The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
ABCG2 overexpression in colon cancer cells resistant to SN38 and in irinotecan‐treated metastases
Open accessAbstract
Overcoming drug resistance has become an important issue in cancer chemotherapy. Among all known mechanisms that confer resistance, active efflux of chemotherapeutic agents by proteins from the ATP‐binding cassette family has been extensively reported. The aim of the present study was to determine the involvement of ABCG2 in resistance to SN38 (the active metabolite of irinotecan) in colorectal cancer. By progressive exposure to increasing concentrations of SN38, we isolated 2 resistant clones from the human colon carcinoma cell line HCT116. These clones were 6‐ and 53‐fold more resistant to SN38 than the HCT116‐derived sensitive clone. Topoisomerase I expression was unchanged in our resistant variants. The highest resistance level correlated with an ABCG2 amplification. This overexpression was associated with a marked decrease in the intracellular accumulation of SN38. The inhibition of ABCG2 function by Ko143 demonstrated that enhanced drug efflux from resistant cells was mediated by the activity of ABCG2 protein and confirmed that ABCG2 is directly involved in acquired resistance to SN38. Furthermore, we show, for the first time in clinical samples, that the ABCG2 mRNA content in hepatic metastases is higher after an irinotecan‐based chemotherapy than in irinotecan‐naive metastases. In conclusion, this study supports the potential involvement of ABCG2 in the development of irinotecan resistance in vivo. © 2004 Wiley‐Liss, Inc.
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Cites
Multidrug resistance in cancer: role of ATP–dependent transporters
Gottesman, M. M., Fojo, T., & Bates, S. E. (2002) · Nature Reviews Cancer · doi:10.1038/nrc706 · Cited by 5,536
Overexpression of a Transporter Gene in a Multidrug-Resistant Human Lung Cancer Cell Line
Cole, S. P. C., Bhardwaj, G., Gerlach, J. H., Mackie, J. E., Grant, C. E., Almquist, K. C., Stewart, A. J., Kurz, E. U., Duncan, A. M. V., & Deeley, R. G. (1992) · Science · doi:10.1126/science.1360704 · Cited by 3,037
Cited by
Role of the breast cancer resistance protein (ABCG2) in drug transport
Mao, Q. (2005) · The AAPS Journal · doi:10.1208/aapsj070112 · Cited by 405
ABCG2 transports anticancer drugs via a closed-to-open switch
Orlando, B. J., & Liao, M. (2020) · Nature Communications · doi:10.1038/s41467-020-16155-2 · Cited by 198
To, K. K. W., Leung, W. W., & Ng, S. S. M. (2015) · Experimental Cell Research · doi:10.1016/j.yexcr.2015.09.011 · Cited by 99
Metabolism of KO143, an ABCG2 inhibitor
Liu, K., Zhu, J., Huang, Y., Li, C., Lu, J., Sachar, M., Li, S., & Ma, X. (2017) · Drug Metabolism and Pharmacokinetics · doi:10.1016/j.dmpk.2017.02.003 · Cited by 39
Liu, X., Gündel, B., Li, X., Liu, J., Wright, A., Löhr, M., Arvidsson, G., & Heuchel, R. (2021) · Translational Oncology · doi:10.1016/j.tranon.2021.101107 · Cited by 24
Metadata
- Authors
- Candeil, L., Gourdier, I., Peyron, D., Vezzio, N., Copois, V., Bibeau, F., Orsetti, B., Scheffer, G. L., Ychou, M., Khan, Q. A., Pommier, Y., Pau, B., Martineau, P., & Del Rio, M.
- Venue
- International Journal of Cancer
- Publisher
- Wiley
- Published
- 2004-02-03
- Volume
- 109
- Issue
- 6
- Pages
- 848-854
- ISSN
- 0020-7136 (ISSN-L)
- 1097-0215
- OpenAlex
- W2036172570
- Cited by
- 180
- References
- 2
- FWCI
- 2.79
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Candeil, L., Gourdier, I., Peyron, D., Vezzio, N., Copois, V., Bibeau, F., Orsetti, B., Scheffer, G. L., Ychou, M., Khan, Q. A., Pommier, Y., Pau, B., Martineau, P., & Del Rio, M. (2004). ABCG2 overexpression in colon cancer cells resistant to SN38 and in irinotecan‐treated metastases. International Journal of Cancer. https://doi.org/10.1002/ijc.20032
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