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Nat Rev Cancer. 2003 May;3(5):330-8.

5-fluorouracil: mechanisms of action and clinical strategies.

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Cancer Research Centre, Department of Oncology, Queen's University Belfast, University Floor, Belfast City Hospital, 97 Lisburn Road, Belfast BT9 7AB, Northern Ireland.


5-fluorouracil (5-FU) is widely used in the treatment of cancer. Over the past 20 years, increased understanding of the mechanism of action of 5-FU has led to the development of strategies that increase its anticancer activity. Despite these advances, drug resistance remains a significant limitation to the clinical use of 5-FU. Emerging technologies, such as DNA microarray profiling, have the potential to identify novel genes that are involved in mediating resistance to 5-FU. Such target genes might prove to be therapeutically valuable as new targets for chemotherapy, or as predictive biomarkers of response to 5-FU-based chemotherapy.

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