治疗阿尔采末病的药物靶点:β-分泌酶

A drug target for Alzheimers disease: β-secretase

近年来的研究表明,β-淀粉样蛋白(Aβ)是老年斑的主要成分,有明显的神经细胞毒性作用,在阿尔采末病(AD)的发病过程中发挥了重要作用,因此降低脑中Aβ的生成量是治疗AD的策略。Aβ是由β-和γ-分泌酶裂解其前体蛋白(APP)而生成,其中β-分泌酶(BACE)是启动Aβ形成的关键限速酶,因此BACE是开发治疗AD药物的一个具有吸引力的作用靶点。该文就近来对β-分泌酶的研究作一综述。

ABSTRACT Recent research suggests that the β-amyloid peptide (Aβ) is central to the pathophysi-ology of Alzheimers disease (AD). Amyloid plaques, primarily composed of Aβ, have significant neurotoxic effects. So it is therapeutic strategies for AD to lower the production of Aβ in the brain. Aβ is a product of catabolism of amyloid precursor protein ( APP) by β-secretase and y- secretase. BACE ( β-secretase) exhibits all the properties of the β-secretase, and as the key rate-limiting enzyme that initiates the formation of Aβ, BACE is an attractive drug target for AD. The recent research of β-secretase is reviewed in this paper.