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    • 4. 发明申请
    • SCREENING ASSAYS FOR INHIBITORS OF BETA AMYLOID PEPTIDE ION CHANNEL FORMATION
    • β-淀粉样蛋白离子通道形成抑制剂筛选测定
    • WO2008150467A1
    • 2008-12-11
    • PCT/US2008/006885
    • 2008-05-30
    • THE REGENTS OF THE UNIVERSITY OF MICHIGANMAYER, MichaelYANG, Jerry
    • MAYER, MichaelYANG, Jerry
    • A61K49/00G01N33/53A61P43/00
    • G01N33/6896G01N2333/4709G01N2500/00G01N2800/2814
    • Screening assays and methods of employing the screening assays designed to identify potential inhibitors of amyloidal neurodegenerative disease. The screening assays comprises providing a membrane construct disposed on a substrate and contacting the membrane construct with Aß peptide capable of forming an Aß peptide ion channel in the construct. The membrane construct is then contacted with a test compound. Aß peptide ion channel activity is determined after the construct has incubated with the Aß peptide in the presence and in the absence of the test compound. A reduction in the Aß peptide ion channel activity of the membrane construct contacted with the test compound in comparison to a different membrane construct contacted with the same Aß peptide in the absence of said test compound indicates that the test compound is an inhibitor of amyloidal neurodegenerative disease.
    • 筛选试验和采用筛选试验的方法,设计用于鉴定淀粉样变性神经变性疾病的潜在抑制剂。 筛选测定法包括提供设置在底物上的膜构建体并使膜构建体与能够在构建体中形成Aβ肽离子通道的Aβ肽接触。 然后将膜构建体与测试化合物接触。 在存在和不存在测试化合物的情况下,将构建体与Aβ肽孵育后,测定Aβ肽离子通道活性。 与在不存在所述测试化合物的情况下与与相同Aβ肽接触的不同膜构建体相比,与测试化合物接触的膜构建体的Aβ肽离子通道活性的降低表明测试化合物是淀粉样神经变性疾病的抑制剂 。