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    • 4. 发明授权
    • Antagonists of cxcr3-binding cxc chemokines
    • cxcr3结合cxc趋化因子的拮抗剂
    • US07541435B2
    • 2009-06-02
    • US10517726
    • 2003-06-03
    • Amanda ProudfootMarie Kosco-Vilbois
    • Amanda ProudfootMarie Kosco-Vilbois
    • C07K14/00A61K45/00A61K39/00C07H21/04C12P21/02
    • C07K14/522A61K38/00
    • Novel antagonists of CXCR3-binding CXC chemokines, and in particular of human CXCL11, can be obtained by generating mutants of such chemokines in which the binding to glycosaminoglycans (GAGs) is impaired due to non-conservative substitutions of amino acids involved in this interaction. Compounds prepared in accordance with the present invention can be used to block the activity of CXCR3-binding CXC chemokines on CXCR3-expressing cells, thereby providing therapeutic compositions for use in the treatment or prevention of diseases related to excessive activated T cells migration, such as graft rejection and autoimmune diseases, and of diseases needing an increase of vascularization, such as ischemic heart disease.
    • CXCR3结合CXC趋化因子,特别是人CXCL11的新型拮抗剂可以通过产生这样的趋化因子的突变体来获得,其中与糖胺聚糖(GAG)的结合由于涉及该相互作用的氨基酸的非保守取代而受损。 根据本发明制备的化合物可用于阻断CXCR3结合CXC趋化因子对CXCR3表达细胞的活性,从而提供用于治疗或预防与过度活化的T细胞迁移有关的疾病的治疗组合物,例如 移植排斥反应和自身免疫性疾病以及需要增加血管形成的疾病,如缺血性心脏病。
    • 7. 发明申请
    • Novel antagonists of cxcr3-binding cxc chemokines
    • cxcr3结合cxc趋化因子的新型拮抗剂
    • US20060204498A1
    • 2006-09-14
    • US10517726
    • 2003-06-03
    • Amanda ProudfootMarie Kosco-Vilbois
    • Amanda ProudfootMarie Kosco-Vilbois
    • A61K39/395C07H21/04C12P21/06C07K16/24
    • C07K14/522A61K38/00
    • Novel antagonists of CXCR3-binding CXC chemokines, and in particular of human CXCL11, can be obtained by generating mutants of such chemokines in which the binding to glycosaminoglycans (GAGs) is impaired due to non-conservative substitutions of amino acids involved in this interaction. Compounds prepared in accordance with the present invention can be used to block the activity of CXCR3-binding CXC chemokines on CXCR3-expressing cells, thereby providing therapeutic compositions for use in the treatment or prevention of diseases related to excessive activated T cells migration, such as graft rejection and autoimmune diseases, and of diseases needing an increase of vascularization, such as ischemic heart disease.
    • CXCR3结合CXC趋化因子,特别是人CXCL11的新型拮抗剂可以通过产生这样的趋化因子的突变体来获得,其中与糖胺聚糖(GAG)的结合由于涉及该相互作用的氨基酸的非保守取代而受损。 根据本发明制备的化合物可用于阻断CXCR3结合CXC趋化因子对CXCR3表达细胞的活性,从而提供用于治疗或预防与过度活化的T细胞迁移有关的疾病的治疗组合物,例如 移植排斥反应和自身免疫性疾病以及需要增加血管形成的疾病,如缺血性心脏病。