Article
Transporter-mediated protection against thiopurine-induced hematopoietic toxicity.
Cancer research - 1 Jul 2008
Krishnamurthy Partha, Schwab Matthias, Takenaka Kazumasa, Nachagari Deepa, Morgan Jessica, Leslie Mark, Du Weinan, Boyd Kelli, Cheok Meyling, Nakauchi Hiromitsu, Marzolini Catia, Kim Richard B, Poonkuzhali Balasubramanian, Schuetz Erin, Evans William, Relling Mary, Schuetz John D
Abstract excerpt
Thiopurines are effective immunosuppressants and anticancer agents, but intracellular accumulation of their active metabolites (6-thioguanine nucleotides, 6-TGN) causes dose-limiting hematopoietic toxicity. Thiopurine S-methyltransferase deficiency is known to exacerbate thiopurine toxicity. However, many patients are highly sensitive to thiopurines for unknown reasons. We show that multidrug-resistance protein 4...
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