Biomedical Science and Engineering Interdisciplinary Program, Korea Advanced Institute of Science and Technology (KAIST), Daejeon, Republic of Korea.
Department of Biomedical Science and Engineering, Gwangju Institute of Science and Technology, Gwangju, Republic of Korea.
J Clin Invest. 2019 Oct 1;129(10):4207-4223. doi: 10.1172/JCI127032.
Brain somatic mutations confer genomic diversity in the human brain and cause neurodevelopmental disorders. Recently, brain somatic activating mutations in MTOR have been identified as a major etiology of intractable epilepsy in patients with cortical malformations. However, the molecular genetic mechanism of how brain somatic mutations in MTOR cause intractable epilepsy has remained elusive. In this study, translational profiling of intractable epilepsy mouse models with brain somatic mutations and genome-edited cells revealed a novel translational dysregulation mechanism and mTOR activation-sensitive targets mediated by human MTOR mutations that lead to intractable epilepsy with cortical malformation. These mTOR targets were found to be regulated by novel mTOR-responsive 5'-UTR motifs, distinct from known mTOR inhibition-sensitive targets regulated by 5' terminal oligopyrimidine motifs. Novel mTOR target genes were validated in patient brain tissues, and the mTOR downstream effector eIF4E was identified as a new therapeutic target in intractable epilepsy via pharmacological or genetic inhibition. We show that metformin, an FDA-approved eIF4E inhibitor, suppresses intractable epilepsy. Altogether, the present study describes translational dysregulation resulting from brain somatic mutations in MTOR, as well as the pathogenesis and potential therapeutic targets of intractable epilepsy.
脑体突变赋予人类大脑基因组多样性,并导致神经发育障碍。最近,MTOR 的脑体激活突变被确定为皮质畸形患者难治性癫痫的主要病因。然而,MTOR 脑体突变如何导致难治性癫痫的分子遗传机制仍不清楚。在这项研究中,通过具有脑体突变的难治性癫痫小鼠模型和基因组编辑细胞的转化谱分析,揭示了一种新的翻译失调机制和由人类 MTOR 突变介导的 mTOR 激活敏感靶点,导致伴有皮质畸形的难治性癫痫。这些 mTOR 靶标受新型 mTOR 反应性 5'-UTR 基序调控,与受 5'端寡嘧啶基序调控的已知 mTOR 抑制敏感靶标不同。在患者脑组织中验证了新型 mTOR 靶基因,mTOR 下游效应因子 eIF4E 通过药理学或遗传抑制被鉴定为难治性癫痫的新治疗靶点。我们表明,二甲双胍,一种 FDA 批准的 eIF4E 抑制剂,可抑制难治性癫痫。总之,本研究描述了 MTOR 脑体突变引起的翻译失调,以及难治性癫痫的发病机制和潜在治疗靶点。