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1

Chmielewska, Małgorzata, Izabela Skibińska, and Małgorzata Kotwicka. "Mitochondria: Target organelles for estrogen action." Postępy Higieny i Medycyny Doświadczalnej 71, no. 1 (2017): 0. http://dx.doi.org/10.5604/01.3001.0010.3828.

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Estrogens belong to a group of sex hormones, which have been shown to act in multidirectional way. Estrogenic effects are mediated by two types of intracellular receptors: estrogen receptor 1 (ESR1) and estrogen receptor 2 (ESR2). There are two basic mechanisms of estrogen action: 1) classical-genomic, in which the ligand-receptor complex acts as a transcriptional factor and 2) a nongenomic one, which is still not fully understood, but has been seen to lead to distinct biological effects, depending on tissue and ligand type. It is postulated that nongenomic effects may be associated with membr
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2

Arterburn, Jeffrey B., and Eric R. Prossnitz. "G Protein–Coupled Estrogen Receptor GPER: Molecular Pharmacology and Therapeutic Applications." Annual Review of Pharmacology and Toxicology 63, no. 1 (2023): 295–320. http://dx.doi.org/10.1146/annurev-pharmtox-031122-121944.

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The actions of estrogens and related estrogenic molecules are complex and multifaceted in both sexes. A wide array of natural, synthetic, and therapeutic molecules target pathways that produce and respond to estrogens. Multiple receptors promulgate these responses, including the classical estrogen receptors of the nuclear hormone receptor family (estrogen receptors α and β), which function largely as ligand-activated transcription factors, and the 7-transmembrane G protein–coupled estrogen receptor, GPER, which activates a diverse array of signaling pathways. The pharmacology and functional ro
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3

Kumar, Anita, Antara Banerjee, Dipty Singh, et al. "Estradiol: A Steroid with Multiple Facets." Hormone and Metabolic Research 50, no. 05 (2018): 359–74. http://dx.doi.org/10.1055/s-0044-100920.

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AbstractSeventy-five glorious years have passed since estradiol was discovered by Edward Doisy. From discovery in the ovaries to delineation of diverse physiological effects, research on estrogens has covered a lot of ground. Estrogen receptors that mediate estrogenic effects, have been detected not only in reproductive organs, but also in other body organs. Estrogen receptors function either as conventional transcription factors or as rapid signal transducers. These different modes of action are opted by estrogens to elicit an array of reproductive and non-reproductive functions. It is well e
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4

Lee, Heehyoung, and Wenlong Bai. "Regulation of Estrogen Receptor Nuclear Export by Ligand-Induced and p38-Mediated Receptor Phosphorylation." Molecular and Cellular Biology 22, no. 16 (2002): 5835–45. http://dx.doi.org/10.1128/mcb.22.16.5835-5845.2002.

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ABSTRACT Estrogen receptors are phosphoproteins which can be activated by ligands, kinase activators, or phosphatase inhibitors. Our previous study showed that p38 mitogen-activated protein kinase was involved in estrogen receptor activation by estrogens and MEKK1. Here, we report estrogen receptor-dependent p38 activation by estrogens in endometrial adenocarcinoma cells and in vitro and in vivo phosphorylation of the estrogen receptor α mediated through p38. The phosphorylation site was identified as threonine-311 (Thr311), located in helix 1 of the hormone-binding domain. The mutation of thr
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5

Bernasochi, Gabriel B., James R. Bell, Evan R. Simpson, Lea M. D. Delbridge, and Wah Chin Boon. "Impact of Estrogens on the Regulation of White, Beige, and Brown Adipose Tissue Depots." Comprehensive Physiology 9, no. 2 (2019): 457–75. https://doi.org/10.1002/j.2040-4603.2019.tb00071.x.

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ABSTRACTAs adipose tissue depots are active endocrine organs, they secrete a variety of hormones (including estrogens from white adipose) and inflammatory mediators, which have important implications in numerous obesity‐associated diseases. Adipose tissues are broadly characterized as consisting of white, beige, and brown depot types. The endocrine, metabolic, and inflammatory profiles of adipose are depot dependent and influenced by the estrogenic and androgenic status of the adipose tissue. Estrogen receptors mediate both the genomic and nongenomic actions of estrogens and are expressed in t
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Lee, Richard R., and Karen P. Phillips. "Role of Estrogen Receptors in Male Reproductive Physiology." Revue interdisciplinaire des sciences de la santé - Interdisciplinary Journal of Health Sciences 3, no. 1 (2016): 40–45. http://dx.doi.org/10.18192/riss-ijhs.v3i1.1452.

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Canonical estrogen receptors (ER α/β) have a genomic mechanism of action, functioning as nuclear transcription factors for estrogen-dependent genes. Estrogen receptors are well established within the male reproductive tract with estrogen playing an essential role for male fertility. The recent characterization of novel G-protein coupled estrogen receptor GPR30 (alternatively known as GPER1), depending on non-genomic intracellular signaling pathways to transduce estrogenic signals, requires a re-examination of the roles of estrogen receptors in male reproduction. Further, the affinity of enviro
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7

Nilsson, Stefan, Sari Mäkelä, Eckardt Treuter, et al. "Mechanisms of Estrogen Action." Physiological Reviews 81, no. 4 (2001): 1535–65. http://dx.doi.org/10.1152/physrev.2001.81.4.1535.

