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Estrogen receptor alpha

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https://www.readbyqxmd.com/read/28539435/membrane-and-nuclear-estrogen-receptor-alpha-actions-from-tissue-specificity-to-medical-implications
#1
REVIEW
Jean-Francois Arnal, Françoise Lenfant, Raphaël Metivier, Gilles Flouriot, Daniel Henrion, Marine Adlanmerini, Coralie Fontaine, Pierre Gourdy, Pierre Chambon, Benita Katzenellenbogen, John Katzenellenbogen
Estrogen receptor alpha (ERα) has been recognized now for several decades as playing a key role in reproduction and exerting functions in numerous nonreproductive tissues. In this review, we attempt to summarize the in vitro studies that are the basis of our current understanding of the mechanisms of action of ERα as a nuclear receptor and the key roles played by its two activation functions (AFs) in its transcriptional activities. We then depict the consequences of the selective inactivation of these AFs in mouse models, focusing on the prominent roles played by ERα in the reproductive tract and in the vascular system...
July 1, 2017: Physiological Reviews
https://www.readbyqxmd.com/read/28539237/effects-of-sex-steroids-on-the-pattern-of-methylation-and-expression-of-the-promoter-region-of-estrogen-and-androgen-receptors-in-people-with-gender-dysphoria-under-cross-sex-hormone-treatment
#2
Gloria Aranda, Eduardo Fernández-Rebollo, Marta Pradas-Juni, Felicia Alexandra Hanzu, Susana G Kalko, Irene Halperin, Mireia Mora
Cross-sex hormone therapy (CHT) is critical for phenotypical and physiological transition in adults with gender dysphoria (GD). However, the impact of the CHT onto the molecular level/epigenetic regulation has not been comprehensively addressed. We postulate that CHT in GD could drive changes at the androgen receptor (AR), estrogen receptor alpha (ESR1) and estrogen receptor beta (ESR2), affecting their DNA methylation pattern and mRNA expression that may influence in the phenotypical changes associated to CHT...
May 21, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28537895/interaction-of-glycosphingolipids-gd3-and-gd2-with-growth-factor-receptors-maintains-breast-cancer-stem-cell-phenotype
#3
Yuh-Jin Liang, Chen-Yu Wang, I-An Wang, Yi-Wen Chen, Li-Tzu Li, Chuang-Yu Lin, Ming-Yi Ho, Tsung-Lung Chou, Ya-Hui Wang, Shih-Pin Chiou, Yu-Ju Lin, John Yu
Many studies have suggested that disialogangliosides, GD2 and GD3, are involved in the development of various tumor types. However, the functional relationships between ganglioside expression and cancer development or aggressiveness are not fully described. GD3 is upregulated in approximately half of all invasive ductal breast carcinoma cases, and enhanced expression of GD3 synthase (GD3S, alpha-N-acetylneuraminide alpha-2,8-sialyltransferase) in estrogen receptor-negative breast tumors, was shown to correlate with reduced overall patient survival...
May 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28535794/mutation-site-and-context-dependent-effects-of-esr1-mutation-in-genome-edited-breast-cancer-cell-models
#4
Amir Bahreini, Zheqi Li, Peilu Wang, Kevin M Levine, Nilgun Tasdemir, Lan Cao, Hazel M Weir, Shannon L Puhalla, Nancy E Davidson, Andrew M Stern, David Chu, Ben Ho Park, Adrian V Lee, Steffi Oesterreich
BACKGROUND: Mutations in the estrogen receptor alpha (ERα) 1 gene (ESR1) are frequently detected in ER+ metastatic breast cancer, and there is increasing evidence that these mutations confer endocrine resistance in breast cancer patients with advanced disease. However, their functional role is not well-understood, at least in part due to a lack of ESR1 mutant models. Here, we describe the generation and characterization of genome-edited T47D and MCF7 breast cancer cell lines with the two most common ESR1 mutations, Y537S and D538G...
May 23, 2017: Breast Cancer Research: BCR
https://www.readbyqxmd.com/read/28534210/association-study-of-estrogen-receptor-alpha-gene-polymorphisms-with-bone-mass-assessed-by-quantitative-ultrasound-in-young-adults
#5
María Correa-Rodriguez, Jacqueline Schmidt-RioValle, Blanca Rueda-Medina
Different genetic variants in estrogen receptor alpha (ESR1) have been shown to influence bone phenotypes including quantitative bone ultrasound in elderly. We aimed to investigate the role of ESR1 polymorphisms in bone mass assessed by calcaneal quantitative ultrasound (QUS) in a population of young adults. The study sample consisted of 466 healthy individuals of Caucasian ancestry (315 females and 152 males) aged 18 and 25 years (median age 20.39 ± 2.70). Six ESR1 polymorphisms (rs302033, rs2982552, rs2982575, rs2504063, rs2234693-PvuII and rs9340799-XbaI) were selected as genetic markers and genotyped...
