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Estrogen receptor alpha

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https://www.readbyqxmd.com/read/29778442/developmental-profiles-of-progesterone-receptor-transcripts-and-molecular-responses-to-gestagen-exposure-during-silurana-tropicalis-early-development
#1
Paisley Thomson, Valerie S Langlois
Environmental gestagens are an emerging class of contaminants that have been recently measured in surface water and can interfere with reproduction in aquatic vertebrates. Gestagens include endogenous progestogens, such as progesterone (P4), which bind P4-receptors and have critically important roles in vertebrate physiology and reproduction. Gestagens also include synthetic progestins, which are components of human and veterinary drugs, such as melengestrol acetate (MGA). Endogenous progestogens are essential in the regulation of reproduction in mammalian species, but the role of P4 in amphibian larval development remains unclear...
May 17, 2018: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/29777335/a-trisubstituted-pyrazole-derivative-reduces-dmba-induced-mammary-tumor-growth-in-rats-by-inhibiting-estrogen-receptor-%C3%AE-expression
#2
Hanumappa Ananda, Kothanahally S Sharath Kumar, Muddenahalli S Sudhanva, Shobith Rangappa, Kanchugarakoppal S Rangappa
Aberrant expression of estrogen receptor alpha (ER-α) is observed in many pathological complications like breast cancer, endometrial cancer, and in osteoporosis. ER-α plays a vital role in the initiation and progression of breast cancer and confers chemo and radioresistance to the cancer cells by upregulating expression of anti-apoptotic proteins. The synthetic pyrazole derivative 3-(1-(4-bromophenyl)-5-phenyl-1H-pyrazol-3-yl)pyridine (compound 5d) displays significant cytotoxicity against mammary carcinoma cells...
May 18, 2018: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/29772419/duality-of-estrogen-receptor-%C3%AE-action-in-cancer-progression
#3
REVIEW
T C Guillette, Thomas W Jackson, Scott M Belcher
The physiological actions of estrogens are primarily mediated by the nuclear hormone receptors estrogen receptor alpha (ERα) and beta (ERβ). Activities of these nuclear steroid hormone receptors in etiology and progression of many hormone-responsive cancers are well-established, yet the specific role of each receptor, and their various expressed isoforms, in estrogen-responsive cancers remains unclear. Recent advances in nuclear receptor profiling, characterization of expressed splice variants, and the availability of new experimental cancer models, has extended the understanding of the complex interplay between the differentially expressed nuclear estrogen receptors...
May 14, 2018: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/29769420/stress-urinary-incontinent-women-the-influence-of-age-and-hormonal-status-on-estrogen-receptor-alpha-and-beta-gene-expression-and-protein-immunoexpression-in-paraurethral-tissues
#4
A Adamiak-Godlewska, R Tarkowski, I Winkler, K Romanek-Piva, K Skorupska, A J Jakimiuk, T Rechberger
The underlying cause of stress urinary incontinence (SUI) is an anatomical abnormality associated with paraurethral connective tissue dysfunction. The question as to whether estrogens affect the quality of that tissue remains unexplained. Samples of paraurethral connective tissue from 81 women were examined (the SUI's n = 49; the control's n = 32). In both groups, the patients were subdivided into pre- and postmenopausals. Primary study outcome was comparison of the estrogen receptor alpha (ERα) and the estrogen receptor beta (ERβ) gene and protein in paraurethral tissue between SUI and control group...
February 2018: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/29755845/determination-of-binding-affinity-of-molecular-imaging-agents-for-steroid-hormone-receptors-in-breast-cancer
#5
Kelley Salem, Manoj Kumar, Kyle C Kloepping, Ciara J Michel, Yongjun Yan, Amy M Fowler
16α-[18 F]Fluoro-17β-estradiol ([18 F]FES) and 21-[18 F]-Fluoro-16α,17α-[(R)-(1'-α-furylmethylidene)dioxyl]-19-norpregn-4-ene-3,20-dione ([18 F]FFNP) are being investigated as imaging biomarkers for breast cancer patients. Quantitative positron emission tomography (PET) reflects both total receptor content and binding affinity. To study factors that may alter radiopharmaceutical binding and impact PET accuracy, assays that can separate receptor amount from binding affinity are needed. The study purpose was to quantify the binding parameters of [18 F]FES and [18 F]FFNP in breast cancer...
