Ang Wee Han, Khalaila Isam, Allardyce Claire S, Juillerat-Jeanneret Lucienne, Dyson Paul J
Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne, EPFL-BCH, CH 1015 Lausanne, Switzerland.
J Am Chem Soc. 2005 Feb 9;127(5):1382-3. doi: 10.1021/ja0432618.
A rationally designed Pt(IV) anticancer compound is described, employing the novel concept of tethering an inhibitor of glutathione-S-transferase, an enzyme associated with Pt-based drug-resistance, to cisplatin. Its enzyme inhibition activity, investigated using spectrophotometric and mass spectrometry-based techniques, and cytotoxic profile in resistant cancer cells are described.
本文描述了一种合理设计的铂（IV）抗癌化合物，该化合物采用了一种新颖的概念，即将谷胱甘肽-S-转移酶（一种与铂类药物耐药性相关的酶）的抑制剂与顺铂连接起来。文中介绍了其通过分光光度法和基于质谱的技术研究的酶抑制活性，以及在耐药癌细胞中的细胞毒性情况。
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