Whitehead Institute for Biomedical Research, Nine Cambridge Center, Cambridge, MA 02142, USA.
Science. 2013 Jul 26;341(6144):1236566. doi: 10.1126/science.1236566.
The mechanistic target of rapamycin (mTOR) complex 1 (mTORC1) protein kinase promotes growth and is the target of rapamycin, a clinically useful drug that also prolongs life span in model organisms. A persistent mystery is why the phosphorylation of many bona fide mTORC1 substrates is resistant to rapamycin. We find that the in vitro kinase activity of mTORC1 toward peptides encompassing established phosphorylation sites varies widely and correlates strongly with the resistance of the sites to rapamycin, as well as to nutrient and growth factor starvation within cells. Slight modifications of the sites were sufficient to alter mTORC1 activity toward them in vitro and to cause concomitant changes within cells in their sensitivity to rapamycin and starvation. Thus, the intrinsic capacity of a phosphorylation site to serve as an mTORC1 substrate, a property we call substrate quality, is a major determinant of its sensitivity to modulators of the pathway. Our results reveal a mechanism through which mTORC1 effectors can respond differentially to the same signals.
雷帕霉素靶蛋白(mTOR)复合物 1(mTORC1)蛋白激酶促进生长,是雷帕霉素的作用靶点,雷帕霉素是一种临床上有用的药物,也能延长模式生物的寿命。一个持久的谜团是,为什么许多真正的 mTORC1 底物的磷酸化对雷帕霉素有抗性。我们发现,体外涵盖已建立的磷酸化位点的 mTORC1 激酶对肽的激酶活性差异很大,并且与该位点对雷帕霉素以及细胞内营养和生长因子饥饿的抗性强烈相关。这些位点的微小修饰足以改变它们在体外的 mTORC1 活性,并在细胞内引起它们对雷帕霉素和饥饿敏感性的伴随变化。因此,磷酸化位点作为 mTORC1 底物的固有能力,即我们所称的底物质量,是其对该途径调节剂敏感性的主要决定因素。我们的结果揭示了一种机制,通过该机制,mTORC1 效应物可以对相同的信号做出不同的反应。