The results presented here demonstrate that p53 upregulates estrogen receptor-alpha (ER alpha) expression in the human breast cancer cell line MCF-7. Two approaches were used to alter the activity of p53 in the cells. In the first approach, stable transfectants expressing an antisense p53 were established. In the stable clones, expression of antisense p53 resulted in a decrease in the expression of ER alpha protein. In the second approach, MCF-7 cells were transiently transfected with wild-type p53. Overexpression of p53 increased the amount of ER alpha. To determine whether the effects of p53 on the expression of ER alpha were due to changes in transcription, deletion mutants of the ER alpha promoter were used. This experimental approach demonstrated that p53 up-regulates ER alpha gene expression by increasing transcription of the gene through elements located upstream of promoter A. Transfection assays using p53 mutants further demonstrated that the p53-induced increase in ER alpha gene ...
Loss of estrogen receptor α (ERα) expression and gain of TWIST (TWIST1) expression in breast tumors correlate with increased disease recurrence and metastasis and poor disease-free s...
购买重组Estrogen Receptor alpha兔单克隆抗体[EPR703(2)](ab79413),Estrogen Receptor alpha抗体经WB,IHC-P验证,可与人,Baboon样本反应。7个独立用户反馈。
BACKGROUND: Estrogen acutely activates endothelial nitric oxide synthase (eNOS). However, the identity of the receptors involved in this rapid response remains unclear. METHODS AND RESULTS: We detected an estrogen receptor alpha (ERalpha) transcript in human endothelial cells that encodes a truncated 46-kDa ERalpha (Delta1a-hERalpha-46). A corresponding 46-kDa ERalpha protein was identified in endothelial cell lysates. Transfection of cDNAs encoding the full-length ERalpha (ERalpha-66) and Delta1a-hERalpha-46 resulted in appropriately sized recombinant proteins identified by anti-ERalpha antibodies. Confocal microscopy revealed that a proportion of both ERalpha-66 and hERalpha-46 was localized outside the nucleus and mediated specific cell-surface binding of estrogen as assessed by FITC-conjugated, BSA-estrogen binding studies. Both ERalpha isoforms colocalized with eNOS and mediated acute activation of eNOS in response to estrogen stimulation. However, estrogen-stimulated transcriptional activation
BACKGROUND: Estrogen acutely activates endothelial nitric oxide synthase (eNOS). However, the identity of the receptors involved in this rapid response remains unclear. METHODS AND RESULTS: We detected an estrogen receptor alpha (ERalpha) transcript in human endothelial cells that encodes a truncated 46-kDa ERalpha (Delta1a-hERalpha-46). A corresponding 46-kDa ERalpha protein was identified in endothelial cell lysates. Transfection of cDNAs encoding the full-length ERalpha (ERalpha-66) and Delta1a-hERalpha-46 resulted in appropriately sized recombinant proteins identified by anti-ERalpha antibodies. Confocal microscopy revealed that a proportion of both ERalpha-66 and hERalpha-46 was localized outside the nucleus and mediated specific cell-surface binding of estrogen as assessed by FITC-conjugated, BSA-estrogen binding studies. Both ERalpha isoforms colocalized with eNOS and mediated acute activation of eNOS in response to estrogen stimulation. However, estrogen-stimulated transcriptional activation
TY - JOUR. T1 - Estrogen receptor alpha signaling promotes Sle1-induced loss of tolerance and immune cell activation and is responsible for sex bias in B6.Sle1 congenic mice. AU - Yoachim, Shayla D. AU - Nuxoll, Jenny S.. AU - Bynoté, Kimberly K.. AU - Gould, Karen A. PY - 2015/6/1. Y1 - 2015/6/1. N2 - Sex bias in lupus incidence is thought to be due, in part, to the ability of estrogens to promote loss of tolerance. Previously, we showed that estrogens promote lupus via estrogen receptor α (ERα). C57BL/6 (B6) mice carrying the Sle1 lupus susceptibility locus (B6.Sle1) display loss of tolerance and develop anti-nuclear antibodies and immune cell hyperactivation. The incidence of loss of tolerance in B6.Sle1 females is greater than in males. Here, we show that a deficiency of either estrogens or ERα attenuates loss of tolerance and autoantibody development in B6.Sle1 females. Furthermore, we demonstrate that immune cell activation in B6.Sle1 mice shows sex bias and that ERα deficiency ...
