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    Redox-stable, non-phosphorylated cyclic peptide inhibitors of SH2 domain binding to target protein, conjugates thereof, compositions and methods of synthesis and use
    1.
    发明授权
    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

    公开(公告)号：US07259142B2

    公开(公告)日：2007-08-21

    申请号：US11224819

    申请日：2005-09-13

    申请人： Peter P Roller ,  Ya-Qui Long ,  Feng-Di T. Lung ,  C. Richter King ,  Dajun Yang ,  Johannes H. Voigt

    发明人： Peter P Roller ,  Ya-Qui Long ,  Feng-Di T. Lung ,  C. Richter King ,  Dajun Yang ,  Johannes H. Voigt

    IPC分类号： A61K38/12

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K7/56

    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.

    摘要翻译： 下式化合物：其中（i）aa 1是Adi，aa 4是Glu或（ii）aa 1和a a各自独立地选自 Ad1，L是硫，亚砜，氧或亚甲基，该化合物（及其缀合物）与包含SH2结构域的蛋白质中的SH2结构域结合，未被磷酸化，是氧化还原稳定的 在体内，相对于Grb2中的SH2结构域，其体内IC 50小于约4.0μM，并且在结合到Grb2的SH2结构域时具有转向构象。 包含如上所述的化合物和载体的缀合物，包含（i）如上所述的化合物或缀合物和（ii）载体的组合物，抑制包含SH2结构域的蛋白质中SH2结构域结合的方法 涉及一种动物中的靶蛋白，其中SH2结构域与靶蛋白结合抑制有效量的上述化合物或结合物接触，以及合成这种缀合物的方法。