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 |
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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 |
Externally published | Yes |
Keywords
- 17β-estradiol
- BCRP
- Estrone
- MDR
- Reversal of drug resistance
ASJC Scopus subject areas
- Oncology
- Cancer Research