2018: American Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/29755131/kmt2c-mediates-the-estrogen-dependence-of-breast-cancer-through-regulation-of-er%C3%AE-enhancer-function
#6
Kinisha Gala, Qing Li, Amit Sinha, Pedram Razavi, Madeline Dorso, Francisco Sanchez-Vega, Young Rock Chung, Ronald Hendrickson, James Hsieh, Michael Berger, Nikolaus Schultz, Alessandro Pastore, Omar Abdel-Wahab, Sarat Chandarlapaty
Estrogen receptor alpha (ERα) is a ligand-activated nuclear receptor that directs proliferation and differentiation in selected cancer cell types including mammary-derived carcinomas. These master-regulatory functions of ERα require trans-acting elements such as the pioneer factor FOXA1 to establish a genomic landscape conducive to ERα control. Here, we identify the H3K4 methyltransferase KMT2C as necessary for hormone-driven ERα activity and breast cancer proliferation. KMT2C knockdown suppresses estrogen-dependent gene expression and causes H3K4me1 and H3K27ac loss selectively at ERα enhancers...
May 14, 2018: Oncogene
https://www.readbyqxmd.com/read/29753772/increase-in-hyaluronic-acid-degradation-decreases-the-expression-of-estrogen-receptor-alpha-in-mcf7-breast-cancer-cell-line
#7
Vincent Hanoux, Judith Eguida, Emmanuelle Fleurot, Jérôme Levallet, Pierre-Jacques Bonnamy
The loss of estrogen receptor α (ERα) expression in breast cancer constitutes a major hallmark of tumor progression to metastasis and is generally correlated to a strong increase in Hyaluronic Acid (HA) turnover. The aim of our study was to search for a putative link between these two major events of breast cancer progression in the estrogen receptor-positive (ER+) MCF7 breast cancer cell line. The increase in HA turnover was performed by stable overexpression of the standard CD44 (CD44S) isoform and also by treatment with exogenous Hyaluronidase (Hyal) to allow an increase in HA catabolism...
May 10, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29748621/proteomic-profiling-identifies-key-coactivators-utilized-by-mutant-er%C3%AE-proteins-as-potential-new-therapeutic-targets
#8
Leah A Gates, Guowei Gu, Yue Chen, Aarti D Rohira, Jonathan T Lei, Ross A Hamilton, Yang Yu, David M Lonard, Jin Wang, Shu-Ping Wang, David G Edwards, Philip F Lavere, Jiangyong Shao, Ping Yi, Antrix Jain, Sung Yun Jung, Anna Malovannaya, Shunqiang Li, Jieya Shao, Robert G Roeder, Matthew J Ellis, Jun Qin, Suzanne A W Fuqua, Bert W O'Malley, Charles E Foulds
Approximately 75% of breast cancers are estrogen receptor alpha (ERα)-positive and are treatable with endocrine therapies, but often patients develop lethal resistant disease. Frequent mutations (10-40%) in the ligand-binding domain (LBD) codons in the gene encoding ERα (ESR1) have been identified, resulting in ligand-independent, constitutively active receptors. In addition, ESR1 chromosomal translocations can occur, resulting in fusion proteins that lack the LBD and are entirely unresponsive to all endocrine treatments...
May 11, 2018: Oncogene
https://www.readbyqxmd.com/read/29748541/rxr%C3%AE-provokes-tumor-suppression-through-p53-p21-p16-and-pi3k-akt-signaling-pathways-during-stem-cell-differentiation-and-in-cancer-cells
#9
Rui Zhang, Hui Li, Shuangshuang Zhang, Yujie Zhang, Nan Wang, Hao Zhou, Hongpeng He, Guang Hu, Tong-Cun Zhang, Wenjian Ma
The retinoid X receptor alpha (RXRα) is an important therapeutic target impacting diverse biological processes. Activation of RXRα is known to suppress cancer cell growth. However, the cellular mechanism has been elusive. In the present study, we addressed its role during stem cell differentiation and the underlying connections with carcinogenesis. RXRα was significantly upregulated following the differentiation of human mesenchymal stem cell (hMSC) toward the formation of endothelial cell (EC). However, overexpression of RXRα in hMSC provoked a senescence-like phenotype accompanied by the elevation of tumor suppressor p53, p21, and p16...
May 10, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29741891/a-c-estrogens-as-potent-and-selective-estrogen-receptor-beta-agonists-serbas-to-enhance-memory-consolidation-under-low-estrogen-conditions
#10
Alicia M Hanson, K L Iresha Sampathi Perera, Jaekyoon Kim, Rajesh K Pandey, Noreena Sweeney, Xingyun Lu, Andrea Imhoff, Alexander Craig Mackinnon, Adam J Wargolet, Rochelle M Van Hart, Karyn M Frick, William A Donaldson, Daniel S Sem
Estrogen receptor-beta (ERβ) is a drug target for memory consolidation in post-menopausal women. Herein is reported a series of potent and selective ERβ agonists (SERBAs) with in vivo efficacy that are A-C estrogens, lacking the B and D estrogen rings. The most potent and selective A-C estrogen is selective for activating ER relative to seven other nuclear hormone receptors, with a surprising 750-fold selectivity for the beta over alpha isoform, and with EC50's of 20-30 nM in cell-based and direct binding assays...
