Tamoxifen is a treatment for breast cancer patients which can cause side effects of endometrial because it acts as GPER1 agonist. Active compounds from Schleichera oleosa are known to have anticancer potential, such schleicheol and schleicherastatin, especially their ability prevent cell proliferation. This research conducted an in silico study determine the potential active compound S. Oleosa ...

Early events in the action of 17-beta-estradiol can be studied in soluble extracts of rat uterus by exposure of the estradiol-receptor protein to a DNA-cellulose matrix. After complexing with [(3)H]estradiol, the 4S receptor protein binds to the DNA, and it can be eluted with buffer of high ionic strength as a more tightly binding, 5S form. This parallels the in vivo situation, where migration ...

The effect of tamoxifen (TAM) on human endometrial carcinoma was investigated in nude mice bearing an estrogen receptor-positive or estrogen receptor-negative tumor. The receptor-negative tumor grew rapidly, and the rates of tumor growth of 17 beta-estradiol or TAM-treated animals were identical to the rate of controls. The estradiol receptor and progesterone receptor (PR) concentrations in the...

A major problem with current anti-depressant therapy is that it takes on average 6-7 weeks for remission. Since desensitization of serotonin (5-HT)1A receptor signaling contributes to the anti-depressive response, acceleration of the desensitization may reduce this delay in response to antidepressants. The purpose of the present study was to test the hypothesis that estradiol accelerates fluoxe...

During the past ten years much information has been accumulated concerning the interaction of tritiated estrogens with hormone-dependent tissues. Their striking affinity for estradiol, both in vivol-5 and in vitro,6-9 first suggested that such target tissues as uterus, vagina, and anterior pituitary possess unique components called "estrogen receptors." Strong but reversible association of horm...

Reduced nitric oxide synthesis by glomerular endothelial cells and increased proliferation of glomerular mesangial cells is associated with glomerular remodeling that leads to accelerated glomerulosclerosis. Estradiol induces nitric oxide synthesis and slows the progression of renal disease. Because the estradiol metabolites 2-hydroxyestradiol and 2-methoxyestradiol are more potent than estradi...

We used three yeast genetic systems to investigate the estrogen-like activity of octylphenol (OP), bisphenol-A (BPA), o,p'-DDT, and o, p'-DDE to induce human estrogen receptor (hER) dimerization and transcriptional activation. We have demonstrated that OP, BPA, and o, p'-DDT can induce hER ligand-dependent dimerization using a yeast two-hybrid assay. All three xenoestrogens, plus estradiol, enh...

Rapid non-genomic effects of 17β-estradiol are elicited by the activation of different estrogen receptor-α isoforms. Presence of surface binding sites for estrogen have been identified in cells transfected with full-length estrogen receptor-α66 (ER66) and the truncated isoforms, estrogen receptor-α46 (ER46) and estrogen receptor-α36 (ER36). However, the binding affinities of the membrane estrog...

OBJECTIVES: Polycystic ovary syndrome is a heterogeneous endocrine disorder that affects reproductive-age women. The mechanisms underlying the endocrine heterogeneity and neuroendocrinology of polycystic ovary syndrome are still unclear. In this study, we investigated the expression of the kisspeptin system and gonadotropin-releasing hormone pulse regulators in the hypothalamus as well as facto...

Steroid hormones, especially estradiol, facilitate reproductive behaviors in male and female rodents and birds. In green anole lizards estradiol facilitates receptivity in females but, unlike in some other species, is not the activating hormone for courtship and copulatory behavior in males. Instead, testicular androgens directly facilitate male courtship and copulation. Yet, activity of the es...