| GSK-3抑制剂研究进展 |
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| 引用本文： | 张娜,蒋勇军,俞庆森,邹建卫.GSK-3抑制剂研究进展[J].化学进展,2007,19(4):614-623. |
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| 作者姓名： | 张娜 蒋勇军 俞庆森 邹建卫 |
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| 作者单位： | 浙江大学,化学系,杭州,310027;浙江大学宁波理工学院,分子设计与营养工程市重点实验室,宁波,315104 |
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| 基金项目： | 浙江省自然科学基金
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浙江省宁波市自然科学基金 |
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| 摘 要： | 糖原合成酶激酶-3 (Glycogen synthase kinase-3, GSK-3)是一个多功能的丝氨酸/苏氨酸蛋白激酶,不仅参与肝糖代谢过程,而且还参与Wnt和Hedgehog信号通路,通过磷酸化多种底物蛋白来调节细胞的生理过程。GSK-3抑制剂作为目前倍受关注的小分子抑制剂,对治疗神经退化性疾病,癌症,II型糖尿病具有潜在的疗效。本文针对已开发出的GSK-3抑制剂,对其结构,与蛋白的作用模式以及构效关系进行阐述,为进一步设计合理的药物先导化合物和特异性小分子化学探针提供有益的启示。
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| 关 键 词： | GSK-3 抑制剂 构效关系 选择性 药物设计 |
| 文章编号： | 1005-281X（2007）04-0614-10 |
| 收稿时间： | 2006-05 |
| 修稿时间： | 2006-07 |
Studies of Glycogen Synthase Kinase-3 Inhibitors |
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| Zhang Na,Jiang Yongjun,Yu Qingsen,Zou Jianwei.Studies of Glycogen Synthase Kinase-3 Inhibitors[J].Progress in Chemistry,2007,19(4):614-623. |
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| Authors: | Zhang Na Jiang Yongjun Yu Qingsen Zou Jianwei |
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| Institution: | 1 .Department of Chemistry, Zhejiang University, Hangzhou 310027, China;2.Key Laboratory for Molecular Design and Nutrition Engineering of Ningbo City, Ningbo Institute of Technology, Zhejiang University, Ningbo 315104, China |
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| Abstract: | Glycogen synthase kinase-3 (GSK-3),a multifunctional serine-threonine kinase, has played an important role in glycogen metabolism and is known to occupy a central stage in many cellular physiological events by phosphorylation of multifold substrate proteins, including Wnt and Hedgehog signal transduction pathways. Small molecular inhibitors of GSK-3, as new promising drugs for the treatment of neurodegenerative diseases, cancer and type II diabetes, are getting more and more attentions. Information gained from their structures, binding modes and structure-activity relationships provides some clues for the future optimization of drug lead-compounds and selective chemical probes . |
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| Keywords: | GSK-3 inhibitors structure-activity relationship selectivity drug design |
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