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首页> 外国专利> COMPOUNDS AND METHODS FOR THE SELECTIVE INHIBITION OF ABCB1, ABCC1 AND ABCG2 TRANSPORTERS AND THE TREATMENT OF CANCERS, ESPECIALLY DRUG RESISTANT CANCERS AND HIGH THROUGHPUT FLOW CYTOMETRY ASSAY TO DETECT SELECTIVE INHIBITORS

COMPOUNDS AND METHODS FOR THE SELECTIVE INHIBITION OF ABCB1, ABCC1 AND ABCG2 TRANSPORTERS AND THE TREATMENT OF CANCERS, ESPECIALLY DRUG RESISTANT CANCERS AND HIGH THROUGHPUT FLOW CYTOMETRY ASSAY TO DETECT SELECTIVE INHIBITORS

机译：选择性抑制ABCB1，ABCC1和ABCG2转运蛋白和治疗癌症，特别是抗药性癌症和高通量流式细胞术检测选择性抑制剂的化合物和方法

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摘要

Compounds disclosed which inhibit ABCBl transporter protein are useful for treating diseases in which ABCBl transporter protein mediates the disease state, including numerous cancers, including hematopoietic cancers, including various leukemias, especially T-lineage acute lymphoblastic leukemia, as well as cancerous tumors, especially forms which exhibit multiple drug resistance. Pharmaceutical compositions which comprise an inhibitor of ABCBl transporter protein and at least one additional anticancer agent, optionally in combination with a pharmaceutically acceptable carrier, additive or excipient are another aspect of the present invention. A flow cytometry based, high-throughput screening (HST) assay that quantifies ABCBl efflux is also disclosed. Methods of identifying inhibitors of ABCBl, ABCG2 and ABCCl transporter proteins are also disclosed.
机译：公开的抑制ABCB1转运蛋白的化合物可用于治疗其中ABCB1转运蛋白介导疾病状态的疾病，包括多种癌症，包括造血系统癌症，包括各种白血病，尤其是T谱系急性淋巴细胞白血病，以及癌性肿瘤，特别是形式表现出多重耐药性。本发明的另一方面是包含ABCB1转运蛋白抑制剂和至少一种另外的抗癌剂，任选地与药学上可接受的载体，添加剂或赋形剂组合的药物组合物。还公开了基于流式细胞术的高通量筛选（HST）测定，其定量ABCB1流出。还公开了鉴定ABCB1，ABCG2和ABCC1转运蛋白的抑制剂的方法。

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