Endocrine therapies focus on the service of the oestrogen receptor alpha dog (Emergency room) via distinct systems, but it all is not very clear whether breasts tumor cells may adapt to treatment using drug-specific systems. development. Finally, we demonstrate that a CB-based personal might become utilized to improve the stratification of Emergency room breast cancer individuals before adjuvant treatment. Outcomes Version to AI treatment qualified prospects to invasiveness ETs are designed to stop oestrogen-driven expansion by interfering with one particular TF (for example, Emergency room). Nevertheless, we hypothesized that the advancement of level of resistance may follow specific ways and generate alternate phenotypes through the different molecular systems particular to each agent2. To check this speculation, we utilized a series of isogenic cell lines resistant to solitary real estate agents or a mixture of real estate agents (endocrine therapy (ET)-resistant ETR cells, Fig. 1a)15. Our ...
Estrogen is essential for the development and maintenance of optimal bone mass in women and men, and acts through activation of estrogen receptors (ER). We have examined the pathways of estrogen action on the skeleton by seeking to localize the classical estrogen receptor, ER alpha, to particular cells to test the hypotheses that 1) estrogen directly influences growth plate chondrocytes; and 2) estrogen has a principal action on bone tissue via osteoblasts. ER alpha messenger ribonucleic acid (mRNA) was localized by in situ hybridization in human specimens from five males (11-15 yr old), two females (9 and 11 yr old), and three growing rabbits. In all of the human material examined, ER alpha mRNA was consistently identified in chondrocytes. In all of the rabbit tissue studied, ER alpha mRNA was localized in chondrocytes of the growth plate and the subarticular epiphyseal growth center. ER alpha mRNA signals were readily observed in both active osteoblasts and lining cells on trabecular surfaces of all
6HHP: Ternary complex of Estrogen Receptor alpha peptide and 14-3-3 sigma C42 mutant bound to disulfide fragment PPI stabilizer 1
Human estrogen receptor alpha (hERα) is a hormone-responsive nuclear receptor (NR) involved in cell growth and survival that contains both a DNA-binding domain (DBD) and a ligand-binding domain (LBD). Functionally relevant inter-domain interactions between the DBD and LBD have been observed in sever …
Background Breast cancer is currently classified in 3 groups based on estrogen receptor alpha (ER) and human epidermal growth factor receptor 2 (HER2/ERBB2) gene expression: one basal-like (ER-ERBB2-), one HER2−enriched (ERBB2+) and one luminal (ER+). Yet, in transcriptome-based classifications, ER-ERBB2+ group partially overlaps with more recently defined ER-AR+ (androgen receptor positive) group. This type was named molecular apocrine, in reference to the histopathologically characterized apocrine carcinomas (H-Apo), in which a marked activation of AR signaling was demonstrated with a distinct proteomic signature. H-Apo tumors correspond to 1% of invasive breast carcinomas and are clearly morphological distinct from other AR+ tumors. However, no specific H-Apo transcriptome signature has been reported for this sub-group. In an effort to better characterize those tumors, we have performed a meta-analysis of genomic data, focusing on the ER- AR+ breast subset.. Samples and Methods: Chips were ...
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Alternative splicing is critical for generating complex proteomes in response to extracellular signals. Nuclear receptors including estrogen receptor alpha (ERα) and their ligands promote alternative splicing. The endogenous targets of ERα:estradiol (E2)-mediated alternative splicing and the influence of extracellular kinases that phosphorylate ERα on E2-induced splicing are unknown. MCF-7 and its anti-estrogen derivatives were used for the majority of the assays. CD44 mini gene was used to measure the effect of E2 and AKT on alternative splicing. ExonHit array analysis was performed to identify E2 and AKT-regulated endogenous alternatively spliced apoptosis-related genes. Quantitative reverse transcription polymerase chain reaction was performed to verify alternative splicing. ERα binding to alternatively spliced genes was verified by chromatin immunoprecipitation assay. Bromodeoxyuridine incorporation-ELISA and Annexin V labeling assays were done to measure cell proliferation and apoptosis,
Phase 1 of the study will be conducted to determine the maximum tolerated dose (MTD) and/or the recommended Phase 2 dose (RP2D) of H3B-6545 in women with
Commander Estrogen Receptor alpha anticorps monoclonal et polyclonal pour beaucoup dapplications. Selection de fournisseur de qualité pour anti-Estrogen Receptor alpha anticorps.
