Mills John R, Hippo Yoshitaka, Robert Francis, Chen Samuel M H, Malina Abba, Lin Chen-Ju, Trojahn Ulrike, Wendel Hans-Guido, Charest Al, Bronson Roderick T, Kogan Scott C, Nadon Robert, Housman David E, Lowe Scott W, Pelletier Jerry
Department of Biochemistry, McGill University, Montreal, QC, Canada H3G 1Y6.
Proc Natl Acad Sci U S A. 2008 Aug 5;105(31):10853-8. doi: 10.1073/pnas.0804821105. Epub 2008 Jul 29.
Activation of the phosphatidylinositol 3-kinase (PI3K)/AKT signaling pathway is a frequent occurrence in human cancers and a major promoter of chemotherapeutic resistance. Inhibition of one downstream target in this pathway, mTORC1, has shown potential to improve chemosensitivity. However, the mechanisms and genetic modifications that confer sensitivity to mTORC1 inhibitors remain unclear. Here, we demonstrate that loss of TSC2 in the E mu-myc murine lymphoma model leads to mTORC1 activation and accelerated oncogenesis caused by a defective apoptotic program despite compromised AKT phosphorylation. Tumors from Tsc2(+/-)E mu-Myc mice underwent rapid apoptosis upon blockade of mTORC1 by rapamycin. We identified myeloid cell leukemia sequence 1 (Mcl-1), a bcl-2 like family member, as a translationally regulated genetic determinant of mTORC1-dependent survival. Our results indicate that the extent by which rapamycin can modulate expression of Mcl-1 is an important feature of the rapamycin response.
磷脂酰肌醇3-激酶(PI3K)/AKT信号通路的激活在人类癌症中频繁发生,并且是化疗耐药的主要促进因素。抑制该通路中的一个下游靶点mTORC1已显示出改善化疗敏感性的潜力。然而,赋予对mTORC1抑制剂敏感性的机制和基因修饰仍不清楚。在此,我们证明在Eμ-myc小鼠淋巴瘤模型中TSC2缺失导致mTORC1激活以及尽管AKT磷酸化受损但由于凋亡程序缺陷而加速肿瘤发生。来自Tsc2(+/-)Eμ-Myc小鼠的肿瘤在雷帕霉素阻断mTORC1后迅速凋亡。我们鉴定出髓细胞白血病序列1(Mcl-1),一种bcl-2样家族成员,作为mTORC1依赖性存活的翻译调控基因决定因素。我们的结果表明雷帕霉素调节Mcl-1表达的程度是雷帕霉素反应的一个重要特征。