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GPER1

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https://www.readbyqxmd.com/read/28286086/hyper-methylation-of-the-upstream-cpg-island-shore-is-a-likely-mechanism-of-gper1-silencing-in-breast-cancer-cells
#1
Mohan C Manjegowda, Paridhi Singhal Gupta, Anil M Limaye
GPER1, also known as GPR30, is a novel seven-transmembrane G-protein coupled estrogen receptor that mediates both short-term (non-genomic) and long-term (genomic) effects of estrogen in target cells and tissues. A substantial body of work over the last two decades has highlighted its therapeutic or prognostic utility. However, the clinical data on the expression of GPER1 in breast tissue is ambiguous. Analysis of TCGA RNAseq data revealed significantly lower mean expression of GPER1 mRNA in primary breast tumors compared to that in normal breast tissues...
March 7, 2017: Gene
https://www.readbyqxmd.com/read/28263910/depressive-like-effect-of-prenatal-exposure-to-ddt-involves-global-dna-hypomethylation-and-impairment-of-gper1-esr1-protein-levels-but-not-esr2-and-ahr-arnt-signaling
#2
Malgorzata Kajta, Agnieszka Wnuk, Joanna Rzemieniec, Ewa Litwa, Wladyslaw Lason, Agnieszka Zelek-Molik, Irena Nalepa, Zofia Rogóż, Adam Grochowalski, Anna K Wojtowicz
Several lines of evidence suggest that exposures to Endocrine Disrupting Chemicals (EDCs) such as pesticides increase the risks of neuropsychiatric disorders. Despite extended residual persistence of dichlorodiphenyltrichloroethane (DDT) in the environment, the mechanisms of perinatal actions of DDT that could account for adult-onset of depression are largely unknown. This study demonstrated the isomer-specific induction of depressive-like behavior and impairment of Htr1a/serotonin signaling in one-month-old mice that were prenatally exposed to DDT...
March 2, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28258163/g-1-inhibits-breast-cancer-cell-growth-via-targeting-colchicine-binding-site-of-tubulin-to-interfere-with-microtubule-assembly
#3
Xiangmin Lv, Chunbo He, Cong Huang, Guohua Hua, Zhengfeng Wang, Steven W Remmenga, Kerry J Rodabaugh, Adam R Karpf, Jixin Dong, John S Davis, Cheng Wang
G-protein coupled estrogen receptor 1 (GPER1) has been reported to play a significant role in mediating the rapid estrogen actions in a wide range of normal and cancer cells. G-1 was initially developed as a selective agonist for GPER. However, the molecular mechanisms underlying the actions of G-1 are unknown and recent studies report inconsistent effects of G-1 on the growth of breast cancer cells. By employing high-resolution laser scanning confocal microscopy and time-lapse imaging technology, as well as biochemical analyses, in the present study, we provide convincing in vitro and in vivo evidence that G-1 is able to suppress the growth of breast cancer cells independent of the expression status of GPERs and classic estrogen receptors...
March 3, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28126566/rapid-actions-of-aldosterone-revisited-receptors-in-the-limelight
#4
Martin Wehling
Steroid hormones like aldosterone have been conclusively shown to elicit both late genomic and rapid, nongenomically initiated responses. Aldosterone was among the first for which rapid, clinically relevant effects were even shown in humans. Yet, after over 30 years of research, the nature of receptors involved in rapid actions of aldosterone is still unclear. Such effects may be assigned to the classical, intracellular steroid receptors, in this case mineralocorticoid receptors (MR, class IIa action Mannheim classification)...
January 23, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28126236/rs4265085-in-gper1-gene-increases-the-risk-for-unexplained-recurrent-spontaneous-abortion-in-dai-and-bai-ethnic-groups-in-china
#5
Liang Tang, Shui Zheng, Yan Wang, Fang Li, Meihua Bao, Jie Zeng, Ju Xiang, Huaiqing Luo, Jianming Li
Oestrogen receptors are implicated in the pathogenesis of recurrent spontaneous abortion (RSA). Non-genomic oestrogen responses can be mediated by GPER. The prevalence of polymorphisms in GPER1 gene in RSA was assessed in 747 Chinese women from Yunnan province (171 Bai, 258 Chinese Han, 234 Dai, 33 Achang and 51 Jingpo patients). Snapshot technology was used for genotyping the polymorphisms of the GPER1 gene. The rs4265085G was significantly increased in the Dai and Bai groups versus controls (Dai: P < 0...
