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https://www.readbyqxmd.com/read/28501695/expression-of-aromatase-and-estrogen-receptors-in-lumbar-motoneurons-of-mice
#1
Ying-Xiao Ji, Mei Zhao, Ya-Ling Liu, Li-Sha Chen, Peng-Li Hao, Can Sun
Estrogen exerts protective roles in amyotrophic lateral sclerosis (ALS). However, the expression of aromatase (ARO) and estrogen receptors (ERs) in the motoneurons of spinal cord, has not yet been elucidated. By immunohistochemistry, we found that ARO and ERs were present in the ventral horn of adult mice lumbar spinal cord, and colocalized with SMI-32, a motoneuron specific marker. Within motoneurons, we observed that ARO is detected primarily in the cytoplasm, with fewer ARO in the nucleus; ERα and ERβ mainly localized in the nucleus with less in the cytoplasm; while GPR30 is located in soma and processes...
May 10, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28472669/the-role-of-estrogen-g-protein-coupled-receptor-30-gpr30-and-sexual-experience-in-sexual-incentive-motivation-in-male-rats
#2
W R Hawley, C Battista, S R Divack, N B Morales Núñez
Male rats exhibit reductions in sexual motivation following systemic administration of drugs that inhibit the conversion of testosterone to estrogen, which indicates that estrogen signaling plays a role in male rat sexual motivation. Given that estrogen G-protein coupled receptor 30 (GPR30) is expressed in brain areas that are important for male sexual behaviors and endocrine function, the primary aim of the current study was to examine the role that GPR30 plays in sexual motivation in both sexually naïve and sexually experienced male rats...
May 1, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28468943/estradiol-activates-chloride-channels-via-the-estrogen-receptor-alpha-in-the-cell-membrane-in-osteoblasts
#3
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/28465157/gper1-gpr30-in-the-brain-crosstalk-with-classical-estrogen-receptors-and-implications-for-behavior
#4
REVIEW
Maria M Hadjimarkou, Nandini Vasudevan
The GPER1/GPR30 is a membrane estrogen receptor (mER) that binds 17β-estradiol (17β-E) with high affinity and is thought to play a role in cancer progression and cardiovascular health. Though widespread in the central nervous system, less is known about this receptor's function in the brain. GPER1 has been shown to activate kinase cascades and calcium flux within cells rapidly, thus fitting in with the idea of being a mER that mediates non-genomic signaling by estrogens. Signaling from GPER1 has been shown to improve spatial memory, possibly via release of neurotransmitters and generation of new spines on neurons in the hippocampus...
April 29, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28450397/g-protein-coupled-estrogen-receptor-1-gper1-gpr30-increases-erk1-2-activity-through-pdz-dependent-and-independent-mechanisms
#5
Ernesto Gonzalez de Valdivia, Stefan Broselid, Robin Kahn, Björn Olde, L M Fredrik Leeb-Lundberg
G protein-coupled receptor 30 (GPR30), also called G protein-coupled estrogen receptor 1 (GPER1), is thought to play important roles in breast cancer and cardiometabolic regulation, but many questions remain about ligand activation, effector coupling, and subcellular localization. We showed recently that GPR30 interacts through the C-terminal type I PDZ motif with SAP97 and protein kinase A (PKA)-anchoring protein (AKAP) 5, which anchor the receptor in the plasma membrane and mediate an apparently constitutive decrease in cAMP production independently of Gi/o...
April 27, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28450143/crosstalk-between-nuclear-and-g-protein-coupled-estrogen-receptors
#6
REVIEW
Shannon N Romano, Daniel A Gorelick
In 2005, two groups independently discovered that the G protein-coupled receptor GPR30 binds estradiol in cultured cells and, in response, initiates intracellular signaling cascades Revankar et al. (2005), Thomas et al. (2005). GPR30 is now referred to as GPER, the G-protein coupled estrogen receptor Prossnitz and Arterburn (2015). While studies in animal models are illuminating GPER function, there is controversy as to whether GPER acts as an autonomous estrogen receptor in vivo, or whether GPER interacts with nuclear estrogen receptor signaling pathways in response to estrogens...
