β淀粉样蛋白前体（AβPP）选择性 BACE 抑制剂（ASBI）：阿尔茨海默病治疗的新型药物类别。
AβPP-selective BACE inhibitors (ASBI): novel class of therapeutic agents for alzheimer's disease.
机构信息
Buck Institute for Research on Aging, Novato, CA, USA.
出版信息
J Alzheimers Dis. 2013;37(2):343-55. doi: 10.3233/JAD-130578.
Abstract
A systematic approach was used to identify AβPP-selective BACE inhibitors (ASBI) and to evaluate their in vivo ability to modulate AβPP processing selectively. We identified a bioflavonoid nutritional supplement as a molecular lead that acts as an ASBI in cell models, and show that increasing brain levels of this bioflavonoid through a pro-drug approach leads to reduction of Aβ42 in an Alzheimer's disease mouse model. ASBIs represent a novel class of candidate therapeutic agents for Alzheimer's disease.
摘要
采用系统的方法来鉴定 AβPP 选择性 BACE 抑制剂（ASBI），并评估其在体内选择性调节 AβPP 加工的能力。我们鉴定出一种生物类黄酮营养补充剂作为一种在细胞模型中起作用的 ASBI 的分子先导，并且表明通过前药方法增加这种生物类黄酮在大脑中的水平会导致阿尔茨海默病小鼠模型中 Aβ42 的减少。ASBI 代表了一类用于治疗阿尔茨海默病的新型候选治疗剂。
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