Serneels Lutgarde, Dejaegere Tim, Craessaerts Katleen, Horré Katrien, Jorissen Ellen, Tousseyn Thomas, Hébert Sébastien, Coolen Marcel, Martens Gerard, Zwijsen An, Annaert Wim, Hartmann Dieter, De Strooper Bart
Neuronal Cell Biology, Flanders Interuniversity Institute for Biotechnology and Katholieke Universiteit Leuven, Leuven B-3000, Belgium.
Proc Natl Acad Sci U S A. 2005 Feb 1;102(5):1719-24. doi: 10.1073/pnas.0408901102. Epub 2005 Jan 21.
Gamma-secretase is the protease responsible for amyloid beta peptide release and is needed for Notch, N-Cadherin, and possibly other signaling pathways. The protease complex consists of at least four subunits, i.e., Presenilin, Aph1, Pen2, and Nicastrin. Two different genes encode Aph1A and Aph1B in man. A duplication of Aph1B in rodents has given rise to a third gene, Aph1C. Different mixes of gamma-secretase subunits assemble in at least four human and six rodent complexes but it is not known whether they have different activities in vivo. We report here the inactivation of the three Aph1 genes in mice. Aph1A-/- embryos show a lethal phenotype characterized by angiogenesis defects in the yolk sac, neuronal tube malformations, and mild somitogenesis defects. Aph1B-/- or C-/- or the combined Aph1BC-/- mice (which can be considered as a model for total Aph1B loss in human) survive into adulthood. However, Aph1BC-/- deficiency causes a mild but significant reduction in amyloid beta percursor protein processing in selective regions of the adult brain. We conclude that the biochemical and physiological repercussions of genetically reducing gamma-secretase activity via the different Aph1 components are quite divergent and tissue specific. Our work provides in vivo evidence for the concept that different gamma-secretase complexes may exert different biological functions. In the context of Alzheimer's disease therapy, this implies the theoretical possibility that targeting specific gamma-secretase subunit combinations could yield less toxic drugs than the currently available general inhibitors of gamma-secretase activity.
γ-分泌酶是负责释放淀粉样β肽的蛋白酶,是Notch、N-钙黏蛋白以及可能的其他信号通路所必需的。该蛋白酶复合物至少由四个亚基组成,即早老素、Aph1、Pen2和尼卡斯特林。人类中有两个不同的基因编码Aph1A和Aph1B。啮齿动物中Aph1B的复制产生了第三个基因Aph1C。γ-分泌酶亚基的不同组合至少在四种人类和六种啮齿动物复合物中组装,但尚不清楚它们在体内是否具有不同的活性。我们在此报告小鼠中三个Aph1基因的失活情况。Aph1A基因敲除胚胎表现出致死表型,其特征为卵黄囊中血管生成缺陷、神经管畸形和轻度体节发生缺陷。Aph1B基因敲除或C基因敲除小鼠或联合的Aph1BC基因敲除小鼠(可被视为人类Aph1B完全缺失的模型)可存活至成年。然而,Aph1BC基因敲除导致成年大脑特定区域中淀粉样β前体蛋白加工轻度但显著减少。我们得出结论,通过不同的Aph1组分基因降低γ-分泌酶活性的生化和生理影响差异很大且具有组织特异性。我们的工作为不同的γ-分泌酶复合物可能发挥不同生物学功能这一概念提供了体内证据。在阿尔茨海默病治疗的背景下,这意味着理论上有可能靶向特定的γ-分泌酶亚基组合会产生比目前可用的γ-分泌酶活性通用抑制剂毒性更低的药物。