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Cited by 417

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 access
Burger, Herman, van Tol, Hans, Boersma, Antonius W. M., Brok, Mariël, Wiemer, Erik A. C., Stoter, Gerrit, Nooter, Kees·2004·Blood

Abstract

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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Metadata

Authors
Burger, H., van Tol, H., Boersma, A. W. M., Brok, M., Wiemer, E. A. C., Stoter, G., & Nooter, K.
Venue
Blood
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
The paper
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).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.