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  • 标题:Estrogen Receptor-Mediated Transcriptional Activation by 17β-Estradiol and Its Analogs
  • 本地全文:下载
  • 作者:Taiko ODA ; Terumasa TSUCHIYA ; Yoshihiro SATO
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1996
  • 卷号:19
  • 期号:8
  • 页码:1018-1022
  • DOI:10.1248/bpb.19.1018
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要: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.
  • 关键词:estrogen;diethylstilbestrol;estrogen receptor;MCF-7 cell;signal transduction
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