January 17, 2017: Reproductive Biomedicine Online
https://www.readbyqxmd.com/read/28096479/igf-1-receptor-modulates-foxo1-mediated-tamoxifen-response-in-breast-cancer-cells
#6
Ali Vaziri-Gohar, Yan Zheng, Kevin D Houston
Tamoxifen is a common adjuvant treatment for ERalpha-positive breast cancer patients, however acquired resistance abrogates the efficacy of this therapeutic approach. We recently demonstrated that G protein-coupled estrogen receptor 1 (GPER1) mediates tamoxifen action in breast cancer cells by inducing insulin-like growth factor binding protein-1 (IGFBP-1) to inhibit IGF-1-dependent signaling. To determine if dysregulation of IGFBP-1 induction is associated with tamoxifen resistance, IGFBP-1 transcription was measured in tamoxifen-resistant MCF-7 cells (TamR) after tamoxifen (Tam) treatment...
January 17, 2017: Molecular Cancer Research: MCR
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
#7
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...
February 2017: Fertility and Sterility
https://www.readbyqxmd.com/read/27872195/estrogen-receptors-and-signaling-in-fibroids-role-in-pathobiology-and-therapeutic-implications
#8
Mostafa A Borahay, Mehmet R Asoglu, Aymara Mas, Sarah Adam, Gokhan S Kilic, Ayman Al-Hendy
Uterine fibroids are the most common gynecologic tumors with a significant medical and financial burden. Several genetic, hormonal, and biological factors have been shown to contribute to the development and growth of fibroid tumors. Of these factors, estrogen is particularly critical since fibroids are considered estrogen dependent because no prepubertal cases have been described in the literature and tumors tend to regress after menopause. Understanding the role of estrogen in fibroids is not only important for understanding the pathobiology of fibroids but also for the development of successful therapeutics...
November 20, 2016: Reproductive Sciences
https://www.readbyqxmd.com/read/27837347/tamoxifen-resistance-and-metastasis-of-human-breast-cancer-cells-were-mediated-by-the-membrane-associated-estrogen-receptor-er-%C3%AE-36-signaling-in-vitro
#9
Wenwen Gu, Nian Dong, Peng Wang, Changgen Shi, Jun Yang, Jian Wang
The drug resistance and tumor metastasis have been the main obstacles for the longer-term therapeutic effects of tamoxifen (TAM) on estrogen receptor-positive (ER(+)) breast cancer, but the mechanisms underlying the TAM resistance are still unclear. Here, we demonstrated that the membrane-associated estrogen receptor ER-α36 signaling, but not the G protein-coupled estrogen receptor 1 (GPER1) signaling, might be involved in the TAM resistance and metastasis of breast cancer cells. In this study, a model of ER(+) breast cancer cell MCF-7 that involves the up-regulated expression of ER-α36 and unchanged expression of ER-α66 and GPER1 was established via the removal of insulin from the cell culture medium...
April 2017: Cell Biology and Toxicology
https://www.readbyqxmd.com/read/27822058/double-edged-role-of-g-protein-coupled-estrogen-receptor-1-in-breast-cancer-prognosis-an-analysis-of-167-breast-cancer-samples-and-online-data-sets
#10
Fan Yang, Zhi-Min Shao
G protein-coupled estrogen receptor 1 (GPER1) is widely expressed in breast cancer; however, its prognostic significance in breast cancer patients remains controversial. In this study, expression levels of GPER1 were analyzed by using real-time polymerase chain reaction in 167 primary breast cancer samples, and overall survival (OS), recurrence-free survival (RFS), distant metastasis-free survival (DMFS), and disease-free survival (DFS) were analyzed by using Kaplan-Meier curves and multivariable Cox regression...
