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GPR30

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https://www.readbyqxmd.com/read/29680290/estrogen-receptor-beta-signaling-inhibits-pdgf-induced-human-airway-smooth-muscle-proliferation
#1
Nilesh Sudhakar Ambhore, Rathnavali Katragadda, Rama Satyanarayana Raju Kalidhindi, Michael A Thompson, Christina M Pabelick, Y S Prakash, Sathish Venkatachalem
Airway smooth muscle (ASM) cell hyperplasia driven by persistent inflammation is a hallmark feature of remodeling in asthma. Sex steroid signaling in the lungs is of considerable interest, given epidemiological data showing more asthma in pre-menopausal women and aging men. Our previous studies demonstrated that estrogen receptor (ER) expression increases in asthmatic human ASM; however, very limited data are available regarding differential roles of ERα vs. ERβ isoforms in human ASM cell proliferation. In this study, we evaluated the effect of selective ERα and ERβ modulators on platelet-derived growth factor (PDGF)-stimulated ASM proliferation and the mechanisms involved...
April 19, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29608013/17%C3%AE-estradiol-on-the-expression-of-g-protein-coupled-estrogen-receptor-gper-gpr30-mitophagy-and-the-pi3k-akt-signaling-pathway-in-atdc5-chondrocytes-in-vitro
#2
Dong-Xiao Fan, Xu-Hao Yang, Yi-Nan Li, Lei Guo
BACKGROUND Osteoarthritis is a progressive inflammatory joint disease resulting in damage to articular cartilage. G-protein coupled estrogen receptor (GPER/GPR30) activates cell signaling in response to 17β-estradiol, which can be blocked by the GPR30 agonist, G15, an analog of G-1. The aims of this study were to investigate the effects of 17β-estradiol on the expression of G-protein coupled estrogen receptor (GPER/GPR30) on mitophagy and the PI3K/Akt signaling pathway in ATDC5 chondrocytes in vitro. MATERIAL AND METHODS Cultured ATDC5 chondrocytes were treated with increasing concentrations of 17β-estradiol with and without G15, p38 inhibitor (SB203580), JNK inhibitor (SP600125), PI3K inhibitor (LY294002, S1737), and mTOR inhibitor (S1842)...
April 2, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29535608/genistein-a-phytoestrogen-in-soybean-induces-the-expression-of-acetylcholinesterase-via-g-protein-coupled-receptor-30-in-pc12-cells
#3
Etta Y L Liu, Miranda L Xu, Yan Jin, Qiyun Wu, Tina T X Dong, Karl W K Tsim
Genistein, 4',5,7-trihydroxyisoflavone, is a major isoflavone in soybean, which is known as phytestrogen having known benefit to brain functions. Being a common phytestrogen, the possible role of genistein in the brain protection needs to be further explored. In cultured PC12 cells, application of genistein significantly induced the expression of neurofilaments (NFs), markers for neuronal differentiation. In parallel, the expression of tetrameric form of proline-rich membrane anchor (PRiMA)-linked acetyl-cholinesterase (G4 AChE), a key enzyme to hydrolyze acetylcholine in cholinergic synapses, was induced in a dose-dependent manner: this induction included the associated protein PRiMA...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29515057/reconsidering-the-roles-of-endogenous-estrogens-and-xenoestrogens-the-membrane-estradiol-receptor-g-protein-coupled-receptor-30-gpr30-mediates-the-effects-of-various-estrogens
#4
Hiroya Kadokawa, Kiran Pandey, Kereilwe Onalenna, Asrafun Nahar
Estrone (E1) and estriol (E3) are considered "weak" estrogens, which exert suppressive effects through estrogen receptors α and β. However, recent studies have demonstrated that E1 and E3, as well as estradiol (E2), suppress gonadotropin-releasing hormone-induced luteinizing hormone secretion from bovine gonadotrophs via G-protein-coupled receptor 30, which is expressed in various reproductive organs. Currently, there is a lack of fundamental knowledge regarding E1 and E3, including their blood levels...
March 6, 2018: Journal of Reproduction and Development
https://www.readbyqxmd.com/read/29484405/downregulation-of-g%C3%A2-protein%C3%A2-coupled-receptor-30-in-the-hippocampus-attenuates-the-neuroprotection-of-estrogen-in-the-critical-period-hypothesis
#5
Yingxi Wu, Dayun Feng, Jiaji Lin, Yan Qu, Shiming He, Yuan Wang, Guodong Gao, Tianzhi Zhao
The aim of the present study was to investigate the role of G‑protein‑coupled receptor 30 (GPR30) in long‑term 17β‑estradiol (E2) deprivation (LTED) in a rat model with global cerebral ischemia (GCI), and its therapeutic target for ischemic stroke in the clinical setting. Following bilateral ovariectomy, GCI was induced in rats 1 or 10 weeks post‑surgery. To determine the protein and mRNA expression levels of GPR30 in the hippocampal CA1 region of LTED rats, short‑term E2 deprivation (STED) rats and naturally aging rats, western blot analysis and reverse transcription-quantitative polymerase chain reaction were performed...
