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    • 1. 发明申请
    • USE OF ORGANIC CATION TRANSPORTERS FOR CANCER DIAGNOSIS AND THERAPY
    • 有机摄影机使用癌症诊断和治疗方法
    • US20100028259A1
    • 2010-02-04
    • US12296887
    • 2007-04-18
    • Kathleen M. GiacominiJoe W. GrayAnna LapukShuzhong Zhang
    • Kathleen M. GiacominiJoe W. GrayAnna LapukShuzhong Zhang
    • A61K49/00C12Q1/68G01N33/53A61B5/05
    • G01N33/57484G01N33/57407G01N33/57492G01N2800/52
    • The present invention provides, for the first time, the finding that organic cation transporters (OCTs) are major determinants of the anticancer activity of platinum-based drugs such as oxaliplatin, and therefore have clinical significance for selecting oxaliplatin as the preferred therapy for a cancer that expresses one or more OCTs, such as colorectal cancer or liver cancer. In addition, the OCT genotype can also be used to predict oxaliplatin response or to select therapy. The present invention also provides methods of treating or inhibiting cancers that expresses one or more OCTs by administering a therapeutically effective amount of a platinum-based drug such as an oxaliplatin analog having an organic non-leaving group with an increased size. The present invention further provides methods of sensitizing a therapy resistant cancer to a platinum-based drug such as oxaliplatin by administering a therapeutically effective amount of a nucleic acid encoding an OCT. Compositions, kits, and integrated systems for carrying out the diagnostic, prognostic, and therapeutic methods of the present invention are also provided.
    • 本发明首次提出有机阳离子转运蛋白(OCTs)是奥沙利铂等铂类药物的抗癌活性的主要决定因素,因此具有选择奥沙利铂作为癌症优选疗法的临床意义 其表达一个或多个OCT,例如结肠直肠癌或肝癌。 此外,OCT基因型也可用于预测奥沙利铂反应或选择治疗。 本发明还提供了通过施用治疗有效量的具有增加大小的具有有机非离去基团的奥沙利铂类似物的铂基药物来治疗或抑制表达一种或多种OCT的癌症的方法。 本发明进一步提供了通过施用治疗有效量的编码OCT的核酸来使耐药性癌症对铂类药物如奥沙利铂敏感的方法。 还提供了用于实施本发明的诊断,预后和治疗方法的组合物,试剂盒和综合系统。