Cytosol estrogen

Estradiol. The first neuroactive steroid receptor type to be recognized was that for estradiol [3]. In vivo uptake of [3H] estradiol, and binding to cell nuclei isolated from hypothalamus, pituitary and other brain regions, revealed steroid specificity closely resembling that of the uterus, where steroid receptors were first discovered [3]. Cytosolic estrogen receptors isolated from pituitary and brain tissue closely resemble those found in uterus and mammary tissue. A hallmark of the estrogen receptor is its existence... 

Thorpe SM. Immunological quantitation of nuclear receptors in human breast cancer Relation to cytosolic estrogen and progesterone receptors. Cancer Res 1987 47(7) 1830-1835. 

L5. Loven, D., Rakowsky, E., Geier, A., Lunenfeld, B., Rubinstein, A., Klein, B., and Lurie, H., A clinical evaluation of nuclear estrogen receptors combined with cytosolic estrogen and progesterone receptors in breast cancer. Cancer (Philadelphia) 66, 341-346 (1990). 

WS-7528 [132147-69-4][VI] a nonsteroidal estrogen, is an isoflavone which has been isolated from Streptomjces sp. No. 7528 and is an estrogen agonist. It inhibits [3ff]-estradiol binding to its receptor in rat uterine cytosol at an inhibitor for 50% of the rats tested (IC q) concentration of 5.7 nM. It also induces the growth of estrogen-dependent human breast cancer cell line MCE-7 (7). 

In vivo studies in animals suggest that endosulfan may disrupt normal reproductive hormone levels in male animals, but that it is not an endocrine disrupter in females. Persistent depressed testicular testosterone was seen in male rats after intermediate duration oral exposures to endosulfan. In ovariectomized female rats, orally administered endosulfan did not induce normal development of female reproductive tissues, and in female mice and immature female rats, acute parenteral exposure to endosulfan did not affect several endocrine-related end points. In vitro studies have evaluated endosulfan for estrogen receptor (ER) and cytosolic protein binding affinity, ER-mediated reporter gene expression, estrogenic induction of cell proliferation, and alteration of relative abundance of active estradiol metabolites. Overall, in vitro evidence in favor of endosulfan estrogenicity indicates relatively weak potency compared to 17[3-estradiol. Apparently contradictory results were reported in different... 

Navarro D, Ledn L, Chirino R, Fernandez L, Pestano J, Dlaz-Chico BN (1998) The two native estrogen receptor forms of 8S and 4S present in cytosol from human uterine tissues display opposite reactivity with tamoxifen aziridine and the estrogen response element. J Steroid Biochem Mol Biol 64 49... 

Nadal A, Diaz M, Valverde MA (2001) The estrogen trinity membrane, cytosolic, and nuclear effects. News Physiol Sci 16 251-255... 

Meyers CY, Kolb VM, Gass GH, et al. 1988. Doisynolic-type acids - uterotropically potent estrogens which compete poorly with estradiol for cytosolic estradiol receptors. J Steroid Biochem 31 (4A) 393-404. 

Androgens and estrogens are, respectively, male and female sex hormones. They act through cytosolic receptors that, when activated, migrate to the nucleus and influence gene expression. 

Rat uterine cytosol or alpha isoform of the human recombinant estrogen receptor... 

In in vitro studies, weak estrogenic effects of bisphenol A were found in cell line MCF7, which was established from human breast cancer cells, and in studies with cytosol preparations from isolated uteri. InMCF7 cells, the estrogenic effects were seen at 1-5 ng/ml and were manifested as in increase in cell proliferation and the induction of progesterone receptors. Bisphenol A was 1000-5000 times less potent than estradiol-17. 

Nagai, M., Conney, A.H., and Zhu, B.T., Strong inhibitory effects of common tea catechins and bioflavonoids on the O-methylation of catechol estrogens catalyzed by human Ever cytosolic catechol-O-methyltransferase, Drug Metab. Dispos., 32,497, 2004. 

Investigations into the mechanism of CDD-induced decreased fertility revealed blocked estrous cycle in female mice exposed orally to 2,3,7,8-TCDD for an intermediate duration (Umbreit et al. 1987) and dose-dependent decreases in uterine and hepatic cytosolic, and nuclear estrogen and progesterone receptor levels in rats after intraperitoneal 2,3,7,8-TCDD injection (Romkes and Safe 1988). Furthermore,... 

Small lipophilic (lipid-soluble) hormones diffuse across the plasma membrane and then interact with intracellular receptors in the cytosol or nucleus. The resulting hormone-receptor complex often binds to regions of the DNA and affects the transcription of certain genes (see Topic G7). Small lipophilic hormones with intracellular receptors include the steroid hormones which are synthesized from cholesterol (see Topic K5) (e.g. the female sex hormones estrogen and progesterone), thyroxine which is produced by thyroid cells and is the principal iodinated compound in animals, retinoic acid which is derived from vitamin A, and vitamin D which is synthesized in the skin in response to sunlight (see Topic K5). 

The estrogen receptor affinity of EM-652, the active drug of EM-800, was first measured in human breast cancer and normal human uterine cytosol (Asselin et al., 1980). As measured by competition studies in human breast cancer tissue, the affinity of EM-652 (Aj = 0.047 0.003 nM, RBA = 291, relative to 17p -estradiol set at 100), studied in the presence of... 

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