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 journalArticle

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 languageEnglish
Pages (from-to)231-235
Number of pages5
JournalJapanese Journal of Cancer Research
Volume93
Issue number3
DOIs
Publication statusPublished - 2002

Keywords

  • 17β-estradiol
  • BCRP
  • Estrone
  • MDR
  • Reversal of drug resistance

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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