May 9, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29740325/extract-enriched-in-flavan-3-ols-and-mainly-procyanidin-dimers-improves-metabolic-alterations-in-a-mouse-model-of-obesity-related-disorders-partially-via-estrogen-receptor-alpha
#11
Daniela Leonetti, Raffaella Soleti, Nicolas Clere, Luisa Vergori, Caroline Jacques, Lucie Duluc, Catherine Dourguia, Maria C Martínez, Ramaroson Andriantsitohaina
Red wine polyphenol extracts improve cardiovascular and metabolic disorders linked to obesity. Their vascular protection is mediated by the activation of the alpha isoform of the estrogen receptor (ERα). In the present study, we explored the effects of a grape seed extract (GSE) enriched in the flavan-3-ols procyanidin dimers on obesity-related cardiovascular and metabolic disorders; with a particular interest in the role/contribution of ERα. Ovariectomized wild type or ERα knockout (KO) mice were fed with standard or western diet, supplemented or not with GSE, for 12 weeks...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29727907/pancreatic-beta-cell-proliferation-induced-by-estradiol-17%C3%AE-is-foxo1-dependent
#12
Sigal Shaklai, Meital Grafi-Cohen, Orli Sharon, Nadav Sagiv, Gabi Shefer, Dalia Somjen, Naftali Stern
Estradiol-17β (E2) and the Foxo1 transcription factor have each been implicated in the regulation of β-cell proliferation. Interaction between Foxo1and estrogen receptor alpha (ERα), effecting cell cycle, has been demonstrated in breast cancer cells, but has not been studied thus far in β-cells. Using human islets and the INS1-E β-cell line, this study investigated the contribution of Foxo1 to E2-mediated β-cell replication. Foxo1 expression was knocked down in INS1-E cells using siRNA and Foxo1 activity was inhibited in human islets with a specific Foxo1 inhibitor (AS1842856)...
May 4, 2018: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
https://www.readbyqxmd.com/read/29723449/-impacts-of-des-on-the-expressions-of-related-genes-in-the-gubernaculums-testis-of-newborn-mice
#13
Wei-Liao Li, Xuan Zhang, Yuan-Sheng DU, Jian-Hong Li, Xue-Wu Jiang
Objective: To investigate the influence of diethylstilbestrol (DES) on the mRNA expressions of the androgen receptor (AR), estrogen receptor α (ERα), proliferating cell nuclear antigen (PCNA), and actin alpha 1 (ACTα1) in the gubernaculums testis of newborn mice and explore their action mechanisms. METHODS: A total of 140 male Kunming mice were randomly divided into a blank control, a dimethyl sulfoxide (DMSO) control, and 5 experimental groups to be treated subcutaneously with normal saline, DMSO, and DES at 0...
July 2017: Zhonghua Nan Ke Xue, National Journal of Andrology
https://www.readbyqxmd.com/read/29723269/17%C3%AE-estradiol-and-or-estrogen-receptor-alpha-signaling-blocks-protein-phosphatase-1-mediated-iso-induced-cardiac-hypertrophy
#14
Hsin-Yuan Fang, Meng-Yu Hung, Yueh-Min Lin, Sudhir Pandey, Chia-Chien Chang, Kuan-Ho Lin, Chia-Yao Shen, Vijaya Padma Viswanadha, Wei-Wen Kuo, Chih-Yang Huang
Earlier studies have shown that estrogen possess protective function against the development of pathological cardiac hypertrophy. However, the molecular mechanisms of estrogens (E2) protective effect are poorly understood. Additionally, abnormal activation of β-adrenergic signaling have been implicated in the development of pathological cardiac remodeling. However, the role of serine/threonine protein phosphatase 1 (PP1) in pathological cardiac remodeling under the influence of β-adrenergic signaling have been sparsely investigated...
2018: PloS One
https://www.readbyqxmd.com/read/29702263/a-sorafenib-sparing-effect-in-the-treatment-of-thyroid-carcinoma-cells-attained-by-co-treatment-with-a-novel-isoflavone-derivative-and-1-25-dihydroxyvitamin-d3
#15
Elena Izkhakov, Orli Sharon, Esther Knoll, Asaf Aizic, Dan M Fliss, Fortune Kohen, Naftali Stern, Dalia Somjen
BACKGROUND: Sorafenib improves progression-free survival in patients with progressive radioactive iodine-refractory differentiated thyroid carcinoma, but causes severe side effects. Estrogens may accelerate thyroid carcinoma cell growth. Our group recently reported that isoflavone derivative 7-(O)-carboxymethyl daidzein conjugated to N-t-boc-hexylenediamine (cD-tboc), a novel anti-estrogenic compound, retards the growth of both thyroid carcinoma cell lines and cultured human carcinoma cells...
