非肽类β-分泌酶1(BACE1)抑制剂的研究进展

被引：3

作者：

李慧宁

李凤然

程卯生

刘洋

机构：

[1] 沈阳药科大学基于靶点的药物设计与研究教育部重点实验室

来源：

中国药物化学杂志 | 2016年 / 26卷 / 06期

关键词：

β-分泌酶1; 非肽类BACE1抑制剂; β-淀粉样多肽;

D O I：

暂无

中图分类号：

R971 [神经系统药物];

学科分类号：

100115 [医学神经生物学];

摘要：

β-分泌酶1(β-site APP cleaving enzyme 1,BACE1)是存在于中枢神经系统的天冬氨酸蛋白酶,能够催化β-淀粉样多肽(Aβ)形成中的第一步也是关键一步的反应,因而被认为是调节认知障碍、治疗阿尔兹海默症(AD)的关键靶点。自2000年BACE1的结构被解析出来后,其抑制剂的研究始终是药物化学领域的热点。随着高通量筛选和基于片段的药物发现等技术的广泛应用,大量非肽类小分子BACE1抑制剂被设计与合成,并且部分化合物已经进入了临床研究阶段。本文对近5年来非肽类BACE1抑制剂的研究进展进行综述。

引用

页码：498 / 508

页数：11

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