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Our appreciation of the physiological functions of estrogens and the mechanisms through which estrogens bring about these functions has changed during the past decade. Just as transgenic mice were produced in which estrogen receptors had been inactivated and we thought that we were about to understand the role of estrogen receptors in physiology and pathology, it was found that there was not one but two distinct and functional estrogen receptors, now called ERα and ERβ. Transgenic mice in which each of the receptors or both the receptors are inactive have revealed a much broader role for estro
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8

Molina, Luis, Felipe A. Bustamante, Kanti D. Bhoola, Carlos D. Figueroa, and Pamela Ehrenfeld. "Possible role of phytoestrogens in breast cancer via GPER-1/GPR30 signaling." Clinical Science 132, no. 24 (2018): 2583–98. http://dx.doi.org/10.1042/cs20180885.

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Estrogens generated within endocrine organs and the reproductive system act as ligands for at least three types of estrogen receptors. Estrogen receptors α (ERα) and β (ERβ) belong to the so-called classical family of estrogen receptors, whereas the G protein-coupled receptor GPR30, also known as GPER-1, has been described as a novel estrogen receptor sited in the cell membrane of target cells. Furthermore, these receptors are under stimulation of a family of exogenous estrogens, known as phytoestrogens, which are a diverse group of non-steroidal plant compounds derived from plant food consume
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9

Wojnarowski, Konrad, Paulina Cholewińska, Dušan Palić, Małgorzata Bednarska, Magdalena Jarosz, and Iga Wiśniewska. "Estrogen Receptors Mediated Negative Effects of Estrogens and Xenoestrogens in Teleost Fishes—Review." International Journal of Molecular Sciences 23, no. 5 (2022): 2605. http://dx.doi.org/10.3390/ijms23052605.

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Estrogen receptors (ERs) play a key role in many biochemical and physiological processes, that are involved in maintaining organism homeostasis. At the most basic level, they can be divided into nuclear estrogen receptors and membrane estrogen receptors that imply their effect in two ways: slower genomic, and faster non-genomic. In these ways, estrogens and xenoestrogens can negatively affect animal health and welfare. Most of the available literature focuses on human and mammalian physiology, and clearly, we can observe a need for further research focusing on complex mutual interactions betwe
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10

De Giorgi, Vincenzo, Alessia Gori, Marta Grazzini, et al. "Estrogens, estrogen receptors and melanoma." Expert Review of Anticancer Therapy 11, no. 5 (2011): 739–47. http://dx.doi.org/10.1586/era.11.42.

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11

Vásárhelyi, Barna, Katalin Mészáros, Gellért Karvaly, and Attila Patócs. "Fókuszban a szöveti biomarkerek. Az ösztrogének mint a szövetspecifikus immunválasz és autoimmunitás modulálásának kulcsszereplői." Orvosi Hetilap 156, no. 51 (2015): 2070–76. http://dx.doi.org/10.1556/650.2015.30317.

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Estrogens modulate the immune response as well as the risk and progression of autoimmune disorders. Their effects are mediated by nuclear receptors (i.e. estrogen receptor alpha and beta), membrane receptors, and are influenced by their interactions with other hormones. Locally produced hormones and cytokines are the main factors in maintaining tissue homeostasis. The response of immune cells to estrogens is related to their developmental stage. The diverse effects of estrogens on various autoimmune disorders are the result of the versatility of their pathomechanism. In general, progression of
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12

Maitra, Radhashree, Parth Malik, and Tapan Kumar Mukherjee. "Targeting Estrogens and Various Estrogen-Related Receptors against Non-Small Cell Lung Cancers: A Perspective." Cancers 14, no. 1 (2021): 80. http://dx.doi.org/10.3390/cancers14010080.

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Non-small cell lung cancers (NSCLCs) account for ~85% of lung cancer cases worldwide. Mammalian lungs are exposed to both endogenous and exogenous estrogens. The expression of estrogen receptors (ERs) in lung cancer cells has evoked the necessity to evaluate the role of estrogens in the disease progression. Estrogens, specifically 17β-estradiol, promote maturation of several tissue types including lungs. Recent epidemiologic data indicate that women have a higher risk of lung adenocarcinoma, a type of NSCLC, when compared to men, independent of smoking status. Besides ERs, pulmonary tissues bo
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13

Lazari, Maria Fatima Magalhães, Thais Fabiana Gameiro Lucas, Fabiana Yasuhara, et al. "Estrogen receptors and function in the male reproductive system." Arquivos Brasileiros de Endocrinologia & Metabologia 53, no. 8 (2009): 923–33. http://dx.doi.org/10.1590/s0004-27302009000800005.