February 16, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29452160/orchiectomy-and-letrozole-differentially-regulate-synaptic-plasticity-and-spatial-memory-in-a-manner-that-is-mediated-by-src-1-in-the-hippocampus-of-male-mice
#6
Jikai Zhao, Chen Bian, Mengying Liu, Yangang Zhao, Tao Sun, Fangzhou Xing, Jiqiang Zhang
Hippocampal synaptic plasticity is the basis of spatial memory and cognition and is strongly regulated by both testicular androgens (testosterone, T) and hippocampal estrogens (17β-estradiol, E2) converted from T by aromatase, which is inhibited by letrozole (LET), but the contribution of each pathway to spatial memory and the associated mechanisms are unclear. In this study, we first used orchiectomy (ORX) and LET injection to investigate the effects of T and hippocampal E2 on spatial memory and hippocampal synaptic plasticity...
February 13, 2018: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29438359/effects-of-17%C3%AE-estradiol-on-mitophagy-in-the-murine-mc3t3-e1-osteoblast-cell-line-is-mediated-via-g-protein-coupled-estrogen-receptor-and-the-erk1-2-signaling-pathway
#7
Xiaoqi Sun, Xuhao Yang, Yuyan Zhao, Yinan Li, Lei Guo
BACKGROUND Osteoporosis is associated with 17β-estradiol deficiency. The G protein-coupled receptor 30 (GPR30) is known to be an estrogen-responsive receptor, but its role in the degradation of mitochondria in osteoblasts by autophagy, or mitophagy, remains unclear. The aim of this in vitro study was to evaluate the effects of 17β-estradiol, GPR30, and its signaling pathway, on mitophagy in the murine MC3T3-E1 osteoblast cell line. MATERIAL AND METHODS In the murine MC3T3-E1 osteoblast cell line, cells were treated with 17β-estradiol, or G15, a selective GPR30 antagonist, or U0126, a mitogen-activated protein (MAP) kinase (ERK1/2) inhibitor, or with vehicle as control...
February 13, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29421611/gpr30-activation-improves-memory-and-facilitates-dhpg-induced-ltd-in-the-hippocampal-ca3-of-middle-aged-mice
#8
Wen Xu, Jian Cao, Yan Zhou, Lina Wang, Guoqi Zhu
Reduced estrogen levels and decreased expression of related receptors are typical cerebral features of aging. The G protein-coupled estrogen receptor 1 (GPER1, also known as GPR30) is considered a novel therapeutic target for neurodegenerative diseases. In this study, we demonstrated that hippocampal GPR30 expression was reduced in middle-aged mice compared with young adult mice. GPR30 agonist G1 improved both fear and spatial memory in both male and female middle-aged mice, but not in young adult mice, which were blocked by the GPR30 antagonist G15...
February 5, 2018: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/29391778/ipriflavone-promotes-proliferation-and-osteogenic-differentiation-of-periodontal-ligament-cells-by-activating-gpr30-pi3k-akt-signaling-pathway
#9
Yuanyuan Han, Xuxia Wang, Dan Ma, Xiaoxiao Wu, Panpan Yang, Jun Zhang
Objectives: This study was performed to investigate the effects and mechanism of ipriflavone (IP) on the proliferation and osteoblastic differentiation of periodontal ligament cells in vitro and periodontal tissue remodeling following orthodontic tooth movement (OTM) in vivo. Materials and methods: Human periodontal ligament cells (hPDLCs) were cultured in vitro and cell counting kit-8, alkaline phosphatase (ALP) activity assay, plate clone formation assay, and alizarin red staining were used to test proliferation and osteogenic differentiation of hPDLCs...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29385707/sex-hormone-receptors-in-benign-and-malignant-salivary-gland-tumors-prognostic-and-predictive-role
#10
Gabriella Aquino, Francesca Collina, Rocco Sabatino, Margherita Cerrone, Francesco Longo, Franco Ionna, Nunzia Simona Losito, Rossella De Cecio, Monica Cantile, Giuseppe Pannone, Gerardo Botti
The role of sex hormone receptors in human cancer development and progression has been well documented in numerous studies, as has the success of sex hormone antagonists in the biological therapy of many human tumors. In salivary gland tumors (SGTs), little and conflicting information about the role of the estrogen receptor alpha (ERα), progesterone receptor (PgR) and androgen receptor (AR) has been described and in most cases the use of sex hormone antagonists is not contemplated in clinical practice. In this study, we analyzed a panel of sex hormone receptors that have not been widely investigated in SGTs-ERα, PgR, AR, but also ERβ and GPR30-to define their expression pattern and their prognostic and predictive value in a case series of 69 benign and malignant SGTs...
