keyword
MENU ▼
Read by QxMD icon Read
search

GPR30

keyword
https://www.readbyqxmd.com/read/27908592/activation-of-gpr30-stimulates-gtp-binding-of-g%C3%AE-i1-protein-to-sustain-activation-of-erk1-2-in-inhibition-of-prostate-cancer-cell-growth-and-modulates-metastatic-properties
#1
Kin-Mang Lau, Fanny Man-Ting Ma, Jenny Tian Xia, Queeny Kwan Yi Chan, Chi-Fai Ng, Ka-Fai To
Previously, we reported that GPR30 activation by the receptor-specific, non-estrogenic ligand G-1 inhibited in vitro and in vivo growth of prostate cancer (PCa) cells via sustained Erk1/2 activation. Mechanism underlying the sustained Erk1/2 activation for PCa cell growth inhibition remains unclear. Here we report that G-1, through GPR30, activated Gαi1 proteins to sustain Erk1/2 activation but failed to activate adenylyl cyclase (AC) for cAMP production in PCa cells. The chemical-induced activation of AC-cAMP-PKA signaling attenuated Erk1/2 activity and blocked the cell growth inhibitory effects of G-1...
November 28, 2016: Experimental Cell Research
https://www.readbyqxmd.com/read/27889612/tet1-gper-pi3k-akt-pathway-is-involved-in-insulin-driven-endometrial-cancer-cell-proliferation
#2
Bing-Ying Xie, Qiao-Ying Lv, Cheng-Cheng Ning, Bing-Yi Yang, Wei-Wei Shan, Ya-Li Cheng, Chao Gu, Xue-Zhen Luo, Zhen-Bo Zhang, Xiao-Jun Chen, Xiao-Wei Xi, You-Ji Feng
Large amount of clinical evidence has demonstrated that insulin resistance is closely related to oncogenesis of endometrial cancer (EC). Despite recent studies showed the up-regulatory role of insulin in G protein-coupled estrogen receptor (GPER/GPR30) expression, GPER expression was not decreased compared to control when insulin receptor was blocked even in insulin treatment. The purpose of this study was to explore the possible mechanism by which insulin up-regulates GPER that drives EC cell proliferation...
November 23, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27888566/functional-expression-of-g-protein-coupled-receptor-30-in-immature-rat-epididymal-epithelium
#3
Xiaonian Cao, Jiehong Huang, Geng Zhang, Wulin Zuo, Chongfeng Lan, Qing Sun, Dengliang Yang, Dongdong Gao, Christopher H K Cheng, Wen-Liang Zhou
The aim of this study is to investigate the functional role of G protein-coupled receptor 30 (GPR30) in the epididymis. We found that GPR30 is expressed in the epithelium of the immature rat epididymis and is involved in chloride secretion into the caudal epididymis lumen. The short-circuit current (Isc) experiments showed that in primary cultured caudal epididymis epithelium, activation of GPR30 by its specific agonist G1 induced a mono-phasic current increase, and G15, the specific antagonist of GPR30, could completely inhibit the current induced by G1...
November 26, 2016: Cell Biology International
https://www.readbyqxmd.com/read/27880919/activation-of-g-protein-coupled-receptor-30-by-thiodiphenol-promotes-proliferation-of-estrogen-receptor-%C3%AE-positive-breast-cancer-cells
#4
Bingli Lei, Wei Peng, Gang Xu, Minghong Wu, Yu Wen, Jie Xu, Zhiqiang Yu, Yipei Wang
Many studies have been shown that environmental estrogen bisphenol A (BPA) can activate nuclear receptor (estrogen receptor alpha, ERα) or membrane receptor (G-protein-coupled receptor, GPR30) in breast cancer cells and exerts genomic or nongenomic actions inducing cell proliferation. 4,4'-thiodiphenol (TDP) as one of BPA derivatives exhibits more potent estrogenic activity than BPA does. However, comparatively little is known about the ways in which TDP interferes with these signaling pathways and produces cell biological changes...
November 20, 2016: Chemosphere
https://www.readbyqxmd.com/read/27876458/relative-abundance-of-g-protein-coupled-receptor-30-and-localization-in-testis-and-epididymis-of-sheep-at-different-developmental-stages
#5
Peiyao Lu, Fuchuan Wang, Xianyi Song, Yang Liu, Kai Zhang, Ningxian Cao
The G protein-coupled receptor 30 (GPR30) is a transmembrane estrogen receptor that binds to estrogen, and has been confirmed to have an important role in testicular cell proliferation and development. The main objective of this study was to examine GPR30 gene expression and localization in the testis and epididymis of sheep at different developmental stages. Testes, including the epididymis, were collected from Polled Dorset x Mongolian cross rams at one (n=4; wt), three (n=4; wt), six (n=4; wt), nine (n=4; wt) and 12 (n=4; wt) months of age...
