PMID-sentid Pub_year Sent_text comp_official_name comp_offset protein_name organism prot_offset 33621883-5 2021 Low concentrations of BPAF markedly increased the expression of G protein-coupled estrogen receptor (GPER1), c-Myc, CyclinD1 and c-Fos proteins, and enhanced phosphorylation of extracellular signal-regulated kinase (Erk) and protein kinase B (Akt) in SKBR-3 cells. 4,4'-hexafluorisopropylidene diphenol 22-26 G protein-coupled estrogen receptor 1 Homo sapiens 101-106 33848615-5 2021 In this study, MTT, Western blot, immunocytochemical staining, phagocytosis assay and wound healing assay were employed to detect the effect of GPR30 in N9 microglial cells after exposure to glutamate. Glutamic Acid 191-200 G protein-coupled estrogen receptor 1 Homo sapiens 144-149 33848615-6 2021 We found that the treatment of GPR30 specific agonist G1 inhibited glutamate-induced proliferation and activation in N9 microglial cells. Glutamic Acid 67-76 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 33621883-9 2021 The findings showed that GPER1 could independently regulate BPAF-induced proliferation of SKBR-3 cells without requiring ERalpha. 4,4'-hexafluorisopropylidene diphenol 60-64 G protein-coupled estrogen receptor 1 Homo sapiens 25-30 34021926-10 2021 Conversely, GPER1 antagonist G15 reversed all these features induced by estrogen. CHEMBL583543 29-32 G protein-coupled estrogen receptor 1 Homo sapiens 12-17 33868470-0 2021 Activation of GPER by E2 promotes proliferation, invasion and migration of breast cancer cells by regulating the miR-124/CD151 pathway. Estradiol 22-24 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 33868470-10 2021 The results demonstrated that E2 downregulated miR-124 expression, while upregulating G protein -coupled estrogen receptor (GPER) expression in MCF-7 cells. Estradiol 30-32 G protein-coupled estrogen receptor 1 Homo sapiens 86-122 33868470-10 2021 The results demonstrated that E2 downregulated miR-124 expression, while upregulating G protein -coupled estrogen receptor (GPER) expression in MCF-7 cells. Estradiol 30-32 G protein-coupled estrogen receptor 1 Homo sapiens 124-128 33868470-11 2021 Following treatment with the GPER antagonist, G15, miR-124 expression was significantly enhanced and E2-induced proliferation, invasion and migration of MCF-7 cells were notably inhibited. Estradiol 101-103 G protein-coupled estrogen receptor 1 Homo sapiens 29-33 33868470-14 2021 Taken together, these results suggest that upregulation of GPER expression induced by E2 promotes proliferation, invasion and migration of breast cancer cells by regulating the miR-124/CD151 pathway. Estradiol 86-88 G protein-coupled estrogen receptor 1 Homo sapiens 59-63 34032001-11 2021 Combined with the bioinformatics analysis, XBP-1, IRF-4 and GPER-1 expression was related to E2 levels, both in vivo and in vitro. Estradiol 93-95 G protein-coupled estrogen receptor 1 Homo sapiens 60-66 33893075-3 2021 MATERIALS AND METHODS: Parental and sunitinib-resistant 786-O cells were treated with GPER1 agonist G-1, and quantitative phosphoproteomics was performed. Sunitinib 36-45 G protein-coupled estrogen receptor 1 Homo sapiens 86-91 33938030-9 2021 Our results pinpoint the function of GPR30 in prostate CAFs on regulating the CAF-TAM interaction in the TME and provide new insights into PCa therapies via regulating TME. tam 82-85 G protein-coupled estrogen receptor 1 Homo sapiens 37-42 33893075-8 2021 CONCLUSION: Our results open up the possibility for managing RCC and sunitinib resistance by GPER1 agonist G-1 and its regulated pathways. Sunitinib 69-78 G protein-coupled estrogen receptor 1 Homo sapiens 93-98 33879537-10 2021 Altogether, the findings suggest that E2 activates ERbeta and GPER1 in the PrL-PFC to attenuate the GABA-mediated constraint of key outputs that mediate cocaine seeking.Significance StatementSusceptibility to drug craving and relapse is heightened in women with cocaine use disorder and varies across the reproductive cycle, likely reflecting the influence of the estrogen, 17beta-estradiol. Estradiol 38-40 G protein-coupled estrogen receptor 1 Homo sapiens 62-67 33923905-7 2021 The classic ERs have been acknowledged to function in mediating estrogen effects on glucose metabolism, but 17beta-estradiol also rapidly promotes endothelial glycolysis by increasing glucose transporter 1 (GLUT1) and 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) levels through GPER-dependent mechanisms. Estradiol 108-124 G protein-coupled estrogen receptor 1 Homo sapiens 296-300 33582643-0 2021 Insight into the mechanism of tetrachlorobisphenol A (TCBPA)-induced proliferation of breast cancer cells by GPER-mediated signaling pathways. tetrachlorodian 30-52 G protein-coupled estrogen receptor 1 Homo sapiens 109-113 33582643-0 2021 Insight into the mechanism of tetrachlorobisphenol A (TCBPA)-induced proliferation of breast cancer cells by GPER-mediated signaling pathways. tetrachlorodian 54-59 G protein-coupled estrogen receptor 1 Homo sapiens 109-113 33582643-2 2021 However, there is only limited data on the mechanisms through which TCBPA-associated estrogenic activity is related to the membrane G protein-coupled estrogen receptor (GPER) pathway. tetrachlorodian 68-73 G protein-coupled estrogen receptor 1 Homo sapiens 132-167 33582643-2 2021 However, there is only limited data on the mechanisms through which TCBPA-associated estrogenic activity is related to the membrane G protein-coupled estrogen receptor (GPER) pathway. tetrachlorodian 68-73 G protein-coupled estrogen receptor 1 Homo sapiens 169-173 33582643-4 2021 The role of GPER signaling in TCBPA-induced cell proliferation was studied by analyzing the protein expression and mRNA levels of relevant signal targets. tetrachlorodian 30-35 G protein-coupled estrogen receptor 1 Homo sapiens 12-16 33582643-6 2021 Low-concentration TCBPA also upregulated the expression of GPER, CyclinD1, c-Myc, and c-Fos proteins, as well as increased the phosphorylation of extracellular signal-regulated-kinase 1/2 (Erk1/2) and protein kinase B (Akt). tetrachlorodian 18-23 G protein-coupled estrogen receptor 1 Homo sapiens 59-63 33582643-8 2021 However, the phosphorylation of Erk1/2 and Akt decreased when the cells were treated with GPER inhibitor G15 and phosphatidylinositide 3-kinase (PI3K) inhibitor wortmannin (WM) prior to TCBPA exposure. tetrachlorodian 186-191 G protein-coupled estrogen receptor 1 Homo sapiens 90-94 33582643-10 2021 In ERalpha-positive MCF-7 cells, TCBPA also upregulated ERalpha expression, and ERalpha was found to interact with GPER-mediated signaling. tetrachlorodian 33-38 G protein-coupled estrogen receptor 1 Homo sapiens 115-119 33582643-11 2021 The results indicate that GPER activates the PI3K/Akt and Erk1/2 signal cascades to drive the cell proliferation observed for low concentrations of TCBPA. tetrachlorodian 148-153 G protein-coupled estrogen receptor 1 Homo sapiens 26-30 33582643-12 2021 The presented results suggest a new mechanism by which TCBPA exerts estrogenic action in breast cancer cells, namely, GPER signaling in an ERalpha-independent manner, and also highlights the potential risks to human health of the usage of TCBPA. tetrachlorodian 55-60 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 33582643-12 2021 The presented results suggest a new mechanism by which TCBPA exerts estrogenic action in breast cancer cells, namely, GPER signaling in an ERalpha-independent manner, and also highlights the potential risks to human health of the usage of TCBPA. tetrachlorodian 239-244 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 33879537-10 2021 Altogether, the findings suggest that E2 activates ERbeta and GPER1 in the PrL-PFC to attenuate the GABA-mediated constraint of key outputs that mediate cocaine seeking.Significance StatementSusceptibility to drug craving and relapse is heightened in women with cocaine use disorder and varies across the reproductive cycle, likely reflecting the influence of the estrogen, 17beta-estradiol. gamma-Aminobutyric Acid 100-104 G protein-coupled estrogen receptor 1 Homo sapiens 62-67 33879537-10 2021 Altogether, the findings suggest that E2 activates ERbeta and GPER1 in the PrL-PFC to attenuate the GABA-mediated constraint of key outputs that mediate cocaine seeking.Significance StatementSusceptibility to drug craving and relapse is heightened in women with cocaine use disorder and varies across the reproductive cycle, likely reflecting the influence of the estrogen, 17beta-estradiol. Cocaine 153-160 G protein-coupled estrogen receptor 1 Homo sapiens 62-67 33915037-0 2021 Eplerenone inhibits oxidized low-density lipoprotein-induced proliferation and migration of vascular smooth muscle cells by downregulating GPER expression. Eplerenone 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 139-143 33915037-13 2021 CONCLUSIONS: Eplerenone suppressed ox-LDL-induced proliferation and migration of VSMCs partly through downregulation of GPER, providing a new mechanism of support for EPL use in the clinical treatment of AS. Eplerenone 13-23 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 32971159-0 2021 Formononetin attenuates atopic dermatitis by upregulating A20 expression via activation of G protein-coupled estrogen receptor. formononetin 0-12 G protein-coupled estrogen receptor 1 Homo sapiens 91-126 33460806-3 2021 In this study, the molecular mechanism of fluoxetine-induced the proliferation of breast cancer SKBR3 and MCF-7 cells was evaluated by detecting ERalpha and GPR30-mediated ERK and PI3K/AKT signals. Fluoxetine 42-52 G protein-coupled estrogen receptor 1 Homo sapiens 157-162 33460806-4 2021 We found that low concentrations of fluoxetine upregulated the expression of GPR30, ERalpha, CyclinD1, and C-MYC proteins, as well as elevated the phosphorylation of ERK and AKT. Fluoxetine 36-46 G protein-coupled estrogen receptor 1 Homo sapiens 77-82 33460806-5 2021 The phosphorylation of ERK and AKT decreased when the cells were pretreated with ERalpha inhibitor ICI, GPR30 inhibitor G15, and PI3K inhibitor WM prior to fluoxetine exposure. Fluoxetine 156-166 G protein-coupled estrogen receptor 1 Homo sapiens 104-109 33460806-7 2021 These findings indicated that fluoxetine activated the PI3K/AKT and ERK signaling cascades via GPR30 to derive the cell proliferation. Fluoxetine 30-40 G protein-coupled estrogen receptor 1 Homo sapiens 95-100 33460806-8 2021 It suggests that fluoxetine has the potential to exert estrogen actions via GPR30. Fluoxetine 17-27 G protein-coupled estrogen receptor 1 Homo sapiens 76-81 33508329-9 2021 Moreover, E2 and E2-BSA induced cAMP production in the in vitro incubated follicles at mid-vitellogenic stage but not the GVBD stage, and the induction could be completely abolished by G-15, a Gper1 inhibitor. Cyclic AMP 32-36 G protein-coupled estrogen receptor 1 Homo sapiens 193-198 33795755-8 2021 G protein-coupled estrogenic receptor 1 (GPER) protein expression was promoted upon ZEA treatment suggesting the involvement of GPER. Zearalenone 84-87 G protein-coupled estrogen receptor 1 Homo sapiens 0-39 33795755-8 2021 G protein-coupled estrogenic receptor 1 (GPER) protein expression was promoted upon ZEA treatment suggesting the involvement of GPER. Zearalenone 84-87 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 33795755-8 2021 G protein-coupled estrogenic receptor 1 (GPER) protein expression was promoted upon ZEA treatment suggesting the involvement of GPER. Zearalenone 84-87 G protein-coupled estrogen receptor 1 Homo sapiens 128-132 33629579-7 2021 However, knockdown of GPR30 by shRNA significantly counteracted the cardioprotective effect of DEX. Dexmedetomidine 95-98 G protein-coupled estrogen receptor 1 Homo sapiens 22-27 33739385-5 2022 Sex steroids such as androgens, progestins, and estrogen and their receptors (ERalpha, ERbeta, GPER; PR-A, PR-B; AR) have been identified as important modifiers of angiogenesis, and sex differences have been reported for anti-angiogenic drugs. Steroids 4-12 G protein-coupled estrogen receptor 1 Homo sapiens 95-99 33314369-0 2021 Downregulated GPR30 Expression in the Epileptogenic Foci of Female Patients with Focal Cortical Dysplasia Type IIb and Tuberous Sclerosis Complex Is Correlated with 18 F-FDG PET-CT Values. Fluorodeoxyglucose F18 165-173 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 33314369-3 2021 Therefore, we investigated the role of GPR30 in patients with FCDIIb and TSC. fcdiib 62-68 G protein-coupled estrogen receptor 1 Homo sapiens 39-44 33314369-12 2021 Taken together, our results suggest a potential protective effect of GPR30 in the epileptogenesis of female patients with FCDIIb and TSC. fcdiib 122-128 G protein-coupled estrogen receptor 1 Homo sapiens 69-74 33574796-5 2020 In human seminoma cell line, while 17beta-estradiol (E2) inhibits in vitro cell proliferation through an ERbeta-dependent mechanism, an impermeable E2 conjugate (E2 coupled to BSA), in vitro cell proliferation is stimulated by activating ERK1/2 and protein kinase A through a membrane GPCR that we further identified as GPER/GPR30. Estradiol 35-51 G protein-coupled estrogen receptor 1 Homo sapiens 320-324 33069770-6 2021 Functionally, GPER1 activation inhibits 17beta-oestradiol (E2)-induced ER + breast cancer cell proliferation, migration, and invasion in vitro and tumour growth in vivo. Estradiol 40-57 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 33069770-6 2021 Functionally, GPER1 activation inhibits 17beta-oestradiol (E2)-induced ER + breast cancer cell proliferation, migration, and invasion in vitro and tumour growth in vivo. Estradiol 59-61 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 33574796-5 2020 In human seminoma cell line, while 17beta-estradiol (E2) inhibits in vitro cell proliferation through an ERbeta-dependent mechanism, an impermeable E2 conjugate (E2 coupled to BSA), in vitro cell proliferation is stimulated by activating ERK1/2 and protein kinase A through a membrane GPCR that we further identified as GPER/GPR30. Estradiol 35-51 G protein-coupled estrogen receptor 1 Homo sapiens 325-330 33574796-5 2020 In human seminoma cell line, while 17beta-estradiol (E2) inhibits in vitro cell proliferation through an ERbeta-dependent mechanism, an impermeable E2 conjugate (E2 coupled to BSA), in vitro cell proliferation is stimulated by activating ERK1/2 and protein kinase A through a membrane GPCR that we further identified as GPER/GPR30. Estradiol 53-55 G protein-coupled estrogen receptor 1 Homo sapiens 320-324 33574796-5 2020 In human seminoma cell line, while 17beta-estradiol (E2) inhibits in vitro cell proliferation through an ERbeta-dependent mechanism, an impermeable E2 conjugate (E2 coupled to BSA), in vitro cell proliferation is stimulated by activating ERK1/2 and protein kinase A through a membrane GPCR that we further identified as GPER/GPR30. Estradiol 53-55 G protein-coupled estrogen receptor 1 Homo sapiens 325-330 33039870-0 2021 Bisphenol A induces apoptosis through GPER-dependent activation of the ROS/Ca2+-ASK1-JNK pathway in human granulosa cell line KGN. bis(4-hydroxyphenyl)sulfone 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 38-42 33039870-0 2021 Bisphenol A induces apoptosis through GPER-dependent activation of the ROS/Ca2+-ASK1-JNK pathway in human granulosa cell line KGN. Reactive Oxygen Species 71-74 G protein-coupled estrogen receptor 1 Homo sapiens 38-42 33039870-9 2021 We pretreated with G15 (a GPER inhibitor) and found that BPA-induced ROS generation and Ca2+ accumulation and apoptosis were significantly inhibited. bisphenol A 57-60 G protein-coupled estrogen receptor 1 Homo sapiens 26-30 33039870-9 2021 We pretreated with G15 (a GPER inhibitor) and found that BPA-induced ROS generation and Ca2+ accumulation and apoptosis were significantly inhibited. Reactive Oxygen Species 69-72 G protein-coupled estrogen receptor 1 Homo sapiens 26-30 33039870-10 2021 These results suggest that BPA exposure induces KGN cell apoptosis through GPER-dependent activation of the ROS/Ca2+-ASK1-JNK signaling pathway. bisphenol A 27-30 G protein-coupled estrogen receptor 1 Homo sapiens 75-79 33039870-10 2021 These results suggest that BPA exposure induces KGN cell apoptosis through GPER-dependent activation of the ROS/Ca2+-ASK1-JNK signaling pathway. Reactive Oxygen Species 108-111 G protein-coupled estrogen receptor 1 Homo sapiens 75-79 33435260-0 2021 Modifications on the Tetrahydroquinoline Scaffold Targeting a Phenylalanine Cluster on GPER as Antiproliferative Compounds against Renal, Liver and Pancreatic Cancer Cells. 1,2,3,4-tetrahydroquinoline 21-40 G protein-coupled estrogen receptor 1 Homo sapiens 87-91 33435260-0 2021 Modifications on the Tetrahydroquinoline Scaffold Targeting a Phenylalanine Cluster on GPER as Antiproliferative Compounds against Renal, Liver and Pancreatic Cancer Cells. Phenylalanine 62-75 G protein-coupled estrogen receptor 1 Homo sapiens 87-91 33435260-2 2021 In this study, three new compounds were designed and synthesized with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-tox) properties and high affinity for the G protein-coupled estrogen receptor (GPER) binding site by in silico methods, which correlated with the growth inhibitory activity tested in a cluster of cancer cell lines. adme 141-145 G protein-coupled estrogen receptor 1 Homo sapiens 188-223 33435260-2 2021 In this study, three new compounds were designed and synthesized with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-tox) properties and high affinity for the G protein-coupled estrogen receptor (GPER) binding site by in silico methods, which correlated with the growth inhibitory activity tested in a cluster of cancer cell lines. adme 141-145 G protein-coupled estrogen receptor 1 Homo sapiens 225-229 33435260-4 2021 These in silico studies showed that the compounds reached the GPER binding site, establishing interactions with a phenylalanine cluster (F206, F208 and F278) required for GPER molecular recognition of its agonist and antagonist ligands. Phenylalanine 114-127 G protein-coupled estrogen receptor 1 Homo sapiens 62-66 33435260-4 2021 These in silico studies showed that the compounds reached the GPER binding site, establishing interactions with a phenylalanine cluster (F206, F208 and F278) required for GPER molecular recognition of its agonist and antagonist ligands. Phenylalanine 114-127 G protein-coupled estrogen receptor 1 Homo sapiens 171-175 33035625-0 2021 Anti-inflammatory effect of IGF-1 is mediated by IGF-1R cross talk with GPER in MPTP/MPP+-induced astrocyte activation. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 80-84 G protein-coupled estrogen receptor 1 Homo sapiens 72-76 32985706-7 2021 NDV-D90 promoted apoptosis via the intrinsic signaling pathway in BT549 cells (ER-negative cells), possibly by impairing E2-mediated GPER expression. Estradiol 121-123 G protein-coupled estrogen receptor 1 Homo sapiens 133-137 33022573-12 2021 Further results showed that BPA upregulated WDR5 expression through the G protein-coupled estrogen receptor (GPER)-mediated PI3K/mTOR signaling pathway. bisphenol A 28-31 G protein-coupled estrogen receptor 1 Homo sapiens 72-107 33022573-12 2021 Further results showed that BPA upregulated WDR5 expression through the G protein-coupled estrogen receptor (GPER)-mediated PI3K/mTOR signaling pathway. bisphenol A 28-31 G protein-coupled estrogen receptor 1 Homo sapiens 109-113 33035625-0 2021 Anti-inflammatory effect of IGF-1 is mediated by IGF-1R cross talk with GPER in MPTP/MPP+-induced astrocyte activation. mangion-purified polysaccharide (Candida albicans) 85-89 G protein-coupled estrogen receptor 1 Homo sapiens 72-76 33035625-5 2021 The IGF-1R antagonist JB-1 and the GPER antagonist G15 could antagonize the anti-inflammatory effect of IGF-1. CHEMBL583543 51-54 G protein-coupled estrogen receptor 1 Homo sapiens 35-39 33035625-6 2021 Silencing GPER abrogated the inhibitory effect of IGF-1 on 1-methyl-4-phenylpyridinium (MPP+)-induced upregulation of COX-2 and iNOS in primary astrocytes. 1-Methyl-4-phenylpyridinium 59-86 G protein-coupled estrogen receptor 1 Homo sapiens 10-14 33035625-6 2021 Silencing GPER abrogated the inhibitory effect of IGF-1 on 1-methyl-4-phenylpyridinium (MPP+)-induced upregulation of COX-2 and iNOS in primary astrocytes. mangion-purified polysaccharide (Candida albicans) 88-92 G protein-coupled estrogen receptor 1 Homo sapiens 10-14 33035625-10 2021 Furthermore, IGF-1 treatment alone increased the expression of GPER, which was blocked by JB-1, the phosphatidylinositol 3-kinase (PI3-K) antagonist LY294002 and the MEK antagonist PD98059 in primary astrocytes. 