May 22, 2017: Rheumatology International
https://www.readbyqxmd.com/read/28529129/estrogen-receptor-%C3%AE-36-is-involved-in-icaritin-induced-growth-inhibition-of-triple-negative-breast-cancer-cells
#6
Xue Wang, Nan Zheng, Jing Dong, Xuming Wang, Lijiang Liu, Jian Huang
A sub-class of ER-negative breast cancer that is negative for ER, PR and HER2 expression known as triple-negative breast cancer (TNBC) is highly malignant and lacks effective treatment. Recently, it has been reported that an isoform of estrogen receptor-alpha ER-α36 is expressed and plays a critical role in development of TNBC. ER-α36 forms a positive regulatory loop with epidermal growth factor receptor (EGFR), which promotes malignant growth of TNBC cells. Thus, ER-α36 has been proposed as an important target for development of novel drugs for TNBC...
May 18, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28528409/polychlorinated-biphenyl-related-alterations-of-the-expression-of-essential-genes-in-harbour-seals-phoca-vitulina-from-coastal-sites-in-canada-and-the-united-states
#7
Marie Noël, Neil Dangerfield, Steve Jeffries, Dyanna Lambourn, Monique Lance, Caren Helbing, Michel Lebeuf, Peter S Ross
As long-lived marine mammals found throughout the temperate coastal waters of the North Pacific and Atlantic Oceans, harbour seals (Phoca vitulina) have become an invaluable sentinel of food-web contamination. Their relatively high trophic position predisposes harbour seals to the accumulation of harmful levels of persistent organic pollutants (POPs). We obtained skin/blubber biopsy samples from live-captured young harbour seals from various sites in the northeastern Pacific (British Columbia, Canada, and Washington State, USA) as well as the northwestern Atlantic (Newfoundland and Quebec, Canada)...
May 20, 2017: Archives of Environmental Contamination and Toxicology
https://www.readbyqxmd.com/read/28527569/estrogen-hormone-biology
#8
Katherine J Hamilton, Sylvia C Hewitt, Yukitomo Arao, Kenneth S Korach
The hormone estrogen is involved in both female and male reproduction, as well as numerous other biological systems including the neuroendocrine, vascular, skeletal, and immune systems. Therefore, it is also implicated in many different diseases and conditions such as infertility, obesity, osteoporosis, endometriosis, and a variety of cancers. Estrogen works through its two distinct nuclear receptors, estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). Various transcriptional regulation mechanisms have been identified as the mode of action for estrogen, mainly the classical mechanism with direct DNA binding but also a nongenomic mode of action and one using tethered or indirect binding...
2017: Current Topics in Developmental Biology
https://www.readbyqxmd.com/read/28525844/the-discovery-of-novel-potent-err-alpha-inverse-agonists-for-the-treatment-of-triple-negative-breast-cancer
#9
Yongli Du, Lianhua Song, Liudi Zhang, Hao Ling, Yanhui Zhang, Haifei Chen, Huijie Qi, Xiaojin Shi, Qunyi Li
The estrogen-related receptor α (ERRα) is an orphan receptor and a novel target for solid tumor therapy, conceivably through effects on the regulation of tumor cell energy metabolism associated with energy stress within solid tumor micro environments. Here we describe the discovery of novel potent inverse agonists of ERRα. In vitro, compound 11 potently inhibits ERRα's transcriptional activity by preventing endogenous PGC-1α and ERRα binding and suppresses the proliferation of different human cancer cell lines and the migration of breast cancer cells (MDA-MB-231)...
April 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28520870/defining-the-role-of-estrogen-receptor-beta-in-the-regulation-of-female-fertility
#10
Ma Karim Rumi, Prabhakar Singh, Katherine F Roby, Xiao Zhao, Khursheed Iqbal, Anamika Ratri, Tianhua Lei, Wei Cui, Shaon Borosha, Pramod Dhakal, Kaiyu Kubota, Damayanti Chakraborty, Jay L Vivian, Michael W Wolfe, Michael J Soares
Estrogens are essential hormones for the regulation of fertility. Cellular responses to estrogens are mediated by estrogen receptor alpha (ESR1) and estrogen receptor beta (ESR2). In mouse and rat models, disruption of Esr1 causes infertility in both males and females. However, the role of ESR2 in reproductive function remains undecided due to a wide variation in phenotypic observations among Esr2 mutant mouse strains. Regulatory pathways independent of ESR2 binding to its cognate DNA response element have also been implicated in ESR2 signaling...
