Estrogen Receptor-Mediated Transcriptional Activation by 17β-Estradiol and Its Analogs
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概要
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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 (E_2), 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 E_2 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.
- 公益社団法人日本薬学会の論文
- 1996-08-15
著者
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SATO Yoshihiro
Kyoritsu College of Pharmacy
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Oda Taiko
Kyoritsu College Of Pharmacy
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TSUCHIYA Terumasa
Medical Research Institute, Tokyo Medical and Dental University
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YASUKOCHI Yukio
Medical Research Institute, Tokyo Medical and Dental University
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Tsuchiya Terumasa
東京医科歯科大学難治疾患研究所
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Yasukochi Y
Tokyo Medical And Dental Univ. Tokyo Jpn
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