γ-分泌酶抑制剂研究进展

Recent Advances in the Research of γ-Secretase Inhibitors

阿尔茨海默病(AD)是老年人常见的神经系统变性疾病。近来研究认为阿尔茨海默病的产生主要起因于β淀粉样蛋白(β-amyloid,Aβ)在大脑内的沉积,而由γ-分泌酶切割β淀粉样前体蛋白产生的疏水性Aβ42是形成Aβ的主要原因,γ-分泌酶是防治阿尔茨海默病很有潜力的靶点。本文就Aβ的形成、γ-分泌酶的生物学研究以及目前γ-分泌酶抑制剂的研究进展作一综述。

Alzheimer＇s disease （AD） is a hypothesis for the cause of this disease is that it progressive neurodegenerative disorder in the elderly. The is the result of aberrant production of β-amyloid （Aβ） and current plaque deposition in the brain. Aβ42, less soluble and forming the major component of the amyloid plaques, is generated via the cleavage of β-amyloid protein precursor （β-APP） by γ-secretase, a key enzyme in the production of Aβ. Therefore γ- secretase is potential target for the treatment of Alzheimer＇s disease. This review focuses on the studies of the formation of Aβ and the biology of γ-secretase, and the development of γ-secretase inhibitors.