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one 149-157 G protein-coupled estrogen receptor 1 Homo sapiens 63-67 33035625-10 2021 Furthermore, IGF-1 treatment alone increased the expression of GPER, which was blocked by JB-1, the phosphatidylinositol 3-kinase (PI3-K) antagonist LY294002 and the MEK antagonist PD98059 in primary astrocytes. 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one 181-188 G protein-coupled estrogen receptor 1 Homo sapiens 63-67 33035625-11 2021 Overall, we show for the first time that GPER may contribute to the anti-inflammatory effect of IGF-1 against MPTP/MPP + -induced astrocyte activation. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 110-114 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 33035625-11 2021 Overall, we show for the first time that GPER may contribute to the anti-inflammatory effect of IGF-1 against MPTP/MPP + -induced astrocyte activation. mangion-purified polysaccharide (Candida albicans) 115-120 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 33068422-2 2020 Here, we observed that both estradiol and the GPER-specific agonist G1 rapidly induced cAMP production in cumulus cells, leading to transient stimulation of phosphorylated cAMP response element binding protein (CREB), which was conducive to the transcription of epidermal growth factor (EGF)-like factors, amphiregulin, epiregulin, and betacellulin. Cyclic AMP 87-91 G protein-coupled estrogen receptor 1 Homo sapiens 46-50 33425895-6 2020 Moreover, 740Y-P, a PI3K activator, reversed the effects of GPER1 knockdown on EMT processes. 740y-p 10-16 G protein-coupled estrogen receptor 1 Homo sapiens 60-65 33068422-3 2020 Inhibition of GPER by G15 significantly reduced estradiol-induced CREB phosphorylation and EGF-like factor gene expression. Estradiol 48-57 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 33068422-0 2020 Mechanisms of estradiol-induced EGF-like factor expression and oocyte maturation via G protein-coupled estrogen receptor. Estradiol 14-23 G protein-coupled estrogen receptor 1 Homo sapiens 85-120 33068422-4 2020 Consistently, the silencing of GPER expression in cultured cumulus cells abrogated the estradiol-induced CREB phosphorylation and EGF-like factor transcription. Estradiol 87-96 G protein-coupled estrogen receptor 1 Homo sapiens 31-35 33299978-3 2020 We found that the G-protein-coupled estrogen receptor (GPER) heteromerizes with FSHR, reprogramming cAMP/death signals into proliferative stimuli fundamental for sustaining oocyte survival. Cyclic AMP 100-104 G protein-coupled estrogen receptor 1 Homo sapiens 18-53 33299978-3 2020 We found that the G-protein-coupled estrogen receptor (GPER) heteromerizes with FSHR, reprogramming cAMP/death signals into proliferative stimuli fundamental for sustaining oocyte survival. Cyclic AMP 100-104 G protein-coupled estrogen receptor 1 Homo sapiens 55-59 33299978-4 2020 In human granulosa cells, survival signals are missing at high FSHR:GPER ratio, which negatively impacts follicle maturation and strongly correlates with preferential Galphas protein/cAMP-pathway coupling and FSH responsiveness of patients undergoing controlled ovarian stimulation. Cyclic AMP 183-187 G protein-coupled estrogen receptor 1 Homo sapiens 68-72 33193095-2 2020 We recently reported that acute application of E2 at the onset of reperfusion in vivo induces cardioprotective effects against I/R injury via activation of its non-steroidal receptor, G protein-coupled estrogen receptor 1 (GPER1). Estradiol 47-49 G protein-coupled estrogen receptor 1 Homo sapiens 184-221 33193108-6 2020 In the non-genomic pathway, 17beta-estradiol binds a putative plasma membrane ER (mER) such as GPR30/GPER1 to rapidly signal via kinases or calcium flux. Estradiol 28-44 G protein-coupled estrogen receptor 1 Homo sapiens 95-100 33193108-6 2020 In the non-genomic pathway, 17beta-estradiol binds a putative plasma membrane ER (mER) such as GPR30/GPER1 to rapidly signal via kinases or calcium flux. Estradiol 28-44 G protein-coupled estrogen receptor 1 Homo sapiens 101-106 33193108-6 2020 In the non-genomic pathway, 17beta-estradiol binds a putative plasma membrane ER (mER) such as GPR30/GPER1 to rapidly signal via kinases or calcium flux. Calcium 140-147 G protein-coupled estrogen receptor 1 Homo sapiens 95-100 33193108-6 2020 In the non-genomic pathway, 17beta-estradiol binds a putative plasma membrane ER (mER) such as GPR30/GPER1 to rapidly signal via kinases or calcium flux. Calcium 140-147 G protein-coupled estrogen receptor 1 Homo sapiens 101-106 33091936-9 2021 GPER1 expression was detected in 62.2% of the GH-secreting adenomas and 45% of NFAs. Niflumic Acid 79-83 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 33091936-13 2021 CONCLUSIONS: GPER1 is expressed at both gene and protein level in a substantial portion of GH-secreting adenomas and NFAs. Niflumic Acid 117-121 G protein-coupled estrogen receptor 1 Homo sapiens 13-18 33193095-2 2020 We recently reported that acute application of E2 at the onset of reperfusion in vivo induces cardioprotective effects against I/R injury via activation of its non-steroidal receptor, G protein-coupled estrogen receptor 1 (GPER1). Estradiol 47-49 G protein-coupled estrogen receptor 1 Homo sapiens 223-228 33066495-4 2020 Bisphenol A (BPA) is among the most common EDCs and exerts its effects via receptors which are widely distributed in human tissues, including nuclear oestrogen receptors (ERalpha and ERbeta), membrane-bound oestrogen receptor (G protein-coupled receptor 30; GPR30), and human nuclear receptor oestrogen-related receptor gamma. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 227-256 33066495-4 2020 Bisphenol A (BPA) is among the most common EDCs and exerts its effects via receptors which are widely distributed in human tissues, including nuclear oestrogen receptors (ERalpha and ERbeta), membrane-bound oestrogen receptor (G protein-coupled receptor 30; GPR30), and human nuclear receptor oestrogen-related receptor gamma. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 258-263 33066495-4 2020 Bisphenol A (BPA) is among the most common EDCs and exerts its effects via receptors which are widely distributed in human tissues, including nuclear oestrogen receptors (ERalpha and ERbeta), membrane-bound oestrogen receptor (G protein-coupled receptor 30; GPR30), and human nuclear receptor oestrogen-related receptor gamma. bisphenol A 13-16 G protein-coupled estrogen receptor 1 Homo sapiens 227-256 33066495-4 2020 Bisphenol A (BPA) is among the most common EDCs and exerts its effects via receptors which are widely distributed in human tissues, including nuclear oestrogen receptors (ERalpha and ERbeta), membrane-bound oestrogen receptor (G protein-coupled receptor 30; GPR30), and human nuclear receptor oestrogen-related receptor gamma. bisphenol A 13-16 G protein-coupled estrogen receptor 1 Homo sapiens 258-263 33066495-6 2020 Interestingly, GPR30 appears to exhibit greater co-localisation with TMPRSS2 in key tissues like lung and prostate, suggesting that BPA exposure may impact on the local expression of these SARS-CoV-2 infection mediators. bisphenol A 132-135 G protein-coupled estrogen receptor 1 Homo sapiens 15-20 32628929-0 2020 beta-estradiol adjusts intestinal function via ERbeta and GPR30 mediated PI3K/AKT signaling activation to alleviate postmenopausal dyslipidemia. Estradiol 0-14 G protein-coupled estrogen receptor 1 Homo sapiens 58-63 32865008-9 2020 These data suggest that IGF-1 inhibits MPTP/MPP+-induced autophagy on dopaminergic neurons through the IGF-1R/PI3k-Akt-mTOR pathway and GPER. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 39-43 G protein-coupled estrogen receptor 1 Homo sapiens 136-140 32827762-7 2020 Treatment with G15, a G-protein coupled estrogen receptor 1 antagonist, abolishes the effect of increased sphingolipid and non-sphingolipid levels in SKBr3 cells. Sphingolipids 106-118 G protein-coupled estrogen receptor 1 Homo sapiens 22-59 32628929-8 2020 ERbeta or GPR30 inhibition decreased the protective effect of beta-estradiol on cholesterol accumulation, tight junctions, and inflammation in cholesterol incubated Caco-2 cells, while silencing both ERbeta and GPR30 completely eliminated the protective effect of beta-estradiol. Estradiol 62-76 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 32628929-8 2020 ERbeta or GPR30 inhibition decreased the protective effect of beta-estradiol on cholesterol accumulation, tight junctions, and inflammation in cholesterol incubated Caco-2 cells, while silencing both ERbeta and GPR30 completely eliminated the protective effect of beta-estradiol. Cholesterol 80-91 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 32628929-8 2020 ERbeta or GPR30 inhibition decreased the protective effect of beta-estradiol on cholesterol accumulation, tight junctions, and inflammation in cholesterol incubated Caco-2 cells, while silencing both ERbeta and GPR30 completely eliminated the protective effect of beta-estradiol. Cholesterol 143-154 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 32628929-8 2020 ERbeta or GPR30 inhibition decreased the protective effect of beta-estradiol on cholesterol accumulation, tight junctions, and inflammation in cholesterol incubated Caco-2 cells, while silencing both ERbeta and GPR30 completely eliminated the protective effect of beta-estradiol. Estradiol 264-278 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 32628929-10 2020 Our results provide evidence that beta-estradiol regulates intestinal function via ERbeta and GPR30 mediated PI3K/AKT signaling activation to alleviate postmenopausal dyslipidemia. Estradiol 34-48 G protein-coupled estrogen receptor 1 Homo sapiens 94-99 32827762-7 2020 Treatment with G15, a G-protein coupled estrogen receptor 1 antagonist, abolishes the effect of increased sphingolipid and non-sphingolipid levels in SKBr3 cells. Sphingolipids 127-139 G protein-coupled estrogen receptor 1 Homo sapiens 22-59 33117280-0 2020 Continuous Exposure of Breast Cancer Cells to Tamoxifen Upregulates GPER-1 and Increases Cell Proliferation. Tamoxifen 46-55 G protein-coupled estrogen receptor 1 Homo sapiens 68-74 32513838-2 2020 Estradiol-induced cellular changes are mediated through the activation of nuclear and extranuclear estrogen receptors (ERs), which include ERalpha, ERbeta, and the G-protein coupled receptor, GPER1. Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 192-197 33117280-3 2020 Moreover, absence of GPER-1 improves the prognosis of patients treated with tamoxifen, the most used selective estrogen receptor modulator to treat ERalpha-positive breast cancer. Tamoxifen 76-85 G protein-coupled estrogen receptor 1 Homo sapiens 21-27 33117280-4 2020 MCF-7 breast cancer cells were continuously treated with 1,000 nM tamoxifen for 7 days to investigate its effect on GPER-1 protein expression, cell proliferation and intracellular [Ca2+]i mobilization, a key signaling pathway. Tamoxifen 66-75 G protein-coupled estrogen receptor 1 Homo sapiens 116-122 33117280-5 2020 Breast cancer cells continuously treated with tamoxifen, exhibited a robust [Ca2+]i mobilization after stimulation with 1,000 nM tamoxifen, a response that was blunted by preincubation of cells with G15, a commercial GPER-1 antagonist. Tamoxifen 46-55 G protein-coupled estrogen receptor 1 Homo sapiens 217-223 33117280-5 2020 Breast cancer cells continuously treated with tamoxifen, exhibited a robust [Ca2+]i mobilization after stimulation with 1,000 nM tamoxifen, a response that was blunted by preincubation of cells with G15, a commercial GPER-1 antagonist. Tamoxifen 129-138 G protein-coupled estrogen receptor 1 Homo sapiens 217-223 33117280-7 2020 Proliferation of cells continuously treated with tamoxifen and stimulated with 2,000 nM tamoxifen, was also higher than that observed in untreated cells in a degree that was approximately 90% attributable to GPER-1. Tamoxifen 49-58 G protein-coupled estrogen receptor 1 Homo sapiens 208-214 33117280-7 2020 Proliferation of cells continuously treated with tamoxifen and stimulated with 2,000 nM tamoxifen, was also higher than that observed in untreated cells in a degree that was approximately 90% attributable to GPER-1. Tamoxifen 88-97 G protein-coupled estrogen receptor 1 Homo sapiens 208-214 33117280-9 2020 Although we cannot fully extrapolate the results obtained in vitro to the patients, our results shed some light on the occurrence of drug resistance in breast cancer patients who are ERalpha/GPER-1 positive, have been treated with tamoxifen and display low survival rate. Tamoxifen 231-240 G protein-coupled estrogen receptor 1 Homo sapiens 191-197 32559878-6 2020 Both ToCP and TpCP activated GPER-mediated cAMP production and calcium mobilization, whereas TmCP had different mode of action, it only triggered GPER-mediated calcium mobilization, as evidenced by using the specific GPER inhibitor (G15) and GPER overexpressing experiments. Cyclic AMP 43-47 G protein-coupled estrogen receptor 1 Homo sapiens 29-33 33133016-2 2020 Via three receptors known to date, including estrogen receptors alpha (ERalpha) and beta (ERbeta) and the G protein-coupled estrogen receptor 1 (GPER, aka GPR30), E2 regulates numerous calcium-dependent activities in cardiovascular tissues. Calcium 185-192 G protein-coupled estrogen receptor 1 Homo sapiens 106-143 33133016-2 2020 Via three receptors known to date, including estrogen receptors alpha (ERalpha) and beta (ERbeta) and the G protein-coupled estrogen receptor 1 (GPER, aka GPR30), E2 regulates numerous calcium-dependent activities in cardiovascular tissues. Calcium 185-192 G protein-coupled estrogen receptor 1 Homo sapiens 145-149 33133016-2 2020 Via three receptors known to date, including estrogen receptors alpha (ERalpha) and beta (ERbeta) and the G protein-coupled estrogen receptor 1 (GPER, aka GPR30), E2 regulates numerous calcium-dependent activities in cardiovascular tissues. Calcium 185-192 G protein-coupled estrogen receptor 1 Homo sapiens 155-160 32978426-2 2020 Our previous work in activated human peripheral blood mononuclear cells demonstrated that exposure to "low-dose" BPA diminished telomerase activity via an ER/GPR30-ERK signalling pathway. bisphenol A 113-116 G protein-coupled estrogen receptor 1 Homo sapiens 158-163 32957524-2 2020 Fifteen years ago, it was discovered that a member of the G protein-coupled receptor family, GPR30, which binds also with high affinity to estradiol and is responsible, in part, for the rapid non-genomic actions of estrogens. Estradiol 139-148 G protein-coupled estrogen receptor 1 Homo sapiens 93-98 32906618-5 2020 The estrogen-agonistic effect of tamoxifen in endometrial cancers can also be explained by the expression of G-protein coupled estrogen receptor 1 (GPER-1), a membrane-bound estrogen receptor for which tamoxifen and other "antiestrogens" are pure agonists. Tamoxifen 33-42 G protein-coupled estrogen receptor 1 Homo sapiens 109-146 32906618-5 2020 The estrogen-agonistic effect of tamoxifen in endometrial cancers can also be explained by the expression of G-protein coupled estrogen receptor 1 (GPER-1), a membrane-bound estrogen receptor for which tamoxifen and other "antiestrogens" are pure agonists. Tamoxifen 33-42 G protein-coupled estrogen receptor 1 Homo sapiens 148-154 32906618-5 2020 The estrogen-agonistic effect of tamoxifen in endometrial cancers can also be explained by the expression of G-protein coupled estrogen receptor 1 (GPER-1), a membrane-bound estrogen receptor for which tamoxifen and other "antiestrogens" are pure agonists. Tamoxifen 202-211 G protein-coupled estrogen receptor 1 Homo sapiens 109-146 32906618-5 2020 The estrogen-agonistic effect of tamoxifen in endometrial cancers can also be explained by the expression of G-protein coupled estrogen receptor 1 (GPER-1), a membrane-bound estrogen receptor for which tamoxifen and other "antiestrogens" are pure agonists. Tamoxifen 202-211 G protein-coupled estrogen receptor 1 Homo sapiens 148-154 32907599-3 2020 Certain GPCRs have been shown to bind steroid hormones, for example, G protein-coupled estrogen receptor 1 (GPER1) binds estrogen in humans, and Drosophila dopamine/ecdysteroid receptor (DopEcR) binds the molting hormone 20-hydroxyecdysone (20E) in insects. Steroids 38-45 G protein-coupled estrogen receptor 1 Homo sapiens 69-106 32907599-3 2020 Certain GPCRs have been shown to bind steroid hormones, for example, G protein-coupled estrogen receptor 1 (GPER1) binds estrogen in humans, and Drosophila dopamine/ecdysteroid receptor (DopEcR) binds the molting hormone 20-hydroxyecdysone (20E) in insects. Steroids 38-45 G protein-coupled estrogen receptor 1 Homo sapiens 108-113 32907599-3 2020 Certain GPCRs have been shown to bind steroid hormones, for example, G protein-coupled estrogen receptor 1 (GPER1) binds estrogen in humans, and Drosophila dopamine/ecdysteroid receptor (DopEcR) binds the molting hormone 20-hydroxyecdysone (20E) in insects. Ecdysterone 221-239 G protein-coupled estrogen receptor 1 Homo sapiens 69-106 32907599-3 2020 Certain GPCRs have been shown to bind steroid hormones, for example, G protein-coupled estrogen receptor 1 (GPER1) binds estrogen in humans, and Drosophila dopamine/ecdysteroid receptor (DopEcR) binds the molting hormone 20-hydroxyecdysone (20E) in insects. Ecdysterone 221-239 G protein-coupled estrogen receptor 1 Homo sapiens 108-113 32907599-3 2020 Certain GPCRs have been shown to bind steroid hormones, for example, G protein-coupled estrogen receptor 1 (GPER1) binds estrogen in humans, and Drosophila dopamine/ecdysteroid receptor (DopEcR) binds the molting hormone 20-hydroxyecdysone (20E) in insects. Ecdysterone 241-244 G protein-coupled estrogen receptor 1 Homo sapiens 69-106 32907599-3 2020 Certain GPCRs have been shown to bind steroid hormones, for example, G protein-coupled estrogen receptor 1 (GPER1) binds estrogen in humans, and Drosophila dopamine/ecdysteroid receptor (DopEcR) binds the molting hormone 20-hydroxyecdysone (20E) in insects. Ecdysterone 241-244 G protein-coupled estrogen receptor 1 Homo sapiens 108-113 33061416-8 2020 Moreover, the overexpression of ERRalpha induced by estrogen and G1 (GPER agonist) was reversed by knocking down of GPER and blocking the MAPK signaling with PD98059 in both cell lines. 