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. 2005 Feb 9;127(5):1382-3.
doi: 10.1021/ja0432618.

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

Wee Han Ang  1 , Isam Khalaila, Claire S Allardyce, Lucienne Juillerat-Jeanneret, Paul J Dyson
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Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance

Wee Han Ang et al. J Am Chem Soc. .

Abstract

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.

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