Department of Medicine, University of California San Diego, La Jolla, California 92093-0613, USA.
J Clin Invest. 2010 Aug;120(8):2805-16. doi: 10.1172/JCI43008. Epub 2010 Jul 19.
Mechanistic target of rapamycin (MTOR) plays a critical role in the regulation of cell growth and in the response to energy state changes. Drugs inhibiting MTOR are increasingly used in antineoplastic therapies. Myocardial MTOR activity changes during hypertrophy and heart failure (HF). However, whether MTOR exerts a positive or a negative effect on myocardial function remains to be fully elucidated. Here, we show that ablation of Mtor in the adult mouse myocardium results in a fatal, dilated cardiomyopathy that is characterized by apoptosis, autophagy, altered mitochondrial structure, and accumulation of eukaryotic translation initiation factor 4E-binding protein 1 (4E-BP1). 4E-BP1 is an MTOR-containing multiprotein complex-1 (MTORC1) substrate that inhibits translation initiation. When subjected to pressure overload, Mtor-ablated mice demonstrated an impaired hypertrophic response and accelerated HF progression. When the gene encoding 4E-BP1 was ablated together with Mtor, marked improvements were observed in apoptosis, heart function, and survival. Our results demonstrate a role for the MTORC1 signaling network in the myocardial response to stress. In particular, they highlight the role of 4E-BP1 in regulating cardiomyocyte viability and in HF. Because the effects of reduced MTOR activity were mediated through increased 4E-BP1 inhibitory activity, blunting this mechanism may represent a novel therapeutic strategy for improving cardiac function in clinical HF.
雷帕霉素靶蛋白(MTOR)在调节细胞生长和对能量状态变化的反应中起着关键作用。抑制 MTOR 的药物越来越多地用于抗肿瘤治疗。心肌 MTOR 活性在肥大和心力衰竭(HF)期间发生变化。然而,MTOR 是否对心肌功能产生积极或消极影响仍有待充分阐明。在这里,我们表明,成年小鼠心肌中 Mtor 的缺失会导致致命的扩张型心肌病,其特征为细胞凋亡、自噬、线粒体结构改变和真核翻译起始因子 4E 结合蛋白 1(4E-BP1)的积累。4E-BP1 是一种含有 MTOR 的多蛋白复合物 1(MTORC1)底物,可抑制翻译起始。在经受压力超负荷时,Mtor 缺失的小鼠表现出受损的肥大反应和加速的 HF 进展。当与 Mtor 一起缺失编码 4E-BP1 的基因时,观察到凋亡、心脏功能和存活率的显著改善。我们的结果表明 MTORC1 信号网络在心肌对压力的反应中起作用。特别是,它们突出了 4E-BP1 在调节心肌细胞活力和 HF 中的作用。由于减少的 MTOR 活性的作用是通过增加 4E-BP1 的抑制活性介导的,因此减弱这种机制可能代表改善临床 HF 中心脏功能的一种新的治疗策略。