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首页> 外文期刊>Journal of Medicinal Chemistry >Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimers Disease: Design, synthesis, and characterization of pyrazines
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Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimers Disease: Design, synthesis, and characterization of pyrazines

机译：发现用于阿尔茨海默氏病的新型有效且高度选择性的糖原合酶激酶3β（GSK3β）抑制剂：吡嗪的设计，合成和表征

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摘要

Glycogen synthase kinase-3β, also called tau phosphorylating kinase, is a proline-directed serine/threonine kinase which was originally identified due to its role in glycogen metabolism. Active forms of GSK3β localize to pretangle pathology including dystrophic neuritis and neurofibrillary tangles in Alzheimers disease (AD) brain. By using a high throughput screening (HTS) approach to search for new chemical series and cocrystallization of key analogues to guide the optimization and synthesis of our pyrazine series, we have developed highly potent and selective inhibitors showing cellular efficacy and bloo-brain barrier penetrance. The inhibitors are suitable for in vivo efficacy testing and may serve as a new treatment strategy for Alzheimers disease.
机译：糖原合酶激酶3β，也称为tau磷酸化激酶，是脯氨酸定向的丝氨酸/苏氨酸激酶，最初由于其在糖原代谢中的作用而被鉴定。 GSK3β的活性形式定位于缠结前病理，包括阿尔茨海默氏病（AD）脑中的营养不良性神经炎和神经原纤维缠结。通过使用高通量筛选（HTS）方法来寻找新的化学系列和关键类似物的共结晶以指导我们的吡嗪系列的优化和合成，我们开发了显示细胞功效和血脑屏障渗透性的高效抑制剂。该抑制剂适用于体内功效测试，并可作为阿尔茨海默氏病的新治疗策略。

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