Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance

被引:289
作者
Ang, WH
Khalaila, I
Allardyce, CS
Juillerat-Jeanneret, L
Dyson, PJ [1 ]
机构
[1] Ecole Polytech Fed Lausanne, BCH, Inst Sci & Ingn Chim, CH-1015 Lausanne, Switzerland
[2] Univ Lausanne, CHU Vaudois, Inst Pathol, CH-1011 Lausanne, Switzerland
关键词
D O I
10.1021/ja0432618
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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. Copyright © 2005 American Chemical Society.
引用
收藏
页码:1382 / 1383
页数:2
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