Nogueira Veronique, Park Youngkyu, Chen Chia-Chen, Xu Pei-Zhang, Chen Mei-Ling, Tonic Ivana, Unterman Terry, Hay Nissim
Department of Biochemistry and Molecular Genetics, University of Illinois at Chicago, Chicago, IL 60607, USA.
Cancer Cell. 2008 Dec 9;14(6):458-70. doi: 10.1016/j.ccr.2008.11.003.
Akt deficiency causes resistance to replicative senescence, to oxidative stress- and oncogenic Ras-induced premature senescence, and to reactive oxygen species (ROS)-mediated apoptosis. Akt activation induces premature senescence and sensitizes cells to ROS-mediated apoptosis by increasing intracellular ROS through increased oxygen consumption and by inhibiting the expression of ROS scavengers downstream of FoxO, particularly sestrin 3. This uncovers an Achilles' heel of Akt, since in contrast to its ability to inhibit apoptosis induced by multiple apoptotic stimuli, Akt could not inhibit ROS-mediated apoptosis. Furthermore, treatment with rapamycin that led to further Akt activation and resistance to etoposide hypersensitized cancer cells to ROS-mediated apoptosis. Given that rapamycin alone is mainly cytostatic, this constitutes a strategy for cancer therapy that selectively eradicates cancer cells via Akt activation.
Akt缺陷导致细胞对复制性衰老、氧化应激和致癌性Ras诱导的早衰以及活性氧(ROS)介导的凋亡产生抗性。Akt激活通过增加氧消耗从而增加细胞内ROS,并通过抑制FoxO下游的ROS清除剂(特别是 sestrin 3)的表达来诱导早衰并使细胞对ROS介导的凋亡敏感。这揭示了Akt的一个致命弱点,因为与其抑制多种凋亡刺激诱导的凋亡的能力相反,Akt无法抑制ROS介导的凋亡。此外,用雷帕霉素处理导致Akt进一步激活并对依托泊苷产生抗性,却使癌细胞对ROS介导的凋亡高度敏感。鉴于单独使用雷帕霉素主要具有细胞生长抑制作用,这构成了一种癌症治疗策略,即通过激活Akt选择性地根除癌细胞。