Imatinib-resistant CML cells have low ENT activity but maintain sensitivity to gemcitabine
Imatinib-resistant CML cells have low ENT activity but maintain sensitivity to gemcitabine
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DOI：
10.1080/15257770802145892
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发表时间：
2008-01-01
影响因子：
1.3
通讯作者：
Graves, Lee M.
中科院分区：
文献类型：
--
作者：
Leisewitz, Andrea V.;Zimmerman, Eric I.;Graves, Lee M.
Philadelphia chromosome-positive chronic myelogenus leukemia (CML) is widely treated with imatinib mesylate (imatinib), a potent inhibitor of the Bcr-Abl tyrosine kinase. However, resistance to this compound remains a concern. Current treatment approaches include combinations of imatinib with nucleoside analogs such as gemcitabine, which requires equilibrative nucleoside transporters (ENTs) for uptake, to overcome this resistance. Here we report that imatinib treatment decreased ENT1-dependent activity and mRNA expression. Although, imatinib-resistant cells showed decreased levels of both ENT1 and ENT2 activity and expression, these cells remained sensitive to gemcitabine, suggesting that nucleoside analogs can be used as adjunctive therapy.
