γ-分泌酶抑制剂的研发现状  

Current Trends in the Study of γ-secretase Inhibitors

作　　者：刘剑敏[1] 姜凤超[1] 

机构地区：[1]华中科技大学同济医学院药学院,湖北武汉430030

出　　处：《药学进展》2004年第11期491-497,共7页Progress in Pharmaceutical Sciences

摘　　要：β淀粉样蛋白沉积是阿尔茨海默病的主要病理特征之一 ,β淀粉样蛋白是经β 和γ 分泌酶水解 β淀粉样蛋白前体蛋白而产生 ,故 β 和γ 分泌酶是 β淀粉样蛋白前体蛋白代谢的关键性酶 ,因而成为治疗阿尔茨海默病的很有潜力的靶点。根据 β淀粉样蛋白前体蛋白的代谢、β淀粉样蛋白的形成过程及γ 分泌酶的结构、特性和作用机制 ,分类综述γ 分泌酶抑制剂抑制 β淀粉样蛋白前体蛋白的活性及构效关系。Progressive cerebral β-am yl oid (Aβ) deposition is believed to play a central role in the pathogenesis of A lzheimer's disease (AD). Aβ is generated by the cleavage of amyloid β-protein precursor (APP) via β- and γ-secretase. Thus these two critical enzymes of A PP metabolism are becoming the top therapeutic targets for anti-AD agents. The metabolism of APP, the production of Aβ and the structure, characteristics and role of these secretases were introduced. Inhibition activity and structure-act ivity relationship of several kinds of promising γ-secretase inhibitors were r eviewed. [

关 键 词：阿尔茨海默病 β淀粉样蛋白前体蛋白 Β淀粉样蛋白 分泌酶 Γ-分泌酶抑制剂 

分 类 号：R971[医药卫生—药品]