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    • 2. 发明申请
    • Compositions and methods of therapy for cancers characterized by expression of the tumor-associated antigen mn/ca ix
    • 以肿瘤相关抗原mn / ca ix表达为特征的癌症治疗的组合物和方法
    • US20090252738A1
    • 2009-10-08
    • US10525535
    • 2003-08-25
    • Justin WongJill WinterGuita LalehzadehRobert Warne
    • Justin WongJill WinterGuita LalehzadehRobert Warne
    • A61K39/395G01N33/53C07K2/00A61K38/00C07K14/00C07K16/18A61P35/00
    • A61K38/02C07K16/40C12Q1/527G01N2500/04
    • Compositions and methods useful in inhibiting proliferation of CA IX+preneoplastic or neoplastic cells in a mammal are provided. The compositions are antagonist anti-CA IX antibodies and other inhibitory agents that target carbonic anhydrase activity of CA IX on these cells. The antagonist anti-CA IX antibodies or antigen-binding fragments thereof are specifically reactive with an inhibitory epitope of CA IX or biologically active variant thereof. Formation of an antibody-antigen complex between the antagonist anti-CA IX antibodies or antigen-binding fragments thereof and the respective inhibitory epitopes results in inhibition of carbonic anhydrase activity of CA IX or biologically active variant thereof. Other small molecule agents that inhibit carbonic anhydrase activity of CA IX or biologically active variant thereof and screening assays for identifying such agents are also provided. The antagonist anti-CA IX antibodies, antigen-binding fragments thereof, and other CA IX inhibitory agents identified herein are useful in the treatment of cancers characterized by the expression of the CA IX tumor-associated antigen.
    • 提供了可用于抑制哺乳动物中CA IX +肿瘤前和肿瘤细胞增殖的组合物和方法。 该组合物是拮抗性抗CA IX抗体和其它抑制剂,其靶向这些细胞上CA IX的碳酸酐酶活性。 拮抗性抗CA IX抗体或其抗原结合片段与CA IX或其生物活性变体的抑制性表位特异性反应。 拮抗性抗CA IX抗体或其抗原结合片段之间的抗体 - 抗原复合物的形成和各自的抑制性表位导致CA IX或其生物活性变体的碳酸酐酶活性的抑制。 还提供了抑制CA IX或其生物活性变体的碳酸酐酶活性的其它小分子试剂和用于鉴定这些试剂的筛选试验。 本文鉴定的拮抗性抗CAⅨ抗体,其抗原结合片段和其它CAⅨ抑制剂可用于治疗特征在于表达CAⅨ肿瘤相关抗原的癌症。