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one 158-165 G protein-coupled estrogen receptor 1 Homo sapiens 69-73 32559878-0 2020 Tricresyl phosphate isomers exert estrogenic effects via G protein-coupled estrogen receptor-mediated pathways. Tritolyl Phosphates 0-19 G protein-coupled estrogen receptor 1 Homo sapiens 57-92 32559878-6 2020 Both ToCP and TpCP activated GPER-mediated cAMP production and calcium mobilization, whereas TmCP had different mode of action, it only triggered GPER-mediated calcium mobilization, as evidenced by using the specific GPER inhibitor (G15) and GPER overexpressing experiments. tmcp 93-97 G protein-coupled estrogen receptor 1 Homo sapiens 146-150 32559878-6 2020 Both ToCP and TpCP activated GPER-mediated cAMP production and calcium mobilization, whereas TmCP had different mode of action, it only triggered GPER-mediated calcium mobilization, as evidenced by using the specific GPER inhibitor (G15) and GPER overexpressing experiments. tmcp 93-97 G protein-coupled estrogen receptor 1 Homo sapiens 146-150 32559878-6 2020 Both ToCP and TpCP activated GPER-mediated cAMP production and calcium mobilization, whereas TmCP had different mode of action, it only triggered GPER-mediated calcium mobilization, as evidenced by using the specific GPER inhibitor (G15) and GPER overexpressing experiments. tmcp 93-97 G protein-coupled estrogen receptor 1 Homo sapiens 146-150 32559878-6 2020 Both ToCP and TpCP activated GPER-mediated cAMP production and calcium mobilization, whereas TmCP had different mode of action, it only triggered GPER-mediated calcium mobilization, as evidenced by using the specific GPER inhibitor (G15) and GPER overexpressing experiments. Calcium 160-167 G protein-coupled estrogen receptor 1 Homo sapiens 146-150 32559878-6 2020 Both ToCP and TpCP activated GPER-mediated cAMP production and calcium mobilization, whereas TmCP had different mode of action, it only triggered GPER-mediated calcium mobilization, as evidenced by using the specific GPER inhibitor (G15) and GPER overexpressing experiments. Calcium 160-167 G protein-coupled estrogen receptor 1 Homo sapiens 146-150 32559878-6 2020 Both ToCP and TpCP activated GPER-mediated cAMP production and calcium mobilization, whereas TmCP had different mode of action, it only triggered GPER-mediated calcium mobilization, as evidenced by using the specific GPER inhibitor (G15) and GPER overexpressing experiments. Calcium 160-167 G protein-coupled estrogen receptor 1 Homo sapiens 146-150 32559878-8 2020 Our results, for the first time, found a new target, GPER, for TCPs exerting their estrogen-disrupting effects, and demonstrated complex estrogen-disrupting effects of three TCP isomers involved their opposite activities toward ERalpha and GPER. Tritolyl Phosphates 63-66 G protein-coupled estrogen receptor 1 Homo sapiens 53-57 32559878-8 2020 Our results, for the first time, found a new target, GPER, for TCPs exerting their estrogen-disrupting effects, and demonstrated complex estrogen-disrupting effects of three TCP isomers involved their opposite activities toward ERalpha and GPER. Tritolyl Phosphates 63-66 G protein-coupled estrogen receptor 1 Homo sapiens 240-244 33084596-7 2020 Estradiol and GPER ligands provide a similar pattern of fit to adenine nucleotide. Adenine Nucleotides 63-81 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 32757462-2 2020 We recently showed that 17beta-estradiol (E2) triggers angiogenesis via the membrane G-protein coupled estrogen receptor (GPER) and the key glycolytic protein PFKFB3 as a downstream effector. Estradiol 24-40 G protein-coupled estrogen receptor 1 Homo sapiens 85-120 32757462-2 2020 We recently showed that 17beta-estradiol (E2) triggers angiogenesis via the membrane G-protein coupled estrogen receptor (GPER) and the key glycolytic protein PFKFB3 as a downstream effector. Estradiol 24-40 G protein-coupled estrogen receptor 1 Homo sapiens 122-126 32757462-2 2020 We recently showed that 17beta-estradiol (E2) triggers angiogenesis via the membrane G-protein coupled estrogen receptor (GPER) and the key glycolytic protein PFKFB3 as a downstream effector. Estradiol 42-44 G protein-coupled estrogen receptor 1 Homo sapiens 85-120 32757462-2 2020 We recently showed that 17beta-estradiol (E2) triggers angiogenesis via the membrane G-protein coupled estrogen receptor (GPER) and the key glycolytic protein PFKFB3 as a downstream effector. Estradiol 42-44 G protein-coupled estrogen receptor 1 Homo sapiens 122-126 32757462-5 2020 In the presence of cycloheximide, E2 and G1 treatment counteracted PFKFB3 degradation over time, whereas E2-induced PFKFB3 stabilization was abolished by the GPER antagonist G15. CHEMBL583543 174-177 G protein-coupled estrogen receptor 1 Homo sapiens 158-162 33070824-3 2020 RESULTS: The high concentration of genistein promoted the expression of ERbeta and GPR30 in the SW579 cells, but ERalpha was not expressed. Genistein 35-44 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 32757462-10 2020 Finally, E2 and G1 treatments rapidly enhanced glucose transporter GLUT1 levels via GPER independent of transcriptional activation. Glucose 47-54 G protein-coupled estrogen receptor 1 Homo sapiens 84-88 33070824-5 2020 CONCLUSION: Genistein can obiviously promote the cell proliferation in the SW579 cells, which may be related to the action of GPR30. Genistein 12-21 G protein-coupled estrogen receptor 1 Homo sapiens 126-131 33070824-2 2020 METHODS: The real-time PCR was applied to detect the expression of estrogen receptor(ER)alpha ERbeta and G protein-coupled receptor(GPR)30 in human thyroid squamous cell line SW579; MTT was used to test the effect of genistein on cell proliferation in the SW579 cells before and after blocking GPR30; flow cytometry was explorited to measure the effect of genistein on the cell cycle and apoptosis in the SW579 was detected before and after blocking GPR30. monooxyethylene trimethylolpropane tristearate 182-185 G protein-coupled estrogen receptor 1 Homo sapiens 294-299 33070824-2 2020 METHODS: The real-time PCR was applied to detect the expression of estrogen receptor(ER)alpha ERbeta and G protein-coupled receptor(GPR)30 in human thyroid squamous cell line SW579; MTT was used to test the effect of genistein on cell proliferation in the SW579 cells before and after blocking GPR30; flow cytometry was explorited to measure the effect of genistein on the cell cycle and apoptosis in the SW579 was detected before and after blocking GPR30. monooxyethylene trimethylolpropane tristearate 182-185 G protein-coupled estrogen receptor 1 Homo sapiens 450-455 32973677-5 2020 Besides, the G protein-coupled estrogen receptor (GPER, formerly known as GPR30) was recently described as a seven-transmembrane receptor that mediates non-genomic estrogenic signaling, including calcium mobilization, cAMP synthesis, cleavage of matrix metalloproteinases, transactivation of epidermal growth factor receptor (EGFR), and the subsequent activation of PI3K and MAPK signaling pathways, which are the reasons why it is related to cellular processes, such as cell-cycle progression, cellular proliferation, differentiation, apoptosis, migration, and invasion. Calcium 196-203 G protein-coupled estrogen receptor 1 Homo sapiens 13-48 32743632-3 2020 Among these techniques, steady-state fluorescence and ultraviolet-visible spectroscopic analyses showed that PFBA, PFOA and PFDoA quenched the endogenous GPER fluorescence by combined dynamic and static quenching and non-radiative energy transfer. perfluorobutyric acid 109-113 G protein-coupled estrogen receptor 1 Homo sapiens 154-158 32743632-3 2020 Among these techniques, steady-state fluorescence and ultraviolet-visible spectroscopic analyses showed that PFBA, PFOA and PFDoA quenched the endogenous GPER fluorescence by combined dynamic and static quenching and non-radiative energy transfer. perfluorooctanoic acid 115-119 G protein-coupled estrogen receptor 1 Homo sapiens 154-158 32743632-3 2020 Among these techniques, steady-state fluorescence and ultraviolet-visible spectroscopic analyses showed that PFBA, PFOA and PFDoA quenched the endogenous GPER fluorescence by combined dynamic and static quenching and non-radiative energy transfer. perfluorododecanoic acid 124-129 G protein-coupled estrogen receptor 1 Homo sapiens 154-158 32743632-5 2020 Fourier transform infrared spectroscopy and three-dimensional fluorescence showed that the secondary structure of the GPER changed after binding to PFCAs. pfcas 148-153 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 32743632-6 2020 Thermodynamic analysis showed DeltaG < 0, which indicated that the interaction between the GPER and PFCAs was spontaneous. pfcas 100-105 G protein-coupled estrogen receptor 1 Homo sapiens 91-95 32743632-7 2020 For the binding of PFBA and PFOA to the GPER, DeltaH > 0 and DeltaS > 0, indicating that the interaction was mainly driven by hydrophobic forces; for the binding of PFDoA to the GPER, DeltaH < 0 and DeltaS < 0, suggesting that van der Waals force and hydrogen bonding were the main interaction forces. Hydrogen 251-259 G protein-coupled estrogen receptor 1 Homo sapiens 40-44 32743632-8 2020 Molecular dynamics simulations suggested that the stability of the GPER-PFCA complexes was higher than that of the free GPER, and also that the structure and hydrophobicity of the GPER changed after binding to PFCAs. pfca 72-76 G protein-coupled estrogen receptor 1 Homo sapiens 67-71 32743632-8 2020 Molecular dynamics simulations suggested that the stability of the GPER-PFCA complexes was higher than that of the free GPER, and also that the structure and hydrophobicity of the GPER changed after binding to PFCAs. pfca 72-76 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 32743632-8 2020 Molecular dynamics simulations suggested that the stability of the GPER-PFCA complexes was higher than that of the free GPER, and also that the structure and hydrophobicity of the GPER changed after binding to PFCAs. pfca 72-76 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 32743632-8 2020 Molecular dynamics simulations suggested that the stability of the GPER-PFCA complexes was higher than that of the free GPER, and also that the structure and hydrophobicity of the GPER changed after binding to PFCAs. pfcas 210-215 G protein-coupled estrogen receptor 1 Homo sapiens 67-71 32743632-8 2020 Molecular dynamics simulations suggested that the stability of the GPER-PFCA complexes was higher than that of the free GPER, and also that the structure and hydrophobicity of the GPER changed after binding to PFCAs. pfcas 210-215 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 32743632-8 2020 Molecular dynamics simulations suggested that the stability of the GPER-PFCA complexes was higher than that of the free GPER, and also that the structure and hydrophobicity of the GPER changed after binding to PFCAs. pfcas 210-215 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 32743632-9 2020 Molecular docking analysis showed that all three PFCAs could form hydrogen bonds with the GPER, which improved the stability of the complex. Hydrogen 66-74 G protein-coupled estrogen receptor 1 Homo sapiens 90-94 32743632-0 2020 Investigating the interaction between three perfluorinated carboxylic acids and the G protein-coupled estrogen receptor: spectroscopic analyses and computational simulations. Carboxylic Acids 59-75 G protein-coupled estrogen receptor 1 Homo sapiens 84-119 32743632-1 2020 In this paper, perfluorinated compounds (PFCs), such as perfluorobutyric acid (PFBA), perfluorooctanoic acid (PFOA) and perfluorododecanoic acid (PFDoA), were selected as typical representatives of perfluorinated carboxylic acids (PFCAs) to study the effects of PFCAs on the G protein-coupled estrogen receptor (GPER). perfluorinated compounds 15-39 G protein-coupled estrogen receptor 1 Homo sapiens 275-310 32743632-1 2020 In this paper, perfluorinated compounds (PFCs), such as perfluorobutyric acid (PFBA), perfluorooctanoic acid (PFOA) and perfluorododecanoic acid (PFDoA), were selected as typical representatives of perfluorinated carboxylic acids (PFCAs) to study the effects of PFCAs on the G protein-coupled estrogen receptor (GPER). perfluorinated compounds 15-39 G protein-coupled estrogen receptor 1 Homo sapiens 312-316 32743632-1 2020 In this paper, perfluorinated compounds (PFCs), such as perfluorobutyric acid (PFBA), perfluorooctanoic acid (PFOA) and perfluorododecanoic acid (PFDoA), were selected as typical representatives of perfluorinated carboxylic acids (PFCAs) to study the effects of PFCAs on the G protein-coupled estrogen receptor (GPER). pfcs 41-45 G protein-coupled estrogen receptor 1 Homo sapiens 275-310 32743632-1 2020 In this paper, perfluorinated compounds (PFCs), such as perfluorobutyric acid (PFBA), perfluorooctanoic acid (PFOA) and perfluorododecanoic acid (PFDoA), were selected as typical representatives of perfluorinated carboxylic acids (PFCAs) to study the effects of PFCAs on the G protein-coupled estrogen receptor (GPER). pfcs 41-45 G protein-coupled estrogen receptor 1 Homo sapiens 312-316 32249236-7 2020 GPR30 is activated by other endogenous estrogens, estrone and estriol. Estrone 50-57 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 32249236-7 2020 GPR30 is activated by other endogenous estrogens, estrone and estriol. Estriol 62-69 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 32249236-8 2020 Moreover, GPR30 activation by zearalenone, a nonsteroidal mycoestrogen, suppresses LH secretion. Zearalenone 30-41 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 32973677-5 2020 Besides, the G protein-coupled estrogen receptor (GPER, formerly known as GPR30) was recently described as a seven-transmembrane receptor that mediates non-genomic estrogenic signaling, including calcium mobilization, cAMP synthesis, cleavage of matrix metalloproteinases, transactivation of epidermal growth factor receptor (EGFR), and the subsequent activation of PI3K and MAPK signaling pathways, which are the reasons why it is related to cellular processes, such as cell-cycle progression, cellular proliferation, differentiation, apoptosis, migration, and invasion. Calcium 196-203 G protein-coupled estrogen receptor 1 Homo sapiens 50-54 32249236-8 2020 Moreover, GPR30 activation by zearalenone, a nonsteroidal mycoestrogen, suppresses LH secretion. Luteinizing Hormone 83-85 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 32973677-5 2020 Besides, the G protein-coupled estrogen receptor (GPER, formerly known as GPR30) was recently described as a seven-transmembrane receptor that mediates non-genomic estrogenic signaling, including calcium mobilization, cAMP synthesis, cleavage of matrix metalloproteinases, transactivation of epidermal growth factor receptor (EGFR), and the subsequent activation of PI3K and MAPK signaling pathways, which are the reasons why it is related to cellular processes, such as cell-cycle progression, cellular proliferation, differentiation, apoptosis, migration, and invasion. Calcium 196-203 G protein-coupled estrogen receptor 1 Homo sapiens 74-79 32973677-5 2020 Besides, the G protein-coupled estrogen receptor (GPER, formerly known as GPR30) was recently described as a seven-transmembrane receptor that mediates non-genomic estrogenic signaling, including calcium mobilization, cAMP synthesis, cleavage of matrix metalloproteinases, transactivation of epidermal growth factor receptor (EGFR), and the subsequent activation of PI3K and MAPK signaling pathways, which are the reasons why it is related to cellular processes, such as cell-cycle progression, cellular proliferation, differentiation, apoptosis, migration, and invasion. Cyclic AMP 218-222 G protein-coupled estrogen receptor 1 Homo sapiens 13-48 32973677-5 2020 Besides, the G protein-coupled estrogen receptor (GPER, formerly known as GPR30) was recently described as a seven-transmembrane receptor that mediates non-genomic estrogenic signaling, including calcium mobilization, cAMP synthesis, cleavage of matrix metalloproteinases, transactivation of epidermal growth factor receptor (EGFR), and the subsequent activation of PI3K and MAPK signaling pathways, which are the reasons why it is related to cellular processes, such as cell-cycle progression, cellular proliferation, differentiation, apoptosis, migration, and invasion. Cyclic AMP 218-222 G protein-coupled estrogen receptor 1 Homo sapiens 50-54 32973677-5 2020 Besides, the G protein-coupled estrogen receptor (GPER, formerly known as GPR30) was recently described as a seven-transmembrane receptor that mediates non-genomic estrogenic signaling, including calcium mobilization, cAMP synthesis, cleavage of matrix metalloproteinases, transactivation of epidermal growth factor receptor (EGFR), and the subsequent activation of PI3K and MAPK signaling pathways, which are the reasons why it is related to cellular processes, such as cell-cycle progression, cellular proliferation, differentiation, apoptosis, migration, and invasion. Cyclic AMP 218-222 G protein-coupled estrogen receptor 1 Homo sapiens 74-79 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. tphp 206-210 G protein-coupled estrogen receptor 1 Homo sapiens 107-136 32849310-1 2020 G protein-coupled estrogen receptor (GPER) in the amygdala and the dorsal hippocampus mediates actions of estradiol on anxiety, social recognition and spatial memory. Estradiol 106-115 G protein-coupled estrogen receptor 1 Homo sapiens 0-35 32849310-1 2020 G protein-coupled estrogen receptor (GPER) in the amygdala and the dorsal hippocampus mediates actions of estradiol on anxiety, social recognition and spatial memory. Estradiol 106-115 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 32325111-0 2020 Bisphenol A induces focal adhesions assembly and activation of FAK, Src and ERK2 via GPER in MDA-MB-231 breast cancer cells. bis(4-hydroxyphenyl)sulfone 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 85-89 32325111-4 2020 The G protein-coupled estrogen receptor (GPER) is a G protein-coupled receptor coupled with Gs proteins that is activated by estrogen and estrogenic compounds and it is the receptor for BPA. bisphenol A 186-189 G protein-coupled estrogen receptor 1 Homo sapiens 4-39 32325111-4 2020 The G protein-coupled estrogen receptor (GPER) is a G protein-coupled receptor coupled with Gs proteins that is activated by estrogen and estrogenic compounds and it is the receptor for BPA. bisphenol A 186-189 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 32325111-6 2020 Here, we demonstrate that BPA induces an increase of GPER expression and activation of FAK, Src and ERK2, and an increase of focal adhesion assembly via GPER in TNBC MDA-MB-231 cells. bisphenol A 26-29 G protein-coupled estrogen receptor 1 Homo sapiens 53-57 32325111-6 2020 Here, we demonstrate that BPA induces an increase of GPER expression and activation of FAK, Src and ERK2, and an increase of focal adhesion assembly via GPER in TNBC MDA-MB-231 cells. bisphenol A 26-29 G protein-coupled estrogen receptor 1 Homo sapiens 153-157 32325111-8 2020 Collectively our data showed that BPA via GPER and/or EGFR transactivation induces activation of signal transduction pathways that mediate migration in TNBC MDA-MB-231 cells. bisphenol A 34-37 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 31967341-4 2020 However, whether GPER is involved in estrogen-dependent visceral hypersensitivity via mast cell degranulation is still unknown. Estrogens 37-45 G protein-coupled estrogen receptor 1 Homo sapiens 17-21 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. tphp 206-210 G protein-coupled estrogen receptor 1 Homo sapiens 138-143 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. N-(3,4,5-trichlorophenyl)succinimide 212-215 G protein-coupled estrogen receptor 1 Homo sapiens 107-136 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. N-(3,4,5-trichlorophenyl)succinimide 212-215 G protein-coupled estrogen receptor 1 Homo sapiens 138-143 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. 2-methyl-1,1-diphenyl-3-(1-pyrrolidyl)-1-propanol 217-221 G protein-coupled estrogen receptor 1 Homo sapiens 107-136 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. 