December 2016: Animal Reproduction Science
https://www.readbyqxmd.com/read/27853434/expression-of-steroid-receptors-in-ameloblasts-during-amelogenesis-in-rat-incisors
#6
Sophia Houari, Sophia Loiodice, Katia Jedeon, Ariane Berdal, Sylvie Babajko
Endocrine disrupting chemicals (EDCs) play a part in the modern burst of diseases and interfere with the steroid hormone axis. Bisphenol A (BPA), one of the most active and widely used EDCs, affects ameloblast functions, leading to an enamel hypomineralization pattern similar to that of Molar Incisor Hypomineralization (MIH). In order to explore the molecular pathways stimulated by BPA during amelogenesis, we thoroughly investigated the receptors known to directly or indirectly mediate the effects of BPA. The expression patterns of high affinity BPA receptors (ERRγ, GPR30), of ketosteroid receptors (ERs, AR, PGR, GR, MR), of the retinoid receptor RXRα, and PPARγ were established using RT-qPCR analysis of RNAs extracted from microdissected enamel organ of adult rats...
2016: Frontiers in Physiology
https://www.readbyqxmd.com/read/27814026/gper-gpr30-a-nongenomic-receptor-gpcr-for-steroid-hormones-with-implications-for-cardiovascular-disease-and-cancer
#7
Ross D Feldman, Lee E Limbird
Although the rapid effects of steroids, such as estrogen and aldosterone, were postulated originally to be nongenomic, it is now appreciated that activation of such signaling pathways via a steroid-acting G protein-coupled receptor, the G protein estrogen receptor (GPER), has important transcription-dependent outcomes in the regulation of cell growth and programmed cell death secondary to GPER-regulated second-messenger pathways. GPER is expressed ubiquitously and has diverse biological effects, including regulation of endocrine, immune, neuronal, and cardiovascular functions...
October 21, 2016: Annual Review of Pharmacology and Toxicology
https://www.readbyqxmd.com/read/27799463/estrogen-receptors-and-esterol-dependent-neuroprotective-actions-a-pilot-study
#8
Ekaterine Tskitishvili, Christel Pequeux, Carine Munaut, Renaud Viellevoye, Michelle Nisolle, Agnes Noel, Jean-Michel Foidart
Estetrol (E4) has strong antioxidative, neuro- and angiogenic effects in neural system resulting in attenuation of neonatal hypoxic-ischemic encephalopathy. We aimed to define the role of estrogen receptors in E4-dependent actions in neuronal cell cultures and prove the promyelinating effect of E4. In vitro the antioxidative and cell survival/proliferating effects of E4 on H202-induced oxidative stress in primary hippocampal cell cultures were studied by using different combinations of specific inhibitors for ERα (MPP dihydrochloride), ERβ (PHTTP), GPR30 (G15) and palmytoilation (2-BR)...
October 31, 2016: Journal of Endocrinology
https://www.readbyqxmd.com/read/27796870/gpr30-activation-contributes-to-the-puerarin-mediated-neuroprotection-in-mpp-induced-sh-sy5y-cell-death
#9
Yue-Fa Cheng, Guoqi Zhu, Qing-Wen Wu, Yue-Sheng Xie, Yan Jiang, Lan Guo, Ya-Li Guan, Ying-Shuo Liu, Jun Zhang
The neuroprotective action of puerarin in Parkinson's disease (PD) models has been well investigated. However, the mechanisms involved in protection have not been completely understood. G protein-coupled receptor 30 (GPR30) is a G protein-coupled estrogen receptor and considered a potential target in the neuroprotection against PD. In this study, we investigated whether puerarin prevented against 1-methyl-4-phenylpyridinium (MPP(+))-induced cell death via GPR30. Our results showed that the GPR30 agonist, G1, exhibited puerarin-mediated neuroprotection against MPP(+)-induced cell death of SH-SY5Y cells...
