EVIDENCE IN SUPPORT OF THE PLASMA-MEMBRANE AS THE TARGET FOR TRANSFERRIN-ADRIAMYCIN CONJUGATES IN K562 CELLS
EVIDENCE IN SUPPORT OF THE PLASMA-MEMBRANE AS THE TARGET FOR TRANSFERRIN-ADRIAMYCIN CONJUGATES IN K562 CELLS
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DOI：
10.1111/j.1600-0897.1991.tb01078.x
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发表时间：
1991-04-01
影响因子：
3.6
通讯作者：
FAULK, WP
中科院分区：
文献类型：
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作者：
BARABAS, K;SIZENSKY, JA;FAULK, WP
我们已经使用转铁蛋白-阿霉素缀合物将药物递送至转铁蛋白受体，并且已经显示缀合物在体内和体外结合并杀死肿瘤细胞。 这已经研究了使用定性和定量测定。 在这份报告中，我们提出的证据表明，转铁蛋白阿霉素细胞毒性的主要目标是质膜。 这是使用荧光分光光度法，利用阿霉素的荧光特性。 结果表明，虽然DNA嵌入可能是游离阿霉素细胞毒性的主要机制，但未观察到转铁蛋白-阿霉素缀合物与核DNA相互作用。 这可能是一个有用的考虑，在未来的化疗研究设计与转铁蛋白共轭物的抗癌药物。
We have used transferrin-adriamycin conjugates to deliver drug to transferrin receptors and have shown that the conjugates bind to and kill tumor cells in vivo and in vitro. This has been studied with the use of qualitative and quantitative assays. In this report, we present evidence indicating that the primary target of transferrin-adriamycin cytotoxicity is the plasma membrane. This was done using a spectrofluorometric method that takes advantage of the fluorescence properties of adriamycin. It was shown that, while DNA intercalation may be the primary mechanism of cytotoxicity for free adriamycin, transferrin-adriamycin conjugates were not observed to interact with nuclear DNA. This may be a useful consideration in the design of future chemotherapeutic studies with transferrin conjugates of anticancer drugs.