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https://www.readbyqxmd.com/read/28061972/estrogen-receptors-modulation-of-anxiety-like-behavior
#1
A P Borrow, R J Handa
Estrogens exert profound effects on the expression of anxiety in humans and rodents; however, the directionality of these effects varies considerably within both clinical and preclinical literature. It is believed that discrepancies regarding the nature of estrogens' effects on anxiety are attributable to the differential effects of specific estrogen receptor (ER) subtypes. In this chapter we will discuss the relative impact on anxiety and anxiety-like behavior of each of the three main ERs: ERα, which has a generally anxiogenic effect, ERβ, which has a generally anxiolytic effect, and the G-protein-coupled ER known as GPR30, which has been found to both increase and decrease anxiety-like behavior...
2017: Vitamins and Hormones
https://www.readbyqxmd.com/read/28060756/baicalein-has-protective-effects-on-the-17%C3%AE-estradiol-induced-transformation-of-breast-epithelial-cells
#2
Yan Chen, Jing Wang, Duan-Yang Hong, Lin Chen, Yan-Yan Zhang, Yi-Ni Xu, Di Pan, Ling-Yun Fu, Ling Tao, Hong Luo, Xiang-Chun Shen
Epidemiologic and systematic studies have indicated that flavonoid consumption is associated with a lower incidence of breast cancer. Baicalein is the primary flavonoid derived from the roots of Scutellaria baicalensis Georgi. In the current study, the long-term exposure of breast epithelial cells to 17β-estradiol (E2) was used to investigate the chemopreventive potential of baicalein on neoplastic transformation. The results demonstrated that baicalein significantly inhibited E2-induced cell growth, motility, and invasiveness, and suppressed E2-induced misshapen acini formation in 3D cultures...
January 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28007532/role-of-g-protein-coupled-estrogen-receptor-gper-gpr30-in-maintenance-of-meiotic-arrest-in-fish-oocytes
#3
REVIEW
Peter Thomas
An essential role for GPER (formerly known as GPR30) in regulating mammalian reproduction has not been identified to date, although it has shown to be involved in the regulation a broad range of other estrogen-dependent functions. In contrast, an important reproductive role for GPER in the maintenance of oocyte meiotic arrest has been identified in teleost fishes, which is briefly reviewed here. Recent studies have clearly shown that ovarian follicle production of estradiol-17β (E2) maintains meiotic arrest in several teleost species through activation of GPER coupled to a stimulatory G protein (Gs) on oocyte plasma membranes resulting in stimulation of cAMP production and maintenance of elevated cAMP levels...
December 19, 2016: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/27959426/17%C3%AE-estradiol-induced-growth-of-triple-negative-breast-cancer-cells-is-prevented-by-the-reduction-of-gper-expression-after-treatment-with-gefitinib
#4
Rainer Girgert, Günter Emons, Carsten Gründker
Triple-negative breast cancers (TNBCs) are neither susceptible to endocrine therapy due to a lack of estrogen receptor α expression nor trastuzumab. TNBCs frequently overexpress epidermal growth factor receptor (EGFR) and membrane bound estrogen receptor, GPER. To a certain extent the growth of TNBCs is stimulated by 17β-estradiol via GPER. We analyzed whether inhibition of EGFR by gefitinib reduces the expression of GPER and subsequent signal transduction in TNBC cells. Dependence of proliferation on 17β-estradiol was determined using Alamar Blue assay...
December 8, 2016: Oncology Reports
https://www.readbyqxmd.com/read/27939762/estrogen-stabilizes-hypoxia-inducible-factor-1%C3%AE-through-g-protein-coupled-estrogen-receptor-1-in-eutopic-endometrium-of-endometriosis
#5
Ling Zhang, Wenqian Xiong, Na Li, Hengwei Liu, Haitang He, Yu Du, Zhibing Zhang, Yi Liu
OBJECTIVE: To investigate whether G protein-coupled estrogen receptor (GPER, also known as GPR30 and GPER1) stabilizes hypoxia-inducible factor 1α (HIF-1α) in eutopic endometrium (EuEM) of endometriosis. DESIGN: Immunohistochemical analysis and experimental in vitro study. SETTING: University hospital. PATIENT(S): Patients with or without endometriosis. INTERVENTION(S): The EuEM and normal control endometrium (CoEM) were obtained by curettage...
