Phytoestrogens are estrogen-like compounds of plant origin. The pharmacological activities of phytoestrogens are predominantly due to their antioxidant, anti-inflammatory and lipid-lowering properties, which are mediated via the estrogen receptors (ERs): estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) and possibly G protein-coupled estrogen receptor 1 (GPER). Gypenoside XVII (GP-...

ERα LBD structures may explain instability in the absence of ligand or with specific ligands 1,2,7,9. Nettles et al. 5 address this instability through use of a specific point mutation, Y537S, which stabilizes H12 in an agonist con-formation and is shown to overcome misfold-ing of the apo-ERα LBD. One might predict that stabilizing H12 on top of the ligand binding cavity with the Y537S mutation...

While the clinical benefit of MEK inhibitor (MEKi)-based therapy is well established in Raf mutant malignancies, its utility as a suppressor of hyperactive MAPK signaling in the absence of mutated Raf or Ras, is an area of ongoing research. MAPK activation is associated with loss of ERα expression and hormonal resistance in numerous malignancies. Herein, we demonstrate that MEKi induces a feedb...

Zearalenone (ZEA), a mycotoxin produced in the genus Fusarium, binds to estrogen receptors (ER) and is therefore regarded as an endocrine disruptor. ZEA has also been found to modulate the proliferation and apoptosis of prostate cancer cells in a dose-dependent manner. This study evaluates whether the effect of a low dose of ZEA (0.1 and 0.001 nM) on the invasion and migration of prostate cance...

Sex differences exist in the activation of the hypothalamic-pituitary-adrenal axis following exposure to stress, and the stress response is further affected by aging. This study was conducted to elucidate the mechanism of hypophagia in aged female mice exposed to stress. Immediately after a stress load, aged female mice exhibited acute hypophagia and a rise in plasma corticosterone levels. The ...

Objective: To detect the effects of 17β-estradiol (E2) on the expression of calbindin-D9k (CaBP-9k) in pituitary GH3 cells, and to determine the antagonistic effect of a selective estrogen receptor (ER) antagonist (ICI 182 780) on CaBP-9k expression. Methods: A rat pituitary prolactinoma cell line (GH3 cells) was used in an in vitro model. The localization of CaBP-9k in GH3 cells was observed b...

Our laboratory has demonstrated that 17β-estradiol (E2) enhances hippocampal memory consolidation via rapid activation of multiple intracellular signaling cascades, including the ERK/MAPK cascade (Fernandez et al., 2008; Fan et al., 2010). However, the receptor mechanisms responsible for these effects of E2 remain unclear. In vitro, estrogen receptor α (ERα) signaling through metabotropic gluta...

Male rat sexual behavior requires aromatization of testosterone (T) to estradiol (E2) in the medial preoptic area (MPO) where estrogen receptors (ER) exist in two isoforms, ERα and ERβ. We hypothesized that E2 acts through estrogen receptor α (ERα) in the MPO to promote male mating behavior. Four groups of male rats were castrated, administered DHT s.c. and bilateral MPO implants delivering eit...

Ferutinin is a daucane sesquiterpene with a high estrogenic activity in vitro and in vivo (Appendino et al., 2002; Zavatti et al., 2009). Recently, we demonstrated that ferutinin is able to enhance proliferation and osteogenic differentiation of human amniotic fluid stem cells (AFSCs) (Zavatti et al., 2013). Morover, the oral administration in rats of this phytoestrogen improved the bone regene...

BACKGROUND Liver Receptor Homolog 1 (LRH-1, NR5A2) is an orphan nuclear receptor that is over-expressed in cancers in tissues such as the breast, colon and pancreas. LRH-1 plays important roles in embryonic development, steroidogenesis and cholesterol homeostasis. In tumor cells, LRH-1 induces proliferation and cell cycle progression. High LRH-1 expression is demonstrated in breast cancers, pos...