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A substantial advance in our understanding on the estrogen signaling occurred in the last decade. Estrogens interact with two receptors, ESR1 and ESR2, also known as ERα and ERβ, respectively. ESR1 and ESR2 belong to the nuclear receptor family of transcription factors. In addition to the well established transcriptional effects, estrogens can mediate rapid signaling, triggered within seconds or minutes. These rapid effects can be mediated by ESRs or the G protein-coupled estrogen receptor GPER, also known as GPR30. The effects of estrogen on cell proliferation, differentiation and apoptosis a
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14

Prins, Gail S., Lynn Birch, Helga Habermann, et al. "Influence of neonatal estrogens on rat prostate development." Reproduction, Fertility and Development 13, no. 4 (2001): 241. http://dx.doi.org/10.1071/rd00107.

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Brief exposure of rodents to estrogens during early development alters prostate branching morphogenesis and cellular differentiation in a dose-dependant manner. If estrogenic exposures are high, these disturbances lead to permanent imprints of the prostate, which include reduced growth, differentiation defects of the epithelial cells, altered secretory function and reduced responsiveness to androgens in adulthood. This process, referred to as neonatal imprinting or developmental estrogenization, is associated with an increased incidence of prostatic lesions with aging, which include hyperplasi
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15

Berger, Trish, Valerie Guerrero, Rosalina Boeldt, Erin Legacki, Megan Roberts, and Alan J. Conley. "Development of Porcine Accessory Sex Glands." Animals 14, no. 3 (2024): 462. http://dx.doi.org/10.3390/ani14030462.

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Accessory sex glands are recognized as targets of human disease and may have roles in reproductive success in livestock. The current experiments evaluated the influences of endogenous steroids on the development of porcine accessory sex glands, primarily in the neonatal period. When the aromatase inhibitor, letrozole, was used to inhibit the production of endogenous estrogens in the postnatal interval, growth of the seminal vesicles, prostate, and bulbourethral glands was stimulated. The weights of seminal vesicles, prostate, and bulbourethral glands approximately doubled at 6.5 weeks of age w
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16

Mérot, Yohann, François Ferrière, Edith Debroas, Gilles Flouriot, Dominique Duval, and Christian Saligaut. "Estrogen receptor alpha mediates neuronal differentiation and neuroprotection in PC12 cells: critical role of the A/B domain of the receptor." Journal of Molecular Endocrinology 35, no. 2 (2005): 257–67. http://dx.doi.org/10.1677/jme.1.01826.

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Numerous studies, both in vivo and in vitro, have reported neuronal differentiating and neuroprotective actions of estrogens. Most of these estrogenic effects are mediated through specific receptors termed estrogen receptors. The aim of this study was to assess the importance of the N-terminal A/B domain of the estrogen receptor-alpha (ERα) in its neuronal aspects. Consequently, estrogen effects on (i) the transcriptional activity of target genes, (ii) neuronal differentiation and (iii) neuroprotection in PC12 cells transfected with either a full length form of ERα or an A/B domain truncated f
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17

Diez-Perez, Adolfo. "Selective estrogen receptor modulators (SERMS)." Arquivos Brasileiros de Endocrinologia & Metabologia 50, no. 4 (2006): 720–34. http://dx.doi.org/10.1590/s0004-27302006000400017.

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Hormone receptors and, specifically, estrogen receptors were described about four decades ago. For estrogens, there are two receptors, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta). The two receptors are coded by different genes and their tissue expression varies across organs. ERalpha is predominantly expressed in reproductive tissues (uterus, breast, ovaries) liver and central nervous system, whereas ERbeta is expressed in other tissues such as bone, endothelium, lungs, urogenital tract, ovaries, central nervous system and prostate. More than seventy molecules that be
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18

Kozieł, Marta Justyna, and Agnieszka Wanda Piastowska-Ciesielska. "Estrogens, Estrogen Receptors and Tumor Microenvironment in Ovarian Cancer." International Journal of Molecular Sciences 24, no. 19 (2023): 14673. http://dx.doi.org/10.3390/ijms241914673.

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Ovarian cancer is one of the most common cancers in women and the most concerning issues in gynecological oncology in recent years. It is postulated that many factors may contribute to the development of ovarian cancer, including hormonal imbalance. Estrogens are a group of hormones that have an important role both in physiological and pathological processes. In ovarian cancer, they may regulate proliferation, invasiveness and epithelial to mesenchymal transition. Estrogen signaling also takes part in the regulation of the biology of the tumor microenvironment. This review summarizes the infor
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Bai, Jin, Qian-Rong Qi, Yan Li, et al. "Estrogen Receptors and Estrogen-Induced Uterine Vasodilation in Pregnancy." International Journal of Molecular Sciences 21, no. 12 (2020): 4349. http://dx.doi.org/10.3390/ijms21124349.