December 8, 2016: Fertility and Sterility
https://www.readbyqxmd.com/read/27908592/activation-of-gpr30-stimulates-gtp-binding-of-g%C3%AE-i1-protein-to-sustain-activation-of-erk1-2-in-inhibition-of-prostate-cancer-cell-growth-and-modulates-metastatic-properties
#6
Kin-Mang Lau, Fanny Man-Ting Ma, Jenny Tian Xia, Queeny Kwan Yi Chan, Chi-Fai Ng, Ka-Fai To
Previously, we reported that GPR30 activation by the receptor-specific, non-estrogenic ligand G-1 inhibited in vitro and in vivo growth of prostate cancer (PCa) cells via sustained Erk1/2 activation. Mechanism underlying the sustained Erk1/2 activation for PCa cell growth inhibition remains unclear. Here we report that G-1, through GPR30, activated Gαi1 proteins to sustain Erk1/2 activation but failed to activate adenylyl cyclase (AC) for cAMP production in PCa cells. The chemical-induced activation of AC-cAMP-PKA signaling attenuated Erk1/2 activity and blocked the cell growth inhibitory effects of G-1...
January 1, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/27889612/tet1-gper-pi3k-akt-pathway-is-involved-in-insulin-driven-endometrial-cancer-cell-proliferation
#7
Bing-Ying Xie, Qiao-Ying Lv, Cheng-Cheng Ning, Bing-Yi Yang, Wei-Wei Shan, Ya-Li Cheng, Chao Gu, Xue-Zhen Luo, Zhen-Bo Zhang, Xiao-Jun Chen, Xiao-Wei Xi, You-Ji Feng
Large amount of clinical evidence has demonstrated that insulin resistance is closely related to oncogenesis of endometrial cancer (EC). Despite recent studies showed the up-regulatory role of insulin in G protein-coupled estrogen receptor (GPER/GPR30) expression, GPER expression was not decreased compared to control when insulin receptor was blocked even in insulin treatment. The purpose of this study was to explore the possible mechanism by which insulin up-regulates GPER that drives EC cell proliferation...
November 23, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27888566/functional-expression-of-g-protein-coupled-receptor-30-in-immature-rat-epididymal-epithelium
#8
Xiaonian Cao, Jiehong Huang, Geng Zhang, Wulin Zuo, Chongfeng Lan, Qing Sun, Dengliang Yang, Dongdong Gao, Christopher H K Cheng, Wen-Liang Zhou
The aim of this study is to investigate the functional role of G protein-coupled receptor 30 (GPR30) in the epididymis. We found that GPR30 is expressed in the epithelium of the immature rat epididymis and is involved in chloride secretion into the caudal epididymis lumen. The short-circuit current (Isc) experiments showed that in primary cultured caudal epididymis epithelium, activation of GPR30 by its specific agonist G1 induced a mono-phasic current increase, and G15, the specific antagonist of GPR30, could completely inhibit the current induced by G1...
November 26, 2016: Cell Biology International
https://www.readbyqxmd.com/read/27880919/activation-of-g-protein-coupled-receptor-30-by-thiodiphenol-promotes-proliferation-of-estrogen-receptor-%C3%AE-positive-breast-cancer-cells
#9
Bingli Lei, Wei Peng, Gang Xu, Minghong Wu, Yu Wen, Jie Xu, Zhiqiang Yu, Yipei Wang
Many studies have been shown that environmental estrogen bisphenol A (BPA) can activate nuclear receptor (estrogen receptor alpha, ERα) or membrane receptor (G-protein-coupled receptor, GPR30) in breast cancer cells and exerts genomic or nongenomic actions inducing cell proliferation. 4,4'-thiodiphenol (TDP) as one of BPA derivatives exhibits more potent estrogenic activity than BPA does. However, comparatively little is known about the ways in which TDP interferes with these signaling pathways and produces cell biological changes...
February 2017: Chemosphere
https://www.readbyqxmd.com/read/27876458/relative-abundance-of-g-protein-coupled-receptor-30-and-localization-in-testis-and-epididymis-of-sheep-at-different-developmental-stages
#10
Peiyao Lu, Fuchuan Wang, Xianyi Song, Yang Liu, Kai Zhang, Ningxian Cao
The G protein-coupled receptor 30 (GPR30) is a transmembrane estrogen receptor that binds to estrogen, and has been confirmed to have an important role in testicular cell proliferation and development. The main objective of this study was to examine GPR30 gene expression and localization in the testis and epididymis of sheep at different developmental stages. Testes, including the epididymis, were collected from Polled Dorset x Mongolian cross rams at one (n=4; wt), three (n=4; wt), six (n=4; wt), nine (n=4; wt) and 12 (n=4; wt) months of age...
