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Review Article

β淀粉样蛋白裂解酶1（BACE1）在阿尔茨海默病治疗中的概述：阐明其外源结合抗体和变构抑制剂

卷 29, 期 1, 2022

发表于: 08 June, 2021

页: [114 - 135] 页: 22

弟呕挨: 10.2174/0929867328666210608145357

价格: $65

摘要

经过几十年的鉴定，许多过去和正在进行的研究都集中在β淀粉样蛋白切割酶1（BACE1）作为治疗阿尔茨海默病（AD）的靶标的治疗作用上。尽管在3期临床试验中最初的BACE1抑制剂大大减少了AD患者β淀粉样蛋白相关斑块，但研究人员最终因缺乏效力而停止了测试。这种停产导致针对BACE1的药物开发和发现有限，尽管对痴呆症和AD疗法的需求很高。因此，必须详细描述BACE1治疗方案在神经系统疾病中的潜在生物学基础。在这里，我们强调了BACE1的生物活性，遗传特性和在神经退行性治疗中的作用。我们回顾了BACE1外源结合抗体和变构抑制剂开发作为AD疗法的研究贡献。该评价还涵盖了BACE1生物学功能、疾病相关机制以及淀粉样蛋白前体蛋白位点分裂的酶条件。基于本综述，我们建议进一步研究抗BACE1外显性抗体和BACE1变构抑制剂。非活性位点抑制可能是阿尔茨海默氏症神经系统疾病BACE1治疗的前进方向。

关键词: BACE1生物学性质，阿尔茨海默病，BACE1外显性抗体，BACE1底物，基因表达，变构抑制剂。

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