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Normal pregnancy is associated with dramatic increases in uterine blood flow to facilitate the bidirectional maternal–fetal exchanges of respiratory gases and to provide sole nutrient support for fetal growth and survival. The mechanism(s) underlying pregnancy-associated uterine vasodilation remain incompletely understood, but this is associated with elevated estrogens, which stimulate specific estrogen receptor (ER)-dependent vasodilator production in the uterine artery (UA). The classical ERs (ERα and ERβ) and the plasma-bound G protein-coupled ER (GPR30/GPER) are expressed in UA endothelial
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20

Zhong, Ling Ying, Xiao Xiang, Jing Ye, et al. "Application of the MCF-7 Breast Cancer Cells in Endocrine-Disrupting Area." Advanced Materials Research 955-959 (June 2014): 928–35. http://dx.doi.org/10.4028/www.scientific.net/amr.955-959.928.

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MCF-7 breast cancer cell line was first developed by Dr. Herbert Soule from a pleural effusion taken from a patient with metastatic breast cancer. This estrogen-responsive and estrogen receptor containing cell line can also express androgen, progesterone, glucocorticoid and retinoid receptors. It has been extensively used in identifying environmental estrogens and exploring the toxicity mechanisms, as well as the pathologic study and the disease treatment. This mini review article will focus on the development and application of MCF-7 cells in endocrine-disrupting area, especially in study of
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21

Hall, Keith A., and Edward J. Filardo. "The G Protein-Coupled Estrogen Receptor (GPER): A Critical Therapeutic Target for Cancer." Cells 12, no. 20 (2023): 2460. http://dx.doi.org/10.3390/cells12202460.

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Estrogens have been implicated in the pathogenesis of various cancers, with increasing concern regarding the overall rising incidence of disease and exposure to environmental estrogens. Estrogens, both endogenous and environmental, manifest their actions through intracellular and plasma membrane receptors, named ERα, ERβ, and GPER. Collectively, they act to promote a broad transcriptional response that is mediated through multiple regulatory enhancers, including estrogen response elements (EREs), serum response elements (SREs), and cyclic AMP response elements (CREs). Yet, the design and ratio
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Lizcano, Fernando, and Guillermo Guzmán. "Estrogen Deficiency and the Origin of Obesity during Menopause." BioMed Research International 2014 (2014): 1–11. http://dx.doi.org/10.1155/2014/757461.

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Sex hormones strongly influence body fat distribution and adipocyte differentiation. Estrogens and testosterone differentially affect adipocyte physiology, but the importance of estrogens in the development of metabolic diseases during menopause is disputed. Estrogens and estrogen receptors regulate various aspects of glucose and lipid metabolism. Disturbances of this metabolic signal lead to the development of metabolic syndrome and a higher cardiovascular risk in women. The absence of estrogens is a clue factor in the onset of cardiovascular disease during the menopausal period, which is cha
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Nalvarte, Ivan, and Per Antonson. "Estrogen Receptor Knockout Mice and Their Effects on Fertility." Receptors 2, no. 1 (2023): 116–26. http://dx.doi.org/10.3390/receptors2010007.

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Estrogens play a crucial role in sexual development and fertility as well as many other physiological processes, and it is estrogen receptors that mediate the physiological responses. To study the role of the estrogen receptors in these processes, several genetic mouse models have been developed using different strategies, which also in some cases yield different results. Here, we summarize the models that have been made and their impact on fertility in relation to known cases of human estrogen receptor mutations.
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Sulliman, Entesar A., Maher A. Ibrahim, Ammar Ibrahim, and Raghad Fadhel Jasim. "Molecular Docking Study on Tamoxifen and Toremifene's Effects on the Breast Cancer Receptors." Turkish Computational and Theoretical Chemistry 8, no. 4 (2024): 62–69. http://dx.doi.org/10.33435/tcandtc.1400422.

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Both toremifene (TOR) and tamoxifen (TAM), selective estrogen receptor modulators, are equally effective therapies for breast cancer (BrCa). In high-risk women, anti-estrogenic tamoxifen is frequently used for both (BrCa) treatment and prevention. Another anti-estrogen that is successful in the treatment of (BrCa) is toremifene. Anti-estrogens have emerged as one of the most widely utilized medicine classes among women because (BrCa) is the most frequent malignancy in this population. Consequently, we performed a docking study to assess the effects of tamoxifen and toremifene therapy on the (B
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Morselli, Eugenia, Roberta de Souza Santos, Su Gao та ін. "Impact of estrogens and estrogen receptor-α in brain lipid metabolism". American Journal of Physiology-Endocrinology and Metabolism 315, № 1 (2018): E7—E14. http://dx.doi.org/10.1152/ajpendo.00473.2017.

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Estrogens and their receptors play key roles in regulating body weight, energy expenditure, and metabolic homeostasis. It is known that lack of estrogens promotes increased food intake and induces the expansion of adipose tissues, for which much is known. An area of estrogenic research that has received less attention is the role of estrogens and their receptors in influencing intermediary lipid metabolism in organs such as the brain. In this review, we highlight the actions of estrogens and their receptors in regulating their impact on modulating fatty acid content, utilization, and oxidation
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Alonso, de Leciñana María, and Jose Antonio Egido. "Estrogens as neuroprotectants against ischemic stroke." Cerebrovascular Diseases 21, Suppl 2 (2006): 48–53. https://doi.org/10.1159/000091703.