2016: OncoTargets and Therapy
https://www.readbyqxmd.com/read/27760898/activation-of-g-protein-coupled-estrogen-receptor-1-mimics-but-does-not-mediate-the-anti-proliferative-action-of-estradiol-on-pituitary-lactotrophs-in-primary-culture
#11
Tetsuo Mitsui, Maho Ishida, Michi Izawa, Jun Arita
Estrogen binds to nuclear estrogen receptors (ERs) to modulate transcription of target genes in estrogen-responsive cells. However, recent studies have shown that estrogen also binds to cytoplasmic membrane ERs to modulate protein kinase signaling cascades, leading to non-genomic actions. We investigated whether either nuclear or membrane ERs, including G protein-coupled estrogen receptor 1 (Gper1), mediate the inhibitory action of estrogen on insulin-like growth factor-1 (IGF-1)-induced proliferation of pituitary lactotrophs in primary culture...
October 19, 2016: Endocrine Journal
https://www.readbyqxmd.com/read/27644075/neuroprotective-and-immunomodulatory-effects-of-raloxifene-in-the-myenteric-plexus-of-a-mouse-model-of-parkinson-s-disease
#12
Andrée-Anne Poirier, Mélissa Côté, Mélanie Bourque, Marc Morissette, Thérèse Di Paolo, Denis Soulet
Motor symptoms in Parkinson's disease (PD) are often preceded by nonmotor symptoms related to dysfunctions of the autonomic nervous system such as constipation, defecatory problems, and delayed gastric emptying. These gastrointestinal impairments are associated with the alteration of dopaminergic (DAergic) neurons in the myenteric plexus of the gut. Recently, we demonstrated the anti-inflammatory properties of estrogens to treat intestinal neurodegeneration in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of PD...
December 2016: Neurobiology of Aging
https://www.readbyqxmd.com/read/27641676/progesterone-estrogen-and-androgen-receptors-in-the-corpus-luteum-of-the-domestic-cat-iberian-lynx-lynx-pardinus-and-eurasian-lynx-lynx-lynx
#13
Olga Amelkina, Lina Zschockelt, Johanna Painer, Rodrigo Serra, Francisco Villaespesa, Eberhard Krause, Katarina Jewgenow, Beate C Braun
In contrast to the species studied, the corpus luteum (CL) of Iberian and Eurasian lynx physiologically persists in the ovary for more than 2 years and continues to secrete progesterone. Such persistent CL (perCL) transition into the next cycle and are present in the ovary together with the freshly formed CL (frCL) of a new ovulation. To date, the mechanisms supporting such CL persistence are not known. We analyzed the potential receptivity of feline CL to sex steroids through mRNA measurements of progesterone receptor (PGR), progesterone receptor membrane components (PGRMC) 1 and 2, estrogen receptor (ESR) 1 and ESR2, G protein-coupled estrogen receptor 1 (GPER1), and androgen receptor (AR)...
December 2016: Theriogenology
https://www.readbyqxmd.com/read/27572936/ultrasound-targeted-microbubble-destruction-of-calcium-channel-subunit%C3%A2-%C3%AE-1d-sirna-inhibits-breast-cancer-via-g%C3%A2-protein-coupled-receptor-30
#14
Yanlei Ji, Zhen Han, Limei Shao, Yuehuan Zhao
Estrogen has been closely associated with breast cancer. Several studies reported that Ca2+ signal and Ca2+ channels act in estrogen-modulated non-genomic pathway of breast cancer, however little was revealed on the function of L-type Ca2+ channels. The L-type Ca2+ channel subunit α 1D, named Cav1.3 was found in breast cancer cells. We aimed to investigate the expression and activity of Cav1.3 in human breast cancer, and reveal the effect of estrogen in regulating the expression of Cav1.3. The qRT-PCR and western blotting were employed to show that Cav1...
October 2016: Oncology Reports
https://www.readbyqxmd.com/read/27512921/serum-levels-of-g-protein-coupled-estrogen-receptor-1-gper1-in-drug-naive-patients-with-generalized-anxiety-disorder
#15
Ebru Fındıklı, Mehmet Akif Camkurt, Mehmet Fatih Karaaslan, Ergul Belge Kurutas, Hatice Altun, Filiz İzci, Hüseyin Avni Fındıklı, Selçuk Kardas
Sex hormones, particularly estrogen, are suggested to play a role in the physiopathology of generalized anxiety disorder (GAD). Estrogen functions through the estrogen receptors alpha and beta and the recently discovered G protein-coupled estrogen receptor 1 (GPER1). This study aimed, for the first time, to evaluate serum GPER1 levels in drug-naive patients with GAD. This study included 40 newly diagnosed drug-naive patients with GAD aged between 18 and 50 years and 40 age- and gender-matched healthy controls...