December 2016: Animal Reproduction Science
https://www.readbyqxmd.com/read/27853434/expression-of-steroid-receptors-in-ameloblasts-during-amelogenesis-in-rat-incisors
#11
Sophia Houari, Sophia Loiodice, Katia Jedeon, Ariane Berdal, Sylvie Babajko
Endocrine disrupting chemicals (EDCs) play a part in the modern burst of diseases and interfere with the steroid hormone axis. Bisphenol A (BPA), one of the most active and widely used EDCs, affects ameloblast functions, leading to an enamel hypomineralization pattern similar to that of Molar Incisor Hypomineralization (MIH). In order to explore the molecular pathways stimulated by BPA during amelogenesis, we thoroughly investigated the receptors known to directly or indirectly mediate the effects of BPA. The expression patterns of high affinity BPA receptors (ERRγ, GPR30), of ketosteroid receptors (ERs, AR, PGR, GR, MR), of the retinoid receptor RXRα, and PPARγ were established using RT-qPCR analysis of RNAs extracted from microdissected enamel organ of adult rats...
2016: Frontiers in Physiology
https://www.readbyqxmd.com/read/27814026/gper-gpr30-a-nongenomic-receptor-gpcr-for-steroid-hormones-with-implications-for-cardiovascular-disease-and-cancer
#12
Ross D Feldman, Lee E Limbird
Although the rapid effects of steroids, such as estrogen and aldosterone, were postulated originally to be nongenomic, it is now appreciated that activation of such signaling pathways via a steroid-acting G protein-coupled receptor, the G protein estrogen receptor (GPER), has important transcription-dependent outcomes in the regulation of cell growth and programmed cell death secondary to GPER-regulated second-messenger pathways. GPER is expressed ubiquitously and has diverse biological effects, including regulation of endocrine, immune, neuronal, and cardiovascular functions...
January 6, 2017: Annual Review of Pharmacology and Toxicology
https://www.readbyqxmd.com/read/27799463/estrogen-receptors-and-estetrol-dependent-neuroprotective-actions-a-pilot-study
#13
Ekaterine Tskitishvili, Christel Pequeux, Carine Munaut, Renaud Viellevoye, Michelle Nisolle, Agnes Noël, Jean-Michel Foidart
Estetrol (E4) has strong antioxidative, neurogenic and angiogenic effects in neural system resulting in the attenuation of neonatal hypoxic-ischemic encephalopathy. We aimed to define the role of estrogen receptors in E4-dependent actions in neuronal cell cultures and prove the promyelinating effect of E4. In vitro the antioxidative and cell survival/proliferating effects of E4 on H2O2-induced oxidative stress in primary hippocampal cell cultures were studied using different combinations of specific inhibitors for ERα (MPP dihydrochloride), ERβ (PHTTP), GPR30 (G15) and palmytoilation (2-BR)...
January 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/27796870/gpr30-activation-contributes-to-the-puerarin-mediated-neuroprotection-in-mpp-induced-sh-sy5y-cell-death
#14
Yue-Fa Cheng, Guoqi Zhu, Qing-Wen Wu, Yue-Sheng Xie, Yan Jiang, Lan Guo, Ya-Li Guan, Ying-Shuo Liu, Jun Zhang
The neuroprotective action of puerarin in Parkinson's disease (PD) models has been well investigated. However, the mechanisms involved in protection have not been completely understood. G protein-coupled receptor 30 (GPR30) is a G protein-coupled estrogen receptor and considered a potential target in the neuroprotection against PD. In this study, we investigated whether puerarin prevented against 1-methyl-4-phenylpyridinium (MPP(+))-induced cell death via GPR30. Our results showed that the GPR30 agonist, G1, exhibited puerarin-mediated neuroprotection against MPP(+)-induced cell death of SH-SY5Y cells...
October 30, 2016: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/27745655/bisphenol-a-exposure-alters-release-of-immune-and-developmental-modulators-and-expression-of-estrogen-receptors-in-human-fetal-lung-fibroblasts
#15
Laziyan Mahemuti, Qixuan Chen, Melanie C Coughlan, Min Zhang, Maria Florian, Ryan J Mailloux, Xu-Liang Cao, Kylie A Scoggan, William G Willmore, Xiaolei Jin
Bisphenol A (BPA) has been shown to exert biological effects through estrogen receptor (ER)-dependent and ER-independent mechanisms. Recent studies suggest that prenatal exposure to BPA may increase the risk of childhood asthma. To investigate the underlying mechanisms in the actions of BPA, human fetal lung fibroblasts (hFLFs) were exposed to varying doses of BPA in culture for 24hr. Effects of BPA on localization and uptake of BPA, cell viability, release of immune and developmental modulators, cellular localization and expression of ERα, ERβ and G-protein coupled estrogen receptor 30 (GPR30), and effects of ERs antagonists on BPA-induced changes in endothelin-1 (ET-1) release were examined...
