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    Protein tyrosine phosphatase inhibitors
    4.
    发明授权
    Protein tyrosine phosphatase inhibitors 有权
    蛋白酪氨酸磷酸酶抑制剂

    公开(公告)号：US08242092B2

    公开(公告)日：2012-08-14

    申请号：US12366562

    申请日：2009-02-05

    申请人： Brent Townshend ,  Michel Tremblay

    发明人： Brent Townshend ,  Michel Tremblay

    IPC分类号： A61K48/00

    CPC分类号： C12N15/115 ,  C12N2310/16 ,  C12Y301/03048

    摘要： The present invention provides compositions and methods for binding and/or modulating enzymatic activity of human protein tyrosine phosphatases such as PTP1B. Additionally, the invention provides methods of identifying and using such nucleic acid ligands.

    摘要翻译： 本发明提供了用于结合和/或调节人蛋白质酪氨酸磷酸酶如PTP1B的酶活性的组合物和方法。 另外，本发明提供鉴定和使用这种核酸配体的方法。

    Compositions and methods for inhibiting the enzymatic activity of PTP-1B
    6.
    发明申请
    Compositions and methods for inhibiting the enzymatic activity of PTP-1B 审中-公开
    抑制PTP-1B酶活性的组合物和方法

    公开(公告)号：US20060070135A1

    公开(公告)日：2006-03-30

    申请号：US11127934

    申请日：2005-05-12

    申请人： Michel Tremblay ,  Dan Leung ,  Timothy Daynard

    发明人： Michel Tremblay ,  Dan Leung ,  Timothy Daynard

    IPC分类号： A01K67/027 ,  C12Q1/54 ,  C12Q1/37

    CPC分类号： C12Q1/42 ,  C12N15/8509 ,  G01N2500/04

    摘要： The present invention provides mice that have had their PTP-1B genes disrupted by targeted homologous recombination. The mice have no detectable PTP-1B protein, yet appear to be physiologically normal. However, in the fed state on a normal diet, the mice have half the level of circulating insulin as their wild-type littermates. In glucose and insulin tolerance tests, the mice show an increased insulin sensitivity. When fed a high fat, high carbohydrate diet, the mice show a resistance to weight gain as compared to their wild-type littermates. Methods of making the mice and cell lines derived from the mice are also provided. The present invention also provides methods of identifying inhibitors of the enzymatic activity of PTP-1B as well as inhibitors identified by such methods.

    摘要翻译： 本发明提供了通过靶向同源重组破坏其PTP-1B基因的小鼠。 小鼠没有可检测的PTP-1B蛋白，但似乎在生理上正常。 然而，在正常饮食中的喂养状态下，小鼠具有作为野生型同窝出生物循环胰岛素水平的一半水平。 在葡萄糖和胰岛素耐量测试中，小鼠显示胰岛素敏感性增加。 当饲喂高脂肪，高碳水化合物饮食时，与野生型同窝仔相比，小鼠显示出对体重增加的抵抗力。 还提供了制备来自小鼠的小鼠和细胞系的方法。 本发明还提供鉴定PTP-1B的酶活性抑制剂以及通过这些方法鉴定的抑制剂的方法。