2-methyl-1,1-diphenyl-3-(1-pyrrolidyl)-1-propanol 217-221 G protein-coupled estrogen receptor 1 Homo sapiens 138-143 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. ippdp 223-228 G protein-coupled estrogen receptor 1 Homo sapiens 107-136 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. ippdp 223-228 G protein-coupled estrogen receptor 1 Homo sapiens 138-143 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. Cytidine Diphosphate 230-233 G protein-coupled estrogen receptor 1 Homo sapiens 107-136 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. Cytidine Diphosphate 230-233 G protein-coupled estrogen receptor 1 Homo sapiens 138-143 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. mphp 238-242 G protein-coupled estrogen receptor 1 Homo sapiens 107-136 32766240-9 2020 The GPER antagonist G15 and siGPER obviously abolished the above effects by icariin. icariin 76-83 G protein-coupled estrogen receptor 1 Homo sapiens 4-8 32766240-0 2020 Icariin Prevents Extracellular Matrix Accumulation and Ameliorates Experimental Diabetic Kidney Disease by Inhibiting Oxidative Stress via GPER Mediated p62-Dependent Keap1 Degradation and Nrf2 Activation. icariin 0-7 G protein-coupled estrogen receptor 1 Homo sapiens 139-143 32330712-6 2020 The results from the E-SCREEN assay showed that all tested OPFRs except TMP had estrogenic properties, and G protein-coupled receptor 30 (GPR30) was involved in the estrogenicity of eight OPFRs, TiBP, THP, TPhP, TCP, MDPP, IPPDP, CDP and MPhP. mphp 238-242 G protein-coupled estrogen receptor 1 Homo sapiens 138-143 32587576-8 2020 Interestingly, GPER is reported to mediate many of the rapid responses of estradiol in the adult brain, and is widely distributed in the mammalian brain including the plasma membrane of hippocampal neurons (23-31). Estradiol 74-83 G protein-coupled estrogen receptor 1 Homo sapiens 15-19 32682779-0 2020 Panax ginseng metabolite (GIM-1) modulates the effects of monobutyl phthalate (MBP) on the GPR30/GPER1 canonical pathway in human Sertoli cells. monobutyl phthalate 58-77 G protein-coupled estrogen receptor 1 Homo sapiens 91-96 32682779-0 2020 Panax ginseng metabolite (GIM-1) modulates the effects of monobutyl phthalate (MBP) on the GPR30/GPER1 canonical pathway in human Sertoli cells. monobutyl phthalate 58-77 G protein-coupled estrogen receptor 1 Homo sapiens 97-102 32682779-1 2020 This study was performed to evaluate the effect of monobutyl phthalate (MBP) on GPR30-activated pathways in Sertoli cells. monobutyl phthalate 51-70 G protein-coupled estrogen receptor 1 Homo sapiens 80-85 32138466-3 2020 A modified protein lipid overlay assay (PLO) was used t o further verify whether EPA was a ligand of GPR30 in ES2 cells. Eicosapentaenoic Acid 82-85 G protein-coupled estrogen receptor 1 Homo sapiens 102-107 32138466-5 2020 Finally, inhibitory effect of EPA on tumor growth via GPR30 was determined in vitro and in vivo. Eicosapentaenoic Acid 30-33 G protein-coupled estrogen receptor 1 Homo sapiens 54-59 32138466-6 2020 Results: EPA suppressed ES2 ovarian clear cell carcinoma cells growth via GPR30, a novel EPA receptor, by inducing apoptosis. Eicosapentaenoic Acid 9-12 G protein-coupled estrogen receptor 1 Homo sapiens 74-79 32138466-7 2020 As a ligand of GPR30, EPA activated the GPR30-cAMP-PKA signaling pathway. Eicosapentaenoic Acid 22-25 G protein-coupled estrogen receptor 1 Homo sapiens 15-20 32138466-7 2020 As a ligand of GPR30, EPA activated the GPR30-cAMP-PKA signaling pathway. Eicosapentaenoic Acid 22-25 G protein-coupled estrogen receptor 1 Homo sapiens 40-45 32138466-7 2020 As a ligand of GPR30, EPA activated the GPR30-cAMP-PKA signaling pathway. Cyclic AMP 46-50 G protein-coupled estrogen receptor 1 Homo sapiens 15-20 32138466-7 2020 As a ligand of GPR30, EPA activated the GPR30-cAMP-PKA signaling pathway. Cyclic AMP 46-50 G protein-coupled estrogen receptor 1 Homo sapiens 40-45 32138466-11 2020 Conclusion: These results confirm that EPA is a tumor suppressor in human ovarian clear cell carcinoma cells and functions through a novel fatty acid receptor, GPR30, indicating a mechanistic linkage between omega-3 fatty acids and cancers. Eicosapentaenoic Acid 39-42 G protein-coupled estrogen receptor 1 Homo sapiens 160-165 32138466-11 2020 Conclusion: These results confirm that EPA is a tumor suppressor in human ovarian clear cell carcinoma cells and functions through a novel fatty acid receptor, GPR30, indicating a mechanistic linkage between omega-3 fatty acids and cancers. Fatty Acids, Omega-3 208-227 G protein-coupled estrogen receptor 1 Homo sapiens 160-165 32587576-9 2020 GPER modulates second messenger signaling cascades involving Galphas- and Galphai/o-associated increase in cyclic adenosine monophosphate and phosphoinositide 3-kinase or Src protein kinase respectively (32, 33). Adenosine 114-123 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 32587576-10 2020 Activation of GPER is also associated with phospholipase C, and the inositol receptor and ryanodine receptor-mediated increase in intracellular calcium (24, 34). Calcium 144-151 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 32647687-4 2020 Results: Estradiol inhibited the proliferation of VSMCs by upregulating the expression of ESR1, ESR2, and GPER and downregulating the expression of caspase-3, MYOCD, and SRF, thereby inhibiting the apoptosis of vascular smooth muscle. Estradiol 9-18 G protein-coupled estrogen receptor 1 Homo sapiens 106-110 32487604-0 2020 Interaction Between CCL18 and GPR30 Differs from the Interaction Between Estradiol and GPR30. Estradiol 73-82 G protein-coupled estrogen receptor 1 Homo sapiens 87-92 32487604-2 2020 The Gs-coupled seven-transmembrane receptor GPR30 is known as both a CCL18 and an estrogen receptor; its activation by estradiol leads to a transactivation of membrane-tethered pro-heparin-binding EGF-like growth factor and the MAPK/ERK pathway. Estradiol 119-128 G protein-coupled estrogen receptor 1 Homo sapiens 44-49 32401166-4 2020 Here, we report that 17beta-estradiol (E2), TAM, and FUL stabilize MORC2 (MORC family CW-type zinc finger 2), an emerging oncoprotein in human cancer, in a GPER1-dependent manner. Estradiol 21-37 G protein-coupled estrogen receptor 1 Homo sapiens 156-161 32487604-6 2020 RESULTS: Many similarities on the effect of CCL18 on the already known estradiol-activated signaling pathway via the G protein-coupled estrogen receptor GPR30 were identified. Estradiol 71-80 G protein-coupled estrogen receptor 1 Homo sapiens 153-158 32487604-11 2020 This is a rather unexpected result, because the estrogen estradiol and CCL18 both activate GPR30. Estradiol 57-66 G protein-coupled estrogen receptor 1 Homo sapiens 91-96 32487604-18 2020 CCL18 and estradiol may not lead to the same signaling pathway after activating GPR30. Estradiol 10-19 G protein-coupled estrogen receptor 1 Homo sapiens 80-85 32401166-4 2020 Here, we report that 17beta-estradiol (E2), TAM, and FUL stabilize MORC2 (MORC family CW-type zinc finger 2), an emerging oncoprotein in human cancer, in a GPER1-dependent manner. Estradiol 39-41 G protein-coupled estrogen receptor 1 Homo sapiens 156-161 32401166-4 2020 Here, we report that 17beta-estradiol (E2), TAM, and FUL stabilize MORC2 (MORC family CW-type zinc finger 2), an emerging oncoprotein in human cancer, in a GPER1-dependent manner. Tamoxifen 44-47 G protein-coupled estrogen receptor 1 Homo sapiens 156-161 32401166-5 2020 Mechanistically, GPER1 activates PRKACA (protein kinase cAMP-activated catalytic subunit alpha), which in turn phosphorylates MORC2 at threonine 582 (T582). Threonine 135-144 G protein-coupled estrogen receptor 1 Homo sapiens 17-22 32670863-8 2020 Finally, the study identified targeting AhR and/or GPR30 with specific antagonists as a strategy capable of inhibiting carcinogenesis associated with chronic exposure to low doses of B[a]P and BPA in MCF10AT1 cells. bisphenol A 193-196 G protein-coupled estrogen receptor 1 Homo sapiens 51-56 32390531-13 2020 These results highlight GPER as a potential therapeutic target for salt-sensitive hypertension in postmenopausal women. Salts 67-71 G protein-coupled estrogen receptor 1 Homo sapiens 24-28 32361597-0 2020 GPER1 Signaling Initiates Migration of Female V-SVZ-Derived Cells. svz 48-51 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 32361597-5 2020 Blocking of GPER1 in Matrigel cultures of female animals significantly impairs migration of V-SVZ-derived cells. svz 94-97 G protein-coupled estrogen receptor 1 Homo sapiens 12-17 32670863-0 2020 Long-Term Exposure of Early-Transformed Human Mammary Cells to Low Doses of Benzo[a]pyrene and/or Bisphenol A Enhances Their Cancerous Phenotype via an AhR/GPR30 Interplay. Benzo(a)pyrene 76-90 G protein-coupled estrogen receptor 1 Homo sapiens 156-161 32670863-0 2020 Long-Term Exposure of Early-Transformed Human Mammary Cells to Low Doses of Benzo[a]pyrene and/or Bisphenol A Enhances Their Cancerous Phenotype via an AhR/GPR30 Interplay. bis(4-hydroxyphenyl)sulfone 98-107 G protein-coupled estrogen receptor 1 Homo sapiens 156-161 32670863-5 2020 This study provided new insights into the existence of a functional interplay between the aryl hydrocarbon receptor (AhR) and the G protein-coupled receptor 30 (GPR30) by which chronic and low-dose exposure of B[a]P and/or BPA fosters the progression of MCF10AT1 cells into a more aggressive substage. Benzo(a)pyrene 210-215 G protein-coupled estrogen receptor 1 Homo sapiens 130-159 32670863-5 2020 This study provided new insights into the existence of a functional interplay between the aryl hydrocarbon receptor (AhR) and the G protein-coupled receptor 30 (GPR30) by which chronic and low-dose exposure of B[a]P and/or BPA fosters the progression of MCF10AT1 cells into a more aggressive substage. Benzo(a)pyrene 210-215 G protein-coupled estrogen receptor 1 Homo sapiens 161-166 32670863-5 2020 This study provided new insights into the existence of a functional interplay between the aryl hydrocarbon receptor (AhR) and the G protein-coupled receptor 30 (GPR30) by which chronic and low-dose exposure of B[a]P and/or BPA fosters the progression of MCF10AT1 cells into a more aggressive substage. bisphenol A 223-226 G protein-coupled estrogen receptor 1 Homo sapiens 130-159 32670863-5 2020 This study provided new insights into the existence of a functional interplay between the aryl hydrocarbon receptor (AhR) and the G protein-coupled receptor 30 (GPR30) by which chronic and low-dose exposure of B[a]P and/or BPA fosters the progression of MCF10AT1 cells into a more aggressive substage. bisphenol A 223-226 G protein-coupled estrogen receptor 1 Homo sapiens 161-166 32670863-6 2020 Experiments using AhR or GPR30 antagonists, siRNA strategies, and RNAseq analysis led us to propose a model in which AhR signaling plays a "driver role" in the AhR/GPR30 cross-talk in mediating long-term and low-dose exposure of B[a]P and/or BPA. Phosphorus 26-27 G protein-coupled estrogen receptor 1 Homo sapiens 164-169 32670863-6 2020 Experiments using AhR or GPR30 antagonists, siRNA strategies, and RNAseq analysis led us to propose a model in which AhR signaling plays a "driver role" in the AhR/GPR30 cross-talk in mediating long-term and low-dose exposure of B[a]P and/or BPA. bisphenol A 242-245 G protein-coupled estrogen receptor 1 Homo sapiens 25-30 32670863-6 2020 Experiments using AhR or GPR30 antagonists, siRNA strategies, and RNAseq analysis led us to propose a model in which AhR signaling plays a "driver role" in the AhR/GPR30 cross-talk in mediating long-term and low-dose exposure of B[a]P and/or BPA. bisphenol A 242-245 G protein-coupled estrogen receptor 1 Homo sapiens 164-169 32670863-8 2020 Finally, the study identified targeting AhR and/or GPR30 with specific antagonists as a strategy capable of inhibiting carcinogenesis associated with chronic exposure to low doses of B[a]P and BPA in MCF10AT1 cells. Benzo(a)pyrene 183-188 G protein-coupled estrogen receptor 1 Homo sapiens 51-56 32087276-0 2020 GPER mediates decreased chemosensitivity via regulation of ABCG2 expression and localization in tamoxifen-resistant breast cancer cells. Tamoxifen 96-105 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 32197950-3 2020 Herein, was studied the role of aromatase activation and the GPER1 pathway on sodium arsenite-induced promotion and progression of MDA-MB-231 and MDA-MB-453 BCa cell lines. sodium arsenite 78-93 G protein-coupled estrogen receptor 1 Homo sapiens 61-66 32197950-5 2020 Using letrozole (an aromatase inhibitor) and G-15 (a GPER1-selective antagonist), we demonstrated that sodium arsenite-induced proliferation and migration is mediated by induction of aromatase enzyme and, at least in part, by GPER1 activation in MDA-MB-231 and MDA-MB-453 cells. G-15 45-49 G protein-coupled estrogen receptor 1 Homo sapiens 53-58 32197950-5 2020 Using letrozole (an aromatase inhibitor) and G-15 (a GPER1-selective antagonist), we demonstrated that sodium arsenite-induced proliferation and migration is mediated by induction of aromatase enzyme and, at least in part, by GPER1 activation in MDA-MB-231 and MDA-MB-453 cells. G-15 45-49 G protein-coupled estrogen receptor 1 Homo sapiens 226-231 32197950-5 2020 Using letrozole (an aromatase inhibitor) and G-15 (a GPER1-selective antagonist), we demonstrated that sodium arsenite-induced proliferation and migration is mediated by induction of aromatase enzyme and, at least in part, by GPER1 activation in MDA-MB-231 and MDA-MB-453 cells. sodium arsenite 103-118 G protein-coupled estrogen receptor 1 Homo sapiens 53-58 32440148-9 2020 Conclusion: GPR30 may contribute to the pathogenesis of LEVVs by promoting the maintenance of a synthetic phenotype in VSMCs by activating the ERK1/2 and AKT pathways, and GPR30 might be a novel therapeutic target for clinical LEVV treatment. levv 56-60 G protein-coupled estrogen receptor 1 Homo sapiens 12-17 32069725-3 2020 Herein, a previously developed membrane electrochemical reactor (MER) was coupled with Fenton oxidation through providing synergistic benefits with the low solution pH, reduced organics, and ammonia removal/recovery. Ammonia 191-198 G protein-coupled estrogen receptor 1 Homo sapiens 31-63 32069725-3 2020 Herein, a previously developed membrane electrochemical reactor (MER) was coupled with Fenton oxidation through providing synergistic benefits with the low solution pH, reduced organics, and ammonia removal/recovery. Ammonia 191-198 G protein-coupled estrogen receptor 1 Homo sapiens 65-68 32069725-6 2020 At a dimensionless oxidant dose of 1.0, the coupled MER-Fenton system reduced the consumption of both FeSO4 7H2O and H2O2 by 39%, H2SO4 by 100%, and NaOH by 55%. feso4 7h2o 102-112 G protein-coupled estrogen receptor 1 Homo sapiens 52-55 32069725-6 2020 At a dimensionless oxidant dose of 1.0, the coupled MER-Fenton system reduced the consumption of both FeSO4 7H2O and H2O2 by 39%, H2SO4 by 100%, and NaOH by 55%. Hydrogen Peroxide 117-121 G protein-coupled estrogen receptor 1 Homo sapiens 52-55 32069725-6 2020 At a dimensionless oxidant dose of 1.0, the coupled MER-Fenton system reduced the consumption of both FeSO4 7H2O and H2O2 by 39%, H2SO4 by 100%, and NaOH by 55%. sulfuric acid 130-135 G protein-coupled estrogen receptor 1 Homo sapiens 52-55 32069725-6 2020 At a dimensionless oxidant dose of 1.0, the coupled MER-Fenton system reduced the consumption of both FeSO4 7H2O and H2O2 by 39%, H2SO4 by 100%, and NaOH by 55%. Sodium Hydroxide 149-153 G protein-coupled estrogen receptor 1 Homo sapiens 52-55 32069725-9 2020 More notably, direct Fenton oxidation removed only 21% of ammonia; in comparison the MER-Fenton system removed ammonia by 98% with the possibility for recovery at a rate of 30.6-55.2 kg N m-3 reactor d-1. Ammonia 111-118 G protein-coupled estrogen receptor 1 Homo sapiens 85-88 32069725-10 2020 Those results demonstrate that coupling MER with Fenton process could mitigate some inherent drawbacks of Fenton oxidation such as ineffective ammonia removal, high acid and chemical reagents dose requirements, and a large amount of sludge generation. Ammonia 143-150 G protein-coupled estrogen receptor 1 Homo sapiens 40-43 32197950-5 2020 Using letrozole (an aromatase inhibitor) and G-15 (a GPER1-selective antagonist), we demonstrated that sodium arsenite-induced proliferation and migration is mediated by induction of aromatase enzyme and, at least in part, by GPER1 activation in MDA-MB-231 and MDA-MB-453 cells. sodium arsenite 103-118 G protein-coupled estrogen receptor 1 Homo sapiens 226-231 32197950-7 2020 Overall, data suggests that sodium arsenite induces a positive-feedback loop, resulting in the promotion and progression of BCa cells, through induction of aromatase activity, E2 production, GPER1 stimulation, and Src activation. sodium arsenite 28-43 G protein-coupled estrogen receptor 1 Homo sapiens 191-196 32357920-0 2020 Inhibition of PI3K/AKT molecular pathway mediated by membrane estrogen receptor GPER accounts for cryptotanshinone induced antiproliferative effect on breast cancer SKBR-3 cells. cryptotanshinone 98-114 G protein-coupled estrogen receptor 1 Homo sapiens 53-79 32357920-0 2020 Inhibition of PI3K/AKT molecular pathway mediated by membrane estrogen receptor GPER accounts for cryptotanshinone induced antiproliferative effect on breast cancer SKBR-3 cells. cryptotanshinone 98-114 G protein-coupled estrogen receptor 1 Homo sapiens 80-84 32323852-5 2020 In addition, through transient expression assays in breast cancer cells, it was revealed that a transcriptional mechanism dependent on protein kinase A and susceptible to retinoic acid in ER-positive cells induces GPR30 expression through a cis-regulatory element for E26 transformation-specific transcription factors, located between -631 and -625 bp from the GPR30 translation start codon. Tretinoin 171-184 G protein-coupled estrogen receptor 1 Homo sapiens 214-219 32323852-5 2020 In addition, through transient expression assays in breast cancer cells, it was revealed that a transcriptional mechanism dependent on protein kinase A and susceptible to retinoic acid in ER-positive cells induces GPR30 expression through a cis-regulatory element for E26 transformation-specific transcription factors, located between -631 and -625 bp from the GPR30 translation start codon. Tretinoin 171-184 G protein-coupled estrogen receptor 1 Homo sapiens 361-366 32302351-2 2020 GPR30 associates with breast cancer (BC) outcome and may contribute to tamoxifen resistance. Tamoxifen 71-80 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 32302351-3 2020 We investigated the expression and prognostic significance of GPR30 in metachronous contralateral breast cancer (CBC) as a model of tamoxifen resistance. Tamoxifen 132-141 G protein-coupled estrogen receptor 1 Homo sapiens 62-67 32302351-11 2020 However, BC2 that were diagnosed during tamoxifen treatment were more likely to express GPR30PM than BC2 diagnosed after treatment completion (p = 0.01). Tamoxifen 40-49 G protein-coupled estrogen receptor 1 Homo sapiens 88-93 32302351-12 2020 Furthermore, a trend was observed that patients with GPR30PM in an ER-positive BC2 had greater benefit from tamoxifen treatment. Tamoxifen 108-117 G protein-coupled estrogen receptor 1 Homo sapiens 53-58 32087276-4 2020 Here, we are the first to show that the expression levels of GPER and ABCG2 are markedly increased in tamoxifen-resistant ER + metastases compared to the corresponding primary tumors. Tamoxifen 102-111 G protein-coupled estrogen receptor 1 Homo sapiens 61-65 32087276-6 2020 Furthermore, both ER modulator tamoxifen, GPER-specific agonist G1 and pure ER antagonist ICI 182,780 significantly enhanced ABCG2 expression in tamoxifen-resistant breast cancer cells (MCF-7R) but not in tamoxifen-sensitive cells (MCF-7). Tamoxifen 145-154 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 32087276-6 2020 Furthermore, both ER modulator tamoxifen, GPER-specific agonist G1 and pure ER antagonist ICI 182,780 significantly enhanced ABCG2 expression in tamoxifen-resistant breast cancer cells (MCF-7R) but not in tamoxifen-sensitive cells (MCF-7). Tamoxifen 145-154 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 32087276-9 2020 More importantly, the tamoxifen-induced GPER/ABCG2 signaling axis was shown to play a pivotal role in the development of chemotherapy (doxorubicin) resistance both in vitro and in vivo. Tamoxifen 22-31 G protein-coupled estrogen receptor 1 Homo sapiens 40-44 32087276-9 2020 More importantly, the tamoxifen-induced GPER/ABCG2 signaling axis was shown to play a pivotal role in the development of chemotherapy (doxorubicin) resistance both in vitro and in vivo. Doxorubicin 135-146 G protein-coupled estrogen receptor 1 Homo sapiens 40-44 32087276-10 2020 The clinical data further revealed that tamoxifen-resistant patients with high GPER/ABCG2 signaling activation had poor progression-free survival (PFS) when given rescue anthracycline chemotherapy. Tamoxifen 40-49 G protein-coupled estrogen receptor 1 Homo sapiens 79-83 32087276-10 2020 The clinical data further revealed that tamoxifen-resistant patients with high GPER/ABCG2 signaling activation had poor progression-free survival (PFS) when given rescue anthracycline chemotherapy. Anthracyclines 170-183 G protein-coupled estrogen receptor 1 Homo sapiens 79-83 32087276-11 2020 Therefore, our data provide novel insights into GPER-mediated chemoresistance and provide a rationale for the GPER/ABCG2 signaling axis being a promising target for reversing chemoresistance in patients with advanced ER + tamoxifen-resistant breast cancer. Tamoxifen 222-231 G protein-coupled estrogen receptor 1 Homo sapiens 48-52 32087276-11 2020 Therefore, our data provide novel insights into GPER-mediated chemoresistance and provide a rationale for the GPER/ABCG2 signaling axis being a promising target for reversing chemoresistance in patients with advanced ER + tamoxifen-resistant breast cancer. Tamoxifen 222-231 G protein-coupled estrogen receptor 1 Homo sapiens 110-114 32030797-0 2020 GPER-regulated lncRNA-Glu promotes glutamate secretion to enhance cellular invasion and metastasis in triple-negative breast cancer. Glutamic Acid 35-44 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 31989268-6 2020 RESULTS: In the MF patients, the GPER-1 level determined of mean 3.68 (1.95-4.26) pg/ml, 17 beta dehydrogenase of 5.25 (2.73-6.77) ng/ml, and cAMP of 24.62 (11.62-30.35) ng/ml were statistically signficantly higher than those of the control group (p = 0.008, p = 0.002, p = 0.003, respectively). Cyclic AMP 142-146 G protein-coupled estrogen receptor 1 Homo sapiens 33-39 31340060-6 2020 Activation of GPER by its ligands, including tamoxifen (TMX), induced phosphorylation of PKA and BAD-Ser118 to sustain BCSC characteristics. Tamoxifen 45-54 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 31340060-6 2020 Activation of GPER by its ligands, including tamoxifen (TMX), induced phosphorylation of PKA and BAD-Ser118 to sustain BCSC characteristics. Tamoxifen 56-59 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 32094002-6 2020 Then, cell ultrastructure, expression and localization of GPER, ERRbeta, PPARgamma together with the molecular receptor mechanism, through cyclic AMP and Raf/Ras/extracellular signal activated kinases (ERK), in the control of cholesterol concentration and estrogen production by Leydig cells were studied. Cyclic AMP 139-149 G protein-coupled estrogen receptor 1 Homo sapiens 58-62 32094002-6 2020 Then, cell ultrastructure, expression and localization of GPER, ERRbeta, PPARgamma together with the molecular receptor mechanism, through cyclic AMP and Raf/Ras/extracellular signal activated kinases (ERK), in the control of cholesterol concentration and estrogen production