October 2016: Journal of Environmental Sciences (China)
https://www.readbyqxmd.com/read/27698362/gpr30-regulates-diet-induced-adiposity-in-female-mice-and-adipogenesis-in-vitro
#16
Aihua Wang, Jing Luo, William Moore, Hana Alkhalidy, Ling Wu, Jinhua Zhang, Wei Zhen, Yao Wang, Deborah J Clegg, Bin Xu, Zhiyong Cheng, Ryan P McMillan, Matthew W Hulver, Dongmin Liu
Recent studies showed that GPR30, a seven-transmembrane G-protein-coupled receptor, is a novel estrogen receptor (ER) that mediates some biological events elicited by estrogen in several types of cancer cells. However, its physiological or pathological role in vivo is unclear. Here, we show that GPR30 knockout (GPRKO) female mice were protected from high-fat diet (HFD)-induced obesity, blood glucose intolerance, and insulin resistance. The decreased body weight gain in GPRKO female mice is due to the reduction in body fat mass...
October 4, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27629493/estrogen-receptor-signaling-in-the-ferutinin-induced-osteoblastic-differentiation-of-human-amniotic-fluid-stem-cells
#17
M Zavatti, M Guida, T Maraldi, F Beretti, L Bertoni, G B La Sala, A De Pol
AIMS: Ferutinin is a diaucane sesquiterpene with a high estrogenic activity. Since ferutinin is able to enhance osteoblastic differentiation of human amniotic fluid stem cells (hAFSCs), the aim of this study was to evaluate the role of the estrogen receptors α (ERα) and G-protein coupled receptor 30 (GPR30) in ferutinin-mediated osteoblastic differentiation. Moreover, it was investigated if MEK/ERK and PI3K/Akt signaling pathways are involved in ferutinin-induced effects. MAIN METHODS: hAFSCs were cultured in a standard medium or in an osteoblastic medium for 14 or 21days and ferutinin was added at 10(-8)M...
November 1, 2016: Life Sciences
https://www.readbyqxmd.com/read/27608844/gpr30-disrupts-the-balance-of-gabaergic-and-glutamatergic-transmission-in-the-spinal-cord-driving-to-the-development-of-bone-cancer-pain
#18
Jie Luo, Xiaoxia Huang, Yali Li, Yang Li, Xueqin Xu, Yan Gao, Ruoshi Shi, Wanjun Yao, Juying Liu, Changbin Ke
Cancer induced bone pain is a very complicated clinical pain states that has proven difficult to be treated effectively due to poorly understand of underlying mechanism, but bone cancer pain (BCP) seems to be enhanced by a state of spinal sensitization. In the present study, we showed that carcinoma tibia implantation induced notable pain sensitization and up-regulation of G-protein-coupled estrogen receptor (GPR30) in the spinal cord of rats which was reversed by GPR30 knockdown. Further studies indicated that upregulation of GPR30 induced by cancer implantation resulted in a select loss of γ-aminobutyric acid-ergic (GABAergic) neurons and functionally diminished the inhibitory transmission due to reduce expression of the vesicular GABA transporter (VGAT)...
September 6, 2016: Oncotarget
https://www.readbyqxmd.com/read/27607345/protective-role-of-gper-agonist-g-1-on-cardiotoxicity-induced-by-doxorubicin
#19
Ernestina M De Francesco, Carmine Rocca, Francesco Scavello, Daniela Amelio, Teresa Pasqua, Damiano C Rigiracciolo, Andrea Scarpelli, Silvia Avino, Francesca Cirillo, Nicola Amodio, Maria C Cerra, Marcello Maggiolini, Tommaso Angelone
The use of Doxorubicin (Dox), a frontline drug for many cancers, is often complicated by dose-limiting cardiotoxicity in approximately 20% of patients. The G-protein estrogen receptor GPER/GPR30 mediates estrogen action as the cardioprotection under certain stressful conditions. For instance, GPER activation by the selective agonist G-1 reduced myocardial inflammation, improved immunosuppression, triggered pro-survival signaling cascades, improved myocardial mechanical performance and reduced infarct size after ischemia/reperfusion (I/R) injury...
September 8, 2016: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/27589731/importance-of-estrogenic-signaling-and-its-mediated-receptors-in-prostate-cancer
#20
REVIEW
Kin-Mang Lau, Ka-Fai To
Prostate cancer (PCa) treatment was first established by Huggins and Hodges in 1941, primarily described as androgen deprivation via interference of testicular androgen production. The disease remains incurable with relapse of hormone-refractory cancer after treatments. Epidemiological and clinical studies disclosed the importance of estrogens in PCa. Discovery of estrogen receptor ERβ prompted direct estrogenic actions, in conjunction with ERα, on PCa cells. Mechanistically, ERs upon ligand binding transactivate target genes at consensus genomic sites via interactions with various transcriptional co-regulators to mold estrogenic signaling...
August 31, 2016: International Journal of Molecular Sciences
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