Abstract
Breast cancer resistance protein (BCRP), an adenosine triphosphate-binding cassette transporter, confers resistance to a series of anticancer reagents, including mitoxantrone, SN-38 and topotecan. In the present study, we found that estrone and 17β-estradiol potentiated the cytotoxicity of mitoxantrone, SN-38 and topotecan in BCRP-transduced K562 cells (K562/BCRP). These estrogens showed only a marginal effect, or none, in parental K562 cells. Estrone and 17β-estradiol increased the cellular accumulation of topotecan in K562/BCRP cells, but not in K562 cells, suggesting that these estrogens inhibit the BCRP-mediated drug efflux and overcome drug resistance.
| Original language | English |
|---|---|
| Pages (from-to) | 231-235 |
| Number of pages | 5 |
| Journal | Japanese Journal of Cancer Research |
| Volume | 93 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - 2002 |
Keywords
- 17β-estradiol
- BCRP
- Estrone
- MDR
- Reversal of drug resistance
ASJC Scopus subject areas
- Oncology
- Cancer Research
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Cite this
Imai, Y., Tsukahara, S., Ishikawa, E., Tsuruo, T., & Sugimoto, Y. (2002). Estrone and 17β-estradiol reverse breast cancer resistance protein-mediated multidrug resistance. Japanese Journal of Cancer Research, 93(3), 231-235. https://doi.org/10.1111/j.1349-7006.2002.tb02162.x