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Estrogens have proven vasoprotective properties against atherosclerosis that depend on the direct effect on vascular smooth muscle and endothelium and on systemic actions that imply serum lipids, coagulation and fibrinolytic cascades, vasoactive proteins and antioxidant systems. They also have neuroprotective effects against cerebral ischemia that include antioxidant and anti-inflammatory effects, modulation of protein synthesis, inhibition of apoptosis and trophic effects and preservation of microvascular blood flow in the ischemic area. Estrogenic actions depend on activation of specific est
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Elloso, M. Merle, Kristen Phiel, Ruth A. Henderson, Heather A. Harris, and Steven J. Adelman. "Suppression of experimental autoimmune encephalomyelitis using estrogen receptor-selective ligands." Journal of Endocrinology 185, no. 2 (2005): 243–52. http://dx.doi.org/10.1677/joe.1.06063.

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Estrogens have been shown to modulate disease activity in experimental autoimmune encephalomyelitis (EAE), the mouse model for multiple sclerosis. Consistent with these findings, the severity of disease is reduced in pregnant women with multiple sclerosis when levels of estrogens are high. Estrogens bind to two known estrogen receptors (ER), ERα and ERβ. The relative contribution of these receptors to estrogen-mediated suppression of EAE was explored using ER-selective ligands. The ER antagonist ICI 182 780 reversed the suppressive effects of 17β-estradiol (E2), demonstrating that the protecti
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POTIER, MYLENE, SHARON J. ELLIOT, IVAN TACK, et al. "Expression and Regulation of Estrogen Receptors in Mesangial Cells: Influence on Matrix Metalloproteinase-9." Journal of the American Society of Nephrology 12, no. 2 (2001): 241–51. http://dx.doi.org/10.1681/asn.v122241.

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Abstract. Diabetic glomerulosclerosis is characterized by the accumulation of extracellular matrix (ECM) in the mesangium. Estrogens seem to retard whereas estrogen deficiency seems to accelerate progressive glomerulosclerosis. Thus, mesangial cells (MC) may be a target for estrogens. Estrogen action is mediated via estrogen receptor (ER) subtypes ERα and ERβ. Both ER subtypes were expressed in human and mouse MC. Using an estrogen-responsive reporter construct in transfection assays, it also was demonstrated that the nuclear ER were transcriptionally active. In the presence of 17β-estradiol (
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Honma, Naoko, Yoko Matsuda, and Tetuo Mikami. "Carcinogenesis of Triple-Negative Breast Cancer and Sex Steroid Hormones." Cancers 13, no. 11 (2021): 2588. http://dx.doi.org/10.3390/cancers13112588.

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Triple-negative breast cancer (TNBC) lacks an effective treatment target and is usually associated with a poor clinical outcome; however, hormone unresponsiveness, which is the most important biological characteristic of TNBC, only means the lack of nuclear estrogenic signaling through the classical estrogen receptor (ER), ER-α. Several sex steroid receptors other than ER-α: androgen receptor (AR), second ER, ER-β, and non-nuclear receptors represented by G-protein-coupled estrogen receptor (GPER), are frequently expressed in TNBC and their biological and clinical importance has been suggested
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Schüler-Toprak, Susanne, Maciej Skrzypczak, Carsten Gründker, Olaf Ortmann та Oliver Treeck. "Role of Estrogen Receptor β, G-Protein Coupled Estrogen Receptor and Estrogen-Related Receptors in Endometrial and Ovarian Cancer". Cancers 15, № 10 (2023): 2845. http://dx.doi.org/10.3390/cancers15102845.

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Ovarian and endometrial cancers are affected by estrogens and their receptors. It has been long known that in different types of cancers, estrogens activate tumor cell proliferation via estrogen receptor α (ERα). In contrast, the role of ERs discovered later, including ERβ and G-protein-coupled ER (GPER1), in cancer is less well understood, but the current state of knowledge indicates them to have a considerable impact on both cancer development and progression. Moreover, estrogen related receptors (ERRs) have been reported to affect pathobiology of many tumor types. This article provides a su
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Katsu, Yoshinao, Kaoru Kubokawa, Hiroshi Urushitani, and Taisen Iguchi. "Estrogen-Dependent Transactivation of Amphioxus Steroid Hormone Receptor via Both Estrogen and Androgen Response Elements." Endocrinology 151, no. 2 (2010): 639–48. http://dx.doi.org/10.1210/en.2009-0766.

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Estrogens are necessary for ovarian differentiation during critical developmental windows in most vertebrates and promote the growth and differentiation of the adult female reproductive system. Estrogen actions are largely mediated through the estrogen receptors (ERs), which are ligand-activated transcription factors. To understand the molecular evolution of sex steroid hormone receptors, we isolated cDNAs encoding two steroid receptors from Japanese amphioxus, Branchiostoma belcheri: an ER ortholog and a ketosteroid receptor (SR) ortholog. Reporter gene assays revealed that the SR ortholog ha
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Pentikäinen, Virve, Krista Erkkilä, Laura Suomalainen, Martti Parvinen, and Leo Dunkel. "Estradiol Acts as a Germ Cell Survival Factor in the Human Testis in Vitro*." Journal of Clinical Endocrinology & Metabolism 85, no. 5 (2000): 2057–67. http://dx.doi.org/10.1210/jcem.85.5.6600.