Approximately 75% of breast cancers are estrogen receptor (ERα) positive, underscoring the dependence of cancer cells on estrogen for growth and survival. Patients treated with endocrine therapy often develop resistance, either de novo or acquired, which is caused by aberrations within the growth factor signaling pathways. The mechanistic target of rapamycin complex 1 (mTORC1) has emerged as a critical node in estrogenic signaling. We have previously shown that mTORC1 can phosphorylate and activate ERα on S167 via its effector the 40S ribosomal S6 kinase 1 (S6K1). Presently, we have uncovered a direct link between mTORC1 and ERα. We found that ERα binds to regulatory-associated protein of mTOR (Raptor) and causes it to translocate to the nucleus upon estrogen stimulation. Additionally, we identified mTOR as the kinase that directly phosphorylates ERα and activates transcription of ER target genes. Our findings show a direct link between mTORC1 and ERα, which further implicates mTORC1 ...
Rabbit polyclonal Estrogen Receptor alpha antibody validated for WB, IHC and tested in Human and Mouse. Immunogen corresponding to synthetic peptide
Rabbit recombinant monoclonal Estrogen Receptor alpha antibody [EPR703(2)] validated for WB, IHC and tested in Human and Bb. With 7 independent reviews.
Estrogen Receptor alpha兔多克隆抗体可与小鼠, 人样本反应并经WB, ELISA, IHC实验严格验证,被4篇文献引用并得到1个独立的用户反馈。
AS05 065 Aquaculture antibodies, antibodies to fish stress proteins, estrogen receptor, antibodies to estrogen receptor alpha and beta,PO3372, Q92731, nuclear receptor subfamily 3 group A member 2 antibody
Endocrine therapy is an effective option for the treatment of estrogen receptor alpha (ERα)-positive breast cancers. Unfortunately, a large fraction of women ...
Alonso A, Fernandez R, Ordanyonez P, Moreno M, Patterson buy cardarone safely online AM, et al. (2006) Regulation of estrogen receptor alpha past estradiol in buy generic cardarone pregnant and estradiol treated rats. Steroids. However, our information showed no interchange in buy generic cardarone GSK3 phosphorylation associated with decreased apartment viability induced at Akt2 and Akt3 disruption. Figure 1 Photochemistry parameters circumspect using the DualPAM. Immediately after the lay unrestricted pressed a button, the corresponding discs on the screen were switched to green (if dominates chose the right button, a hit) or to red (if fields chose a ended of the average button, an error). There was also a nonsignificant gain in amount survival (OS). For example, the examine showed that barely 83% of hospitals utilize automated dispensing cabinets as into a receive of their distribution model; 10% utilize robotic dispensing. The opportunity regions directorial conducive to largeness ...
Summary Two polymorphisms of the aromatase and estrogen receptor genes appeared to interact to influence the risk of hip fractures in women. Introduction Allelic variants of the aromatase gene have been associated with bone mineral density and vertebral fractures. Our objective was to analyze the relationship between two polymorphisms of the aromatase and estrogen receptor genes and hip ...
The transition to the postmenopausal stage is associated with an increased risk for vascular diseases, including myocardial infarction and stroke. This has been linked to a decrease in estrogen production. Estrogens mediate their effects on the brain to a major extent through binding to nuclear receptors, estrogen receptor alpha and beta. It is possible that positive and adverse effects of estrogens are related to interactions between receptor genotypes and hormones. Notably, the estrogen receptor alpha polymorphism c 454-397T/T is associated with increased risk of hemorrhagic stroke, with a synergistic relationship between this genotype and hypertension. In experimental stroke settings estrogens influence recovery of cognitive functions, possibly via induction of neurotrophic factors and specific transcription factors including NGFI-A. This may be related to increased neuroplasticity in the hippocampal formation, a key area for memory processing. Individualized treatment with estrogen receptor ...
