Estrone and 17β-estradiol reverse breast cancer resistance protein-mediated multidrug resistance

Yasuo Imai; Satomi Tsukahara; Etsuko Ishikawa; Takashi Tsuruo; Yoshikazu Sugimoto

doi:10.1111/j.1349-7006.2002.tb02162.x

Estrone and 17β-estradiol reverse breast cancer resistance protein-mediated multidrug resistance

Yasuo Imai, Satomi Tsukahara, Etsuko Ishikawa, Takashi Tsuruo, Yoshikazu Sugimoto

Research output: Contribution to journal › Article › peer-review

83 Citations (Scopus)

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	https://doi.org/10.1111/j.1349-7006.2002.tb02162.x
Publication status	Published - 2002
Externally published	Yes

Keywords

17β-estradiol
BCRP
Estrone
MDR
Reversal of drug resistance

ASJC Scopus subject areas

Oncology
Cancer Research

UN SDGs

This output contributes to the following Sustainable Development Goal(s)

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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.",

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AU - Imai, Yasuo

AU - Tsukahara, Satomi

AU - Ishikawa, Etsuko

AU - Tsuruo, Takashi

AU - Sugimoto, Yoshikazu

PY - 2002

Y1 - 2002

N2 - 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.

AB - 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.

KW - 17β-estradiol

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KW - Estrone

KW - MDR

KW - Reversal of drug resistance

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Estrone and 17β-estradiol reverse breast cancer resistance protein-mediated multidrug resistance

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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