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GPER1

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https://www.readbyqxmd.com/read/29745344/selection-of-g1-paba-as-a-gper1-ligand-compared-to-phenol-red-via-a-ligand-based-virtual-screening-coupled-to-molecular-dynamics-simulations-and-its-anti-proliferative-effects-on-breast-cancer-cells
#1
Correa-Basurto Jose, Jose G Trujillo-Ferrara, Mendoza-Lujambio Irene, Duenas-Gonzalez Alfonso, Chavez-Blanco Alma, Martinez-Archundia Marlet, M Bello, Garcia Sanchez Jose Ruben, Fragoso-Vazquez Manuel Jonathan, Mendez-Luna David, Prestegui-Martel Berenice, Martinez-Munoz Alberto
Recent reports have demonstrated the role of the G protein-coupled estrogen receptor (GPER1) on the growth and proliferation of breast cancer cells. The coupling of GPER1 to estrogen, tamoxifen or fulvestrant triggers cellular signaling pathways (PI3K and ERK) related to cell proliferation. In an effort to develop new therapeutic strategies against breast cancer, we performed an in silico study to explore the binding pose of a set of designed G15 and G1 analogue compounds, including phenol red. First, we included a carboxyl group instead of the acetyl group from G1 to form amides with several moieties to increase the affinity for GPER1...
May 10, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29704544/prenatal-exposure-to-benzophenone-3-bp-3-induces-apoptosis-disrupts-estrogen-receptor-expression-and-alters-the-epigenetic-status-of-mouse-neurons
#2
Agnieszka Wnuk, Joanna Rzemieniec, Ewa Litwa, Władysław Lasoń, Małgorzata Kajta
Current evidence indicates that benzophenone-3 (BP-3) can pass through the placental and blood-brain barriers and thus can likely affect infant neurodevelopment. Despite widespread exposure, data showing the effects of BP-3 on the developing nervous system are scarce. This study revealed for the first time that prenatal exposure to BP-3 led to apoptosis and neurotoxicity, altered the levels of estrogen receptors (ERs) and changed the epigenetic status of mouse neurons. In the present study, multiple subcutaneous injections of pregnant mice with BP-3 at 50 mg/kg, which is an environmentally relevant dose, evoked activation of caspase-3 and lactate dehydrogenase (LDH) release as well as substantial loss of mitochondrial membrane potential in neocortical cells of their embryonic offspring...
April 25, 2018: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29679442/immunolocalization-of-g-protein-coupled-estrogen-receptor-in-the-pig-epididymis
#3
Malivindi Rocco, Aquila Saveria, Rago Vittoria
The presence of estrogen in the genital ducts of different mammalian species has been extensively studied and the estrogen influence on the functional activity of the male genital tract has been hypothesized. Conversely, very few data have been reported on pig excurrent ducts: the localization of classical estrogen receptors (ERα and ERβ) is scarcely known, while the expression of the G protein-coupled receptor (GPER1), a membrane estrogen receptor, is still unknown in pig. The aim of the present study was to evaluate GPER1 expression in the different regions of the mature pig epididymis, using immunohistochemistry, western blot and RT-PCR analyses...
April 20, 2018: Anatomical Record: Advances in Integrative Anatomy and Evolutionary Biology
https://www.readbyqxmd.com/read/29675990/intracranial-administration-of-the-g-protein-coupled-estrogen-receptor-1-antagonist-g-15-selectively-affects-dimorphic-characteristics-of-the-song-system-in-zebra-finches-taeniopygia-guttata
#4
Mahtab Attarhaie Tehrani, Sean L Veney
In zebra finches (Taeniopygia guttata), estradiol contributes to sexual differentiation of the song system but the receptor(s) underlying its action are not exactly known. Whereas mRNA and/or protein for nuclear estrogen receptors ERα and ERβ are minimally expressed, G-protein coupled estrogen receptor 1 (GPER1) has a much greater distribution within neural song regions and the syrinx. At present, however, it is unclear if this receptor contributes to dimorphic development of the song system. To test this, the specific GPER1 antagonist, G-15, was intracranially administered to zebra finches for 25 days beginning on the day of hatching...
