摘要/Abstract

阿尔茨海默病是导致痴呆的主要诱因，它可以对老年人的记忆以及认知能力造成破坏性的损伤，并最终导致死亡.糖原合成酶激酶-3（GSK-3）的过度表达与阿尔茨海默病的发生发展有着密切的关系，因而成为研发阿尔茨海默病治疗药物的热点.综述了近五年报道的GSK-3抑制剂，主要有腺嘌呤核苷三磷酸（ATP）竞争性抑制剂、非ATP竞争性抑制剂、底物竞争性抑制剂、变构抑制剂、不可逆抑制剂和天然产物产物来源的GSK-3抑制剂.就其来源、化学结构、作用机制进行介绍，并展望了GSK-3抑制剂未来的研究方向.
关键词: 阿尔茨海默病, 糖原合成酶激酶-3(GSK-3), 淀粉样斑块, 神经元纤维缠结
Alzheimer's disease is the leading cause of dementia, which can endanger devastating damage to memory and cognition of the elderly and eventually lead to death. Over expression of glycogen synthase kinase-3 (GSK-3) is closely related to the development and progression of Alzheimer's disease, and has become a hot field for the development of therapies for Alzheimer's disease. The GSK-3 inhibitors reported in recent five years, mainly including ATP competitive inhibitors, non-ATP competitive inhibitors, substrate competitive inhibitors, allosteric inhibitors, irreversible inhibitors are summarized and natural products, furthermore, the source, chemical structure and mechanism about GSK-3 inhibitors are introduced. Research prospects in this field are also discussed.
Key words: Alzheimer's disease, glycogen synthase kinase-3 (GSK-3), amyloid plaque, neurofibrillary tangle


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