October 30, 2016: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/27745655/bisphenol-a-exposure-alters-release-of-immune-and-developmental-modulators-and-expression-of-estrogen-receptors-in-human-fetal-lung-fibroblasts
#10
Laziyan Mahemuti, Qixuan Chen, Melanie C Coughlan, Min Zhang, Maria Florian, Ryan J Mailloux, Xu-Liang Cao, Kylie A Scoggan, William G Willmore, Xiaolei Jin
Bisphenol A (BPA) has been shown to exert biological effects through estrogen receptor (ER)-dependent and ER-independent mechanisms. Recent studies suggest that prenatal exposure to BPA may increase the risk of childhood asthma. To investigate the underlying mechanisms in the actions of BPA, human fetal lung fibroblasts (hFLFs) were exposed to varying doses of BPA in culture for 24hr. Effects of BPA on localization and uptake of BPA, cell viability, release of immune and developmental modulators, cellular localization and expression of ERα, ERβ and G-protein coupled estrogen receptor 30 (GPR30), and effects of ERs antagonists on BPA-induced changes in endothelin-1 (ET-1) release were examined...
October 2016: Journal of Environmental Sciences (China)
https://www.readbyqxmd.com/read/27698362/gpr30-regulates-diet-induced-adiposity-in-female-mice-and-adipogenesis-in-vitro
#11
Aihua Wang, Jing Luo, William Moore, Hana Alkhalidy, Ling Wu, Jinhua Zhang, Wei Zhen, Yao Wang, Deborah J Clegg, Bin Xu, Zhiyong Cheng, Ryan P McMillan, Matthew W Hulver, Dongmin Liu
Recent studies showed that GPR30, a seven-transmembrane G-protein-coupled receptor, is a novel estrogen receptor (ER) that mediates some biological events elicited by estrogen in several types of cancer cells. However, its physiological or pathological role in vivo is unclear. Here, we show that GPR30 knockout (GPRKO) female mice were protected from high-fat diet (HFD)-induced obesity, blood glucose intolerance, and insulin resistance. The decreased body weight gain in GPRKO female mice is due to the reduction in body fat mass...
October 4, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27629493/estrogen-receptor-signaling-in-the-ferutinin-induced-osteoblastic-differentiation-of-human-amniotic-fluid-stem-cells
#12
M Zavatti, M Guida, T Maraldi, F Beretti, L Bertoni, G B La Sala, A De Pol
AIMS: Ferutinin is a daucane sesquiterpene with a high estrogenic activity. Since ferutinin is able to enhance osteoblastic differentiation of human amniotic fluid stem cells (hAFSCs), the aim of this study was to evaluate the role of the estrogen receptors α (ERα) and G-protein coupled receptor 30 (GPR30) in ferutinin-mediated osteoblastic differentiation. Moreover, it was investigated if MEK/ERK and PI3K/Akt signaling pathways are involved in ferutinin-induced effects. MAIN METHODS: hAFSCs were cultured in a standard medium or in an osteoblastic medium for 14 or 21days and ferutinin was added at 10(-8)M...
September 11, 2016: Life Sciences
https://www.readbyqxmd.com/read/27608844/gpr30-disrupts-the-balance-of-gabaergic-and-glutamatergic-transmission-in-the-spinal-cord-driving-to-the-development-of-bone-cancer-pain
#13
Jie Luo, Xiaoxia Huang, Yali Li, Yang Li, Xueqin Xu, Yan Gao, Ruoshi Shi, Wanjun Yao, Juying Liu, Changbin Ke
Cancer induced bone pain is a very complicated clinical pain states that has proven difficult to be treated effectively due to poorly understand of underlying mechanism, but bone cancer pain (BCP) seems to be enhanced by a state of spinal sensitization. In the present study, we showed that carcinoma tibia implantation induced notable pain sensitization and up-regulation of G-protein-coupled estrogen receptor (GPR30) in the spinal cord of rats which was reversed by GPR30 knockdown. Further studies indicated that upregulation of GPR30 induced by cancer implantation resulted in a select loss of γ-aminobutyric acid-ergic (GABAergic) neurons and functionally diminished the inhibitory transmission due to reduce expression of the vesicular GABA transporter (VGAT)...
September 6, 2016: Oncotarget
https://www.readbyqxmd.com/read/27607345/protective-role-of-gper-agonist-g-1-on-cardiotoxicity-induced-by-doxorubicin
#14
Ernestina M De Francesco, Carmine Rocca, Francesco Scavello, Daniela Amelio, Teresa Pasqua, Damiano C Rigiracciolo, Andrea Scarpelli, Silvia Avino, Francesca Cirillo, Nicola Amodio, Maria C Cerra, Marcello Maggiolini, Tommaso Angelone
The use of Doxorubicin (Dox), a frontline drug for many cancers, is often complicated by dose-limiting cardiotoxicity in approximately 20% of patients. The G-protein estrogen receptor GPER/GPR30 mediates estrogen action as the cardioprotection under certain stressful conditions. For instance, GPER activation by the selective agonist G-1 reduced myocardial inflammation, improved immunosuppression, triggered pro-survival signaling cascades, improved myocardial mechanical performance and reduced infarct size after ischemia/reperfusion (I/R) injury...