April 25, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28446726/low-concentration-of-bpa-induces-mice-spermatocytes-apoptosis-via-gpr30
#7
Chaoliang Wang, Jianxiang Zhang, Qi Li, Tianbiao Zhang, Zishi Deng, Jing Lian, Donghui Jia, Rui Li, Tao Zheng, Xiaoju Ding, Fan Yang, Chao Ma, Rui Wang, Weixing Zhang, Jian Guo Wen
Bisphenol A (BPA) acts as xenoestrogen and has a great impact on disorders of human reproductive system. However, the mechanism through which BPA can affect human testicular function remains to be indentified. GPR30 is a novel membrane estrogen receptor with high-affinity and low-capacity binding to estrogens. We demonstrated that estrogen receptor α (ERα), estrogen receptor β (ERβ) as well as GPR30 are expressed in mouse spermatocyte-derived GC-2 cells using Real-time PCR. We treated the cells with different doses of BPA and found that even low doses of BPA can inhibit GC-2 cell growth using MTT assay...
April 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28440394/g-protein-coupled-receptor-30-mediates-the-effects-of-estrogen-on-endothelial-cell-tube-formation-in%C3%A2-vitro
#8
Liyuan Zhou, Hong Chen, Xun Mao, Hongbo Qi, Philip N Baker, Hua Zhang
The placenta is the exchange organ between the mother and the fetus. The inadequate function of this organ is associated with a number of pregnancy disorders. Hypoxia and oxidative stress during placental development may induce endothelial dysfunction, resulting in the reduction in the perfusion of the placenta. During pregnancy, the levels of estrogen are increased. Decreased estrogen levels have been reported in women with preeclampsia. However, whether estrogen is involved in placental angiogenesis remains unclear...
June 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28427772/seasonal-variations-of-aromatase-and-estrogen-receptors-expression-in-the-testis-of-free-ranging-sand-rats
#9
Rafik Menad, Souaâd Smaï, Xavier Bonnet, Thérèse Gernigon-Spychalowicz, Elara Moudilou, Farida Khammar, Jean-Marie Exbrayat
An increasing number of studies revealed the importance of estrogen in male reproduction. However, most research was conducted in laboratory rodents subjected to standardized environmental conditions. Therefore, seasonal regulations of estrogen pathways remain poorly understood under natural conditions. Using immunohistochemistry, the expression of several molecules involved in the functioning of testis (i.e. 17-β estradiol [E2], P450 aromatase, estrogen receptors ESR1, ESR2, and GPER1 [also known as GPR30]) were investigated in free-ranging fat sand rats, Psammomys obesus, during the breeding and resting seasons...
April 17, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28412354/role-of-gpr30-in-estrogen-induced-prostate-epithelial-apoptosis-and-benign-prostatic-hyperplasia
#10
Deng-Liang Yang, Jia-Wen Xu, Jian-Guo Zhu, Yi-Lin Zhang, Jian-Bang Xu, Qing Sun, Xiao-Nian Cao, Wu-Lin Zuo, Ruo-Shui Xu, Jie-Hong Huang, Fu-Neng Jiang, Yang-Jia Zhuo, Bai-Quan Xiao, Yun-Zhong Liu, Dong-Bo Yuan, Zhao-Lin Sun, Hui-Chan He, Zhao-Rong Lun, Wei-De Zhong, Wen-Liang Zhou
Several studies have implicated estrogen and the estrogen receptor (ER) in the pathogenesis of benign prostatic hyperplasia (BPH); however, the mechanism underlying this effect remains elusive. In the present study, we demonstrated that estrogen (17β-estradiol, or E2)-induced activation of the G protein-coupled receptor 30 (GPR30) triggered Ca(2+) release from the endoplasmic reticulum, increased the mitochondrial Ca(2+) concentration, and thus induced prostate epithelial cell (PEC) apoptosis. Both E2 and the GPR30-specific agonist G1 induced a transient intracellular Ca(2+) release in PECs via the phospholipase C (PLC)-inositol 1, 4, 5-triphosphate (IP3) pathway, and this was abolished by treatment with the GPR30 antagonist G15...