TY - JOUR. T1 - Expression of estrogen receptor gene in mouse oocyte and during embryogenesis. AU - Wu, T. C J. AU - Wang, L.. AU - Wan, Yu-Jui Yvonne. PY - 1992. Y1 - 1992. N2 - Estrogen is required for oocyte maturation and embryonic development in vivo; however, the mechanism involved is not clear. Since the effect of estrogen is mediated through the estrogen receptor (ER), we examined the ontogeny and expression of the ER gene in mouse oocytes and embryos of various gestational stages using the highly sensitive reverse transcriptase- polymerase chain reaction (RT-PCR) technique. Total RNA, extracted from 40 ovulated oocytes, 2-cell embryos, morulae, and blastocysts, was reverse transcribed into cDNA. A pair of primers flanking the 453-bp region encoding the hormone-binding domain of ER was used for 30 cycles of PCR. The identity of the amplified product was confirmed by sizing and Southern blot hybridization. The results indicated that ER gene is expressed in unfertilized oocytes and ...
TY - JOUR. T1 - Novel estrogen receptor ligands based on an anthranylaldoxime structure. T2 - Role of the phenol-type pseudocycle in the binding process. AU - Minutolo, Filippo. AU - Antonello, Michela. AU - Bertini, Simone. AU - Ortore, Gabriella. AU - Placanica, Giorgio. AU - Rapposelli, Simona. AU - Sheng, Shubin. AU - Carlson, Kathryn E.. AU - Katzenellenbogen, Benita S. AU - Katzenellenbogen, John A.. AU - Macchia, Marco. PY - 2003/9/11. Y1 - 2003/9/11. N2 - The 3,4-diphenylsalicylaldoxime system 1 is an estrogen receptor (ER) ligand of unusual structure, having a hydrogen-bonded pseudocyclic A′-ring in place of the paradigmatic phenolic A-ring that is characteristic of most estrogens. We have investigated the role played by the pseudocycle A′ in binding to the ER by preparing 3,4-diphenylbenzaldoxime (4), a compound that completely lacks this ring but still preserves all of the other features of the original molecule 1, as well as a series of 3,4-diphenylanthranylaldoximes (5a-c) in ...
TY - JOUR. T1 - The changes of estrogen receptor-β variants expression in breast carcinogenesis. T2 - Decrease of estrogen receptor-β2 expression is the key event in breast cancer development. AU - Park, Byeongwoo. AU - Kim, Ki Suk. AU - Heo, Min Kyu. AU - Yang, Woo Ick. AU - Kim, Seung Il. AU - Kim, Joo Hang. AU - Kim, Gwi Eon. AU - Lee, Kyong Sik. PY - 2006/5/1. Y1 - 2006/5/1. N2 - Backgound and Objectives: Although more than five variant forms of estrogen receptor-β (ERβ) have been identilied, their role has not been identified. This study was carried out to investigate the changes of ERβ variants in breast cancer development. Methods: Using reverse transcription polymerase chain reaction (RT-PCR) and triple primer PCR (TP-PCR), the expression levels of ERβ variants mRNA were measured in 66 paired normal and cancer tissues. The relative expression level of ERβ variants were compared between normal and cancer tissues, and also compared according to various clinicopathological ...
Background Assess the relation between the presence of PVUII and XBAI polymorphisms in the estrogen receptor alpha gene and mammographic density in postmenopausal women.. Methods For the present analysis, 189 postmenopausal women who had never used hormonal therapy and who did not have clinical or mammographic features were selected. Based on the ACR-BIRADSâ 2003 classification, the mammographic density was determined by three independent readers (two subjective ratings and one computerized - Adobe Photoshop â 7.0 software). Blood samples were available to extract DNA according to KIT GFX â protocol. PCR-RFLP (Polymerase Chain Reaction - Restriction Fragment Length Polymorphism) was then used to identify the polymorphisms.. Results There was a high degree of agreement among the three readers to determine the mammographic density (Kappa,0.75). Sixty women (32%) had dense breasts and 129 (68%) had non-dense breasts. The PVUII polymorphism was found in 132 (69.8%) of 189 women, while the XBAI ...
TY - JOUR. T1 - Abnormal vascular function and hypertension in mice deficient in estrogen receptor β. AU - Zhu, Yan. AU - Bian, Zhao. AU - Lu, Ping. AU - Karas, Richard H.. AU - Bao, Lin. AU - Cox, Daniel. AU - Hodgin, Jeffrey. AU - Shaul, Philip W.. AU - Thorén, Peter. AU - Smithies, Oliver. AU - Gustafsson, Jan Åke. AU - Mendelsohn, Michael E.. PY - 2002/1/18. Y1 - 2002/1/18. N2 - Blood vessels express estrogen receptors, but their role in cardiovascular physiology is not well understood. We show that vascular smooth muscle cells and blood vessels from estrogen receptor β (ERβ) - deficient mice exhibit multiple functional abnormalities. In wild-type mouse blood vessels, estrogen attenuates vasoconstriction by an ERβ-mediated increase in inducible nitric oxide synthase expression. In contrast, estrogen augments vasoconstriction in blood vessels from ERβ-deficient mice. Vascular smooth muscle cells isolated from ERβ-deficient mice show multiple abnormalities of ion channel function. ...