January 30, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29365274/2-methoxyestradiol-causes-mmp-9-mediated-transactivation-of-egfr-and-angiotensin-type-1-receptor-downregulation-in-rat-aortic-smooth-muscle-cells
#11
Benard Ogola, Yong Zhang, Laxmi Iyer, Thomas Thekkumkara
Studies have demonstrated the therapeutic potential of estrogen metabolite 2-Methoxyestradiol (2ME2) in several cardiovascular disorders, including hypertension. However, the exact mechanism(s) remains unknown. In this study, primary rat aortic smooth muscle cells (RASMCs) were exposed to 2ME2 and angiotensin type 1 receptor (AT1R) expression, function and associated signaling pathways were evaluated. 2ME2 downregulated AT1R expression in a concentration and time-dependent manner, which was correlated with reduced mRNA expression...
January 24, 2018: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/29360751/estrogenic-effects-of-the-extracts-from-the-chinese-yam-dioscorea-opposite-thunb-and-its-effective-compounds-in-vitro-and-in-vivo
#12
Mengnan Zeng, Li Zhang, Miao Li, Beibei Zhang, Ning Zhou, Yingying Ke, Weisheng Feng, Xiaoke Zheng
BACKGROUND: The aim of this study was to explore the estrogenic effects of the extracts from Chinese yam and its effective compounds. METHODS: The activity of the yam was investigated by the uterine weight gain of mice and a proliferation assay of breast cancer cell lines (MCF-7 cell); the estrogenic activity was comprehensively evaluated by a serum pharmacology experiment. The levels of estradiol (E2), follicle stimulating hormone (FSH), and luteinizing hormone (LH) were also measured...
January 23, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29352507/nuclear-and-membrane-estrogen-receptor-antagonists-induce-similar-mtorc2-activation-reversible-changes-in-synaptic-protein-expression-and-actin-polymerization-in-the-mouse-hippocampus
#13
Fang-Zhou Xing, Yan-Gang Zhao, Yuan-Yuan Zhang, Li He, Ji-Kai Zhao, Meng-Ying Liu, Yan Liu, Ji-Qiang Zhang
AIMS: Estrogens play pivotal roles in hippocampal synaptic plasticity through nuclear receptors (nERs; including ERα and ERβ) and the membrane receptor (mER; also called GPR30), but the underlying mechanism and the contributions of nERs and mER remain unclear. Mammalian target of rapamycin complex 2 (mTORC2) is involved in actin cytoskeleton polymerization and long-term memory, but whether mTORC2 is involved in the regulation of hippocampal synaptic plasticity by ERs is unclear. METHODS: We treated animals with nER antagonists (MPP/PHTPP) or the mER antagonist (G15) alone or in combination with A-443654, an activator of mTORC2...
January 19, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29298702/correction-to-calycosin-inhibits-the-in-vitro-and-in-vivo-growth-of-breast-cancer-cells-through-wdr7-7-gpr30-signaling
#14
Jing Tian, Yong Wang, Xing Zhang, Qianyao Ren, Rong Li, Yue Huang, Huiling Lu, Jian Chen
In the publication of this article [1], the molecule weight of GPR30 in figures was incorrectly, this should have been 55 kDa, and not 38 kDa. This has now been included in this erratum.
December 15, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/29275510/bisphenol-a-induces-dsb-atm-p53-signaling-leading-to-cell-cycle-arrest-senescence-autophagy-stress-response-and-estrogen-release-in-human-fetal-lung-fibroblasts
#15
Laziyan Mahemuti, Qixuan Chen, Melanie C Coughlan, Cunye Qiao, Nikolai L Chepelev, Maria Florian, Dillon Dong, Robert G Woodworth, Jin Yan, Xu-Liang Cao, Kylie A Scoggan, Xiaolei Jin, William G Willmore
Experimental and/or epidemiological studies suggest that prenatal exposure to bisphenol A (BPA) may delay fetal lung development and maturation and increase the susceptibility to childhood respiratory disease. However, the underlying mechanisms remain to be elucidated. In our previous study with cultured human fetal lung fibroblasts (HFLF), we demonstrated that 24-h exposure to 1 and 100 µM BPA increased GPR30 protein in the nuclear fraction. Exposure to 100 μM BPA had no effects on cell viability, but increased cytoplasmic expression of ERβ and release of GDF-15, as well as decreased release of IL-6, ET-1, and IP-10 through suppression of NFκB phosphorylation...