by Leydig cells were studied. Cholesterol 226-237 G protein-coupled estrogen receptor 1 Homo sapiens 58-62 32001259-4 2020 At the cellular level, the mechanisms by which estrogens regulate diverse cellular functions including reproduction and behavior is by binding to estrogen receptors alpha, beta (ERalpha and ERbeta) and G-protein coupled ER (GPER1). Estrogens 47-56 G protein-coupled estrogen receptor 1 Homo sapiens 224-229 32001259-4 2020 At the cellular level, the mechanisms by which estrogens regulate diverse cellular functions including reproduction and behavior is by binding to estrogen receptors alpha, beta (ERalpha and ERbeta) and G-protein coupled ER (GPER1). Estrogens 47-55 G protein-coupled estrogen receptor 1 Homo sapiens 224-229 32036685-0 2020 Rutin promotes osteogenic differentiation of periodontal ligament stem cells through the GPR30-mediated PI3K/AKT/mTOR signaling pathway. Rutin 0-5 G protein-coupled estrogen receptor 1 Homo sapiens 89-94 32030797-2 2020 TNBC has been recognized as estrogen-independent breast cancer, while the novel estrogen receptor, namely G protein-coupled estrogen receptor (GPER), was claimed to mediate estrogenic actions in TNBC tissues and cell lines. Estrogens 80-88 G protein-coupled estrogen receptor 1 Homo sapiens 106-141 32030797-2 2020 TNBC has been recognized as estrogen-independent breast cancer, while the novel estrogen receptor, namely G protein-coupled estrogen receptor (GPER), was claimed to mediate estrogenic actions in TNBC tissues and cell lines. Estrogens 80-88 G protein-coupled estrogen receptor 1 Homo sapiens 143-147 32030797-3 2020 Through mRNA microarrays, lncRNA microarrays, and bioinformatics analysis, we found that GPER is activated by 17beta-estradiol (E2) and GPER-specific agonist G1, which downregulates a novel lncRNA (termed as lncRNA-Glu). Estradiol 110-126 G protein-coupled estrogen receptor 1 Homo sapiens 89-93 32030797-3 2020 Through mRNA microarrays, lncRNA microarrays, and bioinformatics analysis, we found that GPER is activated by 17beta-estradiol (E2) and GPER-specific agonist G1, which downregulates a novel lncRNA (termed as lncRNA-Glu). Estradiol 110-126 G protein-coupled estrogen receptor 1 Homo sapiens 136-140 32030797-5 2020 GPER-mediated reduction of lncRNA-Glu promotes glutamate transport activity and transcriptional activity of VGLUT2. Glutamic Acid 47-56 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 32030797-6 2020 Furthermore, GPER-mediated activation of cAMP-PKA signaling contributes to glutamate secretion. Cyclic AMP 41-45 G protein-coupled estrogen receptor 1 Homo sapiens 13-17 32030797-6 2020 Furthermore, GPER-mediated activation of cAMP-PKA signaling contributes to glutamate secretion. Glutamic Acid 75-84 G protein-coupled estrogen receptor 1 Homo sapiens 13-17 32030797-8 2020 Our data provide new insights into GPER-mediated glutamate secretion and its downstream signaling NMDAR-CaMK/MEK-MAPK during TNBC invasion. Glutamic Acid 49-58 G protein-coupled estrogen receptor 1 Homo sapiens 35-39 31698960-0 2020 Environmental polycyclic aromatic hydrocarbons mixture, in human blood levels, decreased oestradiol secretion by granulosa cells via ESR1 and GPER1 but not ESR2 receptor. Polycyclic Aromatic Hydrocarbons 14-46 G protein-coupled estrogen receptor 1 Homo sapiens 142-147 31698960-7 2020 This study showed that both classic ESR1 and GPER1 were involved in the inhibitory effect of both PAH mixtures on E2 secretion and confirmed that expression of P450arom could be downregulated through the aryl hydrocarbon receptor and additionally through the ESR2. Polycyclic Aromatic Hydrocarbons 98-101 G protein-coupled estrogen receptor 1 Homo sapiens 45-50 31698960-7 2020 This study showed that both classic ESR1 and GPER1 were involved in the inhibitory effect of both PAH mixtures on E2 secretion and confirmed that expression of P450arom could be downregulated through the aryl hydrocarbon receptor and additionally through the ESR2. Estradiol 114-116 G protein-coupled estrogen receptor 1 Homo sapiens 45-50 32077170-0 2020 The G protein-coupled oestrogen receptor, GPER1, mediates direct anti-inflammatory effects of oestrogens in human cholinergic neurones from the nucleus basalis of Meynert. Estrogens 22-31 G protein-coupled estrogen receptor 1 Homo sapiens 42-47 32052561-0 2020 Cisplatin resistance in gastric cancer cells is involved with GPR30-mediated epithelial-mesenchymal transition. Cisplatin 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 62-67 32052561-3 2020 GPR30 is a novel oestrogen receptor that is involved in the invasion, metastasis and drug resistance of many tumours. Estrogens 17-26 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 32052561-7 2020 In this study, we demonstrated that GPR30 is involved in cisplatin resistance by promoting EMT in gastric cancer. Cisplatin 57-66 G protein-coupled estrogen receptor 1 Homo sapiens 36-41 32052561-8 2020 GPR30 knockdown resulted in increased sensitivity of different gastric cancer (GC) cells to cisplatin and alterations in the epithelial/mesenchymal markers. Cisplatin 92-101 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 32052561-12 2020 Taken together, these results revealed the role of GPR30 in the formation of cisplatin resistance, suggesting that targeting GPR30 signalling may be a potential strategy for improving the efficacy of chemotherapy in gastric cancer. Cisplatin 77-86 G protein-coupled estrogen receptor 1 Homo sapiens 51-56 32052561-12 2020 Taken together, these results revealed the role of GPR30 in the formation of cisplatin resistance, suggesting that targeting GPR30 signalling may be a potential strategy for improving the efficacy of chemotherapy in gastric cancer. Cisplatin 77-86 G protein-coupled estrogen receptor 1 Homo sapiens 125-130 32077170-0 2020 The G protein-coupled oestrogen receptor, GPER1, mediates direct anti-inflammatory effects of oestrogens in human cholinergic neurones from the nucleus basalis of Meynert. Estrogens 94-104 G protein-coupled estrogen receptor 1 Homo sapiens 42-47 32077170-6 2020 These effects were inhibited by treatment with either 17beta-oestradiol (E2 ) (10 nmol L-1 ) or G1 (100 nmol L-1 ), the selective agonist of the G protein-coupled oestrogen receptor (GPER1). Estradiol 54-71 G protein-coupled estrogen receptor 1 Homo sapiens 183-188 32077170-6 2020 These effects were inhibited by treatment with either 17beta-oestradiol (E2 ) (10 nmol L-1 ) or G1 (100 nmol L-1 ), the selective agonist of the G protein-coupled oestrogen receptor (GPER1). Estrogens 163-172 G protein-coupled estrogen receptor 1 Homo sapiens 183-188 32077170-12 2020 The results obtained in the present study indicate a modulatory functional role of GPER1 with respect to mediating the oestrogen neuroprotective effect against inflammation in brain cholinergic neurones and, accordingly, may help to identify protective strategies for preventing cognitive impairments. Estrogens 119-128 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 31689473-8 2020 Furthermore, in comparison with MCF-7 cells, the LTED cells expressed very low levels of G protein-coupled estrogen receptor 1 (GPER1), a membrane ER capable of stimulating the estrogenic activity of Cd. Cadmium 200-202 G protein-coupled estrogen receptor 1 Homo sapiens 89-126 32028606-6 2020 RESULTS: Treatment with 3 nM BPA led to an increase in cell number and altered the phosphorylation status of p38, an effect mediated primarily via the membrane-bound estrogen receptor (GPR30). bisphenol A 29-32 G protein-coupled estrogen receptor 1 Homo sapiens 185-190 32028606-6 2020 RESULTS: Treatment with 3 nM BPA led to an increase in cell number and altered the phosphorylation status of p38, an effect mediated primarily via the membrane-bound estrogen receptor (GPR30). Estrogens 166-174 G protein-coupled estrogen receptor 1 Homo sapiens 185-190 32046440-8 2020 The effects of BPA on HESCs could be blocked by G protein-coupled estrogen receptor (GPER) inhibitor or mitogen-activated protein kinase/extracellular signal-regulated kinase (MAPK/ERK) inhibitor. bisphenol A 15-18 G protein-coupled estrogen receptor 1 Homo sapiens 48-83 32046440-8 2020 The effects of BPA on HESCs could be blocked by G protein-coupled estrogen receptor (GPER) inhibitor or mitogen-activated protein kinase/extracellular signal-regulated kinase (MAPK/ERK) inhibitor. bisphenol A 15-18 G protein-coupled estrogen receptor 1 Homo sapiens 85-89 31981723-6 2020 Furthermore, BPAF exposure at concentrations from 8 to 1000 ng/ml results in an increase in G protein-coupled estrogen receptor (GPER) expression. 4,4'-hexafluorisopropylidene diphenol 13-17 G protein-coupled estrogen receptor 1 Homo sapiens 92-127 31981723-6 2020 Furthermore, BPAF exposure at concentrations from 8 to 1000 ng/ml results in an increase in G protein-coupled estrogen receptor (GPER) expression. 4,4'-hexafluorisopropylidene diphenol 13-17 G protein-coupled estrogen receptor 1 Homo sapiens 129-133 32075246-1 2020 The peptide ERalpha17p, which corresponds to the 295-311 fragment of the hinge/AF2 domains of the human estrogen receptor alpha (ERalpha), exerts apoptosis in breast cancer cells through a mechanism involving the G protein-coupled estrogen-dependent receptor GPER. Estrogens 104-112 G protein-coupled estrogen receptor 1 Homo sapiens 259-263 31900584-0 2020 GPER-1 expression is associated with a decreased response rate to primary tamoxifen therapy of breast cancer patients. Tamoxifen 74-83 G protein-coupled estrogen receptor 1 Homo sapiens 0-6 31900584-11 2020 We observed a continuous reduction of mean tumor size in patients treated with aromatase inhibitors irrespective of the GPER-1 status and in GPER-1 negative patients treated with TAM. Tamoxifen 179-182 G protein-coupled estrogen receptor 1 Homo sapiens 141-147 31900584-12 2020 In contrast, in GPER-1 positive patients treated with TAM, a reduction of mean tumor size was observed only in the first 2 months after beginning of treatment. Tamoxifen 54-57 G protein-coupled estrogen receptor 1 Homo sapiens 16-22 31900584-14 2020 CONCLUSIONS: GPER-1 expression is significantly associated with a reduced effect of primary treatment with tamoxifen in breast cancer patients. Tamoxifen 107-116 G protein-coupled estrogen receptor 1 Homo sapiens 13-19 31689473-8 2020 Furthermore, in comparison with MCF-7 cells, the LTED cells expressed very low levels of G protein-coupled estrogen receptor 1 (GPER1), a membrane ER capable of stimulating the estrogenic activity of Cd. Cadmium 200-202 G protein-coupled estrogen receptor 1 Homo sapiens 128-133 32082252-0 2019 17beta-Estradiol Inhibits PCSK9-Mediated LDLR Degradation Through GPER/PLC Activation in HepG2 Cells. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 66-70 32082252-5 2019 Here, we report that 17beta-estradiol (betaE2) reduces PCSK9-mediated LDLR degradation by a mechanism that involves activation of the G protein-coupled estrogen receptor (GPER). Estradiol 21-37 G protein-coupled estrogen receptor 1 Homo sapiens 134-169 32082252-5 2019 Here, we report that 17beta-estradiol (betaE2) reduces PCSK9-mediated LDLR degradation by a mechanism that involves activation of the G protein-coupled estrogen receptor (GPER). Estradiol 21-37 G protein-coupled estrogen receptor 1 Homo sapiens 171-175 31790688-2 2020 As 17-beta-estradiol (E2) has been shown to have a proliferative effect on benign and malignant thyroid cells, G protein-coupled estrogen receptor (GPER1) could have a role on the pathogenesis of thyroid cancer. Estrogens 129-137 G protein-coupled estrogen receptor 1 Homo sapiens 148-153 31991740-4 2020 Agonists of the G protein-coupled oestrogen receptor (GPER), such as tamoxifen, have been largely used in the clinic, and interest in GPER, which is abundantly expressed in tissues, has greatly increased despite a lack of understanding regarding the mechanisms which promote its multiple effects. Tamoxifen 69-78 G protein-coupled estrogen receptor 1 Homo sapiens 16-52 31991740-4 2020 Agonists of the G protein-coupled oestrogen receptor (GPER), such as tamoxifen, have been largely used in the clinic, and interest in GPER, which is abundantly expressed in tissues, has greatly increased despite a lack of understanding regarding the mechanisms which promote its multiple effects. Tamoxifen 69-78 G protein-coupled estrogen receptor 1 Homo sapiens 54-58 31759979-0 2020 Regulation of Beta Adrenoceptor-mediated Myocardial Contraction and Calcium Dynamics by the G Protein-coupled Estrogen Receptor 1. Calcium 68-75 G protein-coupled estrogen receptor 1 Homo sapiens 92-129 31993020-1 2019 The G Protein-Coupled Estrogen Receptor (GPER) is a novel membrane-bound receptor that mediates non-genomic actions of the primary female sex hormone 17beta-estradiol. Estradiol 150-166 G protein-coupled estrogen receptor 1 Homo sapiens 4-39 31993020-1 2019 The G Protein-Coupled Estrogen Receptor (GPER) is a novel membrane-bound receptor that mediates non-genomic actions of the primary female sex hormone 17beta-estradiol. Estradiol 150-166 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 31993020-3 2019 This review will focus specifically on the cardiac actions of GPER, since this receptor is expressed in cardiomyocytes as well as other cells within the heart and most likely contributes to estrogen-induced cardioprotection. Estrogens 190-198 G protein-coupled estrogen receptor 1 Homo sapiens 62-66 31759979-5 2020 Administration of the GPER agonist G-1 during the plateau phase of isoproterenol-induced LVP increase rapidly restores LVP to baseline levels and reduces the frequency of ectopic contractions. Isoproterenol 67-80 G protein-coupled estrogen receptor 1 Homo sapiens 22-26 31759979-13 2020 Our data indicate that GPER functions as an intrinsic component of beta1AR signaling to moderate myocardial Ca2+ dynamics and contraction. Calcium 108-112 G protein-coupled estrogen receptor 1 Homo sapiens 23-27 31920512-8 2019 The GPER antagonist G15, the PLC inhibitor U73122 and the IP3 receptor inhibitor 2-APB each virtually abolished the calcium responses to E2 or G-1. Calcium 116-123 G protein-coupled estrogen receptor 1 Homo sapiens 4-8 31706983-2 2019 In addition to the classical nuclear estrogen receptors (ERalpha and ERbeta), the G protein-coupled estrogen receptor GPER is an important mediator of estrogen action. Estrogens 100-108 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 31706983-2 2019 In addition to the classical nuclear estrogen receptors (ERalpha and ERbeta), the G protein-coupled estrogen receptor GPER is an important mediator of estrogen action. Estrogens 100-108 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 31920512-0 2019 Activation of the G Protein-Coupled Estrogen Receptor Elicits Store Calcium Release and Phosphorylation of the Mu-Opioid Receptors in the Human Neuroblastoma SH-SY5Y Cells. Calcium 68-75 G protein-coupled estrogen receptor 1 Homo sapiens 18-53 31920512-4 2019 The receptors responsible for the rapid actions of estrogens remain uncertain, but recent evidence points to the G protein-coupled estrogen receptor (GPER), which has been shown to be expressed widely in the nervous system. Estrogens 51-60 G protein-coupled estrogen receptor 1 Homo sapiens 113-148 31920512-11 2019 In conclusion, the present study has revealed a novel GPER-mediated estrogenic signaling in neuroblastoma cells in which activation of GPER is followed by rapid calcium mobilization, PKC activation and MOR phosphorylation. Calcium 161-168 G protein-coupled estrogen receptor 1 Homo sapiens 54-58 31920512-4 2019 The receptors responsible for the rapid actions of estrogens remain uncertain, but recent evidence points to the G protein-coupled estrogen receptor (GPER), which has been shown to be expressed widely in the nervous system. Estrogens 51-60 G protein-coupled estrogen receptor 1 Homo sapiens 150-154 31920512-5 2019 In the current study, we test the hypothesis that activation of GPER may mediate rapid calcium signaling, which may promote phosphorylation of MOR through the calcium-dependent protein kinases in neuronal cells. Calcium 87-94 G protein-coupled estrogen receptor 1 Homo sapiens 64-68 31920512-12 2019 GPER-mediated rapid calcium signal may also be transmitted to the nucleus to impact on gene transcription. Calcium 20-27 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 31920512-5 2019 In the current study, we test the hypothesis that activation of GPER may mediate rapid calcium signaling, which may promote phosphorylation of MOR through the calcium-dependent protein kinases in neuronal cells. Calcium 159-166 G protein-coupled estrogen receptor 1 Homo sapiens 64-68 31920512-7 2019 Activation of GPER by 17beta-estradiol (E2) and G-1 (GPER selective agonist) evoked a rapid calcium rise in a concentration-dependent manner, which was due to store release rather than calcium entry. Estradiol 22-38 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 31125081-0 2019 Aldosterone Stimulates Its Biosynthesis Via A Novel GPER Mediated Mechanism. Aldosterone 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 52-56 31920512-7 2019 Activation of GPER by 17beta-estradiol (E2) and G-1 (GPER selective agonist) evoked a rapid calcium rise in a concentration-dependent manner, which was due to store release rather than calcium entry. Estradiol 22-38 G protein-coupled estrogen receptor 1 Homo sapiens 53-57 31920512-7 2019 Activation of GPER by 17beta-estradiol (E2) and G-1 (GPER selective agonist) evoked a rapid calcium rise in a concentration-dependent manner, which was due to store release rather than calcium entry. Calcium 92-99 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 31920512-7 2019 Activation of GPER by 17beta-estradiol (E2) and G-1 (GPER selective agonist) evoked a rapid calcium rise in a concentration-dependent manner, which was due to store release rather than calcium entry. Calcium 92-99 G protein-coupled estrogen receptor 1 Homo sapiens 53-57 31920512-7 2019 Activation of GPER by 17beta-estradiol (E2) and G-1 (GPER selective agonist) evoked a rapid calcium rise in a concentration-dependent manner, which was due to store release rather than calcium entry. Calcium 185-192 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 31920512-7 2019 Activation of GPER by 17beta-estradiol (E2) and G-1 (GPER selective agonist) evoked a rapid calcium rise in a concentration-dependent manner, which was due to store release rather than calcium entry. Calcium 185-192 G protein-coupled estrogen receptor 1 Homo sapiens 53-57 31568691-7 2019 Transcriptome analysis indicated activation of G-protein-coupled estrogen receptor (GPER1) as the main underlying mechanism of action, which was corroborated using GPER1-selective agonists and antagonists. Estrogens 65-73 G protein-coupled estrogen receptor 1 Homo sapiens 84-89 31568691-7 2019 Transcriptome analysis indicated activation of G-protein-coupled estrogen receptor (GPER1) as the main underlying mechanism of action, which was corroborated using GPER1-selective agonists and antagonists. Estrogens 65-73 G protein-coupled estrogen receptor 1 Homo sapiens 164-169 31125081-1 2019 CONTEXT: The G protein-coupled estrogen receptor (GPER) mediates an aldosterone secretagogue effect of 17beta-estradiol in human HAC15 adrenocortical cells after estrogen receptor beta blockade. Estradiol 103-119 G protein-coupled estrogen receptor 1 Homo sapiens 13-48 31125081-1 2019 CONTEXT: The G protein-coupled estrogen receptor (GPER) mediates an aldosterone secretagogue effect of 17beta-estradiol in human HAC15 adrenocortical cells after estrogen receptor beta blockade. Estradiol 103-119 G protein-coupled estrogen receptor 1 Homo sapiens 50-54 31125081-2 2019 As GPER mediates mineralocorticoid receptor-independent aldosterone effects in other cell types, we hypothesized that aldosterone could modulate its own synthesis via GPER activation. Aldosterone 56-67 G protein-coupled estrogen receptor 1 Homo sapiens 3-7 31125081-6 2019 RESULTS: Aldosterone markedly increased CYP11B2 mRNA and protein expression (vs untreated samples, p<0.001) in both models by acting via GPER, as these effects were abolished by G36 (p<0.01) and not by canrenone. Canrenone 208-217 G protein-coupled estrogen receptor 1 Homo sapiens 140-144 31125081-7 2019 GPER-silencing (p<0.01) abolished the aldosterone-induced increase of CYP11B2, thus proving that aldosterone acts via GPER to augment the step-limiting mitochondrial enzyme (CYP11B2) of its synthesis. Aldosterone 41-52 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 31125081-7 2019 GPER-silencing (p<0.01) abolished the aldosterone-induced increase of CYP11B2, thus proving that aldosterone acts via GPER to augment the step-limiting