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Estradienolone (also referred to as estradiol dienolone) is a novel endogenous 19-nor steroid hormone identified in pregnant women. It is an isomer of estradiol that acts as a natural inverse agonist of the estrogen-related receptors alpha (ERRα) and gamma (ERRγ), directly interacting with these receptors to inhibit their transcriptional activity. Estradienolone has demonstrated strong anti-mitogenic properties, inhibiting the growth of both estrogen receptor-positive and estrogen receptor-negative breast cancer cells in a dose-dependent manner while showing minimal effect on normal epithelial breast cells. It also binds with high affinity to the progesterone receptor and sex hormone-binding globulin (SHBG). The compound is being investigated by researchers at McGill University and the University of Montreal as a potential therapeutic strategy for breast cancer.
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