April 20, 2018: Developmental Neurobiology
https://www.readbyqxmd.com/read/29543707/estrogen-angiogenesis-immunity-and-cell-metabolism-solving-the-puzzle
#5
REVIEW
Annalisa Trenti, Serena Tedesco, Carlotta Boscaro, Lucia Trevisi, Chiara Bolego, Andrea Cignarella
Estrogen plays an important role in the regulation of cardiovascular physiology and the immune system by inducing direct effects on multiple cell types including immune and vascular cells. Sex steroid hormones are implicated in cardiovascular protection, including endothelial healing in case of arterial injury and collateral vessel formation in ischemic tissue. Estrogen can exert potent modulation effects at all levels of the innate and adaptive immune systems. Their action is mediated by interaction with classical estrogen receptors (ERs), ERα and ERβ, as well as the more recently identified G-protein coupled receptor 30/G-protein estrogen receptor 1 (GPER1), via both genomic and non-genomic mechanisms...
March 15, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29486622/a-novel-functional-crosstalk-between-ddr1-and-the-igf-axis-and-its-relevance-for-breast-cancer
#6
Antonino Belfiore, Roberta Malaguarnera, Maria Luisa Nicolosi, Rosamaria Lappano, Marco Ragusa, Andrea Morrione, Veronica Vella
In the last decades increasing importance has been attributed to the Insulin/Insulin-like Growth Factor signaling (IIGFs) in cancer development, progression and resistance to therapy. In fact, IIGFs is often deregulated in cancer. In particular, the mitogenic insulin receptor isoform A (IR-A) and the insulin-like growth factor receptor (IGF-1R) are frequently overexpressed in cancer together with their cognate ligands IGF-1 and IGF-2. Recently, we identified discoidin domain receptor 1 (DDR1) as a new IR-A interacting protein...
March 23, 2018: Cell Adhesion & Migration
https://www.readbyqxmd.com/read/29421611/gpr30-activation-improves-memory-and-facilitates-dhpg-induced-ltd-in-the-hippocampal-ca3-of-middle-aged-mice
#7
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...
March 2018: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/29378226/membrane-initiated-estrogen-signaling-via-gq-coupled-gpcr-in-the-central-nervous-system
#8
Gwyndolin Vail, Troy A Roepke
The last few decades have revealed increasing complexity and depth to our knowledge of receptor-mediated estrogen signaling. Nuclear estrogen receptors (ERs) ERα and ERβ remain the fundamental dogma, but recent research targeting membrane-bound ERs urges for a more expanded view on ER signaling. ERα and ERβ are also involved in membrane-delineated signaling alongside membrane-specific G protein-coupled estrogen receptor 1 (GPER1), ER-X, and the Gq-coupled membrane ER (Gq-mER). Membrane ERs are responsible for eliciting rapid responses to estrogen signaling, and their importance has been increasingly indicated in central nervous system (CNS) regulation of such functions as reproduction, energy homeostasis, and stress...
January 29, 2018: Steroids
https://www.readbyqxmd.com/read/29351614/a-membrane-g-protein-coupled-estrogen-receptor-is-necessary-but-not-sufficient-for-sex-differences-in-zebra-finch-auditory-coding
#9
Amanda A Krentzel, Matheus Macedo-Lima, Maaya Z Ikeda, Luke Remage-Healey
Estradiol acts as a neuromodulator in brain regions important for cognition and sensory processing. Estradiol also shapes brain sex differences but rarely have these concepts been considered simultaneously. In male and female songbirds, estradiol rapidly increases within the auditory forebrain during song exposure and enhances local auditory processing. We tested whether G-protein-coupled estrogen receptor 1 (GPER1), a membrane-bound estrogen receptor, is necessary and sufficient for neuroestrogen regulation of forebrain auditory processing in male and female zebra finches (Taeniopygia guttata)...
