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GPR30

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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
#1
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...
April 20, 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
#2
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
#3
Deng-Liang Yang, Jia-Wen Xu, Jianguo Zhu, Yi-Lin Zhang, Jian-Bang Xu, Qing Sun, Xiao-Nian Cao, Wu-Lin Zuo, Ruo-Shui Xu, Jiehong Huang, Fu-Neng Jiang, Yang-Jia Zhuo, Bai-Quan Xiao, Yun-Zhong Liu, Dongbo Yuan, Zhaolin 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
#4
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
#5
Matthias Barton, Edward J Filardo, Stephen J Lolait, Peter Thomas, Marcello Maggiolini, Eric R Prossnitz
Estrogens play a critical role in many aspects of female physiology, particularly reproductive function, but also in pathophysiology, and are associated with protection from numerous diseases in premenopausal women. Steroids and particularly estrogen action 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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
https://www.readbyqxmd.com/read/28189066/mdh2-stimulated-by-estrogen-gpr30-pathway-down-regulated-pten-expression-promoting-the-proliferation-and-invasion-of-cells-in-endometrial-cancer
#14
Yan Zhuang, Jiangdong Xiang, Wei Bao, Ya Sun, Lina Wang, Meihua Tan, Yinyan He, Xiaowei Xi
PURPOSE: The relationship between endometrial carcinoma and cellular metabolism is unknown. In endometrial cancer, mutation rate of PTEN has been reported very high. Malate dehydrogenase 2 (MDH2) is one of the isoforms of malate dehydrogenase, which is involved in citric acid cycle in mitochondria. Our study aimed to investigate the role MDH2 played in PTEN-regulated endometrial carcinoma. METHODS: To reveal the expression of MDH2 and the co-localization of PTEN and MDH2, immunohistochemistry and immunofluorescent staining were used...
April 2017: Translational Oncology
https://www.readbyqxmd.com/read/28098854/lsd1-sustains-estrogen-driven-endometrial-carcinoma-cell-proliferation-through-the-pi3k-akt-pathway-via-di-demethylating-h3k9-of-cyclin%C3%A2-d1
#15
Chunqin Chen, Yanan Wang, Shiyu Wang, Yuan Liu, Jiawen Zhang, Yuyao Xu, Zhenbo Zhang, Wei Bao, Sufang Wu
A recent study reported that histone lysine specific demethylase 1 (LSD1, KDM1A) is overexpressed in endometrioid endometrial carcinoma (EEC) and associated with tumor progression as well as poor prognosis. However, the physiological function and mechanism of LSD1 in endometrial cancer (EC) remains largely unknown. In this study, we demonstrate that β-estradiol (E2) treatment increased LSD1 expression via the GPR30/PI3K/AKT pathway in endometrial cancer cells. Both siGPR30 and the PI3K inhibitor LY294002 block this effect...
March 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28089920/g-protein-coupled-estrogen-receptor-mediated-non-genomic-facilitatory-effect-of-estrogen-on-cooling-induced-reduction-of-skin-blood-flow-in-mice
#16
Izumi Serizawa, Nozomi Iwasaki, Hirotake Ishida, Shin-Ya Saito, Tomohisa Ishikawa
An enhanced vasoconstrictor activity of cutaneous arteries participates in the reduction of skin blood flow induced by cooling stimulation. Raynaud's phenomenon, which is characterized by intense cooling-induced constriction of cutaneous arteries, is more common in women during the period from menarche to menopause. We thus investigated the effect of 17β-estradiol (E2) on cooling-induced reduction of plantar skin blood flow (PSBF) in mouse in vivo. Ovariectomized female ddY mice, anaesthetized with pentobarbital, were treated with tetrodotoxin for eliminating the sympathetic nerve tone and artificially ventilated...
February 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28061972/estrogen-receptors-modulation-of-anxiety-like-behavior
#17
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
#18
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...
February 7, 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
#19
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...
March 2017: 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
#20
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...
February 2017: Oncology Reports
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