Shineman Diana W, Zhang Bin, Leight Susan N, Pratico Domenico, Lee Virginia M-Y
Department of Pathology and Laboratory Medicine, Center for Neurodegenerative Disease Research, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA.
J Neurosci. 2008 Apr 30;28(18):4785-94. doi: 10.1523/JNEUROSCI.0684-08.2008.
Alzheimer's disease (AD) amyloid plaques are composed of amyloid-beta (Abeta) peptides produced from proteolytic cleavage of amyloid precursor protein (APP). Isoprostanes, markers of in vivo oxidative stress, are elevated in AD patients and in the Tg2576 mouse model of AD-like Abeta brain pathology. To determine whether isoprostanes increase Abeta production, we delivered isoprostane iPF(2alpha)-III into the brains of Tg2576 mice. Although treated mice showed increased brain Abeta levels and plaque-like deposits, this was blocked by a thromboxane (TP) receptor antagonist, suggesting that TP receptor activation mediates the effects of iPF(2alpha)-III on Abeta. This hypothesis was supported by cell culture studies that showed that TP receptor activation increased Abeta and secreted APP ectodomains. This increase was a result of increased APP mRNA stability leading to elevated APP mRNA and protein levels. The increased APP provides more substrate for alpha and beta secretase proteolytic cleavages, thereby increasing Abeta generation and amyloid plaque deposition. To test the effectiveness of targeting the TP receptor for AD therapy, Tg2576 mice underwent long-term treatment with S18886, an orally available TP receptor antagonist. S18886 treatment reduced amyloid plaques, insoluble Abeta, and APP levels, thereby implicating TP receptor signaling as a novel target for AD therapy.
阿尔茨海默病(AD)淀粉样斑块由淀粉样前体蛋白(APP)经蛋白水解切割产生的β淀粉样蛋白(Aβ)肽组成。异前列腺素是体内氧化应激的标志物,在AD患者以及具有类似AD的Aβ脑病理特征的Tg2576小鼠模型中水平升高。为了确定异前列腺素是否会增加Aβ的产生,我们将异前列腺素iPF(2α)-III注入Tg2576小鼠的大脑。尽管接受治疗的小鼠脑内Aβ水平升高且出现斑块样沉积物,但这被血栓素(TP)受体拮抗剂所阻断,这表明TP受体激活介导了iPF(2α)-III对Aβ的作用。细胞培养研究支持了这一假说,该研究表明TP受体激活会增加Aβ和分泌型APP胞外域。这种增加是APP mRNA稳定性增加导致APP mRNA和蛋白质水平升高的结果。增加的APP为α和β分泌酶的蛋白水解切割提供了更多底物,从而增加了Aβ的产生和淀粉样斑块的沉积。为了测试靶向TP受体用于AD治疗的有效性,Tg2576小鼠接受了口服可用的TP受体拮抗剂S18886的长期治疗。S18886治疗降低了淀粉样斑块、不溶性Aβ和APP水平,从而表明TP受体信号传导是AD治疗的一个新靶点。
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