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    Activation of mutated RAC-PK
    8.
    发明授权
    Activation of mutated RAC-PK 有权
    激活突变的RAC-PK

    公开(公告)号：US07897371B2

    公开(公告)日：2011-03-01

    申请号：US11682135

    申请日：2007-03-05

    申请人： Dario Alessi ,  Mirjana Andjelkovic ,  Philip Cohen ,  Peter David Cron ,  Darren Cross ,  Brian A. Hemmings

    发明人： Dario Alessi ,  Mirjana Andjelkovic ,  Philip Cohen ,  Peter David Cron ,  Darren Cross ,  Brian A. Hemmings

    IPC分类号： C12N9/12 ,  C12Q1/48 ,  G01N33/536

    CPC分类号： C07K14/47 ,  A61K38/00 ,  C12N9/12 ,  C12N9/1205 ,  C12Q1/42 ,  C12Q1/48

    摘要： The invention concerns RAC-PK and fragments thereof, as well as activators and inhibitors of RAC-PK for use as medicaments, particularly in the treatment of diseases concerned with abnormalities in processes modulated by insulin, such as cellular proliferation, insulin deficiency and/or excess blood sugar levels. Moreover, the invention provides RAC-PK for use in screening potential mimics or modulators thereof. A method for screening for agents capable of affecting the activity of GSK3 is also disclosed. The invention further provides a screening kit comprising the RAC-PK as an active principle, and a method for screening compounds which are candidate mimics or modulators of RAC-PK activity comprising detecting specific interactions between the candidate compounds and RAC-PK. There is also provided a process for activating RAC-PK comprising treatment thereof with a phosphatase inhibitor.

    摘要翻译： 本发明涉及RAC-PK及其片段，以及用作药物的RAC-PK的活化剂和抑制剂，特别是用于治疗由胰岛素调节的过程如胰岛素缺乏和/或 血糖过高。 此外，本发明提供了用于筛选潜在模拟物或其调节剂的RAC-PK。 还公开了能够影响GSK3活性的试剂的筛选方法。 本发明进一步提供了包含作为活性成分的RAC-PK的筛选试剂盒，以及筛选作为RAC-PK活性的候选模拟物或调节剂的化合物的方法，包括检测候选化合物与RAC-PK之间的特异性相互作用。 还提供了用于激活RAC-PK的方法，其包括用磷酸酶抑制剂处理它。