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    Modulation of protein methylation and phosphoprotein phosphate
    4.
    发明申请
    Modulation of protein methylation and phosphoprotein phosphate 失效
    蛋白质甲基化和磷酸蛋白磷酸调节

    公开(公告)号：US20070031909A1

    公开(公告)日：2007-02-08

    申请号：US10579369

    申请日：2003-03-13

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

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

    IPC分类号： A61K36/00 ,  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。

    Acid Mimic Compounds for the Inhibition of Isoprenyl-S-Cysteinyl Methyltransferase
    7.
    发明申请
    Acid Mimic Compounds for the Inhibition of Isoprenyl-S-Cysteinyl Methyltransferase 审中-公开
    用于抑制异戊二烯基-S-半胱氨酰甲基转移酶的酸性模拟化合物

    公开(公告)号：US20090170917A1

    公开(公告)日：2009-07-02

    申请号：US12326746

    申请日：2008-12-02

    申请人： Seung-Yub Lee ,  Eduardo Perez ,  Keshava Rapole ,  Gopal Sarngadharan ,  Gregory B. Stock ,  Jeffry B. Stock ,  Maxwell Stock ,  Michael Voronkov ,  Peter Wolanin

    发明人： Seung-Yub Lee ,  Eduardo Perez ,  Keshava Rapole ,  Gopal Sarngadharan ,  Gregory B. Stock ,  Jeffry B. Stock ,  Maxwell Stock ,  Michael Voronkov ,  Peter Wolanin

    IPC分类号： A61K31/41 ,  A61K31/27 ,  C07C271/22 ,  A61K31/16 ,  C07C243/34 ,  C07D257/04 ,  A61P11/00

    CPC分类号： C07D231/12 ,  C07C323/60 ,  C07D233/61 ,  C07D235/14 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04

    摘要： Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g., Parkinson's disease).

    摘要翻译： 除此之外，本发明提供能够有效抑制嗜中性粒细胞，巨噬细胞和血小板中G蛋白或GPCR介导的炎症反应的新型化合物。 特别地，本发明的化合物作为水肿抑制剂，红斑抑制剂和MPO抑制剂（髓过氧化物酶），含有相同化合物的药物组合物及其用于治疗可能受益于水肿，红斑和MPO抑制的疾病的用途 例如炎症（急性或慢性），哮喘，自身免疫疾病和慢性阻塞性肺病（COPD）（例如肺气肿，慢性支气管炎和小气道疾病等），免疫系统的炎症反应，皮肤疾病（例如 对于患有酒渣鼻，特应性皮炎，脂溢性皮炎，牛皮癣的患者，肠易激综合征（例如，Chron氏病和溃疡性结肠炎等）以及中枢神经系统疾病（例如帕金森氏病））减少急性皮肤刺激。

    Method of identifying modulators of PP2A methylase
    9.
    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。