Estrogen receptor-mediated transcriptional activation by 17β-estradiol and its analogs

Taiko Oda, Terumasa Tsuchiya, Yoshihiro Sato, Yukio Yasukochi

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4 Citations (Scopus)


We investigated the effects of natural and synthetic estrogens on estrogen receptor-mediated signal transduction and transcription. To assess estrogen receptor-dependent gene expression, we constructed a reporter plasmid that can express the luciferase gene under the control of the estrogen-responsive element. A transcriptional assay was performed by transfection of the reporter plasmid into estrogen-responsive MCF-7 cells. Transcription was completely dependent on the natural estrogen, 17β- estradiol (E2), in a dose-dependent manner. Retinoic acids and other steroid hormones had no effect on gene expression. The effect of synthetic estrogens on estrogen receptor-mediated signal transduction was also examined using the specific reporter assay system. A synthetic estrogen, diethylstilbestrol, exhibited higher activity than E2 at lower concentrations. In addition, transcriptional activities of the (+)- and (-)-enantiomers of indenestrol A, a metabolite of diethylstilbestrol, could be distinguished using the reporter assay system.

Original languageEnglish
Pages (from-to)1018-1022
Number of pages5
JournalBiological and Pharmaceutical Bulletin
Issue number8
Publication statusPublished - 1996 Aug



  • MCF-7 cell
  • diethylstilbestrol
  • estrogen
  • estrogen receptor
  • signal transduction

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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