Method of identifying inhibitors of Lck
    6.
    发明授权
    Method of identifying inhibitors of Lck 有权
    鉴定Lck抑制剂的方法

    公开(公告)号:US07400979B2

    公开(公告)日:2008-07-15

    申请号:US10212346

    申请日:2002-08-05

    IPC分类号: G06F17/11 G06F17/50 G06F19/00

    CPC分类号: C12N9/1205 C07K2299/00

    摘要: The present invention relates to polypeptides which comprise the ligand binding domain of Lck, crystalline forms of these polypeptides, and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Lck. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential selective inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain selectively.

    摘要翻译: 本发明涉及包含Lck的配体结合结构域,这些多肽的结晶形式的多肽,以及这些结晶形式用于确定Lck催化结构域的三维结构的多肽。 本发明还涉及在设计和/或鉴定Lck活性的潜在抑制剂的方法中单独或与抑制剂复合的Lck催化结构域的三维结构的用途,例如抑制结合的化合物 天然底物到Lck催化结构域。 本发明还涉及在设计和/或鉴定Lck活性的潜在选择性抑制剂的方法中单独或与抑制剂复合的Lck催化结构域的三维结构的用途,例如抑制Lck活性结合的化合物 选择性地对Lck催化结构域的天然底物。