March 1, 2018: Endocrinology
https://www.readbyqxmd.com/read/29134695/acute-stimulation-of-a-smooth-muscle-constrictor-by-oestradiol-17%C3%AE-via-gper1-in-bovine-oviducts
#10
T Nishie, Y Kobayashi, K Kimura, K Okuda
Oviducts play roles in reproductive processes, including gametes transport, fertilization and early embryo development. Oviductal transport is controlled by various factors such as endothelins (EDNs) and nitric oxide (NO), smooth muscle contracting and relaxing factor, respectively. EDNs and NO production depend on an ovarian steroid hormone, oestradiol-17β (E2) and E2 quickly exerts their biological functions through G protein-coupled oestrogen receptor 1 (GPER1), which mediates rapid intracellular signalling...
April 2018: Reproduction in Domestic Animals, Zuchthygiene
https://www.readbyqxmd.com/read/29073745/increased-serum-g-protein-coupled-estrogen-receptor-1-levels-and-its-diagnostic-value-in-drug-na%C3%A3-ve-patients-with-major-depressive-disorder
#11
Ebru Findikli, Ergül Belge Kurutas, Mehmet Akif Camkurt, Mehmet Fatih Karaaslan, Filiz Izci, Hüseyin Avni Fındıklı, Selçuk Kardaş, Berat Dag, Hatice Altun
Objective: The facts that depression is more prevalent in females than in males and females are exposed to depression more commonly during certain hormonal fluctuating periods indicate the role of sex hormones in physiopathology. Estrogen acts over estrogen receptors alpha and beta and recently identified G protein-coupled estrogen receptor 1 (GPER1). The present study aimed, for the first time, to evaluate serum GPER1 levels in drug-naïve major depressive disorder (MDD) patients. Methods: The study included 56 newly diagnosed drug-naïve MDD patients aged between 18 and 50 years and 42 age- and gender-matched healthy volunteers...
November 30, 2017: Clinical Psychopharmacology and Neuroscience: the Official Scientific Journal of the Korean College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28906548/activation-of-g-protein-coupled-oestrogen-receptor-1-at-the-onset-of-reperfusion-protects-the-myocardium-against-ischemia-reperfusion-injury-by-reducing-mitochondrial-dysfunction-and-mitophagy
#12
Yansheng Feng, Ngonidzashe B Madungwe, Carolina Victoria da Cruz Junho, Jean C Bopassa
BACKGROUND AND PURPOSE: Recent evidence indicates that GPER (G protein-coupled oestrogen receptor 1) mediates acute pre-ischaemic oestrogen-induced protection of the myocardium from ischaemia/reperfusion injury via a signalling cascade that includes PKC translocation, ERK1/2/ GSK-3β phosphorylation and inhibition of the mitochondrial permeability transition pore (mPTP) opening. Here, we investigated the impact and mechanism involved in post-ischaemic GPER activation in ischaemia/reperfusion injury...
December 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28706519/estrogens-promote-the-production-of-natural-neutralizing-antibodies-in-fish-through-g-protein-coupled-estrogen-receptor-1
#13
María C Rodenas, Isabel Cabas, Nuria E Gómez-González, Marta Arizcun, José Meseguer, Victoriano Mulero, Alfonsa García-Ayala
Natural antibodies play crucial roles in pathogen elimination, B-cell survival and homeostasis, and inflammatory and autoimmune diseases. Although estrogens are able to regulate both innate and adaptive immune responses, their role in the production of natural antibodies is unknown. Here, we show that the dietary intake of the synthetic estradiol analog, 17α-ethinylestradiol (EE2), one of the most potent pharmaceutical estrogens and intensively used in human therapeutics as a component of most oral contraceptives, regulates the abundance and proliferation of T and IgM(+) B lymphocytes in the teleost fish gilthead seabream (Sparus aurata L...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28688795/gper1-in-sand-rat-epididymis-effects-of-seasonal-variations-castration-and-efferent-ducts-ligation
#14
Rafik Menad, Meriem Fernini, Souaâd Smaï, Xavier Bonnet, Thérèse Gernigon-Spychalowicz, Elara Moudilou, Farida Khammar, Jean-Marie Exbrayat
Estrogen plays a crucial role in regulating epididymal function and development. Estrogen signaling is mediated via two main receptors essentially involved in the genomic regulating pathway: ERα and ERβ. Recent studies revealed the contribution of a novel estrogen receptor involved in the non-genomic pathway: GPER1. This receptor belongs to the family of seven-transmembrane G-protein-coupled receptors and it triggers rapid cellular responses. Immuno-histochemical studies and Western Blot analyses were performed to investigate the GPER1 expression in the caput and cauda epididymis of free-ranging fat sand rats (Psammomys obesus) captured during the breeding and resting seasons...