In Silico Prediction of Estrogen Receptor Subtype Binding Affinity and Selectivity Using Statistical Methods and Molecular Docking with 2-Arylnaphthalenes and 2-Arylquinolines. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
There are several potential explanations for the failure of acute hormone replacement therapy to reduce ambulatory ECG ischemia in our study. Although human endothelial cells and smooth muscle cells express estrogen receptors (12,26), Losordo et al. (27)reported that atherosclerotic coronary arteries expressed fewer estrogen receptors than coronary arteries without significant atherosclerosis. Furthermore, Post et al. (28)reported increased rates of estrogen receptor gene promoter methylation with increasing age, both in nondiseased vessels and even more so in areas with atherosclerotic plaque. Increased promoter methylation inactivates estrogen receptor gene transcription. Since women with UA are usually elderly with significant atherosclerosis, they may be unresponsive to hormone therapy due to lack of the estrogen receptor. It also is possible that the concurrent use of nitroglycerin in three-quarters of our patients resulted in maximal endothelial-independent coronary vasodilation, thus ...
Dyslexia, or specific reading disability, is the unexpected failure in learning to read and write when intelligence and senses are normal. One of the susceptibility genes, DYX1C1, has been implicated in neuronal migration, but little is known about its interactions and functions. As DYX1C1 was suggested to interact with the U-box protein CHIP (carboxy terminus of Hsc70-interacting protein), which also participates in the degradation of estrogen receptors alpha (ERalpha) and beta (ERbeta), we hypothesized that the effects of DYX1C1 might be at least in part mediated through the regulation of ERs. ERs have shown to be important in brain development and cognitive functions. Indeed, we show that DYX1C1 interacts with both ERs in the presence of 17beta-estradiol, as determined by co-localization, co-immunoprecipitation and proximity ligation assays. Protein levels of endogenous ERalpha or exogenous ERbeta were reduced upon over-expression of DYX1C1, resulting in decreased transcriptional responses to ...
Epidemiological, clinical and animal studies revealed that sex differences exist in the manifestation and outcome of cardiovascular disease (CVD). The underlying molecular mechanisms implicated in these sex differences are not fully understood. The reasons for sex differences in CVD are definitely multifactorial, but major evidence points to the contribution of sex steroid hormone, 17β-estradiol (E2), and its receptors, estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). In this review, we summarize past and present studies that implicate E2 and ER as important determinants of sexual dimorphism in the physiology and pathophysiology of the heart. In particular, we give an overview of studies aimed to reveal the role of E2 and ER in the physiology of the observed sex differences in CVD using ER knock-out mice. Finally, we discuss recent findings from novel transgenic mouse models, which have provided new information on the sexual dimorphic roles of ER specifically in cardiomyocytes ...
Phosphorylation of estrogen receptor alpha at serine 305 (ER alpha S305-P) by protein kinase A (PKA) or p21-activated kinase 1 (PAK1) has experimentally been associated with tamoxifen sensitivity. Here, we investigated the clinical application of this knowledge to predict tamoxifen resistance in ER-positive breast cancer patients. Using immunohistochemistry, a score including PAK1 and co-expression of PKA and ER alpha S305-P (PKA/ER alpha S305-P) was developed on a training set consisting of 103 patients treated with tamoxifen for metastatic disease, and validated on 231 patients randomized between adjuvant tamoxifen or no treatment. In the training set, PAK1 levels were associated with tumor progression after tamoxifen (HR 1.57, 95% CI 0.99-2.48), as was co-expression of PKA and ER alpha S305-P (HR 2.00, 95% CI 1.14-3.52). In the validation set, a significant tamoxifen benefit was found among the 73% patients negative for PAK1 and PKA/ER alpha S305-P (HR 0.54, 95% CI 0.34-0.87), while others ...
