The anti-estrogen hydroxytamoxifen is a potent antagonist in a novel yeast system.
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.
Liu
J W
JW
Département de Biologie Cellulaire, Université de Genève, Sciences III, Switzerland.
Jeannin
E
E
Picard
D
D
D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004958:Estradiol / Q000031:analogs & derivatives / Q000494:pharmacology; D004965:Estrogen Antagonists / Q000737:chemistry / Q000494:pharmacology*; D047628:Estrogen Receptor alpha; D006801:Humans; D007211:Indoles / Q000494:pharmacology; D009256:Nafoxidine / Q000737:chemistry / Q000494:pharmacology; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology; D053284:Polyunsaturated Alkamides; D011960:Receptors, Estrogen / Q000819:agonists / Q000235:genetics / Q000378:metabolism; D012441:Saccharomyces cerevisiae / Q000235:genetics*; D013450:Sulfones / Q000494:pharmacology; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D020798:Two-Hybrid System Techniques
D004965:Estrogen Antagonists; D047628:Estrogen Receptor alpha; D007211:Indoles; D010880:Piperidines; D053284:Polyunsaturated Alkamides; D011960:Receptors, Estrogen; D013450:Sulfones; C403253:ZK 164015; D013629:Tamoxifen; C016601:afimoxifene; C012121:ritetronium; D009256:Nafoxidine; D004958:Estradiol; C051781:ICI 164384