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首页> 外文期刊>Anticancer Research: International Journal of Cancer Research and Treatment >Multidrug resistance-associated protein (MRP) mediated transport of daunomycin and leukotriene C4 (LTC4) in isolated plasma membrane vesicles.
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Multidrug resistance-associated protein (MRP) mediated transport of daunomycin and leukotriene C4 (LTC4) in isolated plasma membrane vesicles.

机译:多药耐药相关蛋白(MRP)介导的道诺霉素和白三烯C4(LTC4)在分离的质膜囊泡中的转运。

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摘要

Studies have been carried out to examine in vitro drug transport in plasma membrane vesicles isolated from HL60/ADR cells that overexpress MRP. The results demonstrate that glutathione (GSH) enhances transport of daunomycin. A greater increase in transport activity occurs when the reaction is carried out in the presence of both GSH and sodium chloride. Sodium chloride alone has no effect on daunomycin transport. It has also been observed that GSH in the presence of sodium chloride induces a major increase in the transport level of LTC4. Thus far, no metal ion other than sodium chloride has been found to be active in the drug transport system. Kinetic analysis reveals that GSH in the presence of sodium chloride greatly reduces Km and increases Vmax, for daunomycin. Additional studies show that ATPase activity in isolated plasma membrane from HL60/ADR cells is greatly enhanced in the presence of both GSH and sodium chloride. These results suggest the possibility that GSH and sodium chloride stimulate MRP-mediated transport as a result of increased ATPase activity.
机译:已经进行了研究以检查从过度表达MRP的HL60 / ADR细胞分离出的质膜囊泡中的体外药物转运。结果表明,谷胱甘肽(GSH)增强了道诺霉素的转运。当反应在GSH和氯化钠同时存在下进行时,运输活性会大大提高。单独的氯化钠对道诺霉素的运输没有影响。还已经观察到,在氯化钠存在下的GSH引起LTC4转运水平的大幅增加。迄今为止,没有发现除氯化钠以外的金属离子在药物转运系统中具有活性。动力学分析表明,对于道诺霉素,在氯化钠存在下的谷胱甘肽大大降低Km并增加Vmax。其他研究表明,在存在GSH和氯化钠的情况下,从HL60 / ADR细胞分离的质膜中的ATPase活性大大提高。这些结果表明,由于ATPase活性增加,GSH和氯化钠可能刺激MRP介导的转运。

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