Estrogen Receptor (ER) is an important target for pharmaceutical design. Like other ligand-dependent transcription factors, hormone binding regulates ER transcriptional activity. Nevertheless, the mechanisms by which ligands enter and leave ERs and other nuclear receptors remain poorly understood. Here, we report results of locally enhanced sampling molecular dynamics simulations to identify di...

background : this study evaluates estrogen and progesterone expressions in patients with ovarian tumors (both benign and malignant) and their correlation with various clinicopathological prognostic parameters. receptors for estrogen and progesterone are predictive and prognostic markers of endometrial and breast cancers. however, their clinical significance in epithelial ovarian cancer is not c...

Mice, rats, and humans have two types of estrogen receptors, estrogen receptor-alpha (ERalpha) and estrogen receptor-beta (ERbeta). Estrogen receptor-alpha gene-disrupted (ERalpha-disrupted) mice bear two nonfunctional copies of the ERalpha gene. This mutation blocks the synthesis of full-length ERalpha, renders the animals infertile, and inhibits the induction of female sexual behaviors by est...

Sex steroids negatively regulate B lymphopoiesis in adult mice. Paradoxically, lymphocytes arise during fetal life, when estrogen levels are high and maternal lymphopoiesis is suppressed. Here we demonstrate that embryonic B lymphopoiesis was unaffected by estrogen, but sensitive to glucocorticoids. Both fetal and adult precursors contained glucocorticoid receptor transcripts, but only adult pr...

Both cyclin D1 and estrogens have an essential role in regulating proliferation of breast epithelial cells. We show here a novel role for cyclin D1 in growth regulation of estrogen-responsive tissues by potentiating transcription of estrogen receptor-regulated genes. Cyclin D1 mediates this activation independent of complex formation to a CDK partner. Cyclin D1 activates estrogen receptor-media...

Estrogen receptors (ER) are known as nuclear receptors. They exist in the cytoplasm of human cells and serves as a DNA binding transcription factor that regulates gene expression. However the estrogen receptor also has additional functions independent of DNA binding. The human estrogen receptor comes in two forms, alpha and beta. This work focuses on the alpha form of the estrogen receptor. The...

Estrogen has been shown to increase endothelium-dependent vasodilation and expression of endothelial nitric oxide (NO) synthase (eNOS); however, the role of estrogen receptors in mediating estrogen effects on endothelial function remains to be elucidated. The purpose of this study was to test the hypothesis that estrogen modulates NO-dependent vasodilation of coronary arteries through its actio...

BACKGROUND AND OBJECTIVES: Nitric oxide (NO) is a potent vasodilator and estrogen-mediated vasodilation that increases NO production. The association of the vascular endothelium, gender and vasodilation induced by estrogen is due to the activation of two estrogen receptors, alpha (ERa) and beta (ERb). The aim of this study was to compare NO production stimulating receptors ERa and ERb with the ...

We developed a pharmacophore-based evolutionary approach for virtual screening. This tool, termed the Generic Evolutionary Method for molecular DOCKing (GEMDOCK), combines an evolutionary approach with a new pharmacophore-based scoring function. The former integrates discrete and continuous global search strategies with local search strategies to expedite convergence. The latter, integrating an...

The estrogen-induced hamster renal carcinoma contains appreciable amounts of all cytosolic steroid receptor classes sedimenting as 7 to 8S moieties following sucrose gradient centrifugation. Their relative concentrations, expressed in fmol/mg protein +/- S.E. are progesterone (1496 +/- 23) greater than estradiol (218 +/- 3) greater than 5 alpha-dihydrotestosterone (154 +/- 7) greater than dexam...