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    Method of identifying modulators of PP2A methylase
    18.
    发明授权
    Method of identifying modulators of PP2A methylase 失效
    鉴定PP2A甲基化酶的调节剂的方法

    公开(公告)号：US07794965B2

    公开(公告)日：2010-09-14

    申请号：US10579369

    申请日：2003-03-13

    申请人： Gregory Stock ,  Jeffry B. Stock ,  Maxwell Stock ,  Scott Vafai

    发明人： Gregory Stock ,  Jeffry B. Stock ,  Maxwell Stock ,  Scott Vafai

    IPC分类号： C12Q1/42

    CPC分类号： G01N33/6896 ,  C12Q1/42 ,  C12Q1/48 ,  G01N2500/00

    摘要： The invention relates to methylated proteins that control protein phosphorylation, particularly phosphoesterases, such as PP2A. It relates to screening methods for determining agents that affect methylation of these proteins and thus also modulate the level of phosphorylation of phosphoproteins. It relates as well to the agents and to compositions comprising the agents. In a particular aspect in this regard the invention relates to agents that alter PP2A methylation and that thereby affect phosphorylation of phosphoproteins that play an important role in health or disease, such as the tau protein which is implicated in the etiology of Alzheimer's Disease. The invention further relates to diagnostic methods based on protein methylation levels, to compositions comprising agents for affecting methylation of proteins and for controlling the phosphate complement of phosphoproteins. Additionally, the invention relates to methods for administering the agents and compositions to affect methylation of proteins physiologically and to modulate the phosphate complement of phosphoproteins. Examples in this regard include agents and compositions that affect physiological activity of PP2A and alter the phosphate complement of phosphoproteins that are altered in disease.

    摘要翻译： 本发明涉及控制蛋白磷酸化的甲基化蛋白质，特别是磷酸酯酶，例如PP2A。 它涉及用于确定影响这些蛋白质甲基化的试剂的筛选方法，因此也调节磷酸化蛋白的磷酸化水平。 它还涉及试剂和包含试剂的组合物。 在这方面的一个特定方面，本发明涉及改变PP2A甲基化并因此影响在健康或疾病中发挥重要作用的磷酸化蛋白质的磷酸化的试剂，例如与阿尔茨海默病病因有关的tau蛋白。 本发明进一步涉及基于蛋白质甲基化水平的诊断方法，包括影响蛋白质甲基化和控制磷酸蛋白磷酸化补体的试剂的组合物。 此外，本发明涉及用于施用影响蛋白质生理学上的甲基化并调节磷酸蛋白的磷酸盐补体的试剂和组合物的方法。 在这方面的实例包括影响PP2A的生理活性并改变在疾病中改变的磷酸蛋白的磷酸盐补体的药剂和组合物。