发明授权
US08987474B2 Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
有权
NSC-87877，NSC-117199及其类似物抑制Shp2 / PTPN11蛋白酪氨酸磷酸酶
- 专利标题： Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
- 专利标题（中）： NSC-87877，NSC-117199及其类似物抑制Shp2 / PTPN11蛋白酪氨酸磷酸酶
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申请号： US11733023申请日： 2007-04-09
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公开(公告)号： US08987474B2公开(公告)日： 2015-03-24
- 发明人: Jie Wu , Nicholas J. Lawrence , Said M. Sebti , Harshani R. Lawrence
- 申请人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti , Harshani R. Lawrence
- 申请人地址： US FL Tampa US FL Tampa
- 专利权人： University of South Florida,H. Lee Moffitt Cancer Center and Research Institute, Inc.
- 当前专利权人： University of South Florida,H. Lee Moffitt Cancer Center and Research Institute, Inc.
- 当前专利权人地址： US FL Tampa US FL Tampa
- 代理机构： Smith & Hopen, P.A.
- 代理商 Robert J. Varkonyi
- 主分类号： A61K31/404
- IPC分类号： A61K31/404 ; A61K31/405 ; C07D209/40
摘要：
Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Significantly, NSC-87877 is active in cell-based assays and has no detectable off-target effects in the EGF-stimulated Erk 1/2 activation pathway. Additionally, a number of analogs of NSC-117199 have been produced. These analogs exhibit enhanced protein tyrosine phosphatase inhibition and are found to be potent and/or selective inhibitors of Shp1 and/or Shp2 protein tyrosine phosphatases.
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