mitochondrial enzyme (CYP11B2) of its synthesis. Aldosterone 41-52 G protein-coupled estrogen receptor 1 Homo sapiens 121-125 31125081-7 2019 GPER-silencing (p<0.01) abolished the aldosterone-induced increase of CYP11B2, thus proving that aldosterone acts via GPER to augment the step-limiting mitochondrial enzyme (CYP11B2) of its synthesis. Aldosterone 100-111 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 31125081-7 2019 GPER-silencing (p<0.01) abolished the aldosterone-induced increase of CYP11B2, thus proving that aldosterone acts via GPER to augment the step-limiting mitochondrial enzyme (CYP11B2) of its synthesis. Aldosterone 100-111 G protein-coupled estrogen receptor 1 Homo sapiens 121-125 31125081-8 2019 Angiotensin II potentiated the GPER-mediated effect of aldosterone on CYP11B2. Aldosterone 55-66 G protein-coupled estrogen receptor 1 Homo sapiens 31-35 31125081-11 2019 Moreover, as aldosterone-producing adenoma overexpresses GPER this mechanism could contribute to the aldosterone excess that occurs in primary aldosteronism in a seemingly autonomous fashion from angiotensin II. Aldosterone 13-24 G protein-coupled estrogen receptor 1 Homo sapiens 57-61 31499072-3 2019 We have recently discovered a role of estrogen receptors (ER) in controlling aldosterone biosynthesis in the human adrenocortical zona glomerulosa, which expresses both the classical ERalpha and beta receptors and G protein-coupled estrogen receptor (GPER). Aldosterone 77-88 G protein-coupled estrogen receptor 1 Homo sapiens 214-249 31950019-0 2019 Genistein Inhibits Proliferation of BRCA1 Mutated Breast Cancer Cells: The GPR30-Akt Axis as a Potential Target. Genistein 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 75-80 31950019-10 2019 Treatment of BRCA1 silenced breast cancer cells with genistein resulted in the down-regulation of GPR30 expression and the inhibition of Akt phosphorylation as well as the reduced cell viability, migration and colony formation. Genistein 53-62 G protein-coupled estrogen receptor 1 Homo sapiens 98-103 31950019-15 2019 Genistein induces G2/M phase arrest by down-regulating cyclin B1 expression, which is attributable to its suppression of GPR30 activation and Akt phosphorylation in BRCA1 impaired breast cancer cells. Genistein 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 121-126 31499072-5 2019 We found that 17 beta -estradiol exerts a dual effect: it blunts aldosterone production via ERbeta, but displays a potent aldosterone secretagogue effect via GPER activation after ERbeta blockade. Estradiol 14-32 G protein-coupled estrogen receptor 1 Homo sapiens 158-162 31499072-8 2019 Our purpose here was to provide an update on estrogen receptor function in the normal adrenal cortex and its relevance for the sex differences in blood pressure in light of the newly discovered role of GPER in regulating aldosterone synthesis. Aldosterone 221-232 G protein-coupled estrogen receptor 1 Homo sapiens 202-206 31279203-4 2019 Compared to a control reactor that did not have a membrane separator, the MER achieved significantly higher removals of both dissolved organic carbon (61.5 +- 4.1%) and UV254nm absorbance (63.4 +- 8.4%). Carbon 143-149 G protein-coupled estrogen receptor 1 Homo sapiens 74-77 31759407-5 2019 While in our previous studies altered GPER-PPAR partnership was found in human LCT being a possible cause and/or additionally effecting on LCT development, here mouse testes with experimentally induced LCT and mouse tumor Leydig cell (MA-10) treated with BPA chemicals were examined. 4-boronophenylalanine-fructose 255-258 G protein-coupled estrogen receptor 1 Homo sapiens 38-42 31545985-8 2019 Furthermore, shikonin downregulated the expression of ERalpha and GPER, and this effect was not affected by the estrogen environment. shikonin 13-21 G protein-coupled estrogen receptor 1 Homo sapiens 66-70 31546233-0 2019 Low Dose Bisphenol-A Regulates Inflammatory Cytokines through GPR30 in Mammary Adipose Cells. bisphenol A 9-18 G protein-coupled estrogen receptor 1 Homo sapiens 62-67 31546233-3 2019 24 and/or 48 hours exposure to BPA 0.1 nM elicited significant increase of the inflammatory molecules interleukin-6 (IL-6), interleukin-8 (IL-8), Monocyte chemo-attractant protein 1alpha (MCP1alpha) and induced G protein-coupled estrogen receptor 30 (GPR30) levels more than 2-fold both in mature adipocytes and SVF cells. bisphenol A 31-34 G protein-coupled estrogen receptor 1 Homo sapiens 211-249 31546233-3 2019 24 and/or 48 hours exposure to BPA 0.1 nM elicited significant increase of the inflammatory molecules interleukin-6 (IL-6), interleukin-8 (IL-8), Monocyte chemo-attractant protein 1alpha (MCP1alpha) and induced G protein-coupled estrogen receptor 30 (GPR30) levels more than 2-fold both in mature adipocytes and SVF cells. bisphenol A 31-34 G protein-coupled estrogen receptor 1 Homo sapiens 251-256 31546233-5 2019 As a result of BPA-GPR30 signaling activation, Fatty Acid Synthase (FAS) and leptin mRNA levels were significantly higher upon BPA exposure (p<0.05) in mature adipocytes, with an opposite effect on adiponectin (ADIPOQ). bisphenol A 15-18 G protein-coupled estrogen receptor 1 Homo sapiens 19-24 31546233-5 2019 As a result of BPA-GPR30 signaling activation, Fatty Acid Synthase (FAS) and leptin mRNA levels were significantly higher upon BPA exposure (p<0.05) in mature adipocytes, with an opposite effect on adiponectin (ADIPOQ). bisphenol A 127-130 G protein-coupled estrogen receptor 1 Homo sapiens 19-24 31546233-9 2019 All these data suggest that BPA at 0.1nM, a 10 times lower concentration than environmental exposure, increases the expression of pro-inflammatory cytokines via GPR30 both in mature mammary adipocytes and in SVF cells with a possible involvement of IL-8. bisphenol A 28-31 G protein-coupled estrogen receptor 1 Homo sapiens 161-166 31279203-6 2019 The MER was able to remove 89.1 +- 2.9% of total nitrogen from the leachate while recovering about 51% of the influent ammonia in the catholyte, in comparison to 38.1 +- 4.4% of total nitrogen removal by the control reactor. Nitrogen 49-57 G protein-coupled estrogen receptor 1 Homo sapiens 4-7 31279203-6 2019 The MER was able to remove 89.1 +- 2.9% of total nitrogen from the leachate while recovering about 51% of the influent ammonia in the catholyte, in comparison to 38.1 +- 4.4% of total nitrogen removal by the control reactor. Ammonia 119-126 G protein-coupled estrogen receptor 1 Homo sapiens 4-7 31279203-6 2019 The MER was able to remove 89.1 +- 2.9% of total nitrogen from the leachate while recovering about 51% of the influent ammonia in the catholyte, in comparison to 38.1 +- 4.4% of total nitrogen removal by the control reactor. Nitrogen 184-192 G protein-coupled estrogen receptor 1 Homo sapiens 4-7 31872599-0 2019 [Molecular mechanism of apoptosis of breast cancer SKBR-3 cells induced by cryptanshinone via G protein coupled estrogen receptor( GPER) mediated pathway]. cryptanshinone 75-89 G protein-coupled estrogen receptor 1 Homo sapiens 131-135 31872599-0 2019 [Molecular mechanism of apoptosis of breast cancer SKBR-3 cells induced by cryptanshinone via G protein coupled estrogen receptor( GPER) mediated pathway]. Estrogens 112-120 G protein-coupled estrogen receptor 1 Homo sapiens 131-135 31872599-1 2019 The study aimed to illuminate the role of G protein coupled estrogen receptor( GPER) and its mediated PI3 K/AKT signaling pathway in cryptotanshinone( CPT) induced apoptosis of breast cancer SKBR-3 cells,which is GPER positive and ER negative.The apoptosis rate of SKBR-3 cells was tested by Annexin V-FITC/PI staining and apoptosis effector caspase-3 was determined by Western blot. Estrogens 60-68 G protein-coupled estrogen receptor 1 Homo sapiens 79-83 31872599-1 2019 The study aimed to illuminate the role of G protein coupled estrogen receptor( GPER) and its mediated PI3 K/AKT signaling pathway in cryptotanshinone( CPT) induced apoptosis of breast cancer SKBR-3 cells,which is GPER positive and ER negative.The apoptosis rate of SKBR-3 cells was tested by Annexin V-FITC/PI staining and apoptosis effector caspase-3 was determined by Western blot. cryptotanshinone 133-149 G protein-coupled estrogen receptor 1 Homo sapiens 79-83 31872599-1 2019 The study aimed to illuminate the role of G protein coupled estrogen receptor( GPER) and its mediated PI3 K/AKT signaling pathway in cryptotanshinone( CPT) induced apoptosis of breast cancer SKBR-3 cells,which is GPER positive and ER negative.The apoptosis rate of SKBR-3 cells was tested by Annexin V-FITC/PI staining and apoptosis effector caspase-3 was determined by Western blot. cryptotanshinone 133-149 G protein-coupled estrogen receptor 1 Homo sapiens 213-217 31872599-1 2019 The study aimed to illuminate the role of G protein coupled estrogen receptor( GPER) and its mediated PI3 K/AKT signaling pathway in cryptotanshinone( CPT) induced apoptosis of breast cancer SKBR-3 cells,which is GPER positive and ER negative.The apoptosis rate of SKBR-3 cells was tested by Annexin V-FITC/PI staining and apoptosis effector caspase-3 was determined by Western blot. 1,3-dimethyl-8-cyclopentylxanthine 151-154 G protein-coupled estrogen receptor 1 Homo sapiens 79-83 31872599-1 2019 The study aimed to illuminate the role of G protein coupled estrogen receptor( GPER) and its mediated PI3 K/AKT signaling pathway in cryptotanshinone( CPT) induced apoptosis of breast cancer SKBR-3 cells,which is GPER positive and ER negative.The apoptosis rate of SKBR-3 cells was tested by Annexin V-FITC/PI staining and apoptosis effector caspase-3 was determined by Western blot. 1,3-dimethyl-8-cyclopentylxanthine 151-154 G protein-coupled estrogen receptor 1 Homo sapiens 213-217 31872599-16 2019 Furthermore,CPT could downregulate GPER expression in SKBR-3 cells( P<0. 1,3-dimethyl-8-cyclopentylxanthine 12-15 G protein-coupled estrogen receptor 1 Homo sapiens 35-39 31737560-0 2019 Chronic BDE-47 Exposure Aggravates Malignant Phenotypes and Chemoresistance by Activating ERK Through ERalpha and GPR30 in Endometrial Carcinoma. 2,2',4,4'-tetrabromodiphenyl ether 8-14 G protein-coupled estrogen receptor 1 Homo sapiens 114-119 31737560-4 2019 Mechanisms of estrogen receptor alpha (ERalpha) and G-protein-coupled receptor-30 (GPR30) involved in BDE-47 carcinogenesis are yet to be identified. 2,2',4,4'-tetrabromodiphenyl ether 102-108 G protein-coupled estrogen receptor 1 Homo sapiens 52-81 31737560-4 2019 Mechanisms of estrogen receptor alpha (ERalpha) and G-protein-coupled receptor-30 (GPR30) involved in BDE-47 carcinogenesis are yet to be identified. 2,2',4,4'-tetrabromodiphenyl ether 102-108 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 31737560-10 2019 Knockdown of ERalpha or GPR30 by small interfering RNA reversed the stimulating effect of BDE-47 on cell growth, migration and invasion of EC cells. 2,2',4,4'-tetrabromodiphenyl ether 90-96 G protein-coupled estrogen receptor 1 Homo sapiens 24-29 31737560-12 2019 Overall, our results indicate that chronic BDE-47 exposure triggers phenotypic plasticity, promotes progression and even chemoresistance in EC cells, at least in part, via ERalpha/GPR30 and EGFR/ERK signaling pathways. 2,2',4,4'-tetrabromodiphenyl ether 43-49 G protein-coupled estrogen receptor 1 Homo sapiens 180-185 31872599-17 2019 01),which could be inhibited by G1 and enhanced by G15.In conclusion,CPT could induce the apoptosis of ER negative and GPER positive breast cancer SKBR-3 cells and the molecular mechanism is related to its regulatory effect of GPER and its mediated PI3 K/AKT signaling pathway. 1,3-dimethyl-8-cyclopentylxanthine 69-72 G protein-coupled estrogen receptor 1 Homo sapiens 119-123 31872599-17 2019 01),which could be inhibited by G1 and enhanced by G15.In conclusion,CPT could induce the apoptosis of ER negative and GPER positive breast cancer SKBR-3 cells and the molecular mechanism is related to its regulatory effect of GPER and its mediated PI3 K/AKT signaling pathway. 1,3-dimethyl-8-cyclopentylxanthine 69-72 G protein-coupled estrogen receptor 1 Homo sapiens 227-231 31696058-1 2019 Expression patterns of estrogen receptors [ERalpha, ERbeta, and G-protein associated ER (GPER)] in melanoma and skin may suggest their differential roles in carcinogenesis. Estrogens 23-31 G protein-coupled estrogen receptor 1 Homo sapiens 64-87 31708873-1 2019 The G protein-coupled estrogen receptor (GPER) is a seven-transmembrane-domain receptor that mediates non-genomic estrogen related signaling. Estrogens 22-30 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 31708873-4 2019 Therefore, a better understanding of the role GPER plays in cancer biology may lead to the identification of novel therapeutic targets, especially among estrogen-related cancers. Estrogens 153-161 G protein-coupled estrogen receptor 1 Homo sapiens 46-50 31696058-1 2019 Expression patterns of estrogen receptors [ERalpha, ERbeta, and G-protein associated ER (GPER)] in melanoma and skin may suggest their differential roles in carcinogenesis. Estrogens 23-31 G protein-coupled estrogen receptor 1 Homo sapiens 89-93 31545891-0 2019 Activation of G-Protein-Coupled Receptor 30 Protects Neurons against Excitotoxicity through Inhibiting Excessive Autophagy Induced by Glutamate. Glutamic Acid 134-143 G protein-coupled estrogen receptor 1 Homo sapiens 14-43 31545891-4 2019 Activation of G-protein-coupled receptor 30 (GPR30), an estrogen membrane receptor, protects neurons from excitotoxicity-induced cell death. Estrogens 56-64 G protein-coupled estrogen receptor 1 Homo sapiens 14-43 31545891-4 2019 Activation of G-protein-coupled receptor 30 (GPR30), an estrogen membrane receptor, protects neurons from excitotoxicity-induced cell death. Estrogens 56-64 G protein-coupled estrogen receptor 1 Homo sapiens 45-50 31545891-7 2019 Pretreatment of G1 (GPR30 specific agonist) reduced neuronal loss through inhibiting excessive autophagy induced by glutamate exposure, which was blocked by GPR30 antagonist G15, phosphatidylinositol-3-kinase (PI3K), and the mammalian target of rapamycin (mTOR) inhibitors. Glutamic Acid 116-125 G protein-coupled estrogen receptor 1 Homo sapiens 20-25 31545891-7 2019 Pretreatment of G1 (GPR30 specific agonist) reduced neuronal loss through inhibiting excessive autophagy induced by glutamate exposure, which was blocked by GPR30 antagonist G15, phosphatidylinositol-3-kinase (PI3K), and the mammalian target of rapamycin (mTOR) inhibitors. Glutamic Acid 116-125 G protein-coupled estrogen receptor 1 Homo sapiens 157-162 31545891-10 2019 We conclude that GPR30 activation reduces glutamate-induced excessive autophagy in neurons and protects neurons against excitotoxicity. Glutamic Acid 42-51 G protein-coupled estrogen receptor 1 Homo sapiens 17-22 31242463-0 2019 Glucose-dependent GPER1 expression modulates tamoxifen-induced IGFBP-1 accumulation. Glucose 0-7 G protein-coupled estrogen receptor 1 Homo sapiens 18-23 31749762-8 2019 Last two decades has witnessed the discovery of alternate forms of ER-alpha, as well as other receptors for estrogen such as ERRgamma, GPER-1 as well as ER-beta, which are activated not only by estrogen, but also by the therapeutic agents such as tamoxifen that are routinely used in treatment of breast cancer. Estrogens 108-116 G protein-coupled estrogen receptor 1 Homo sapiens 135-141 31468104-0 2019 A nongenomic mechanism for "metalloestrogenic" effects of cadmium in human uterine leiomyoma cells through G protein-coupled estrogen receptor. Cadmium 58-65 G protein-coupled estrogen receptor 1 Homo sapiens 107-142 31468104-10 2019 Overall, Cd-induced proliferation of human fibroid cells was through a nongenomic GPER/p-src/EGFR/MAPK signaling pathway that did not directly involve ERalpha36. Cadmium 9-11 G protein-coupled estrogen receptor 1 Homo sapiens 82-86 31370872-0 2019 AHR and GPER mediate the stimulatory effects induced by 3-methylcholanthrene in breast cancer cells and cancer-associated fibroblasts (CAFs). Methylcholanthrene 56-76 G protein-coupled estrogen receptor 1 Homo sapiens 8-12 31370872-11 2019 RESULTS: We first ascertained by docking simulations the ability of 3MC to interact with GPER. Methylcholanthrene 68-71 G protein-coupled estrogen receptor 1 Homo sapiens 89-93 31370872-12 2019 Thereafter, we established that 3MC activates the EGFR/ERK/c-Fos transduction signaling through both AHR and GPER in SkBr3 cells and CAFs. Methylcholanthrene 32-35 G protein-coupled estrogen receptor 1 Homo sapiens 109-113 31370872-14 2019 CONCLUSIONS: In the present study we have provided novel insights regarding the molecular mechanisms by which 3MC may trigger a physical and functional interaction between AHR and GPER, leading to the stimulation of both SkBr3 breast cancer cells and CAFs. Methylcholanthrene 110-113 G protein-coupled estrogen receptor 1 Homo sapiens 180-184 31370872-15 2019 Altogether, our results indicate that 3MC may engage both GPER and AHR transduction pathways toward breast cancer progression. Methylcholanthrene 38-41 G protein-coupled estrogen receptor 1 Homo sapiens 58-62 31749762-8 2019 Last two decades has witnessed the discovery of alternate forms of ER-alpha, as well as other receptors for estrogen such as ERRgamma, GPER-1 as well as ER-beta, which are activated not only by estrogen, but also by the therapeutic agents such as tamoxifen that are routinely used in treatment of breast cancer. Estrogens 194-202 G protein-coupled estrogen receptor 1 Homo sapiens 135-141 31749762-8 2019 Last two decades has witnessed the discovery of alternate forms of ER-alpha, as well as other receptors for estrogen such as ERRgamma, GPER-1 as well as ER-beta, which are activated not only by estrogen, but also by the therapeutic agents such as tamoxifen that are routinely used in treatment of breast cancer. Tamoxifen 247-256 G protein-coupled estrogen receptor 1 Homo sapiens 135-141 31546660-1 2019 Estrogen receptors (ER) include ER alpha, ER beta and new membrane receptor G protein-coupled receptor 30 (GPR30). Estrogens 0-8 G protein-coupled estrogen receptor 1 Homo sapiens 107-112 31540491-4 2019 The GPER-specific agonist G1 leads to an inhibition of cell proliferation and an elevated level of intracellular calcium (Ca2+). Calcium 113-120 G protein-coupled estrogen receptor 1 Homo sapiens 4-8 31175966-12 2019 Overall, we show for the first time that GPER may contribute to the neuroprotective effects of IGF-1 against MPTP/MPP+-induced dopaminergic neuronal injury. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 109-113 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 31175966-12 2019 Overall, we show for the first time that GPER may contribute to the neuroprotective effects of IGF-1 against MPTP/MPP+-induced dopaminergic neuronal injury. mangion-purified polysaccharide (Candida albicans) 114-118 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 31435166-6 2019 GPER is also involved in cell cycle regulation, endoplasmic reticulum stress, proliferation, apoptosis, vascularization, cell migration, and the regulation of fatty acid and estrogen metabolism in CRC cells. Fatty Acids 159-169 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 31242463-8 2019 To determine if [D-glucose]-dependent GPER1 accumulation altered breast cancer cell response to tamoxifen, cells grown in the presence of decreasing [D-glucose] were co-treated with tamoxifen and IGFBP-1 transcription was measured. Tamoxifen 96-105 G protein-coupled estrogen receptor 1 Homo sapiens 38-43 31242463-8 2019 To determine if [D-glucose]-dependent GPER1 accumulation altered breast cancer cell response to tamoxifen, cells grown in the presence of decreasing [D-glucose] were co-treated with tamoxifen and IGFBP-1 transcription was measured. Glucose 17-26 G protein-coupled estrogen receptor 1 Homo sapiens 38-43 31242463-9 2019 The results from these experiments reveal that D-glucose deprivation increased GPER1-mediated and tamoxifen-induced IGFBP-1 transcription suggesting that [D-glucose] may increase breast cancer cell sensitivity to tamoxifen. Glucose 47-56 G protein-coupled estrogen receptor 1 Homo sapiens 79-84 31242463-9 2019 The results from these experiments reveal that D-glucose deprivation increased GPER1-mediated and tamoxifen-induced IGFBP-1 transcription suggesting that [D-glucose] may increase breast cancer cell sensitivity to tamoxifen. Glucose 155-164 G protein-coupled estrogen receptor 1 Homo sapiens 79-84 31242463-10 2019 Taken together, these results identify a previously unknown mechanism that regulates GPER1 expression that modifies one aspect tamoxifen action in breast cancer cells. Tamoxifen 127-136 G protein-coupled estrogen receptor 1 Homo sapiens 85-90 31242463-0 2019 Glucose-dependent GPER1 expression modulates tamoxifen-induced IGFBP-1 accumulation. Tamoxifen 45-54 G protein-coupled estrogen receptor 1 Homo sapiens 18-23 31242463-3 2019 The recently identified GPER1-dependent mechanism of tamoxifen action in breast cancer cells underscores the importance of identifying mechanisms that regulate GPER1 expression in this cell type. Tamoxifen 53-62 G protein-coupled estrogen receptor 1 Homo sapiens 24-29 31242463-3 2019 The recently identified GPER1-dependent mechanism of tamoxifen action in breast cancer cells underscores the importance of identifying mechanisms that regulate GPER1 expression in this cell type. Tamoxifen 53-62 G protein-coupled estrogen receptor 1 Homo sapiens 160-165 31242463-4 2019 We hypothesized that GPER1 expression in breast cancer cells is sensitive to [D-glucose] and provide data showing increased GPER1 expression when cells were cultured in low [D-glucose]. Glucose 78-87 G protein-coupled estrogen receptor 1 Homo sapiens 21-26 31242463-4 2019 We hypothesized that GPER1 expression in breast cancer cells is sensitive to [D-glucose] and provide data showing increased GPER1 expression when cells were cultured in low [D-glucose]. Glucose 174-183 G protein-coupled estrogen receptor 1 Homo sapiens 21-26 31242463-4 2019 We hypothesized that GPER1 expression in breast cancer cells is sensitive to [D-glucose] and provide data showing increased GPER1 expression when cells were cultured in low [D-glucose]. Glucose 174-183 G protein-coupled estrogen receptor 1 Homo sapiens 124-129 31242463-8 2019 To determine if [D-glucose]-dependent GPER1 accumulation altered breast cancer cell response to tamoxifen, cells grown in the presence of decreasing [D-glucose] were co-treated with tamoxifen and IGFBP-1 transcription was measured. Glucose 19-26 G protein-coupled estrogen receptor 1 Homo sapiens 38-43 31016847-0 2019 Bisphenol A promotes the proliferation of leiomyoma cells by GPR30-EGFR signaling pathway. