发明授权
US07259142B2 Redox-stable, non-phosphorylated cyclic peptide inhibitors of SH2 domain binding to target protein, conjugates thereof, compositions and methods of synthesis and use
有权
与靶蛋白结合的SH2结构域的氧化还原稳定的非磷酸化环肽抑制剂，其结合物，组合物和合成和使用方法
- 专利标题： Redox-stable, non-phosphorylated cyclic peptide inhibitors of SH2 domain binding to target protein, conjugates thereof, compositions and methods of synthesis and use
- 专利标题（中）： 与靶蛋白结合的SH2结构域的氧化还原稳定的非磷酸化环肽抑制剂，其结合物，组合物和合成和使用方法
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申请号： US11224819申请日： 2005-09-13
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公开(公告)号： US07259142B2公开(公告)日： 2007-08-21
- 发明人: Peter P Roller , Ya-Qui Long , Feng-Di T. Lung , C. Richter King , Dajun Yang , Johannes H. Voigt
- 申请人： Peter P Roller , Ya-Qui Long , Feng-Di T. Lung , C. Richter King , Dajun Yang , Johannes H. Voigt
- 申请人地址： US DC Washington
- 专利权人： The United States of America, represented by the Secretary, Department of Health and Human Services
- 当前专利权人： The United States of America, represented by the Secretary, Department of Health and Human Services
- 当前专利权人地址： US DC Washington
- 代理机构： Leydig, Voit & Mayer, Ltd.
- 主分类号： A61K38/12
- IPC分类号： A61K38/12
摘要：
A compound of formula: in which (i) aa1 is Adi and aa4 is Glu or (ii) each of aa1 and aa4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is characterized by an IC50 in vivo of less than about 4.0 μM with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, has a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.
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