April 12, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28357806/apoptosis-induced-by-the-uv-filter-benzophenone-3-in-mouse-neuronal-cells-is-mediated-via-attenuation-of-er%C3%AE-ppar%C3%AE-and-stimulation-of-er%C3%AE-gpr30-signaling
#11
A Wnuk, J Rzemieniec, W Lasoń, W Krzeptowski, M Kajta
Although benzophenone-3 (BP-3) has frequently been reported to play a role in endocrine disruption, there is insufficient data regarding the impact of BP-3 on the nervous system, including its possible adverse effects on the developing brain. Our study demonstrated that BP-3 caused neurotoxicity and activated apoptosis via an intrinsic pathway involving the loss of mitochondrial membrane potential and the activation of caspases-9 and -3 and kinases p38/MAPK and Gsk3β. These biochemical alterations were accompanied by ROS production, increased apoptotic body formation and impaired cell survival, and by an upregulation of the genes involved in apoptosis...
March 29, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28347854/twenty-years-of-the-g-protein-coupled-estrogen-receptor-gper-historical-and-personal-perspectives
#12
Matthias Barton, Edward J Filardo, Stephen J Lolait, Peter Thomas, Marcello Maggiolini, Eric R Prossnitz
Estrogens play a critical role in many aspects of physiology, particularly female reproductive function, but also in pathophysiology, and are associated with protection from numerous diseases in premenopausal women. Steroids and the effects of estrogen have been known for ∼90 years, with the first evidence for a receptor for estrogen presented ∼50 years ago. The original ancestral steroid receptor, extending back into evolution more than 500 million years, was likely an estrogen receptor, whereas G protein-coupled receptors (GPCRs) trace their origins back into history more than one billion years...
March 25, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28344760/severe-pulmonary-hypertension-in-aging-female-apolipoprotein-e-deficient-mice-is-rescued-by-estrogen-replacement-therapy
#13
Soban Umar, Rod Partow-Navid, Gregoire Ruffenach, Andrea Iorga, Shayan Moazeni, Mansoureh Eghbali
BACKGROUND: Apolipoprotein E (ApoE) is a multifunctional protein, and its deficiency leads to the development of atherosclerosis in mice. Patients with pulmonary hypertension (PH) have reduced expression of ApoE in lung tissue. ApoE is known to inhibit endothelial and smooth muscle cell proliferation and has anti-inflammatory and anti-platelet aggregation properties. Young ApoE-deficient mice have been shown to develop PH on high fat diet. The combined role of female sex and aging in the development of PH has not been investigated before...
2017: Biology of Sex Differences
https://www.readbyqxmd.com/read/28338111/g-protein-coupled-receptor-30-gpr30-expression-pattern-in-inflammatory-bowel-disease-patients-suggests-its-key-role-in-the-inflammatory-process-a-preliminary-study
#14
Marcin Włodarczyk, Aleksandra Sobolewska-Włodarczyk, Adam I Cygankiewicz, Damian Jacenik, Aleksandra Piechota-Polańczyk, Krystyna Stec-Michalska, Wanda M Krajewska, Jakub Fichna, Maria Wiśniewska-Jarosińska
BACKGROUND AND AIMS: G protein-coupled receptor 30 (GPR30) is a recently de-orphanized estrogen receptor that mediates the effects of estrogens on different cells. It has been postulated that in inflammatory bowel diseases (IBD) activation of GPR30 blocks the pathways dependent on pro-inflammatory cytokines. The aim of our study was to investigate GPR30 expression in patients with IBD and its potential implication in future therapies. METHODS: Fifty-seven patients were enrolled in our study: 20 subjects with Crohn's disease (CD), 22 with ulcerative colitis (UC) and 15 controls...
