An Affinity Labeling of Estrogen Receptor. II. Synthesis and Biological Activity of 3-Hydroxy-17β- (p-nitrophenyldithio) -1,3,5 (10) -estratriene

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概要

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• 3-Hydroxy-17β-(p-nitrophenyldithio)-1,3,5(10)-estratriene (Reagent A), an affinity labeling reagent for estrogen receptor, was prepared by iodine oxidation of an alkaline mixture of 3-hydroxy-1,3,5(10)-estratriene-17β-thiol and p-nitrothiophenol in 50% ethanol, and was isolated in a pure state. The structure was confirmed by the physical as well as spectral properties. The biological activity of the compound was tested by the measurement of the effects of ^3H-thymidine incorporation into deoxyribonucleic acid (DNA) and on ^<14>C-uridine incorporation into ribonucleic acid (RNA) in a human breast cancer cell line, MCF-7. There were increases of about 2-fold in thymidine incorporation and of about 1.1- to 2-fold in uridine incorporation in cells in-cubated in 10^<-7>M Reagent A compared with the control.

• 公益社団法人日本薬学会の論文
• 1983-10-25

著者

• 池田 充典

  川崎医科大学生化学1

• 池田 充典

  Department of Biochemistry, Kawasaki Medical School

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• The Effects of Estrogen and Antiestrogen on Chromatin in Human Breast Cancer Cell Line, MCF-7. I
• An Affinity Labeling of Estrogen Receptor. II. Synthesis and Biological Activity of 3-Hydroxy-17β- (p-nitrophenyldithio) -1,3,5 (10) -estratriene

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