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雷帕霉素哺乳动物靶点(mTOR)在丝氨酸2448处的磷酸化由p70S6激酶介导。

Phosphorylation of mammalian target of rapamycin (mTOR) at Ser-2448 is mediated by p70S6 kinase.

作者信息

Chiang Gary G, Abraham Robert T

机构信息

Program in Signal Transduction Research, The Burnham Institute, La Jolla, California 92037, USA.

出版信息

J Biol Chem. 2005 Jul 8;280(27):25485-90. doi: 10.1074/jbc.M501707200. Epub 2005 May 16.

Abstract

The mammalian target of rapamycin (mTOR) coordinates cell growth with the growth factor and nutrient/energy status of the cell. The phosphatidylinositol 3-kinase-AKT pathway is centrally involved in the transmission of mitogenic signals to mTOR. Previous studies have shown that mTOR is a direct substrate for the AKT kinase and identified Ser-2448 as the AKT target site in mTOR. In this study, we demonstrate that rapamycin, a specific inhibitor of mTOR function, blocks serum-stimulated Ser-2448 phosphorylation and that this drug effect is not explained by the inhibition of AKT. Furthermore, the phosphorylation of Ser-2448 was dependent on mTOR kinase activity, suggesting that mTOR itself or a protein kinase downstream from mTOR was responsible for the modification of Ser-2448. Here we show that p70S6 kinase phosphorylates mTOR at Ser-2448 in vitro and that ectopic expression of rapamycin-resistant p70S6 kinase restores Ser-2448 phosphorylation in rapamycin-treated cells. In addition, we show that cellular amino acid status, which modulates p70S6 kinase (S6K1) activity via the TSC/Rheb pathway, regulates Ser-2448 phosphorylation. Finally, small interfering RNA-mediated depletion of p70S6 kinase reduces Ser-2448 phosphorylation in cells. Taken together, these results suggest that p70S6 kinase is a major effector of mTOR phosphorylation at Ser-2448 in response to both mitogen- and nutrient-derived stimuli.

摘要

雷帕霉素的哺乳动物靶点(mTOR)将细胞生长与细胞的生长因子以及营养/能量状态相协调。磷脂酰肌醇3激酶-AKT信号通路在有丝分裂信号向mTOR的传递中起核心作用。先前的研究表明,mTOR是AKT激酶的直接底物,并确定Ser-2448是mTOR中的AKT作用靶点。在本研究中,我们证明雷帕霉素(一种mTOR功能的特异性抑制剂)可阻断血清刺激的Ser-2448磷酸化,且这种药物效应不能用对AKT的抑制来解释。此外,Ser-2448的磷酸化依赖于mTOR激酶活性,这表明mTOR自身或mTOR下游的一种蛋白激酶负责Ser-2448的修饰。在此我们表明,p70S6激酶在体外可使mTOR的Ser-2448位点磷酸化,并且雷帕霉素抗性p70S6激酶的异位表达可恢复雷帕霉素处理细胞中的Ser-2448磷酸化。另外,我们表明通过TSC/Rheb途径调节p70S6激酶(S6K1)活性的细胞氨基酸状态可调节Ser-2448磷酸化。最后,小干扰RNA介导的p70S6激酶缺失可降低细胞中的Ser-2448磷酸化。综上所述,这些结果表明p70S6激酶是mTOR在Ser-2448位点磷酸化的主要效应因子,可响应有丝分裂原和营养物质衍生的刺激。

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