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The anti-estrogen hydroxytamoxifen is a potent antagonist in a novel yeast system

Jeannin, Elisabeth
Published in Biological Chemistry. 1999, vol. 380, no. 11, p. 1341-5
Abstract The budding yeast Saccharomyces cerevisiae has been used extensively as a biological 'test tube' to study the regulation of the human estrogen receptor (ER) alpha. However, anti-estrogens, which are of great importance as therapeutic agents and research tools, fail to antagonize the activation by estrogen in yeast. Here, we have surveyed the antagonistic potential of five different anti-estrogens of diverse chemical nature. While they all act as agonists for wild-type ERalpha, we have established a novel yeast assay system for anti-estrogens, in which at least the commonly used anti-estrogen hydroxytamoxifen is a potent antagonist.
Keywords Dose-Response Relationship, DrugDrug Evaluation, Preclinical/methodsEstradiol/analogs & derivatives/pharmacologyEstrogen Antagonists/chemistry/pharmacologyEstrogen Receptor alphaHumansIndoles/pharmacologyNafoxidine/chemistry/pharmacologyPiperidines/chemistry/pharmacologyPolyunsaturated AlkamidesReceptors, Estrogen/agonists/genetics/metabolismSaccharomyces cerevisiae/geneticsSulfones/pharmacologyTamoxifen/analogs & derivatives/chemistry/pharmacologyTwo-Hybrid System Techniques
PMID: 10614829
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LIU, Jia Wei, JEANNIN, Elisabeth, PICARD, Didier. The anti-estrogen hydroxytamoxifen is a potent antagonist in a novel yeast system. In: Biological Chemistry, 1999, vol. 380, n° 11, p. 1341-5. doi: 10.1515/BC.1999.172 https://archive-ouverte.unige.ch/unige:4632

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Deposited on : 2009-12-08

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