April 24, 2018: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29702197/mutations-in-the-estrogen-receptor-alpha-hormone-binding-domain-promote-stem-cell-phenotype-through-notch-activation-in-breast-cancer-cell-lines
#16
L Gelsomino, S Panza, C Giordano, I Barone, G Gu, E Spina, S Catalano, S Fuqua, S Andò
The detection of recurrent mutations affecting the hormone binding domain (HBD) of estrogen receptor alpha (ERα/ESR1) in endocrine therapy-resistant and metastatic breast cancers has prompted interest in functional characterization of these genetic alterations. Here, we explored the role of HBD-ESR1 mutations in influencing the behaviour of breast cancer stem cells (BCSCs), using various BC cell lines stably expressing wild-type or mutant (Y537 N, Y537S, D538G) ERα. Compared to WT-ERα clones, mutant cells showed increased CD44+ /CD24- ratio, mRNA levels of stemness genes, Mammosphere Forming Efficiency (MFE), Self-Renewal and migratory capabilities...
April 24, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29701696/estrogen-and-or-estrogen-receptor-%C3%AE-inhibits-bnip3-induced-apoptosis-and-autophagy-in-h9c2-cardiomyoblast-cells
#17
Bih-Cheng Chen, Yi-Jiun Weng, Marthandam Asokan Shibu, Chien-Kuo Han, Yueh-Sheng Chen, Chia-Yao Shen, Yueh-Min Lin, Vijaya Padma Viswanadha, Hsin-Yueh Liang, Chih-Yang Huang
The process of autophagy in heart cells maintains homeostasis during cellular stress such as hypoxia by removing aggregated proteins and damaged organelles and thereby protects the heart during the times of starvation and ischemia. However, autophagy can lead to substantial cell death under certain circumstances. BCL2/adenovirus E1B 19 kDa protein-interacting protein 3 (BNIP3), a hypoxia-induced marker, has been shown to induce both autophagy and apoptosis. A BNIP3-docked organelle, e.g., mitochondria, also determines whether autophagy or apoptosis will take place...
April 26, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29695491/nest-box-exploration-may-stimulate-breeding-physiology-and-alter-mrna-expression-in-the-medial-preoptic-area-of-female-european-starlings
#18
Jeremy A Spool, Melannie D Jay, Lauren V Riters
Environmental resources are proposed to fine-tune the timing of breeding, yet how they may do so remains unclear. In female European starlings ( Sturnus vulgaris ), nest cavities are limited resources that are necessary for breeding. Females that explore nest cavities, compared to those that do not, readily perform sexually-motivated behaviors. We assigned female starlings to aviaries with 1) no nest boxes, 2) nest boxes, or 3) nest boxes, plants, flowing water, insects and berries to test the hypothesis that environmental resources alter neural systems to stimulate mating behavior...
April 25, 2018: Journal of Experimental Biology
https://www.readbyqxmd.com/read/29684003/17%C3%AE-estradiol-promotes-angiogenesis-of-rat-cardiac-microvascular-endothelial-cells-in-vitro
#19
HaiTao Liu, Yin Tao, Mai Chen, Jin Yu, Wei-Jie Li, Ling Tao, Yan Li, Fei Li
BACKGROUND The formation of new blood vessels, known as angiogenesis, is critical for recovery from ischemic heart disease, and estrogen is considered an important factor in this process. Here, we investigated the effects of 17β-estradiol (17β-E2) on proliferation and migration of cardiac microvascular endothelial cells (CMECs) in vitro. MATERIAL AND METHODS Rat CMECs were isolated and cultured with 17β-E2 (0.001-1 µmol/l) in the absence or presence of the estrogen antagonist tamoxifen. Then, the expression level of estrogen receptor alpha was evaluated by using immunofluorescence assay, RT-PCR, and Western blot...
April 23, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29682196/testosterone-metabolites-inhibit-proliferation-of-castration-and-therapy-resistant-prostate-cancer
#20
Felix Bremmer, Hubertus Jarry, Valerie Unterkircher, Silke Kaulfuss, Peter Burfeind, Heinz-Joachim Radzun, Philipp Ströbel, Paul Thelen
Novel treatments for castration-resistant prostate cancer (CRPC) such as abiraterone acetate (AA) or enzalutamide effectively target the androgen pathway to arrest aberrant signalling and cell proliferation. Testosterone is able to inhibit tumour cell growth in CRPC. Estrogen receptor-beta (ERβ) binds the testosterone-metabolites 3β-androstanediol and 3α-androstanediol in parallel to the canonical estradiol. In the prostate it is widely accepted that ERβ regulates estrogen signalling, mediating anti-proliferative effects...
March 30, 2018: Oncotarget
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