Ozcan Umut, Ozcan Lale, Yilmaz Erkan, Düvel Katrin, Sahin Mustafa, Manning Brendan D, Hotamisligil Gökhan S
Department of Genetics and Complex Diseases, Harvard School of Public Health, Harvard University, Boston, MA 02115, USA.
Mol Cell. 2008 Mar 14;29(5):541-51. doi: 10.1016/j.molcel.2007.12.023.
Mammalian target of rapamycin, mTOR, is a major sensor of nutrient and energy availability in the cell and regulates a variety of cellular processes, including growth, proliferation, and metabolism. Loss of the tuberous sclerosis complex genes (TSC1 or TSC2) leads to constitutive activation of mTOR and downstream signaling elements, resulting in the development of tumors, neurological disorders, and at the cellular level, severe insulin/IGF-1 resistance. Here, we show that loss of TSC1 or TSC2 in cell lines and mouse or human tumors causes endoplasmic reticulum (ER) stress and activates the unfolded protein response (UPR). The resulting ER stress plays a significant role in the mTOR-mediated negative-feedback inhibition of insulin action and increases the vulnerability to apoptosis. These results demonstrate ER stress as a critical component of the pathologies associated with dysregulated mTOR activity and offer the possibility to exploit this mechanism for new therapeutic opportunities.
雷帕霉素哺乳动物靶点(mTOR)是细胞内营养和能量可用性的主要传感器,可调节多种细胞过程,包括生长、增殖和代谢。结节性硬化症复合物基因(TSC1或TSC2)缺失会导致mTOR及其下游信号元件的组成性激活,从而引发肿瘤、神经疾病,在细胞水平上还会导致严重的胰岛素/IGF-1抵抗。在此,我们表明,细胞系以及小鼠或人类肿瘤中TSC1或TSC2的缺失会导致内质网(ER)应激并激活未折叠蛋白反应(UPR)。由此产生的内质网应激在mTOR介导的胰岛素作用负反馈抑制中起重要作用,并增加细胞对凋亡的易感性。这些结果表明内质网应激是与mTOR活性失调相关病理的关键组成部分,并为利用这一机制开发新的治疗机会提供了可能。