December 23, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29239277/nuclear-g-protein-coupled-oestrogen-receptor-gpr30-predicts-poor-survival-in-patients-with-ovarian-cancer
#16
Cai-Xia Zhu, Wei Xiong, Ma-Lie Wang, Juan Yang, Hui-Juan Shi, Han-Qing Chen, Gang Niu
Objective To demonstrate the correlation between nuclear and cytoplasmic G protein-coupled oestrogen receptor (GPR30) expression and clinicopathological features and outcome in patients with ovarian cancer. Methods Nuclear and cytoplasmic GPR30 expressions were determined using immunohistochemistry to identify the intracellular location in tissues from patients with ovarian cancer. Data were correlated with clinicopathological characteristics and outcomes. Results Tissue samples were obtained from 110 patients with epithelial ovarian cancer between 2005 and 2010...
February 2018: Journal of International Medical Research
https://www.readbyqxmd.com/read/29229551/modulation-of-reactive-oxygen-species-via-erk-and-stat3-dependent-signalling-are-involved-in-the-response-of-mesothelioma-cells-to-exemestane
#17
Barbara Nuvoli, Emanuela Camera, Arianna Mastrofrancesco, Stefania Briganti, Rossella Galati
Pleural mesothelioma is a deadly form of cancer. The prognosis is extremely poor due to the limited treatment modalities. Uptake of asbestos fibres, the leading cause of mesothelioma, lead to the accumulation of reactive-oxygen-species (ROS). Interestingly, increasing ROS production by using ROS-generating drugs may offer a strategy to selectively trigger cell death. Exemestane, an aromatase inhibitor, has previously shown anti-tumor properties in mesothelioma preclinical models suggesting a role of G protein-coupled receptor 30 (GPR30) in the drug response...
February 1, 2018: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/29224106/g-protein-coupled-estrogen-receptor-gper-and-sex-specific-metabolic-homeostasis
#18
Geetanjali Sharma, Eric R Prossnitz
Obesity and metabolic syndrome display disparate prevalence and regulation between males and females. Human, as well as rodent, females with regular menstrual/estrous cycles exhibit protection from weight gain and associated chronic diseases. These beneficial effects are predominantly attributed to the female hormone estrogen, specifically 17β-estradiol (E2). E2 exerts its actions via multiple receptors, nuclear and extranuclear estrogen receptor (ER) α and ERβ, and the G-protein-coupled estrogen receptor (GPER, previously termed GPR30)...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29212519/gper-mediates-the-angiocrine-actions-induced-by-igf1-through-the-hif-1%C3%AE-vegf-pathway-in-the-breast-tumor-microenvironment
#19
Ernestina M De Francesco, Andrew H Sims, Marcello Maggiolini, Federica Sotgia, Michael P Lisanti, Robert B Clarke
BACKGROUND: The G protein estrogen receptor GPER/GPR30 mediates estrogen action in breast cancer cells as well as in breast cancer-associated fibroblasts (CAFs), which are key components of microenvironment driving tumor progression. GPER is a transcriptional target of hypoxia inducible factor 1 alpha (HIF-1α) and activates VEGF expression and angiogenesis in hypoxic breast tumor microenvironment. Furthermore, IGF1/IGF1R signaling, which has angiogenic effects, has been shown to activate GPER in breast cancer cells...
December 6, 2017: Breast Cancer Research: BCR
https://www.readbyqxmd.com/read/29207611/the-positivity-of-g-protein-coupled-receptor-30-gpr-30-an-alternative-estrogen-receptor-is-not-different-between-type-1-and-type-2-endometrial-cancer
#20
Jiayi Wan, Yongxiang Yin, Min Zhao, Fang Shen, Miaoxin Chen, Qi Chen
It is well-known that the clinical outcomes are different between type 1 (estrogen dependent) and type 2 (estrogen independent) endometrial cancer. Studies have suggested that the estrogen receptor (ER) is positively correlated with endometrial cancer survival, however we previously reported that there is no difference in the positivity of ER as well as sex hormone levels between subtypes of cancer. G-protein-coupled receptor-30 (GPR 30), an alternative estrogen receptor has been suggested to be negatively correlated with clinical outcomes of endometrial cancer...
October 31, 2017: Oncotarget
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