Department of Biochemistry and Molecular Biology, Michigan State University, East Lansing, MI 48824, USA.
Int J Mol Sci. 2023 Oct 8;24(19):14996. doi: 10.3390/ijms241914996.
The P301L mutation in tau protein is a prevalent pathogenic mutation associated with neurodegenerative frontotemporal dementia, FTD. The mechanism by which P301L triggers or facilitates neurodegeneration at the molecular level remains unclear. In this work, we examined the effect of the P301L mutation on the biochemical and biological characteristics of pathologically relevant hyperphosphorylated tau. Hyperphosphorylated P301L tau forms cytotoxic aggregates more efficiently than hyperphosphorylated wildtype tau or unphosphorylated P301L tau in vitro. Mechanistic studies establish that hyperphosphorylated P301L tau exacerbates endoplasmic reticulum (ER) stress-associated gene upregulation in a neuroblastoma cell line when compared to wildtype hyperphosphorylated tau treatment. Furthermore, the microtubule cytoskeleton is severely disrupted following hyperphosphorylated P301L tau treatment. A hyperphosphorylated tau aggregation inhibitor, apomorphine, also inhibits the harmful effects caused by P301L hyperphosphorylated tau. In short, the P301L single mutation within the core repeat domain of tau renders the underlying hyperphosphorylated tau more potent in eliciting ER stress and cytoskeleton damage. However, the P301L mutation alone, without hyperphosphorylation, is not sufficient to cause these phenotypes. Understanding the conditions and mechanisms whereby selective mutations aggravate the pathogenic activities of tau can provide pivotal clues on novel strategies for drug development for frontotemporal dementia and other related neurodegenerative tauopathies, including Alzheimer's disease.
在 tau 蛋白中,P301L 突变是一种与神经退行性额颞叶痴呆(FTD)相关的常见致病性突变。P301L 如何在分子水平引发或促进神经退行性变的机制尚不清楚。在这项工作中,我们研究了 P301L 突变对病理性相关过度磷酸化 tau 的生化和生物学特性的影响。与野生型过度磷酸化 tau 或未磷酸化 P301L tau 相比,体外过度磷酸化的 P301L tau 更有效地形成细胞毒性聚集体。机制研究表明,与野生型过度磷酸化 tau 处理相比,过度磷酸化的 P301L tau 加剧了神经母细胞瘤细胞系中内质网(ER)应激相关基因的上调。此外,微管细胞骨架在过度磷酸化的 P301L tau 处理后严重受损。一种过度磷酸化 tau 聚集抑制剂,阿朴吗啡,也抑制了由 P301L 过度磷酸化 tau 引起的有害作用。简而言之,tau 核心重复结构域中的 P301L 单突变使潜在的过度磷酸化 tau 在引发 ER 应激和细胞骨架损伤方面更为有效。然而,仅 P301L 突变而没有过度磷酸化不足以引起这些表型。了解选择性突变加剧 tau 致病活性的条件和机制可以为额颞叶痴呆和其他相关神经退行性 tau 病(包括阿尔茨海默病)的药物开发提供新的策略提供关键线索。