of carcinogenesis. Parallel experiments were done in non-carcinogen-treated rats in which effects of DER at 0%, 5%, 10%, 20%, or 40% in liver were investigated. In a DER dose-dependent manner, levels of Thr(172) phosphorylated AMP-activated protein kinase (AMPK) increased in mammary carcinomas with a concomitant increase in phosphorylated acetyl-CoA-carboxylase, a direct target of AMPK, the phosphorylation of which is regarded as an indicator of AMPK activity. Levels of phosphorylated mammalian target of rapamycin (mTOR) decreased with increasing DER, and down-regulation of mTOR activity was verified by a decrease in the phosphorylation state of two mTOR targets, 70-kDa ribosomal protein S6 kinase (p70S6K) and eukaryote initiation factor 4E binding protein 1 (4E-BP1). Coincident with changes in mTOR phosphorylation, levels of activated protein kinase B (Akt) were also reduced. Similar patterns were observed in mammary glands and livers of non-carcinogen-treated rats. This work identifies components of intracellular energy sensing pathways, specifically mTOR, its principal upstream regulators, AMPK and Akt, and its downstream targets, p70S6K and 4E-BP1, as candidate molecules on which to center mechanistic studies of DER.
饮食能量限制(DER)可抑制乳腺癌发生,但其保护作用的机制尚未完全阐明。在本研究中,我们检验了以下假设:DER对细胞内能量感应通路产生影响,导致在癌症调控中起关键作用的磷酸化蛋白发生改变。实验采用1-甲基-1-亚硝基脲诱导的乳腺癌模型,在致癌作用的起始后阶段,大鼠分别进行0%、20%或40%的能量限制。在未用致癌物处理的大鼠中进行了平行实验,研究了0%、5%、10%、20%或40%的DER对肝脏的影响。在乳腺癌中,磷酸化的苏氨酸(Thr)172 AMP激活蛋白激酶(AMPK)水平以DER剂量依赖的方式增加,同时磷酸化的乙酰辅酶A羧化酶水平也增加,乙酰辅酶A羧化酶是AMPK的直接靶点,其磷酸化被视为AMPK活性的指标。随着DER增加,磷酸化的哺乳动物雷帕霉素靶蛋白(mTOR)水平降低,mTOR活性的下调通过两个mTOR靶点70 kDa核糖体蛋白S6激酶(p70S6K)和真核生物起始因子4E结合蛋白1(4E-BP1)磷酸化状态的降低得到证实。与mTOR磷酸化的变化一致,活化蛋白激酶B(Akt)水平也降低。在未用致癌物处理的大鼠的乳腺和肝脏中也观察到类似模式。这项工作确定了细胞内能量感应通路的组成部分,特别是mTOR、其主要上游调节因子AMPK和Akt,以及其下游靶点p70S6K和4E-BP1,作为DER机制研究的候选分子。