May 16, 2017: Endocrinology
https://www.readbyqxmd.com/read/28499274/api5-a-new-cofactor-of-estrogen-receptor-alpha-involved-in-breast-cancer-outcome
#11
Céline Basset, Florence Bonnet-Magnaval, Marina Garcia-Jove Navarro, Christian Touriol, Monique Courtade, Hervé Prats, Barbara Garmy-Susini, Eric Lacazette
Api5 (Apoptosis inhibitor 5) is an anti-apoptotic factor that confers resistance to genotoxic stress in human cancer. Api5 is also expressed in endothelial cells and participates to the Estrogen Receptor α (ERα) signaling to promote cell migration. In this study, we found an over expression of Api5 in human breast cancer. Given that we show that high expression of Api5 in breast cancer patients is associated with shorter recurrence free survival, we investigated the relationship between ERα and Api5 at the molecular level...
April 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/28486190/icariin-stimulates-osteogenic-differentiation-of-rat-bone-marrow-stromal-stem-cells-by-increasing-taz-expression
#12
QiuShi Wei, MinCong He, MeiHui Chen, ZhenQiu Chen, Fan Yang, HaiBin Wang, Jin Zhang, Wei He
Icariin, the major ingredient of Herba Epimedii, promotes the osteogenic differentiation of rat bone marrow stromal cells (rBMSCs) and exerts protective effects against bone loss and increases bone regeneration, but the underlying signaling pathway by which icariin affects osteogenic differentiation remain unclear. Transcriptional coactivator with PDZ-binding motif (TAZ) is a transcriptional modulator of the Hippo signaling pathway, which plays an important role in the osteogenic differentiation of BMSCs by activating Runx2 gene during the terminal osteogenic differentiation...
May 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28481132/disruption-of-estrogen-receptor-alpha-in-rats-results-in-faster-initiation-of-compensatory-regeneration-despite-higher-liver-injury-after-carbon-tetrachloride-treatment
#13
Steven R McGreal, Karim Rumi, Michael J Soares, Benjamin L Woolbright, Hartmut Jaeschke, Udayan Apte
Estrogen receptor alpha (ESR1) is 1 of the 2 intracellular receptors for estrogen and is expressed by hepatocytes in the liver. The role of ESR1 in the regulation of toxicant-induced liver injury and compensatory regeneration is not completely clear. We investigated the role of ESR1 in liver regeneration after carbon tetrachloride (CCl4)-induced liver injury using wild type (WT) and ESR1 knockout (ESR1-KO) rats. Adult female WT and ESR1-KO rats were treated with 1 mL/kg CCl4 and euthanized over a time course of 0 to 48 hours...
January 1, 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28476547/bisphenol-a-exposure-in-utero-programs-a-sexually-dimorphic-estrogenic-state-of-hepatic-metabolic-gene-expression
#14
Ysabel Ilagan, Ramanaiah Mamillapalli, Laura G Goetz, Jehanzeb Kayani, Hugh S Taylor
Bisphenol-A (BPA) exposure in utero affects fetal development and metabolism leading to obesity. However, the mechanisms are not well characterized. We identified sexually dimorphic developmental programming of genes regulating metabolism in the liver after BPA exposure. Pregnant mice were treated with BPA on days 9-18 of gestation. At six weeks, female offspring were ovariectomized; both sexes were subsequently treated with estradiol (E2). Fetal BPA exposure altered the expression of genes in liver, including those involved in glucose and lipid metabolism, and transporters, in both sexes...
May 2, 2017: Reproductive Toxicology
https://www.readbyqxmd.com/read/28473445/estrogen-receptor-control-of-atherosclerotic-calcification-and-smooth-muscle-cell-osteogenic-differentiation
#15
Lucinda S McRobb, Kristine C Y McGrath, Tania Tsatralis, Eleanore C Liong, Joanne T M Tan, Gillian Hughes, David J Handelsman, Alison K Heather
OBJECTIVE: Vascular calcification is associated with increased risk of myocardial infarction and stroke. The objective of this work was to examine the ability of 17β-estradiol (E2) to stimulate calcification of vascular smooth muscle cells (VSMC) in vivo, using aged apolipoprotein E-null mice with advanced atherosclerotic lesions, and subsequently to explore underlying mechanisms in vitro. APPROACH AND RESULTS: Silastic E2 capsules were implanted into male and female apolipoprotein E-null mice aged 34 weeks...