September 8, 2016: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/27589731/importance-of-estrogenic-signaling-and-its-mediated-receptors-in-prostate-cancer
#15
REVIEW
Kin-Mang Lau, Ka-Fai To
Prostate cancer (PCa) treatment was first established by Huggins and Hodges in 1941, primarily described as androgen deprivation via interference of testicular androgen production. The disease remains incurable with relapse of hormone-refractory cancer after treatments. Epidemiological and clinical studies disclosed the importance of estrogens in PCa. Discovery of estrogen receptor ERβ prompted direct estrogenic actions, in conjunction with ERα, on PCa cells. Mechanistically, ERs upon ligand binding transactivate target genes at consensus genomic sites via interactions with various transcriptional co-regulators to mold estrogenic signaling...
2016: International Journal of Molecular Sciences
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
#16
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/27554391/tamoxifen-accelerates-the-repair-of-demyelinated-lesions-in-the-central-nervous-system
#17
Ginez A Gonzalez, Matthias P Hofer, Yasir A Syed, Ana I Amaral, Jon Rundle, Saifur Rahman, Chao Zhao, Mark R N Kotter
Enhancing central nervous system (CNS) myelin regeneration is recognized as an important strategy to ameliorate the devastating consequences of demyelinating diseases such as multiple sclerosis. Previous findings have indicated that myelin proteins, which accumulate following demyelination, inhibit remyelination by blocking the differentiation of rat oligodendrocyte progenitor cells (OPCs) via modulation of PKCα. We therefore screened drugs for their potential to overcome this differentiation block. From our screening, tamoxifen emerges as a potent inducer of OPC differentiation in vitro...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27494699/modulatory-effects-of-sex-steroids-progesterone-and-estradiol-on-odorant-evoked-responses-in-olfactory-receptor-neurons
#18
Ninthujah Kanageswaran, Maximilian Nagel, Paul Scholz, Julia Mohrhardt, Günter Gisselmann, Hanns Hatt
The influence of the sex steroid hormones progesterone and estradiol on physiology and behavior during menstrual cycles and pregnancy is well known. Several studies indicate that olfactory performance changes with cyclically fluctuating steroid hormone levels in females. Knowledge of the exact mechanisms behind how female sex steroids modulate olfactory signaling is limited. A number of different known genomic and non-genomic actions that are mediated by progesterone and estradiol via interactions with different receptors may be responsible for this modulation...
2016: PloS One
https://www.readbyqxmd.com/read/27449129/antioxidant-protection-of-nadph-depleted-oligodendrocyte-precursor-cells-is-dependent-on-supply-of-reduced-glutathione
#19
Ewa Kilanczyk, Sujata Saraswat Ohri, Scott R Whittemore, Michal Hetman
The pentose phosphate pathway is the main source of NADPH, which by reducing oxidized glutathione, contributes to antioxidant defenses. Although oxidative stress plays a major role in white matter injury, significance of NADPH for oligodendrocyte survival has not been yet investigated. It is reported here that the NADPH antimetabolite 6-amino-NADP (6AN) was cytotoxic to cultured adult rat spinal cord oligodendrocyte precursor cells (OPCs) as well as OPC-derived oligodendrocytes. The 6AN-induced necrosis was preceded by increased production of superoxide, NADPH depletion, and lower supply of reduced glutathione...
August 2016: ASN Neuro
https://www.readbyqxmd.com/read/27423484/ameliorative-effect-of-membrane-associated-estrogen-receptor-g-protein-coupled-receptor-30-activation-on-object-recognition-memory-in-mouse-models-of-alzheimer-s-disease
#20
Takashi Kubota, Hiroshi Matsumoto, Yutaka Kirino
Membrane-associated estrogen receptor "G protein-coupled receptor 30" (GPR30) has been implicated in spatial recognition memory and protection against neuronal death. The present study investigated the role of GPR30 in object recognition memory in an Alzheimer's disease (AD) mouse model (5XFAD) by using novel object recognition (NOR) test. Impairment of long-term (24 h) recognition memory was observed in both male and female 5XFAD mice. Selective GPR30 agonist, G-1, ameliorated this impairment in female 5XFAD mice, but not in male mice...
July 2016: Journal of Pharmacological Sciences
keyword
keyword
105975
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"