AβPP-selective BACE inhibitors (ASBI): novel class of therapeutic agents for alzheimer's disease.
AβPP-selective BACE inhibitors (ASBI): novel class of therapeutic agents for alzheimer's disease.
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DOI：
10.3233/jad-130578
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发表时间：
2013
期刊：
影响因子：
--
通讯作者：
John V
中科院分区：
文献类型：
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作者：
Descamps O;Spilman P;Zhang Q;Libeu CP;Poksay K;Gorostiza O;Campagna J;Jagodzinska B;Bredesen DE;John V
采用系统方法鉴定Aβ PP选择性BACE抑制剂（ASBI），并评价其选择性调节AβPP加工的体内能力。我们确定了一种生物素营养补充剂作为分子先导，在细胞模型中充当ASBI，并表明通过前药方法增加这种生物素的脑水平导致阿尔茨海默病小鼠模型中Aβ42的减少。ASBI代表了一类新的阿尔茨海默病候选治疗药物。
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.