Aretrospective study comparing the estrogen receptor (ER) alpha subtype and progesterone receptor (PR) profile of breast carcinomas amongst 1625 cases over 2.5 years was carried out. Strictly speaking it is generally believed that breast carcinomas can biochemically express PR only if they are ER-positive. However, a few ERalpha-PR+ cases do exist paradoxically. This class of tumors was the focus of our study in which we looked at the possible reasons for such an immunophenotype and compared it with a group of ERalpha+PR+ breast carcinomas. An internationally recognized immunohistochemical method employing monoclonal antibodies against estrogen and progesterone receptors was used. Correlations with established risk factors i.e. menopausal status, grade, tumor size and lymph node status were analyzed for our study group (ERalpha-PR+) and compared with a control (ERalpha+PR+). Out of the total 1625 cases, 29.91% (486) were ERalpha+PR+, 5.11% (83) were ERalpha+PR-, 56.86% (924) were ERalpha-PR- and 8.12%
The vascular consequences of estrogen treatment may be driven by its initiation timing. We tested the hypothesis that the duration of ovarian hormone deprivation before estrogen reintroduction affects the role of estrogen as mediator of endothelial f
in Trabajos del Instituto Cajal (2009), LXXXII. Steroid receptors such as estrogen receptors alpha and beta and androgen receptors are transcription factors involved in the transcriptional regulation of a large number of target genes. Steroid-dependent ... [more ▼]. Steroid receptors such as estrogen receptors alpha and beta and androgen receptors are transcription factors involved in the transcriptional regulation of a large number of target genes. Steroid-dependent expression in the brain controls a large array of biological processes including spatial cognition, copulatory behavior and neuroprotection. The discovery of a competition, or squelching, between two different nuclear receptors introduced the notion that common cofactors might be involved in the modulation of transcriptional activity of nuclear receptors. These cofactors, which are now known as coactivators, are involved in chromatin remodeling and stabilization of the general transcription machinery. Since the characterization of ...
MICHAEL PHELPS: PET molecular imaging probes can rapidly search for cancer throughout all tissues of the body, as well as characterize each cancer lesion it detects within an individual patient. Tumors can change their biological properties as they metastasize, so there is a need to characterize the initial tumor and each metastasis. For example, a patient with breast cancer can first present a tumor in the breast tissue with estrogen receptors, but then develop metastases that may or may not have estrogen receptors. Those metastases with estrogen receptors will likely respond to hormonal therapy, while those without estrogen receptors will not respond. About 40 percent of metastases have a different estrogen receptor status than the primary tumor from which they spread. Whole body PET imaging reveals the estrogen receptors in patients, lesion by lesion, to better determine whether response to hormonal therapy will be effective for all lesions. All cancer treatments are in need of better ...
ER-alpha and ER-beta function as transcription factors to modulate expression of target genes. Both interact with nuclear regulatory proteins to enhance or inhibit transcription. We hypothesized that these co-regulators are expressed in breast cancer tissue and may be differentially regulated by estrogen and tamoxifen.. ER-alpha, ER-beta, the co-activator SRC-1, and the co-repressor SMRT were localized within breast tissue by immunohistochemistry, and the spatial co-expression assessed by immunofluoresence. The ability of beta-estradiol and 4-hydroxytamoxifen (4-HOT) to modulate the protein of ER-alpha, ER-beta, SRC-1, and SMRT in primary cell cultures, and MCF-7 and T47-D cell lines was assessed by western blotting.. ER-alpha and ER-beta were found to be co-expressed with the co-regulators SRC-1 and SMRT in the nuclei of breast cancer epithelial cells. Partial and complete response elements for the ER were identified on the promotor region of ER-alpha, ER-beta, SRC-1 and SMRT. Beta-estradiol ...
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of
This study investigates the molecular mechanisms by which critical genes are differentially regulated in the male and female brain. The hormone, estrogen, is cr...