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 61-66 31082617-0 2019 GPER1 influences cellular homeostasis and cytostatic drug resistance via influencing long chain ceramide synthesis in breast cancer cells. Ceramides 96-104 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 31082617-7 2019 However, GPER1 overexpressing cells were less sensitive against doxorubicin as compared to control cells. Doxorubicin 64-75 G protein-coupled estrogen receptor 1 Homo sapiens 9-14 31082617-8 2019 In previous work we showed the effect of transient GPER1 overexpression on the synthesis of several ceramide synthases (CerS) thereby influencing the sphingolipid pathway. Sphingolipids 150-162 G protein-coupled estrogen receptor 1 Homo sapiens 51-56 31016847-1 2019 AIM: To study the molecular mechanism of G protein-coupled receptor 30-epidermal growth factor receptor (GPR30-EGFR) signaling pathway on the proliferation of leiomyoma cells exposed with bisphenol A. bisphenol A 188-199 G protein-coupled estrogen receptor 1 Homo sapiens 105-110 31016847-5 2019 RESULTS: Bisphenol A promoted the growth of UL cells and the expressions of GPR30, EGFR, c-fos and p-ERK1/2. bis(4-hydroxyphenyl)sulfone 9-18 G protein-coupled estrogen receptor 1 Homo sapiens 76-81 30919959-0 2019 Raloxifene decreases cell viability and migratory potential in prostate cancer cells (LNCaP) with GPR30/GPER1 involvement. Raloxifene Hydrochloride 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 98-103 31016847-6 2019 CONCLUSION: Bisphenol A was found to be a promoter specifically to proliferate the human UL cells by activating the transcription and translation of GPR30-EGFR and MAPK/ERK/c-fos signaling pathway members. bisphenol A 12-23 G protein-coupled estrogen receptor 1 Homo sapiens 149-154 30919959-0 2019 Raloxifene decreases cell viability and migratory potential in prostate cancer cells (LNCaP) with GPR30/GPER1 involvement. Raloxifene Hydrochloride 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 104-109 30919959-8 2019 CONCLUSIONS: Raloxifene was able to modulate GPER1 in LNCaP prostate tumour cells, decreasing cell viability and their migratory potential. Raloxifene Hydrochloride 13-23 G protein-coupled estrogen receptor 1 Homo sapiens 45-50 30645008-3 2019 Tamoxifen (TAM), widely used in chemotherapy of ERalpha-positive breast cancer, is considered as an ERalpha antagonist and GPER agonist. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 123-127 30919959-1 2019 OBJECTIVES: This study evaluated raloxifene (ral) effects on LNCaP prostate tumour cells modulating the activity of GPER1/GPR30 receptors. Raloxifene Hydrochloride 33-43 G protein-coupled estrogen receptor 1 Homo sapiens 116-121 30919959-1 2019 OBJECTIVES: This study evaluated raloxifene (ral) effects on LNCaP prostate tumour cells modulating the activity of GPER1/GPR30 receptors. Raloxifene Hydrochloride 33-43 G protein-coupled estrogen receptor 1 Homo sapiens 122-127 30645008-3 2019 Tamoxifen (TAM), widely used in chemotherapy of ERalpha-positive breast cancer, is considered as an ERalpha antagonist and GPER agonist. Tamoxifen 11-14 G protein-coupled estrogen receptor 1 Homo sapiens 123-127 30645008-8 2019 Additionally, TAM induced autophagy in a GPER-dependent manner. Tamoxifen 14-17 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 30851383-0 2019 Structural and energetic basis for novel epicatechin derivatives acting as GPER agonists through the MMGBSA method. Catechin 41-52 G protein-coupled estrogen receptor 1 Homo sapiens 75-79 30851383-1 2019 (-)-Epicatechin (Epi) has been demonstrated to activate pathways involved in GPER-stimulated nitric oxide (NO) production via endothelial NO synthase, known as the eNOS/NO pathway. Catechin 0-15 G protein-coupled estrogen receptor 1 Homo sapiens 77-81 30851383-1 2019 (-)-Epicatechin (Epi) has been demonstrated to activate pathways involved in GPER-stimulated nitric oxide (NO) production via endothelial NO synthase, known as the eNOS/NO pathway. Catechin 4-7 G protein-coupled estrogen receptor 1 Homo sapiens 77-81 30851383-1 2019 (-)-Epicatechin (Epi) has been demonstrated to activate pathways involved in GPER-stimulated nitric oxide (NO) production via endothelial NO synthase, known as the eNOS/NO pathway. Nitric Oxide 93-105 G protein-coupled estrogen receptor 1 Homo sapiens 77-81 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. Catechin 45-48 G protein-coupled estrogen receptor 1 Homo sapiens 141-145 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. Catechin 45-48 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. Catechin 45-48 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-prop 87-95 G protein-coupled estrogen receptor 1 Homo sapiens 141-145 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-prop 87-95 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-prop 87-95 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-4-prop 97-107 G protein-coupled estrogen receptor 1 Homo sapiens 141-145 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-4-prop 97-107 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-4-prop 97-107 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-5-prop 112-122 G protein-coupled estrogen receptor 1 Homo sapiens 141-145 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-5-prop 112-122 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 30851383-2 2019 Previous studies combining synthesis of four Epi derivatives demonstrated that Epi and Epi-prop, Epi-4-prop and Epi-5-prop were able to bind GPER by acting as GPER agonists, whereas docking studies allowed observation of structural details of the binding of these derivatives at the GPER binding site. epi-5-prop 112-122 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 30851383-4 2019 In this contribution, we explore the structural and energetic changes coupling the binding of Epi and its four derivatives to GPER. Catechin 94-97 G protein-coupled estrogen receptor 1 Homo sapiens 126-130 30851383-7 2019 Structural analysis demonstrated that Epi, Epi-4-prop and Epi-5-prop share more similar interactions at GPER binding sites with similar conformational behavior than with Epi-prop and Epi-Ms. Catechin 38-41 G protein-coupled estrogen receptor 1 Homo sapiens 104-108 30851383-7 2019 Structural analysis demonstrated that Epi, Epi-4-prop and Epi-5-prop share more similar interactions at GPER binding sites with similar conformational behavior than with Epi-prop and Epi-Ms. epi-4-prop 43-53 G protein-coupled estrogen receptor 1 Homo sapiens 104-108 30851383-7 2019 Structural analysis demonstrated that Epi, Epi-4-prop and Epi-5-prop share more similar interactions at GPER binding sites with similar conformational behavior than with Epi-prop and Epi-Ms. epi-5-prop 58-68 G protein-coupled estrogen receptor 1 Homo sapiens 104-108 31040364-0 2019 Targeting GPER1 to suppress autophagy as a male-specific therapeutic strategy for iron-induced striatal injury. Iron 82-86 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 30879772-0 2019 Estradiol stimulates cell proliferation via classic estrogen receptor-alpha and G protein-coupled estrogen receptor-1 in human renal tubular epithelial cell primary cultures. Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 80-117 30879772-3 2019 Incubation of HRTEC with the G protein-coupled estrogen receptor 1 (GPER-1) agonist G-1 increased BrdU uptake. Bromodeoxyuridine 98-102 G protein-coupled estrogen receptor 1 Homo sapiens 29-66 30879772-3 2019 Incubation of HRTEC with the G protein-coupled estrogen receptor 1 (GPER-1) agonist G-1 increased BrdU uptake. Bromodeoxyuridine 98-102 G protein-coupled estrogen receptor 1 Homo sapiens 68-74 30879772-5 2019 Treatment of HRTEC with the GPER-1 antagonist G-15, the ER inhibitor ICI182,780, or the beta-catenin inhibitor iCRT14, completely abrogated the increase in BrdU uptake induced by 17betaE. hrtec 13-18 G protein-coupled estrogen receptor 1 Homo sapiens 28-34 30879772-7 2019 In conclusion, estradiol stimulates cell proliferation in HRTEC primary cultures through both ERalpha and GPER-1 estrogen receptors and involves beta-catenin activation. Estradiol 15-24 G protein-coupled estrogen receptor 1 Homo sapiens 106-112 31040364-8 2019 This finding opens the prospect of a male-specific therapeutic strategy targeting GPER1 for autophagy suppression in patients suffering from iron overload after hemorrhage. Iron 141-145 G protein-coupled estrogen receptor 1 Homo sapiens 82-87 30677511-0 2019 Involvement of estrogen receptor and GPER in bisphenol A induced proliferation of vascular smooth muscle cells. bisphenol A 45-56 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 30570746-9 2019 In this study, we also demonstrate that selective activation of GPER induced astrocyte apoptosis via the phospholipase C pathway and subsequent intracellular calcium rise, whereas in neurons, this effect was not observed. Calcium 158-165 G protein-coupled estrogen receptor 1 Homo sapiens 64-68 31028714-2 2019 MATERIAL AND METHODS Expression of GPER mRNA in gastric cancer tissues and normal adjacent tissues was investigated using data from The Cancer Genome Atlas (TCGA), the Gene Expression Omnibus (GEO), and Oncomine database. oncomine 203-211 G protein-coupled estrogen receptor 1 Homo sapiens 35-39 31028714-6 2019 Immunohistochemistry and Western blot evaluated GPER protein expression in tissue microarrays (TMAs) and gastric cancer cell lines. tmas 95-99 G protein-coupled estrogen receptor 1 Homo sapiens 48-52 30575816-0 2019 Tamoxifen mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 66-101 30575816-2 2019 Tamoxifen is also an agonist of the G protein-coupled estrogen receptor (GPER), a GPCR ubiquitously expressed in tissues that mediates the acute response to estrogens. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 36-71 30575816-2 2019 Tamoxifen is also an agonist of the G protein-coupled estrogen receptor (GPER), a GPCR ubiquitously expressed in tissues that mediates the acute response to estrogens. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 73-77 30961827-2 2019 Differentiation of pancreatic stellate cells (PSCs) into myofibroblasts is inhibited by the estrogen-receptor modulator, tamoxifen, which activates a G-protein-coupled receptor (GPCR) for estrogen (GPER). Tamoxifen 121-130 G protein-coupled estrogen receptor 1 Homo sapiens 198-202 30677511-9 2019 Blocking the functions of ERalpha and GPER by their specific inhibitors can attenuate the BPA induced proliferation of VSMCs and expression of Ang II. bisphenol A 90-93 G protein-coupled estrogen receptor 1 Homo sapiens 38-42 30677511-10 2019 Consistently, BPA induced expression of TNFalpha and IL-6 was also attenuated by inhibitors of ERalpha and GPER. bisphenol A 14-17 G protein-coupled estrogen receptor 1 Homo sapiens 107-111 30677511-11 2019 BPA can increase the phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2) though GPER. bisphenol A 0-3 G protein-coupled estrogen receptor 1 Homo sapiens 98-102 30677511-13 2019 Collectively, our present study suggested that BPA can trigger the proliferation of VSMCs via both ERalpha and GPER dependent manners. bisphenol A 47-50 G protein-coupled estrogen receptor 1 Homo sapiens 111-115 30451119-0 2019 Synthesis and In Vitro Evaluation of Tetrahydroquinoline Derivatives as Antiproliferative Compounds of Breast Cancer via Targeting the GPER. 1,2,3,4-tetrahydroquinoline 37-56 G protein-coupled estrogen receptor 1 Homo sapiens 135-139 30889865-5 2019 We propose a novel hypothesis that ER-alpha36-GPER signaling initially induces rapid and temporal activation of NADPH oxidase 1 to generate superoxide, which subsequently activates redox-sensitive neutral sphingomyelinase 2 generating the lipid signaling mediator ceramide. Superoxides 140-150 G protein-coupled estrogen receptor 1 Homo sapiens 46-50 30889865-5 2019 We propose a novel hypothesis that ER-alpha36-GPER signaling initially induces rapid and temporal activation of NADPH oxidase 1 to generate superoxide, which subsequently activates redox-sensitive neutral sphingomyelinase 2 generating the lipid signaling mediator ceramide. Ceramides 264-272 G protein-coupled estrogen receptor 1 Homo sapiens 46-50 30590021-6 2019 Furthermore, GPR30 antagonist pre-treatment inhibited increases in NETosis and PAD4 expression mediated by G-1 and partially inhibited these effects mediated by E2. Estradiol 161-163 G protein-coupled estrogen receptor 1 Homo sapiens 13-18 30590021-7 2019 These results demonstrate that E2 treatment induces NETosis via not only ERalpha/ERbeta but also GPR30 in neutrophil-like HL-60 cells. Estradiol 31-33 G protein-coupled estrogen receptor 1 Homo sapiens 97-102 28877783-5 2019 The effects of activating GPER and function of G15 were analyzed in the proliferation of A549 and H1793 cell lines and development of urethane-induced adenocarcinoma. Urethane 134-142 G protein-coupled estrogen receptor 1 Homo sapiens 26-30 30478785-0 2019 G-protein-coupled estrogen receptor GPER-1 expression in hormone receptor-positive breast cancer is associated with poor benefit of tamoxifen. Tamoxifen 132-141 G protein-coupled estrogen receptor 1 Homo sapiens 36-42 30478785-1 2019 BACKGROUND: The role of G-protein-coupled estrogen receptor 1 (GPER-1) in the development of tamoxifen resistance in breast cancer is a highly controversial issue. Tamoxifen 93-102 G protein-coupled estrogen receptor 1 Homo sapiens 24-61 30478785-1 2019 BACKGROUND: The role of G-protein-coupled estrogen receptor 1 (GPER-1) in the development of tamoxifen resistance in breast cancer is a highly controversial issue. Tamoxifen 93-102 G protein-coupled estrogen receptor 1 Homo sapiens 63-69 30478785-10 2019 DFS between tamoxifen- and aromatase inhibitor-treated GPER-1-positive patients was similar (p = 0.090). Tamoxifen 12-21 G protein-coupled estrogen receptor 1 Homo sapiens 55-61 30478785-11 2019 Notably, after matching the analysis for the most important prognostic factors, DFS for tamoxifen-treated GPER-1-positive patients was 69.1%, which is a percentage that is significantly lower compared to DFS for GPER-1-positive patients treated with aromatase inhibitors (92.7%) (p = 0.005). Tamoxifen 88-97 G protein-coupled estrogen receptor 1 Homo sapiens 106-112 30478785-11 2019 Notably, after matching the analysis for the most important prognostic factors, DFS for tamoxifen-treated GPER-1-positive patients was 69.1%, which is a percentage that is significantly lower compared to DFS for GPER-1-positive patients treated with aromatase inhibitors (92.7%) (p = 0.005). Tamoxifen 88-97 G protein-coupled estrogen receptor 1 Homo sapiens 212-218 30678825-13 2019 The interaction with DOX appears to be cell type dependent, exhibiting a non-monotonic response curve in MRC-5 cells, a GPER expressing cell line. Doxorubicin 21-24 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 30866584-2 2019 By quantitative PCR (qPCR), western blot, immunofluorescence analysis, ELISA and ChIP assays, we demonstrated that 17beta-estradiol (E2) and the G protein estrogen receptor (GPER) agonist G-1 induce the up-regulation and secretion of FGF2 via GPER together with the EGFR/ERK/c-fos/AP-1 signaling cascade in (ER)-negative primary CAFs. Estradiol 115-131 G protein-coupled estrogen receptor 1 Homo sapiens 243-247 30760632-0 2019 Human G protein-coupled receptor 30 is N-glycosylated and N-terminal domain asparagine 44 is required for receptor structure and activity. Nitrogen 39-40 G protein-coupled estrogen receptor 1 Homo sapiens 6-35 30760632-0 2019 Human G protein-coupled receptor 30 is N-glycosylated and N-terminal domain asparagine 44 is required for receptor structure and activity. Asparagine 76-86 G protein-coupled estrogen receptor 1 Homo sapiens 6-35 30760632-4 2019 Here, we used human embryonic kidney (HEK) 293 (HEK293) cells ectopically expressing N-terminally FLAG-tagged human GPR30 and three unique antibodies (Ab) specifically targetting the receptor N-terminal domain (N-domain) to investigate the role of N-glycosylation in receptor maturation and activity, the latter assayed by constitutive receptor-stimulated extracellular-regulated protein kinase (ERK) 1/2 (ERK1/2) activity. Nitrogen 85-86 G protein-coupled estrogen receptor 1 Homo sapiens 116-121 30646517-1 2019 The G-protein coupled estrogen receptor (GPER), an alternate estrogen receptor (ER) with a structure distinct from the two canonical ERs, being ERalpha, and ERbeta, is expressed in 50% to 60% of breast cancer tissues and has been presumed to be associated with the development of tamoxifen resistance in ERalpha positive breast cancer. Tamoxifen 280-289 G protein-coupled estrogen receptor 1 Homo sapiens 4-39 30646517-1 2019 The G-protein coupled estrogen receptor (GPER), an alternate estrogen receptor (ER) with a structure distinct from the two canonical ERs, being ERalpha, and ERbeta, is expressed in 50% to 60% of breast cancer tissues and has been presumed to be associated with the development of tamoxifen resistance in ERalpha positive breast cancer. Tamoxifen 280-289 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 30848227-4 2019 BPA exerts other effects by activating the membrane receptor GPER (GPR30) and/or other receptors such as the estrogen-related receptors (ERRs). bisphenol A 0-3 G protein-coupled estrogen receptor 1 Homo sapiens 61-65 30848227-4 2019 BPA exerts other effects by activating the membrane receptor GPER (GPR30) and/or other receptors such as the estrogen-related receptors (ERRs). bisphenol A 0-3 G protein-coupled estrogen receptor 1 Homo sapiens 67-72 29883692-0 2018 17beta-estradiol potentiates TREK1 channel activity through G protein-coupled estrogen receptor. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 60-95 30538116-3 2019 Here we report that tamoxifen regulates the level and activity of collagen cross-linking and degradative enzymes, and hence the organization of the extracellular matrix, via a mechanism involving both the G protein-coupled estrogen receptor (GPER) and hypoxia-inducible factor-1 alpha (HIF-1A). Tamoxifen 20-29 G protein-coupled estrogen receptor 1 Homo sapiens 205-240 30538116-3 2019 Here we report that tamoxifen regulates the level and activity of collagen cross-linking and degradative enzymes, and hence the organization of the extracellular matrix, via a mechanism involving both the G protein-coupled estrogen receptor (GPER) and hypoxia-inducible factor-1 alpha (HIF-1A). Tamoxifen 20-29 G protein-coupled estrogen receptor 1 Homo sapiens 242-246 30267584-6 2018 The interaction between miR-103 and G protein-coupled estrogen receptor 1 (GPER1) was confirmed with the dual luciferase assays. mir-103 24-31 G protein-coupled estrogen receptor 1 Homo sapiens 36-73 30267584-6 2018 The interaction between miR-103 and G protein-coupled estrogen receptor 1 (GPER1) was confirmed with the dual luciferase assays. mir-103 24-31 G protein-coupled estrogen receptor 1 Homo sapiens 75-80 30538116-6 2019 Our findings implicate the GPER/HIF-1A axis as a master regulator of peri-tumoral stromal remodeling and the fibrovascular tumor microenvironment and offer a paradigm shift for tamoxifen from a well-established drug in breast cancer hormonal therapy to an alternative candidate for stromal targeting strategies in PDAC and possibly other cancers. Tamoxifen 177-186 G protein-coupled estrogen receptor 1 Homo sapiens 27-31 30538117-2 2019 Tamoxifen, an agonist of the G protein-coupled estrogen receptor (GPER), is widely used to treat estrogen-positive breast cancer. