中文摘要：

β-分泌酶作为β-淀粉样蛋白产生的限速酶,被认为是治疗阿尔采末病的靶标之一。抑制β-分泌酶的活性可以降低阿尔采末病关键致病因素β-淀粉样蛋白的生成,阻止β-淀粉样蛋白有害级联反应,从而达到治疗阿尔采末病的目的。目前以β-分泌酶为靶标防治阿尔采末病的药物研发主要有以下几类：一是包括肽类、拟肽类和化学小分子在内的化学药,二是中药和天然产物,另外还有诸如抗体和核酸的生物制剂。该文对以β-分泌酶为靶标的药物研发进展进行了综述。

英文摘要：

β-secretase（β-site amyloid precursor protein cleaving enzyme 1;BACE1） has been identified as the rate-limiting enzyme for amyloid-β（Aβ） production and one of Alzheimer＇s disease（AD） therapeutic target.The inhibition of β-secretase may treat AD by reducing the generation of Aβ,a key factor that contributes to the pathogenesis of AD,and preventing the neuron damages through inhibiting the amyloid cascade.There are several kinds of AD drugs acting on β-secretase in development： one is chemical compound,including peptide and small-molecular compound;another is traditional Chinese medicine and natural product;and the third is biological product,such as antibody and nucleic acid.The advancement of drugs targeting on β-secretase in recent years is reviewed.