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Abstract The necessity of estrogens for male fertility was recently discovered in studies on both estrogen receptor α knockout and aromatase (cyp 19 gene) knockout mice. However, direct testicular effects of estrogens in male reproduction have remained unclear. Here we studied the protein expression of ERα and the recently described estrogen receptor β in the human seminiferous epithelium and evaluated the role of 17β-estradiol, the main physiological estrogen, in male germ cell survival. Interestingly, both estrogen receptors α and β were found in early meiotic spermatocytes and elongating sp
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Abramenko, Nikita, Fréderic Vellieux, Petra Tesařová, et al. "Estrogen Receptor Modulators in Viral Infections Such as SARS−CoV−2: Therapeutic Consequences." International Journal of Molecular Sciences 22, no. 12 (2021): 6551. http://dx.doi.org/10.3390/ijms22126551.

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COVID-19 is a pandemic respiratory disease caused by the SARS−CoV−2 coronavirus. The worldwide epidemiologic data showed higher mortality in males compared to females, suggesting a hypothesis about the protective effect of estrogens against severe disease progression with the ultimate end being patient’s death. This article summarizes the current knowledge regarding the potential effect of estrogens and other modulators of estrogen receptors on COVID-19. While estrogen receptor activation shows complex effects on the patient’s organism, such as an influence on the cardiovascular/pulmonary/immu
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Tsialtas, Ioannis, Achilleas Georgantopoulos, Maria E. Karipidou, et al. "Anti-Apoptotic and Antioxidant Activities of the Mitochondrial Estrogen Receptor Beta in N2A Neuroblastoma Cells." International Journal of Molecular Sciences 22, no. 14 (2021): 7620. http://dx.doi.org/10.3390/ijms22147620.

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Estrogens are steroid hormones that play a crucial role in the regulation of the reproductive and non-reproductive system physiology. Among non-reproductive systems, the nervous system is mainly affected by estrogens due to their antioxidant, anti-apoptotic, and anti-inflammatory activities, which are mediated by membranous and nuclear estrogen receptors, and also by non-estrogen receptor-associated estrogen actions. Neuronal viability and functionality are also associated with the maintenance of mitochondrial functions. Recently, the localization of estrogen receptors, especially estrogen rec
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Kopylova, I. V., V. Yu Sysoeva, T. M. Glybina, and M. A. Kareva. "Expression of estrogen and androgen receptors in tissues of external genitalia of girls with congenital adrenal hyperplasia." Problems of Endocrinology 60, no. 6 (2014): 14–20. http://dx.doi.org/10.14341/probl201460614-20.

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The reason of post-operative introital stenosis in girls with CAH is a poor estrogenization of external genitalia before vaginoplasty. It is possible that the local sensitivity to estrogens can be reduced due to prenatal androgen excess in addition to inadequate compensation, which results to decrease of estrogens production by the ovaries. Objective. To determine the distribution of estrogen and androgen receptors in genital tissue, depending on the form of CAH, the degree of external virilization and serum levels of androgens. Material and methods. The waste surgical tissues obtained during
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Cooke, Paul S., Manjunatha K. Nanjappa, CheMyong Ko, Gail S. Prins, and Rex A. Hess. "Estrogens in Male Physiology." Physiological Reviews 97, no. 3 (2017): 995–1043. http://dx.doi.org/10.1152/physrev.00018.2016.

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Estrogens have historically been associated with female reproduction, but work over the last two decades established that estrogens and their main nuclear receptors (ESR1 and ESR2) and G protein-coupled estrogen receptor (GPER) also regulate male reproductive and nonreproductive organs. 17β-Estradiol (E2) is measureable in blood of men and males of other species, but in rete testis fluids, E2 reaches concentrations normally found only in females and in some species nanomolar concentrations of estrone sulfate are found in semen. Aromatase, which converts androgens to estrogens, is expressed in
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de Andrés, Paloma Jimena, Sara Cáceres, Juan Carlos Illera, et al. "Hormonal Homologies between Canine Mammary Cancer and Human Breast Cancer in a Series of Cases." Veterinary Sciences 9, no. 8 (2022): 395. http://dx.doi.org/10.3390/vetsci9080395.

