Sun Jiandong, Liu Yan, Moreno Stephanie, Baudry Michel, Bi Xiaoning
Basic Medical Sciences, College of Osteopathic Medicine of the Pacific and.
Basic Medical Sciences, College of Osteopathic Medicine of the Pacific and Graduate College of Biomedical Sciences, Western University of Health Sciences, Pomona, California 91766.
J Neurosci. 2015 Mar 18;35(11):4706-18. doi: 10.1523/JNEUROSCI.4276-14.2015.
Angelman syndrome (AS) is a neurogenetic disorder caused by deficiency of maternally expressed ubiquitin-protein ligase E3A (UBE3A), an E3 ligase that targets specific proteins for proteasomal degradation. Although motor function impairment occurs in all patients with AS, very little research has been done to understand and treat it. The present study focuses on Ube3A deficiency-induced alterations in signaling through the mechanistic target of rapamycin (mTOR) pathway in the cerebellum of the AS mouse model and on potential therapeutic applications of rapamycin. Levels of tuberous sclerosis complex 2 (TSC2), a negative regulator of mTOR, were increased in AS mice compared with wild-type mice; however, TSC2 inhibitory phosphorylation was also increased. Correspondingly, levels of phosphorylated/active mTOR were increased. Phosphorylation of the mTORC1 substrates S6 kinase 1 (S6K1) and S6 was elevated, whereas that of the mTORC2 substrates AKT and N-myc downstream regulated 1 was decreased, suggesting enhanced mTORC1 but inhibited mTORC2 signaling. Semi-chronic treatment of AS mice with rapamycin not only improved their motor performance but also normalized mTORC1 and mTORC2 signaling. Furthermore, inhibitory phosphorylation of rictor, a key regulatory/structural subunit of the mTORC2 complex, was increased in AS mice and decreased after rapamycin treatment. These results indicate that Ube3A deficiency leads to overactivation of the mTORC1-S6K1 pathway, which in turn inhibits rictor, resulting in decreased mTORC2 signaling in Purkinje neurons of AS mice. Finally, rapamycin treatment also improved dendritic spine morphology in AS mice, through inhibiting mTORC1 and possibly enhancing mTORC2-mediated regulation of synaptic cytoskeletal elements. Collectively, our results indicate that the imbalance between mTORC1 and mTORC2 activity may contribute to synaptic pathology and motor impairment in AS.
安吉尔曼综合征(AS)是一种神经遗传性疾病,由母源表达的泛素蛋白连接酶E3A(UBE3A)缺乏所致,UBE3A是一种将特定蛋白质靶向蛋白酶体降解的E3连接酶。尽管所有AS患者都会出现运动功能障碍,但针对其理解和治疗的研究却非常少。本研究聚焦于AS小鼠模型小脑中,Ube3A缺乏引起的通过雷帕霉素作用靶点(mTOR)信号通路的改变,以及雷帕霉素的潜在治疗应用。与野生型小鼠相比,AS小鼠中mTOR的负调节因子结节性硬化复合物2(TSC2)水平升高;然而,TSC2的抑制性磷酸化也增加。相应地,磷酸化/活性mTOR水平升高。mTORC1底物S6激酶1(S6K1)和S6的磷酸化升高,而mTORC2底物AKT和N - myc下游调节因子1的磷酸化降低,提示mTORC1信号增强但mTORC2信号受到抑制。用雷帕霉素对AS小鼠进行半慢性治疗,不仅改善了它们的运动表现,还使mTORC1和mTORC2信号正常化。此外,mTORC2复合物的关键调节/结构亚基rictor的抑制性磷酸化在AS小鼠中增加,雷帕霉素治疗后降低。这些结果表明,Ube3A缺乏导致mTORC1 - S6K1通路过度激活,进而抑制rictor,导致AS小鼠浦肯野神经元中mTORC2信号减少。最后,雷帕霉素治疗还通过抑制mTORC1并可能增强mTORC2介导的突触细胞骨架元件调节,改善了AS小鼠的树突棘形态。总的来说,我们的结果表明,mTORC1和mTORC2活性之间的失衡可能导致AS中的突触病理和运动障碍。