October 30, 2016: Psychiatry Research
https://www.readbyqxmd.com/read/27407175/g-1-exerts-neuroprotective-effects-through-g-protein-coupled-estrogen-receptor-1-following-spinal-cord-injury-in-mice
#16
Qiang Cheng, Jia Meng, Xin-Shang Wang, Wen-Bo Kang, Zhen Tian, Kun Zhang, Gang Liu, Jian-Ning Zhao
Spinal cord injury (SCI) always occurs accidently and leads to motor dysfunction because of biochemical and pathological events. Estrogen has been shown to be neuroprotective against SCI through estrogen receptors (ERs), but the underlying mechanisms have not been fully elucidated. In the present study, we investigated the role of a newly found membrane ER, G protein-coupled estrogen receptor 1 (GPR30 or GPER1), and discussed the feasibility of a GPR30 agonist as an estrogen replacement. Forty adult female C57BL/6J mice (10-12 weeks old) were divided randomly into vehicle, G-1, E2, G-1 + G-15 and E2 + G-15 groups...
August 2016: Bioscience Reports
https://www.readbyqxmd.com/read/27392633/emerging-roles-for-the-novel-estrogen-sensing-receptor-gper1-in-the-cns
#17
REVIEW
Amy Alexander, Andrew J Irving, Jenni Harvey
Estrogens play a key role in regulating reproductive and neuroendocrine function by activating classical nuclear steroid receptors that act as ligand gated transcription factors. However evidence is growing that estrogens also promote rapid non-genomic responses via activation of membrane-associated estrogen receptors. The G protein-coupled estrogen receptor (GPER1; also known as GPR30) has been identified as one of the main estrogen-sensitive receptors responsible for the rapid non-genomic actions of estrogen...
February 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27113328/gper1-mediates-estrogen-induced-neuroprotection-against-oxygen-glucose-deprivation-in-the-primary-hippocampal-neurons
#18
Tian-Zhi Zhao, Fei Shi, Jun Hu, Shi-Ming He, Qian Ding, Lian-Ting Ma
It is well-known that the neuroprotective effects of estrogen have potential in the prevention and amelioration of ischemic and degenerative neurological disorders, while the underlying mechanisms for estrogen actions are undefined. As an important mediator for the non-genomic functions of estrogen, GPER1 (G Protein-coupled Estrogen Receptor 1) has been suggested to involve in the beneficial roles of estrogen in neural cells. Here our studies on primary hippocampal neurons have focused on GPER1 in an in vitro model of ischemia using oxygen-glucose deprivation (OGD)...
July 22, 2016: Neuroscience
https://www.readbyqxmd.com/read/27080432/estrogen-receptor-%C3%AE-and-g-protein-coupled-estrogen-receptor-1-are-localized-to-gabaergic-neurons-in-the-dorsal-striatum
#19
Anne Almey, Teresa A Milner, Wayne G Brake
Estrogens affect dopamine transmission in the striatum, increasing dopamine availability, maintaining D2 receptor density, and reducing the availability of the dopamine transporter. Some of these effects of estrogens are rapid, suggesting that they are mediated by membrane associated receptors. Recently our group demonstrated that there is extra-nuclear labeling for ERα, ERβ, and GPER1 in the striatum, but that ERα and GPER1 are not localized to dopaminergic neurons in this region. GABAergic neurons are the most common type of neuron in the striatum, and changes in GABA transmission affect dopamine transmission...
May 27, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/26998610/characterisation-of-signalling-by-the-endogenous-gper1-gpr30-receptor-in-an-embryonic-mouse-hippocampal-cell-line-mhippoe-18
#20
Nicholas J Evans, Asha L Bayliss, Vincenzina Reale, Peter D Evans
Estrogen can modulate neuronal development and signalling by both genomic and non-genomic pathways. Many of its rapid, non-genomic effects on nervous tissue have been suggested to be mediated via the activation of the estrogen sensitive G-protein coupled receptor (GPER1 or GPR30). There has been much controversy over the cellular location, signalling properties and endogenous activators of GPER1. Here we describe the pharmacology and signalling properties of GPER1 in an immortalized embryonic hippocampal cell line, mHippoE-18...
2016: PloS One
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