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The validity of spontaneous canine mammary cancer (CMC) as a natural model for the study of human breast cancer (HBC) from a hormonal point of view has never been thoroughly investigated. In this study, we analyzed the immunohistochemical expression of aromatase (Arom) and steroid receptors [estrogen receptor α (ER α), estrogen receptor β (ER β), progesterone receptor (PR) and androgen receptor (AR)] and intratumor steroid hormone levels of 17β-estradiol (E2), estrone sulfate (SO4E1), progesterone (P4), androstenedione (A4), dehydroepiandrosterone (DHEA), and testosterone (T) in 78 samples of
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Safe, Stephen H., Lea Pallaroni, Kyungsil Yoon, et al. "Toxicology of environmental estrogens." Reproduction, Fertility and Development 13, no. 4 (2001): 307. http://dx.doi.org/10.1071/rd00108.

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It has been hypothesized that environmental contaminants that modulate endocrine signaling pathways may be causally linked to adverse health effects in humans. There has been particular concern regarding synthetic estrogens and their role in disrupting normal development of the male reproductive tract. Most estrogenic industrial compounds, such as bisphenol A (BPA) and nonylphenol, typically bind estrogen receptors α (ERα) and β (ERβ) and induce transactivation of estrogen-responsive genes/reporter genes, but their potencies are usually ≥1000-fold lower than observed for 17β-estradiol (E2). Se
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McEwen, Bruce S. "Invited Review: Estrogens effects on the brain: multiple sites and molecular mechanisms." Journal of Applied Physiology 91, no. 6 (2001): 2785–801. http://dx.doi.org/10.1152/jappl.2001.91.6.2785.

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Besides their well-established actions on reproductive functions, estrogens exert a variety of actions on many regions of the nervous system that influence higher cognitive function, pain mechanisms, fine motor skills, mood, and susceptibility to seizures; they also appear to have neuroprotective actions in relation to stroke damage and Alzheimer's disease. Estrogen actions are now recognized to occur via two different intracellular estrogen receptors, ER-α and ER-β, that reside in the cell nuclei of some nerve cells, as well as by some less well-characterized mechanisms. In the hippocampus, s
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Walters, M. J., T. J. Brown, R. B. Hochberg, and N. J. MacLusky. "In vitro autoradiographic visualization of occupied estrogen receptors in the rat brain with an iodinated estrogen ligand." Journal of Histochemistry & Cytochemistry 41, no. 9 (1993): 1279–90. http://dx.doi.org/10.1177/41.9.8354873.

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Methods have been developed for the selective measurement of occupied estrogen receptors (ER) in brain tissue sections. Cryostat sections of unfixed tissue were incubated with radiolabeled estrogen at physiological temperatures, displacing endogenous receptor-bound estrogen by radioligand and thereby allowing the receptor complexes to be visualized autoradiographically after washing to remove nonspecifically bound steroid. The resultant autoradiographs were analyzed by computer-assisted densitometry. Synthetic 11 beta-methoxy-substituted radiolabeled estrogens gave the best autoradiographic im
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Nikov, GN, M. Eshete, RV Rajnarayanan, and WL Alworth. "Interactions of synthetic estrogens with human estrogen receptors." Journal of Endocrinology 170, no. 1 (2001): 137–45. http://dx.doi.org/10.1677/joe.0.1700137.

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Synthetic estrogens have diverse chemical structures and may either positively or negatively affect the estrogenic signaling pathways through interactions with the estrogen receptors (ERs). Modeling studies suggest that 4-(1-adamantyl)phenol (AdP) and 4,4'-(1,3-adamantanediyl)diphenol (AdDP) can bind in the ligand binding site of ERalpha. We used fluorescence polarization (FP) to compare the binding affinities of AdP, AdDP and 2-(1-adamantyl)-4-methylphenol (AdMP) for human ERalpha and ERbeta with the binding affinities of the known ER ligands, diethylstilbestrol (DES) and 4hydroxytamoxifen (4
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42

Pakdel, Farzad. "The Role of Estrogen Receptors in Health and Disease." International Journal of Molecular Sciences 24, no. 14 (2023): 11354. http://dx.doi.org/10.3390/ijms241411354.

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Many biological and physiological events, including growth, development, and metabolism of reproductive and non-reproductive tissues in men and women, are regulated by estrogens and estrogen receptors (ERs) [...]
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43

Todiodi, Mina. "The Effects of Exogenous Estrogens on Estrogen Receptors in Male Reproductive Organs." Revue interdisciplinaire des sciences de la santé - Interdisciplinary Journal of Health Sciences 1, no. 1 (2010): 66. http://dx.doi.org/10.18192/riss-ijhs.v1i1.1537.

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There is an essential physiological role for estrogen in male reproduction. Conversely, exposure to exogenous sources of estrogen has negative effects on reproductive physiology and fertility in men. Infertility, affecting nearly 15% of couples, is defined as the inability to conceive after one year of unprotected sexual intercourse. In at least 20% of cases, male reproductive pathology is the major cause for a couple’s infertility. Thus, it is essential to investigate potential causes of infertility in adult males. Evidence shows that exposure to certain endocrine disruptors is associated wit
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Stell, Alessia, Silvia Belcredito, Paolo Ciana, and Adriana Maggi. "Molecular Imaging Provides Novel Insights on Estrogen Receptor Activity in Mouse Brain." Molecular Imaging 7, no. 6 (2008): 7290.2008.00027. http://dx.doi.org/10.2310/7290.2008.00027.