June 23, 2017: Animal Reproduction Science
https://www.readbyqxmd.com/read/28645573/evidence-that-fetal-death-is-associated-with-placental-aging
#15
Kaushik Maiti, Zakia Sultana, Robert J Aitken, Jonathan Morris, Felicity Park, Bronwyn Andrew, Simon C Riley, Roger Smith
BACKGROUND: The risk of unexplained fetal death or stillbirth increases late in pregnancy, suggesting that placental aging is an etiological factor. Aging is associated with oxidative damage to DNA, RNA, and lipids. We hypothesized that placentas at >41 completed weeks of gestation (late-term) would show changes consistent with aging that would also be present in placentas associated with stillbirths. OBJECTIVE: We sought to determine whether placentas from late-term pregnancies and unexplained stillbirth show oxidative damage and other biochemical signs of aging...
October 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28465157/gper1-gpr30-in-the-brain-crosstalk-with-classical-estrogen-receptors-and-implications-for-behavior
#16
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...
February 2018: 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-motif-dependent-and-independent-mechanisms
#17
COMPARATIVE STUDY
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 Here, we show that GPR30 also constitutively increases ERK1/2 activity...
June 16, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28427772/seasonal-variations-of-aromatase-and-estrogen-receptors-expression-in-the-testis-of-free-ranging-sand-rats
#18
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...
May 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28401437/estrogens-regulate-life-and-death-in-mitochondria
#19
Carolyn M Klinge
Estrogens coordinate and integrate cellular metabolism and mitochondrial activities by direct and indirect mechanisms mediated by differential expression and localization of estrogen receptors (ER) in a cell-specific manner. Estrogens regulate transcription and cell signaling pathways that converge to stimulate mitochondrial function- including mitochondrial bioenergetics, mitochondrial fusion and fission, calcium homeostasis, and antioxidant defense against free radicals. Estrogens regulate nuclear gene transcription by binding and activating the classical genomic estrogen receptors α and β (ERα and ERβ) and by activating plasma membrane-associated mERα, mERβ, and G-protein coupled ER (GPER, GPER1)...
August 2017: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/28374135/oxabicycloheptene-sulfonate-protects-against-%C3%AE-amyloid-induced-toxicity-by-activation-of-pi3k-akt-and-erk-signaling-pathways-via-gper1-in-c6-cells
#20
Li-Juan Deng, Chen Cheng, Jun Wu, Cai-Hua Wang, Hai-Bing Zhou, Jian Huang
Oxabicycloheptene sulfonate (OBHS) is a novel bicyclic core selective estrogen receptor modulator (SERM) with estrogen receptor (ER) antagonistic-activity and anti-inflammatory activity. However, little is known about protective action of OBHS on neurodegenerative disorders. In the present study, OBHS demonstrated a remarkably protective effect against amyloid beta (Aβ) induced cytotoxicity via G-protein-coupled estrogen receptor 1 (GPER1) in rat astroglial cell line (C6). The C6 cell death induced by Aβ was decreased by OBHS (1 μM) treatment for 45 min...
August 2017: Neurochemical Research
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