Highly water-soluble platinum(II) complexes as GLUT substrates for targeted therapy: improved anticancer efficacy and transporter-mediated cytotoxic properties
Highly water-soluble platinum(II) complexes as GLUT substrates for targeted therapy: improved anticancer efficacy and transporter-mediated cytotoxic properties
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DOI：
10.1039/c3cc38589b
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发表时间：
2013-01-01
影响因子：
4.9
通讯作者：
Gao, Qingzhi
中科院分区：
文献类型：
--
作者：
Liu, Pengxing;Lu, Yanhui;Gao, Qingzhi
葡萄糖偶联丙二酸-铂（II）复合物的设计和合成针对肿瘤特异性活性转运蛋白，即葡萄糖转运蛋白（GLUTs）；与最新一代临床药物奥沙利铂相比，该复合物的水溶性提高了150倍，细胞毒性提高了10倍，治疗指数提高了30倍以上。
Glucose-conjugated malonato-platinum(II) complexes are designed and synthesized to target tumor-specific active transporters, namely, glucose transporters (GLUTs); the complexes exhibit much higher aqueous solubility by 150 times, improved potency in cytotoxicities by 10 times, and increased therapeutic index by over 30 fold compared to the newest generation of clinical drugs oxaliplatin.