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Estrogen receptors have long been known to be expressed in several brain areas in addition to those directly involved in the control of reproductive functions. Investigations in humans and in animal models suggest a strong influence of estrogens on limbic and motor functions, yet the complexity and heterogeneity of neural tissue have limited our approaches to the full understanding of estrogen activity in the central nervous system. The aim of this study was to examine the transcriptional activity of estrogen receptors in the brain of male and female mice. Exploiting the ERE-Luc reporter mouse
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Caerts, Diet, Maria Garmyn, and Canan Güvenç. "A Narrative Review of the Role of Estrogen (Receptors) in Melanoma." International Journal of Molecular Sciences 25, no. 11 (2024): 6251. http://dx.doi.org/10.3390/ijms25116251.

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In this narrative review, we attempt to provide an overview of the evidence regarding the role of estrogen (receptors) in cutaneous melanoma (CM). We reviewed 68 studies and 4 systematic reviews and meta-analyses published from 2002 up to and including 2022. The prevailing presence of estrogen receptor β (ERβ) instead of estrogen receptor α (ERα) in CM is notable, with ERβ potentially playing a protective role and being less frequently detected in progressive cases. While men with CM generally experience a less favorable prognosis, this distinction may become negligible with advancing age. The
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Martin-Jiménez, Cynthia, Diana Milena Gaitán-Vaca, Natalia Areiza, et al. "Astrocytes Mediate Protective Actions of Estrogenic Compounds after Traumatic Brain Injury." Neuroendocrinology 108, no. 2 (2018): 142–60. http://dx.doi.org/10.1159/000495078.

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Traumatic brain injury (TBI) is a serious public health problem. It may result in severe neurological disabilities and in a variety of cellular metabolic alterations for which available therapeutic strategies are limited. In the last decade, the use of estrogenic compounds, which activate protective mechanisms in astrocytes, has been explored as a potential experimental therapeutic approach. Previous works have suggested estradiol (E2) as a neuroprotective hormone that acts in the brain by binding to estrogen receptors (ERs). Several steroidal and nonsteroidal estrogenic compounds can imitate
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Kareva, E. N., О. M. Oleynikova, V. O. Panov, N. L. Shimanovskiy, and V. I. Skvortsova. "ESTROGENS AND BRAIN." Annals of the Russian academy of medical sciences 67, no. 2 (2012): 48–59. http://dx.doi.org/10.15690/vramn.v67i2.122.

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Recent data upon molecular mechanisms of pleiotropic action of estrogens in human brain is presented in the article. Given detailed descriptions of properties of classical and membrane bound estradiol receptors, that maintain gene expression regulation, modulation of neurotransmittent systems and signal cascade activation in neuronal cells. Data upon regional distribution of estradiol receptor subtypes in the brain, their participation in main cell population function control (including progenitor cells) is given. Special attention is paid to estrogen participation in neurogenesis, inflammatio
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Nadal, Angel, Mario Díaz, and Miguel A. Valverde. "The Estrogen Trinity: Membrane, Cytosolic, and Nuclear Effects." Physiology 16, no. 6 (2001): 251–55. http://dx.doi.org/10.1152/physiologyonline.2001.16.6.251.

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Estrogens have a wide array of biological effects, targeting both genomic and nongenomic mechanisms. Classically, the estrogen receptors activating the transcription machinery in the nucleus were thought to be distinct from the extranuclear estrogen receptors. Recently, this conceptual wall has started to be dismantled as the result of the identification of novel routes of estrogen action.
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Jensen, Elwood V. "The Contribution of “Alternative Approaches” to Understanding Steroid Hormone Action." Molecular Endocrinology 19, no. 6 (2005): 1439–42. http://dx.doi.org/10.1210/me.2005-0154.

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Abstract In the 47 yr since the first evidence for a steroid hormone receptor was presented at an international congress to an audience of five persons, the concept of “alternative approach” has played an important role in providing new understanding. By asking not what does an estrogenic hormone do to cellular processes in responsive tissues but what do these cells do to the hormone, it was shown that rat uterus contains a characteristic protein with which the hormone associates to promote growth. In the following decade, it was established that this substance is a true receptor, involved in
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50

Keay, June, Jamie T. Bridgham, and Joseph W. Thornton. "The Octopus vulgaris Estrogen Receptor Is a Constitutive Transcriptional Activator: Evolutionary and Functional Implications." Endocrinology 147, no. 8 (2006): 3861–69. http://dx.doi.org/10.1210/en.2006-0363.

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Steroid hormones such as estrogens and androgens are important regulators of reproduction, physiology, and development in a variety of animal taxa, including vertebrates and mollusks. Steroid hormone receptors, which mediate the classic cellular responses to these hormones, were thought to be vertebrate specific, which left the molecular mechanisms of steroid action in invertebrates unresolved. Recently an estrogen receptor (ER) ortholog was isolated from the sea hare Aplysia californica, but the functional significance of the receptor was unclear because estrogens and other steroids are not k
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