公开(公告)号：WO2003020880A3

公开(公告)日：2003-03-13

申请号：PCT/US2002/024546

申请日：2002-08-02

Applicant: ABBOTT LABORATORIES ,  BORHANI, David, W. ,  CALDERWOOD, David ,  DIXON, Richard, W. ,  HIRST, Gavin, C. ,  HRNCIAR, Peter ,  LOEW, Andreas ,  LEUNG, Adelaine ,  RITTER, Kurt

Inventor： BORHANI, David, W. ,  CALDERWOOD, David ,  DIXON, Richard, W. ,  HIRST, Gavin, C. ,  HRNCIAR, Peter ,  LOEW, Andreas ,  LEUNG, Adelaine ,  RITTER, Kurt

IPC: C07K14/00

Abstract: 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.

公开(公告)号：WO03020880A2

公开(公告)日：2003-03-13

申请号：PCT/US0224546

申请日：2002-08-02

Applicant: ABBOTT LAB ,  BORHANI DAVID W ,  CALDERWOOD DAVID ,  DIXON RICHARD W ,  HIRST GAVIN C ,  HRNCIAR PETER ,  LOEW ANDREAS ,  LEUNG ADELAINE ,  RITTER KURT

Inventor： BORHANI DAVID W ,  CALDERWOOD DAVID ,  DIXON RICHARD W ,  HIRST GAVIN C ,  HRNCIAR PETER ,  LOEW ANDREAS ,  LEUNG ADELAINE ,  RITTER KURT

IPC: C12N9/12 ,  C12N

CPC classification number: C12N9/1205 ,  C07K2299/00

Abstract: 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.

Abstract translation: 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使用这些结晶形式来确定Lck的催化结构域的三维结构。 本发明还涉及单独或与抑制剂复合的Lck催化结构域的三维结构在设计和/或鉴定潜在的Lck活性抑制剂的方法中的用途，例如抑制 天然底物到Lck催化结构域。 本发明还涉及单独或与抑制剂复合的Lck催化结构域的三维结构在设计和/或鉴定潜在的Lck活性选择性抑制剂的方法中的应用，例如抑制 选择性地将天然底物连接到Lck催化结构域。