To develop novel estrogen receptor (ER) ligands, ring-fused derivatives of the hormonally active (1R,2S)/(1S,2R)-1-(2-chloro-4-hydroxyphenyl)-2-(2,6-dichloro-4-hydroxyphenyl)ethylenediamine 4b were synthesized. (2R,3S)/(2S,3R)-2-(2-Chloro-4-hydroxyphenyl)-3-(2,6-dichloro-4-hydroxyphenyl)piperazine 4 induced ligand-dependent gene expression in MCF-7-2a cells, stably transfected with the plasmid ERE(wtc)luc and was therefore used as a lead structure. The influence of the substitution pattern in the aromatic rings (4-OH (1), 2-F,4-OH (2), 2-Cl,4-OH (3), 2,6-Cl2,3-OH (5), and 2,6-Cl2,4-OH (6)) and the effect of N-ethyl chains on the ER binding and activation of gene expression were studied. The synthesis started from the respective methoxy-substituted (1R,2S)/(1S,2R)-configurated 1,2-diarylethylenediamines 6b to 4b, which were reacted with dimethyl oxalate in order to get 5,6-diarylpiperazine-2,3-diones. Reduction with BH3*tetrahydrofuran and ether cleavage with BBr3 yielded the piperazines 1-6. The N
Figure 3 Thermogenic program and β3-adrenergic receptor signaling is mediated by membrane-initiated ERα signaling. A: Immunoblot analysis of UCP1 levels in BAT and pWAT of ERα+/+, ERα−/−, WT, and KRRki/ki mice. Representative immunoblots and quantification are shown (n = 5-8 per group). #P , 0.01. B: qRT-PCR analysis of genes consistent with beige adipocytes in adipose tissues of ERα+/+, ERα−/−, WT, and KRRki/ki mice (n = 6-8). Relative mRNA expression levels are normalized to gapdh. *P , 0.05, #P , 0.01. C: Hematoxylin and eosin staining of pWAT of ERα+/+, ERα−/−, WT, and KRRki/ki mice. Scale bar indicates 100 µm. The graph depicts the quantification of mean cell area (n = 4). #P , 0.01. D: qRT-PCR analysis of genes consistent with beige adipocytes in NIH 3T3-L1 preadipocytes treated with vehicle (control), 100 nmol/L E2, or 2 µmol/L rosiglitazone for 72 h. Relative mRNA expression levels are normalized to gapdh. Data depict the results from three independent experiments. ...
Trial finds estrogen receptor degrader significantly increases progression-free survival in patients with advanced breast cancer.
Communications DOI: 10.1002/anie.201101655 DNA Complexes DNA-Controlled Bivalent Presentation of Ligands for the Estrogen Receptor** Frank Abendroth, Alexander Bujotzek, Min Shan, Rainer Haag, Marcus Weber, and Oliver Seitz* The assembly of DNA complexes proceeds according to known rules. Thus, the mutual recognition of DNA conjugates can be used for the precise positioning of functional groups. For example, chromophores,[1] metals,[2] catalytic units,[3] nanoparticles,[4] fluorophores[5] and even proteins[6] have been arranged at well-defined distances by means of DNA hybridization. Until recently, the main interest was focused on issues within materials science as well as on the immobilization of biomolecules. We and others assumed that the ability to position functional units at defined distances could also be used to address biological problems.[7] According to this, DNA may serve as a molecular ruler to determine the distance between binding pockets in biological receptors. Due to ...
mouse anti-estrogen receptor alpha, ligand binding domain (aa 304-554) hybridoma (ERalpha BZ1) is an eagle-i resource of type Hybridoma cell line at eagle-i Network Shared Resource Repository.
First estrogen eeceptor-α mutation identified in a young woman. A receptor mutation that essentially blocks estrogens action has been identified in a female.
Researchers then monitored the response of estrogen receptor-alpha (ERa) - the bodys main bone-related mediator of the hormone - to the estradiol. In particular, the group wanted to know whether the inhibition of one of the ERas two activation functions, known as AF-1 and AF-2, would redirect estrogen to specific tissues ...
Hormones are vital to our health and vitality. One hormone that is vitally important for many reasons is estrogen. Physical functions and other biochemical parameters are affected with the amount of estrogen found in the body.. In women, estrogen is important during the time frame of puberty. It decelerates height increase, accelerates body fat burning, and reduces muscle bulk. It assists in regulating the menstrual cycle and developing breasts. It helps reduce bone re-absorption and increase bone formation. Good cholesterol (HDL) and triglycerides are increased through estrogen. LDL (bad cholesterol) is lowered and increased fat deposition is a result of having a good level of estrogen. Collagen content and quality is admired through the assistance of estrogen. It helps increase skin thickness and improves blood supply to the skin.. Fluctuating estrogen levels during the transition to menopause can take a toll on your health. There can be: ...
CD218a (IL-18 Receptor alpha) Mouse anti-Human, APC, Clone: H44, eBioscience™ 100 tests; APC CD218a (IL-18 Receptor alpha) Mouse anti-Human, APC, Clone: H44,...