The DOI matches its Crossref record; 21 of the 21 references it cites were found in a registry or an index.
Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump
Open accessAbstract
Imatinib mesylate (STI571), a potent tyrosine kinase inhibitor, is successfully used in the treatment of chronic myelogenous leukemia and gastrointestinal stromal tumors. However, the intended chronic oral administration of imatinib may lead to development of cellular resistance and subsequent treatment failure. Indeed, several molecular mechanisms leading to imatinib resistance have already been reported, including overexpression of the MDR1/ABCB1 drug pump. We examined whether imatinib is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump that is frequently overexpressed in human tumors. Using a panel of well-defined BCRP-overexpressing cell lines, we provide the first evidence that imatinib is a substrate for BCRP, that it competes with mitoxantrone for drug export, and that BCRP-mediated efflux can be reversed by the fumitremorgin C analog Ko-143. Since BCRP is highly expressed in the gastrointestinal tract, BCRP might not only play a role in cellular resistance of tumor cells but also influence the gastrointestinal absorption of imatinib.
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Cites
Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors
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Multidrug resistance mediated by the breast cancer resistance protein BCRP (ABCG2)
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MDR1 gene overexpression confers resistance to imatinib mesylate in leukemia cell line models
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Molecular mechanisms of resistance to imatinib in Philadelphia-chromosome-positive leukaemias
Gambacorti-Passerini, C. B., Gunby, R. H., Piazza, R., Galietta, A., Rostagno, R., & Scapozza, L. (2003) · The Lancet Oncology · doi:10.1016/s1470-2045(03)00979-3 · Cited by 373
Mutations at amino-acid 482 in the ABCG2 gene affect substrate and antagonist specificity
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Cited by
Tumour stem cells and drug resistance
Dean, M., Fojo, T., & Bates, S. (2005) · Nature reviews. Cancer · doi:10.1038/nrc1590 · Cited by 3,668
Corbin, A. S., Agarwal, A., Loriaux, M., Cortes, J., Deininger, M. W., & Druker, B. J. (2011) · Journal of Clinical Investigation · doi:10.1172/jci35721 · Cited by 765
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Park, T.-E., Mustafaoglu, N., Herland, A., Hasselkus, R., Mannix, R., FitzGerald, E. A., Prantil-Baun, R., Watters, A., Henry, O., Benz, M., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-10588-0 · Cited by 594
Metadata
- Authors
- Burger, H., van Tol, H., Boersma, A. W. M., Brok, M., Wiemer, E. A. C., Stoter, G., & Nooter, K.
- Venue
- Blood
- Publisher
- American Society of Hematology
- Published
- 2004-11-01
- Volume
- 104
- Issue
- 9
- Pages
- 2940-2942
- ISSN
- 0006-4971 (ISSN-L)
- 1528-0020
- OpenAlex
- W2129342281
- Cited by
- 417
- References
- 21
- FWCI
- 12.78
- Type
- journal article
- Language
- en
- Open access
- bronze
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- CoChat. (2026). Citation check: Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. https://app.cochat.ai/papers/10.1182/blood-2004-04-1398
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- Burger, H., van Tol, H., Boersma, A. W. M., Brok, M., Wiemer, E. A. C., Stoter, G., & Nooter, K. (2004). Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. https://doi.org/10.1182/blood-2004-04-1398
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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