Estrogen Receptor β-Selective Transcriptional Activity and Recruitment of Coregulators by Phytoestrogens

• DOI: 10.1074/jbc.m100953200
• Publication Date: 2002-07-26T15:09:24Z
• Authors: Jinping An; Christina Tzagara...; Tiffany C. Schars...; Noureddine Lomri; Dale C. Leitman
• Keywords: GPER; Estrogen receptor beta

Estrogens used in hormone replacement therapy regimens may increase the risk of developing breast cancer. Paradoxically, high consumption plant-derived phytoestrogens, particularly soybean isoflavones, is associated with a low incidence To explore molecular basis for these potential different clinical outcomes, we investigated whether isoflavones elicit distinct transcriptional actions from estrogens. Our results demonstrate that estrogen 17beta-estradiol effectively triggers activation and repression pathways both receptors (ERs) ERalpha ERbeta. In contrast, (genistein, daidzein, biochanin A) are ERbeta-selective agonists at physiological levels. The mechanism ERbeta selectivity by involves their capacity to create an function-2 surface has greater affinity coregulators than ERalpha. Phytoestrogens act as natural selective receptor modulators effects estrogens selectively recruiting coregulatory proteins trigger pathways.