Lee Ha E, Lim Dami, Lee Jae Y, Lim Sang M, Pae Ae N
Convergence Research Center for Diagnosis, Treatment & Care System of Dementia, Korea Institute of Science & Technology, Seoul 02792, Republic of Korea.
Division of Bio-Medical Science & Technology, KIST School, Korea University of Science & Technology, Seoul 02792, Republic of Korea.
Pharm Pat Anal. 2019 Jan;8(1):15-39. doi: 10.4155/ppa-2019-0003. Epub 2019 Mar 14.
Alzheimer's disease (AD) is a progressive neurodegenerative disease that is characterized by memory loss and cognitive impairment. As this disease is becoming a serious global health issue, development of disease modifying therapeutics is urgently required. AD is characterized by deposits of two protein, amyloid β and tau. Although amyloid β-based therapeutics have been extensively investigated so far, tau has also received great attention as one of promising molecular targets for AD. In this review, a variety of tau-directed strategies to rescue tau-mediated neurotoxicity will be reviewed especially focusing on small molecules. Subsequently, recent patents published from 2014 to 2018 that integrate efforts to develop tau-directed small molecules for the treatment of AD will be reviewed.
阿尔茨海默病（AD）是一种进行性神经退行性疾病，其特征为记忆丧失和认知障碍。由于该疾病正成为一个严重的全球健康问题，迫切需要开发疾病修饰疗法。AD的特征是两种蛋白质——淀粉样β蛋白和tau蛋白的沉积。尽管迄今为止基于淀粉样β蛋白的疗法已得到广泛研究，但tau蛋白作为AD有前景的分子靶点之一也受到了极大关注。在本综述中，将尤其针对小分子，综述各种旨在挽救tau介导的神经毒性的tau靶向策略。随后，将综述2014年至2018年发表的近期专利，这些专利整合了开发用于治疗AD的tau靶向小分子的努力。
