Kuriyama Mai, Wang Chu Fan, Nagase Tatsuya, Sohma Youhei, Kanai Motomu, Hori Yukiko, Tomita Taisuke
Laboratory of Neuropathology and Neuroscience, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan.
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Wakayama Medical University, Wakayama, Japan; Laboratory of Synthetic Organic Chemistry, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan.
Neurotherapeutics. 2025 Apr;22(3):e00548. doi: 10.1016/j.neurot.2025.e00548. Epub 2025 Feb 11.
Amyloidoses, which are characterized by abnormal accumulation of amyloid proteins leading to organ dysfunction, represent a major therapeutic challenge. They include neurodegenerative diseases, such as Alzheimer disease (AD), tauopathies and synucleinopathies. Since amyloids are causative factors in these diseases, the importance of proteolytic methods to remove amyloid, such as immunotherapy and Proteolysis Targeting Chimera (PROTAC) technology, has been recognized. Immunotherapy removes target proteins by antibody-mediated reactions and is the most studied method in practical use for the treatment of AD. PROTAC is a small molecule that uses the ubiquitin-proteasome system to degrade intracellular target proteins and has demonstrated efficacy in clinical trials for other diseases. In addition, a new modality called photo-oxygenation has been developed. Photo-oxygenation is a method of selectively adding oxygen to amyloid using a photocatalyst, which is a small molecule compound that is activated by light. Studies both in vitro and in vivo have shown promising results in inhibiting amyloid aggregation and enhancing the clearance of amyloid proteins. In this review, we introduce and discuss these proteolytic modalities, and provide insights into potential future directions for the clinical application in amyloidoses.
淀粉样变性以淀粉样蛋白异常积聚导致器官功能障碍为特征,是一个重大的治疗挑战。淀粉样变性包括神经退行性疾病,如阿尔茨海默病(AD)、tau蛋白病和α-突触核蛋白病。由于淀粉样蛋白是这些疾病的致病因素,人们已经认识到蛋白水解方法(如免疫疗法和蛋白酶靶向嵌合体(PROTAC)技术)对于清除淀粉样蛋白的重要性。免疫疗法通过抗体介导的反应去除靶蛋白,是治疗AD实际应用中研究最多的方法。PROTAC是一种利用泛素-蛋白酶体系统降解细胞内靶蛋白的小分子,已在其他疾病的临床试验中显示出疗效。此外,还开发了一种名为光氧化的新方法。光氧化是一种利用光催化剂(一种由光激活的小分子化合物)选择性地向淀粉样蛋白添加氧的方法。体外和体内研究均显示出在抑制淀粉样蛋白聚集和增强淀粉样蛋白清除方面的有前景的结果。在这篇综述中,我们介绍并讨论这些蛋白水解方法,并对淀粉样变性临床应用的潜在未来方向提供见解。