May 4, 2017: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/28468943/estradiol-activates-chloride-channels-via-the-estrogen-receptor-alpha-in-the-cell-membrane-in-osteoblasts
#16
Zhiqin Deng, Shuang Peng, Yanfang Zheng, Xiaoya Yang, Haifeng Zhang, Qiuchan Tan, Xiechou Liang, Hong Gao, Yuan Li, Yanqing Huang, Linyan Zhu, Tim Jc Jacob, Lixin Chen, Liwei Wang
Estrogen plays important roles in regulation of bone formation. Chloride channels in the ClC family are expressed in osteoblasts and are associated with bone physiology and pathology, but the relationship between chloride channels and estrogen is not clear. In this study, the action of estrogen on chloride channels was investigated in osteoblastic MC3T3-E1 cells. Results showed that 17β-estradiol could activate a current which reversed at a potential close to Cl(-) equilibrium potential with the anion selectivity I- >Br->Cl->gluconate and was inhibited by the chloride channel blockers 5-nitro-2-(3-phenylpropylamino)-benzoate (NPPB) and 4,4'-Diisothiocyano-2,2'-stilbenedisulfonic acid (DIDS) and knockdown of ClC-3 chloride channel expression...
May 3, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28465680/sex-differences-in-the-effect-of-resveratrol-on-dss-induced-colitis-in-mice
#17
Alexandra Wagnerova, Janka Babickova, Robert Liptak, Barbora Vlkova, Peter Celec, Roman Gardlik
Resveratrol is a natural polyphenol studied for its possible protective properties in inflammatory bowel diseases. Moreover, it has been shown to interact with estrogen receptors. In the present study, we aimed to investigate possible diverse effects of resveratrol on female and male mice in DSS-induced colitis. Thirty-seven C57BL/6 mice (21 female and 16 male) were divided into three groups for each sex. The first group received pure water (CTRL). The other two groups received 1.5% dextran sulfate sodium (DSS) to induce colitis from which one group was treated with resveratrol (DSS + RSV)...
2017: Gastroenterology Research and Practice
https://www.readbyqxmd.com/read/28463089/purine-5-8-cyclo-2-deoxynucleoside-lesions-formation-by-radical-stress-and-repair-in-human-breast-epithelial-cancer-cells
#18
Marios G Krokidis, Michael A Terzidis, Eleni Efthimiadou, Sevasti-Kiriaki Zervou, George Kordas, Kyriakos Papadopoulos, Anastasia Hiskia, Dimitris Kletsas, Chryssostomos Chatgilialoglu
5',8-Cyclo-2'-deoxyadenosine (cdA) and 5',8-cyclo-2'-deoxyguanosine (cdG) in their two diastereomeric forms, 5'S and 5'R, are tandem lesions produced by the attack of hydroxyl radicals to the purine moieties of DNA. Their formation has been found to challenge the cells' repair machinery, initiating the nucleotide excision repair (NER) for restoring the genome integrity. The involvement of oxidatively induced DNA damage in carcinogenesis and the reduced capacity of some cancer cell lines to repair oxidized DNA base lesions, intrigued us to investigate the implication of these lesions in breast cancer, the most frequently occurring cancer in women...
May 2, 2017: Free Radical Research
https://www.readbyqxmd.com/read/28457941/non-nuclear-estrogen-receptor-alpha-activation-in-endothelium-reduces-cardiac-ischemia-reperfusion-injury-in-mice
#19
Sara Menazza, Junhui Sun, Swathi Appachi, Ken L Chambliss, Sung Hoon Kim, Angel Aponte, Sohaib Khan, John A Katzenellenbogen, Benita S Katzenellenbogen, Philip W Shaul, Elizabeth Murphy
Steroid hormone receptors including estrogen receptors (ER) classically function as ligand-regulated transcription factors. However, estrogens also elicit cellular effects through binding to extra-nuclear ER (ERα, ERβ, and G protein-coupled ER or GPER) that are coupled to kinases. How extra-nuclear ER actions impact cardiac ischemia-reperfusion (I/R) injury is unknown. We treated ovariectomized wild-type female mice with estradiol or an estrogen-dendrimer conjugate (EDC), which selectively activates extra-nuclear ER, or vehicle interventions for two weeks...
April 27, 2017: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/28448182/estrogen-receptor-alpha-xbai-gg-genotype-was-associated-with-severe-preeclampsia
#20
Saeedeh Salimi, Farzaneh Farajian-Mashhadi, Ehsan Tabatabaei, Mahnaz Shahrakipour, Minoo Yaghmaei, Mojgan Mokhtari
PURPOSE: Estrogen receptor-α (ERα) plays an essential role in the adaptation of increased uterine blood flow during gestation. Therefore, ERα gene could be a possible candidate for preeclampsia (PE) susceptibility. In current study we aimed to investigate the association of the ERα gene polymorphisms and PE in an Iranian population. METHODS: A total of 192 pregnant women with PE and 186 normotensive women were genotyped for ERα gene (PvuII and XbaI) polymorphisms by polymerase chain reaction-restriction fragment length polymorphism method...
2017: Clinical and Experimental Hypertension: CHE
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