Weidemann Andreas, Eggert Simone, Reinhard Friedrich B M, Vogel Markus, Paliga Krzysztof, Baier Gottfried, Masters Colin L, Beyreuther Konrad, Evin Geneviève
Zentrum für Molekulare Biologie Heidelberg, INF 282, 69120 Heidelberg, Germany.
Biochemistry. 2002 Feb 26;41(8):2825-35. doi: 10.1021/bi015794o.
Proteolytic processing of the transmembrane domain of the amyloid precursor protein (APP) is a key component of Alzheimer's disease pathogenesis. Using C-terminally tagged APP derivatives, we have identified by amino-terminal sequencing a novel cleavage site of APP, at Leu-49, distal to the gamma-secretase site. This was termed -cleavage. Brefeldin A treatment and pulse-chase experiments indicate that this cleavage occurs late in the secretory pathway. The level of -cleavage is decreased by expression of presenilin-1 mutants known to impair Abeta formation, and it is sensitive to the gamma-secretase inhibitors MDL28170 and L-685,458. Remarkably, it shares similarities with site 3 cleavage of Notch-1: membrane topology, cleavage before a valine, dependence on presenilins, and inhibition profile.
淀粉样前体蛋白(APP)跨膜结构域的蛋白水解加工是阿尔茨海默病发病机制的关键组成部分。利用C末端标记的APP衍生物,我们通过氨基末端测序在APP上鉴定出一个新的切割位点,位于γ-分泌酶位点远端的Leu-49处。这被称为β-切割。布雷菲德菌素A处理和脉冲追踪实验表明,这种切割发生在分泌途径的后期。已知会损害Aβ形成的早老素-1突变体的表达会降低β-切割水平,并且它对γ-分泌酶抑制剂MDL28170和L-685,458敏感。值得注意的是,它与Notch-1的3号位点切割有相似之处:膜拓扑结构、在缬氨酸之前切割、对早老素的依赖性以及抑制谱。