March 2017: Journal of Gastrointestinal and Liver Diseases: JGLD
https://www.readbyqxmd.com/read/28306605/hyperalgesic-priming-type-ii-induced-by-repeated-opioid-exposure-maintenance-mechanisms
#15
Dioneia Araldi, Luiz F Ferrari, Jon D Levine
We previously developed a model of opioid-induced neuroplasticity in the peripheral terminal of the nociceptor that could contribute to opioid-induced hyperalgesia, type II hyperalgesic priming. Repeated administration of mu-opioid receptor (MOR) agonists, such as DAMGO, at the peripheral terminal of the nociceptor, induces long-lasting plasticity expressed, prototypically as opioid-induced hyperalgesia and prolongation of prostaglandin E2-induced hyperalgesia. In this study, we evaluated the mechanisms involved in the maintenance of type II priming...
March 14, 2017: Pain
https://www.readbyqxmd.com/read/28299994/the-changes-of-cytoskeletal-proteins-induced-by-the-fast-effect-of-estrogen-in-mouse-blastocysts-and-its-roles-in-implantation
#16
Shi-Mao Zhang, Lin-Lin Yu, Ting Qu, Ying Hu, Dong-Zhi Yuan, Sheng Zhang, Qian Xu, You-Bo Zhao, Jin-Hu Zhang, Li-Min Yue
It is necessary for estrogen to activate mouse blastocysts, so that they can attach to endometrial epithelium in implantation and in our previous research, we have proved estrogen can induce a fast increase in intracellular calcium of mouse blastocysts through acting on G protein-coupled receptor 30 (GPR30), which further promotes their implantation. Moreover, there has been evidence that cytoskeletal proteins are involved in integrin-mediated adhesion of many kinds of cells, which also plays an important role in implantation...
January 1, 2017: Reproductive Sciences
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
#17
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...
May 30, 2017: Gene
https://www.readbyqxmd.com/read/28285016/gper-modulators-opportunity-nox-on-the-heels-of-a-class-akt
#18
Eric R Prossnitz
The (patho)physiology of estrogen and its receptors is complex. It is therefore not surprising that therapeutic approaches targeting this hormone include stimulation of its activity through supplementation with either the hormone itself or natural or synthetic agonists, inhibition of its activity through the use of antagonists or inhibitors of its synthesis, and tissue-selective modulation of its activity with biased ligands. The physiology of this hormone is further complicated by the existence of at least three receptors, the classical nuclear estrogen receptors α and β (ERα and ERβ), and the 7-transmembrane G protein-coupled estrogen receptor (GPER/GPR30), with overlapping but distinct pharmacologic profiles, particularly of anti-estrogenic ligands...
March 8, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28249728/gper-is-involved-in-the-functional-liaison-between-breast-tumor-cells-and-cancer-associated-fibroblasts-cafs
#19
Rosamaria Lappano, Marcello Maggiolini
The aggressiveness of breast tumors is deeply influenced by the surrounding stroma. In this regard, the functional crosstalk between cancer cells and the tumor microenvironment has received considerable attention in recent years. Cancer-associated fibroblasts (CAFs) are active components of the tumor stroma as they play a main role in the initiation, progression, metastasis and recurrence of breast malignancy. Hence, a better understanding of the mechanisms through which host stroma may contribute to cancer development would lead to novel therapeutic approaches aimed to target both tumor cells and the adjacent microenvironment...
February 26, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28223150/roles-of-g-protein-coupled-estrogen-receptor-gper-in-metabolic-regulation
#20
Geetanjali Sharma, Franck Mauvais-Jarvis, Eric R Prossnitz
Metabolic homeostasis is differentially regulated in males and females. The lower incidence of obesity and associated diseases in pre-menopausal females points towards the beneficial role of the predominant estrogen, 17β-estradiol (E2). The actions of E2 are elicited by nuclear and extra-nuclear estrogen receptor (ER) α and ERβ, as well as the G protein-coupled estrogen receptor (GPER, previously termed GPR30). The roles of GPER in the regulation of metabolism are only beginning to emerge and much remains unclear...
February 20, 2017: Journal of Steroid Biochemistry and Molecular Biology
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