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 29-64 30538117-2 2019 Tamoxifen, an agonist of the G protein-coupled estrogen receptor (GPER), is widely used to treat estrogen-positive breast cancer. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 66-70 30538117-3 2019 Here, we show that tamoxifen mechanically reprograms the tumor microenvironment through a newly identified GPER-mediated mechanism. Tamoxifen 19-28 G protein-coupled estrogen receptor 1 Homo sapiens 107-111 30538117-4 2019 Tamoxifen inhibits the myofibroblastic differentiation of pancreatic stellate cells (PSCs) in the tumor microenvironment of pancreatic cancer in an acto-myosin-dependent manner via RhoA-mediated contractility, YAP deactivation, and GPER signaling. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 232-236 29428396-3 2018 BPA has a weak affinity for ERalpha/beta but interaction with extranuclearly located pathways activated by estrogens such as ERRgamma and GPER reveals how BPA can act at low doses. bisphenol A 0-3 G protein-coupled estrogen receptor 1 Homo sapiens 138-142 29428396-3 2018 BPA has a weak affinity for ERalpha/beta but interaction with extranuclearly located pathways activated by estrogens such as ERRgamma and GPER reveals how BPA can act at low doses. bisphenol A 155-158 G protein-coupled estrogen receptor 1 Homo sapiens 138-142 30048677-5 2018 Some of BPA"s effects are reversed by oestrogen and/or GPER inhibitors. bisphenol A 8-11 G protein-coupled estrogen receptor 1 Homo sapiens 55-59 29883692-3 2018 The G protein-coupled estrogen receptor (GPER) is known to facilitate rapid actions of 17beta-estradiol, though its role in modulation of ion channels is not widely explored. Estradiol 87-103 G protein-coupled estrogen receptor 1 Homo sapiens 4-39 29883692-3 2018 The G protein-coupled estrogen receptor (GPER) is known to facilitate rapid actions of 17beta-estradiol, though its role in modulation of ion channels is not widely explored. Estradiol 87-103 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 29883692-5 2018 In the present study, using single channel cell-attached patch clamp electrophysiology in HEK293 cells, we show that 17beta-estradiol increases the activity of hTREK1 channel by acting through hGPER and increasing the channel opening probability within minutes. Estradiol 117-133 G protein-coupled estrogen receptor 1 Homo sapiens 193-198 29883692-8 2018 Mutational studies revealed the serines at positions 315 and 348 in the C-terminal domain of hTREK1 to be the target sites for dephosphorylation induced by 17beta-estradiol action through hGPER. Serine 32-39 G protein-coupled estrogen receptor 1 Homo sapiens 188-193 29883692-8 2018 Mutational studies revealed the serines at positions 315 and 348 in the C-terminal domain of hTREK1 to be the target sites for dephosphorylation induced by 17beta-estradiol action through hGPER. Estradiol 156-172 G protein-coupled estrogen receptor 1 Homo sapiens 188-193 29883692-9 2018 Elucidation of the pathway for the potentiating action of 17beta-estradiol via hGPER on hTREK1 channel activity will help us understand better one of the many possible neuroprotective mechanisms of 17beta-estradiol and hTREK1 channel. Estradiol 58-74 G protein-coupled estrogen receptor 1 Homo sapiens 79-84 29883692-9 2018 Elucidation of the pathway for the potentiating action of 17beta-estradiol via hGPER on hTREK1 channel activity will help us understand better one of the many possible neuroprotective mechanisms of 17beta-estradiol and hTREK1 channel. Estradiol 198-214 G protein-coupled estrogen receptor 1 Homo sapiens 79-84 30258538-0 2018 A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth. indole-thiazole 12-27 G protein-coupled estrogen receptor 1 Homo sapiens 47-51 29373840-4 2018 Here, we demonstrated that icariin, which is a G protein-coupled estrogen receptor 1 (GPER) agonist, inhibited podocyte apoptosis by reducing ROS, maintaining the integrity of mitochondrial membranes. icariin 27-34 G protein-coupled estrogen receptor 1 Homo sapiens 47-84 29373840-4 2018 Here, we demonstrated that icariin, which is a G protein-coupled estrogen receptor 1 (GPER) agonist, inhibited podocyte apoptosis by reducing ROS, maintaining the integrity of mitochondrial membranes. icariin 27-34 G protein-coupled estrogen receptor 1 Homo sapiens 86-90 29373840-4 2018 Here, we demonstrated that icariin, which is a G protein-coupled estrogen receptor 1 (GPER) agonist, inhibited podocyte apoptosis by reducing ROS, maintaining the integrity of mitochondrial membranes. Reactive Oxygen Species 142-145 G protein-coupled estrogen receptor 1 Homo sapiens 86-90 29964007-4 2018 Rapid non-genomic signaling is initiated from the plasma membrane by a G-protein coupled receptor called GPER1 that binds 17beta-estradiol. Estradiol 122-138 G protein-coupled estrogen receptor 1 Homo sapiens 105-110 29758456-0 2018 GPER/Hippo-YAP signal is involved in Bisphenol S induced migration of triple negative breast cancer (TNBC) cells. bis(4-hydroxyphenyl)sulfone 37-46 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 29758456-7 2018 Inhibition of G protein-coupled estrogen receptor 1 (GPER) and its downstream PLCbeta/PKC signals attenuate the effects of BPS-induced YAP dephosphorylation and CTGF up-regulation. bis(4-hydroxyphenyl)sulfone 123-126 G protein-coupled estrogen receptor 1 Homo sapiens 14-51 29758456-7 2018 Inhibition of G protein-coupled estrogen receptor 1 (GPER) and its downstream PLCbeta/PKC signals attenuate the effects of BPS-induced YAP dephosphorylation and CTGF up-regulation. bis(4-hydroxyphenyl)sulfone 123-126 G protein-coupled estrogen receptor 1 Homo sapiens 53-57 29758456-8 2018 Targeted inhibition of GPER/YAP inhibits BPS-induced migration of TNBC cells. bis(4-hydroxyphenyl)sulfone 41-44 G protein-coupled estrogen receptor 1 Homo sapiens 23-27 29758456-9 2018 Collectively, we reveal that GPER/Hippo-YAP signal is involved in BPS-induced migration of TNBC cells. bis(4-hydroxyphenyl)sulfone 66-69 G protein-coupled estrogen receptor 1 Homo sapiens 29-33 29964007-7 2018 In this review, we describe several notable characteristics of GPER1 such as the ability of several endogenous steroids as well as artificially synthesized molecules to bind the GPER1. Steroids 111-119 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 29964007-7 2018 In this review, we describe several notable characteristics of GPER1 such as the ability of several endogenous steroids as well as artificially synthesized molecules to bind the GPER1. Steroids 111-119 G protein-coupled estrogen receptor 1 Homo sapiens 178-183 29807145-6 2018 Both E2 (17beta-estradiol) and Ral increased the expression of ERalpha and GPR30 and enhanced TDP-25 cell viability, and these effects were completely abolished by treatment with an ERalpha/beta antagonist (ICI 182,780) or GPR30 antagonist (G15). Estradiol 5-7 G protein-coupled estrogen receptor 1 Homo sapiens 75-80 29885598-8 2018 Finally, deletion of GPR30 in beta-cells or islets ablated genistein-induced CREB phosphorylation and its cytoprotective effect. Genistein 59-68 G protein-coupled estrogen receptor 1 Homo sapiens 21-26 29885598-9 2018 These findings demonstrate that genistein is a survival factor for beta-cells via GPR30-initiated, Galphas-mediated activation of CREB. galphas 99-106 G protein-coupled estrogen receptor 1 Homo sapiens 82-87 30050469-0 2018 Tamoxifen-Induced Apoptosis of MCF-7 Cells via GPR30/PI3K/MAPKs Interactions: Verification by ODE Modeling and RNA Sequencing. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 47-52 30050469-6 2018 Evidence that tamoxifen functions as a GPR30 (G-Protein Coupled Receptor 30) agonist activating adenylyl cyclase and EGFR (Epidermal Growth Factor Receptor) intracellular signaling networks, provides yet another means of explaining the multi-functionality of tamoxifen. Tamoxifen 14-23 G protein-coupled estrogen receptor 1 Homo sapiens 39-44 30050469-6 2018 Evidence that tamoxifen functions as a GPR30 (G-Protein Coupled Receptor 30) agonist activating adenylyl cyclase and EGFR (Epidermal Growth Factor Receptor) intracellular signaling networks, provides yet another means of explaining the multi-functionality of tamoxifen. Tamoxifen 14-23 G protein-coupled estrogen receptor 1 Homo sapiens 46-75 30050469-6 2018 Evidence that tamoxifen functions as a GPR30 (G-Protein Coupled Receptor 30) agonist activating adenylyl cyclase and EGFR (Epidermal Growth Factor Receptor) intracellular signaling networks, provides yet another means of explaining the multi-functionality of tamoxifen. Tamoxifen 259-268 G protein-coupled estrogen receptor 1 Homo sapiens 39-44 30050469-6 2018 Evidence that tamoxifen functions as a GPR30 (G-Protein Coupled Receptor 30) agonist activating adenylyl cyclase and EGFR (Epidermal Growth Factor Receptor) intracellular signaling networks, provides yet another means of explaining the multi-functionality of tamoxifen. Tamoxifen 259-268 G protein-coupled estrogen receptor 1 Homo sapiens 46-75 30050469-7 2018 Here ordinary differential equation (ODE) modeling, RNA sequencing and real time qPCR analysis were utilized to establish the necessary data for gene network mapping of tamoxifen-stimulated MCF-7 cells, which express the endogenous ER and GPR30. Tamoxifen 169-178 G protein-coupled estrogen receptor 1 Homo sapiens 239-244 29807145-6 2018 Both E2 (17beta-estradiol) and Ral increased the expression of ERalpha and GPR30 and enhanced TDP-25 cell viability, and these effects were completely abolished by treatment with an ERalpha/beta antagonist (ICI 182,780) or GPR30 antagonist (G15). Estradiol 5-7 G protein-coupled estrogen receptor 1 Homo sapiens 223-228 29807145-6 2018 Both E2 (17beta-estradiol) and Ral increased the expression of ERalpha and GPR30 and enhanced TDP-25 cell viability, and these effects were completely abolished by treatment with an ERalpha/beta antagonist (ICI 182,780) or GPR30 antagonist (G15). Estradiol 9-25 G protein-coupled estrogen receptor 1 Homo sapiens 75-80 29807145-6 2018 Both E2 (17beta-estradiol) and Ral increased the expression of ERalpha and GPR30 and enhanced TDP-25 cell viability, and these effects were completely abolished by treatment with an ERalpha/beta antagonist (ICI 182,780) or GPR30 antagonist (G15). Estradiol 9-25 G protein-coupled estrogen receptor 1 Homo sapiens 223-228 29805678-6 2018 Expression of GPER and activation of c-src and epidermal growth factor receptor (EGFR) by 17beta-estradiol was analyzed by western blotting. Estradiol 90-106 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 29275510-3 2018 In our previous study with cultured human fetal lung fibroblasts (HFLF), we demonstrated that 24-h exposure to 1 and 100 microM BPA increased GPR30 protein in the nuclear fraction. bisphenol A 128-131 G protein-coupled estrogen receptor 1 Homo sapiens 142-147 29608013-0 2018 17beta-Estradiol on the Expression of G-Protein Coupled Estrogen Receptor (GPER/GPR30) Mitophagy, and the PI3K/Akt Signaling Pathway in ATDC5 Chondrocytes In Vitro. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 80-85 29608013-2 2018 G-protein coupled estrogen receptor (GPER/GPR30) activates cell signaling in response to 17beta-estradiol, which can be blocked by the GPR30 agonist, G15, an analog of G-1. Estradiol 89-105 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 29608013-2 2018 G-protein coupled estrogen receptor (GPER/GPR30) activates cell signaling in response to 17beta-estradiol, which can be blocked by the GPR30 agonist, G15, an analog of G-1. Estradiol 89-105 G protein-coupled estrogen receptor 1 Homo sapiens 42-47 29608013-2 2018 G-protein coupled estrogen receptor (GPER/GPR30) activates cell signaling in response to 17beta-estradiol, which can be blocked by the GPR30 agonist, G15, an analog of G-1. Estradiol 89-105 G protein-coupled estrogen receptor 1 Homo sapiens 135-140 29608013-3 2018 The aims of this study were to investigate the effects of 17beta-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. Estradiol 58-74 G protein-coupled estrogen receptor 1 Homo sapiens 133-137 29608013-3 2018 The aims of this study were to investigate the effects of 17beta-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. Estradiol 58-74 G protein-coupled estrogen receptor 1 Homo sapiens 138-143 29608013-9 2018 RESULTS In 17beta-estradiol-treated ATDC5 chondrocytes, increased expression of GPER/GPR30 was found, but fewer mitophagosomes were observed, and decreased numbers of TOM20-positive granules were co-localized with decreased LAMP2 and increased expression levels of TOM20, Hsp60, p-Akt, and p-mTOR, and reduced expression of LC3-II, were found. Estradiol 11-27 G protein-coupled estrogen receptor 1 Homo sapiens 80-84 29608013-9 2018 RESULTS In 17beta-estradiol-treated ATDC5 chondrocytes, increased expression of GPER/GPR30 was found, but fewer mitophagosomes were observed, and decreased numbers of TOM20-positive granules were co-localized with decreased LAMP2 and increased expression levels of TOM20, Hsp60, p-Akt, and p-mTOR, and reduced expression of LC3-II, were found. Estradiol 11-27 G protein-coupled estrogen receptor 1 Homo sapiens 85-90 29608013-11 2018 CONCLUSIONS Treatment with 17beta-estradiol protected ATDC5 chondrocytes against mitophagy via the GPER/GPR30 and the PI3K/Akt signaling pathway. Estradiol 27-43 G protein-coupled estrogen receptor 1 Homo sapiens 99-103 29608013-11 2018 CONCLUSIONS Treatment with 17beta-estradiol protected ATDC5 chondrocytes against mitophagy via the GPER/GPR30 and the PI3K/Akt signaling pathway. Estradiol 27-43 G protein-coupled estrogen receptor 1 Homo sapiens 104-109 29790728-0 2018 Hydroxylated Polybrominated Diphenyl Ethers Exert Estrogenic Effects via Non-Genomic G Protein-Coupled Estrogen Receptor Mediated Pathways. Phenyl Ethers 28-43 G protein-coupled estrogen receptor 1 Homo sapiens 85-120 29790728-3 2018 OBJECTIVE: The present study aimed to investigate the estrogenic effects of PBDEs and OH-PBDEs via nongenomic G protein-coupled estrogen receptor (GPER) pathways. Halogenated Diphenyl Ethers 76-81 G protein-coupled estrogen receptor 1 Homo sapiens 110-145 29790728-3 2018 OBJECTIVE: The present study aimed to investigate the estrogenic effects of PBDEs and OH-PBDEs via nongenomic G protein-coupled estrogen receptor (GPER) pathways. Halogenated Diphenyl Ethers 76-81 G protein-coupled estrogen receptor 1 Homo sapiens 147-151 29790728-3 2018 OBJECTIVE: The present study aimed to investigate the estrogenic effects of PBDEs and OH-PBDEs via nongenomic G protein-coupled estrogen receptor (GPER) pathways. oh-pbdes 86-94 G protein-coupled estrogen receptor 1 Homo sapiens 110-145 29790728-3 2018 OBJECTIVE: The present study aimed to investigate the estrogenic effects of PBDEs and OH-PBDEs via nongenomic G protein-coupled estrogen receptor (GPER) pathways. oh-pbdes 86-94 G protein-coupled estrogen receptor 1 Homo sapiens 147-151 29790728-4 2018 METHODS: The binding affinities of 12 PBDEs and 18 OH-PBDEs with GPER were determined by a fluorescence competitive binding assay in a human breast cancer cell line (SKBR3). 12 pbdes 35-43 G protein-coupled estrogen receptor 1 Homo sapiens 65-69 29790728-4 2018 METHODS: The binding affinities of 12 PBDEs and 18 OH-PBDEs with GPER were determined by a fluorescence competitive binding assay in a human breast cancer cell line (SKBR3). 18 oh-pbdes 48-59 G protein-coupled estrogen receptor 1 Homo sapiens 65-69 29790728-6 2018 Their activities on GPER pathways were investigated by detecting calcium mobilization and cyclic adenosine monophosphate (cAMP) accumulation in SKBR3 cells. Calcium 65-72 G protein-coupled estrogen receptor 1 Homo sapiens 20-24 29790728-6 2018 Their activities on GPER pathways were investigated by detecting calcium mobilization and cyclic adenosine monophosphate (cAMP) accumulation in SKBR3 cells. Cyclic AMP 90-120 G protein-coupled estrogen receptor 1 Homo sapiens 20-24 29790728-6 2018 Their activities on GPER pathways were investigated by detecting calcium mobilization and cyclic adenosine monophosphate (cAMP) accumulation in SKBR3 cells. Cyclic AMP 122-126 G protein-coupled estrogen receptor 1 Homo sapiens 20-24 29790728-8 2018 RESULTS: Our results showed that 11 of the OH-PBDEs but none of the PBDEs bound to GPER directly. oh-pbdes 43-51 G protein-coupled estrogen receptor 1 Homo sapiens 83-87 29790728-8 2018 RESULTS: Our results showed that 11 of the OH-PBDEs but none of the PBDEs bound to GPER directly. Halogenated Diphenyl Ethers 46-51 G protein-coupled estrogen receptor 1 Homo sapiens 83-87 29790728-10 2018 Docking results suggested that the hydroxyl group played an essential role in the binding of OH-PBDEs to GPER by forming hydrogen bond interactions. oh-pbdes 93-101 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 29790728-10 2018 Docking results suggested that the hydroxyl group played an essential role in the binding of OH-PBDEs to GPER by forming hydrogen bond interactions. Hydrogen 121-129 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 29790728-11 2018 Most of the OH-PBDEs activated subsequent GPER signaling pathways. oh-pbdes 12-20 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 29790728-13 2018 These three OH-PBDEs also promoted SKBR3 cell migration via GPER pathways with LOECs of 0.1-1 muM. oh-pbdes 12-20 G protein-coupled estrogen receptor 1 Homo sapiens 60-64 29790728-14 2018 CONCLUSION: OH-PBDEs could bind to GPER, activate the subsequent signaling pathways, and promote SKBR3 cell migration via GPER pathways. oh-pbdes 12-20 G protein-coupled estrogen receptor 1 Homo sapiens 35-39 29790728-14 2018 CONCLUSION: OH-PBDEs could bind to GPER, activate the subsequent signaling pathways, and promote SKBR3 cell migration via GPER pathways. oh-pbdes 12-20 G protein-coupled estrogen receptor 1 Homo sapiens 122-126 29790728-15 2018 OH-PBDEs might exert estrogenic effects by a novel nongenomic mechanism involving the activation of GPER at nanomolar concentrations. oh-pbdes 0-8 G protein-coupled estrogen receptor 1 Homo sapiens 100-104 29382535-0 2018 MEHP promotes the proliferation of cervical cancer via GPER mediated activation of Akt. mono-(2-ethylhexyl)phthalate 0-4 G protein-coupled estrogen receptor 1 Homo sapiens 55-59 29382535-6 2018 In addition, the inhibitor of G protein coupled estrogen receptor (GPER), while not estrogen receptor alpha (ERalpha), can abolish MEHP induced phosphorylation of Akt and cell proliferation, suggesting that GPER is involved in MEHP induced activation of Akt. mono-(2-ethylhexyl)phthalate 131-135 G protein-coupled estrogen receptor 1 Homo sapiens 30-65 29382535-6 2018 In addition, the inhibitor of G protein coupled estrogen receptor (GPER), while not estrogen receptor alpha (ERalpha), can abolish MEHP induced phosphorylation of Akt and cell proliferation, suggesting that GPER is involved in MEHP induced activation of Akt. mono-(2-ethylhexyl)phthalate 131-135 G protein-coupled estrogen receptor 1 Homo sapiens 67-71 29382535-6 2018 In addition, the inhibitor of G protein coupled estrogen receptor (GPER), while not estrogen receptor alpha (ERalpha), can abolish MEHP induced phosphorylation of Akt and cell proliferation, suggesting that GPER is involved in MEHP induced activation of Akt. mono-(2-ethylhexyl)phthalate 131-135 G protein-coupled estrogen receptor 1 Homo sapiens 207-211 29382535-6 2018 In addition, the inhibitor of G protein coupled estrogen receptor (GPER), while not estrogen receptor alpha (ERalpha), can abolish MEHP induced phosphorylation of Akt and cell proliferation, suggesting that GPER is involved in MEHP induced activation of Akt. mono-(2-ethylhexyl)phthalate 227-231 G protein-coupled estrogen receptor 1 Homo sapiens 30-65 29382535-6 2018 In addition, the inhibitor of G protein coupled estrogen receptor (GPER), while not estrogen receptor alpha (ERalpha), can abolish MEHP induced phosphorylation of Akt and cell proliferation, suggesting that GPER is involved in MEHP induced activation of Akt. mono-(2-ethylhexyl)phthalate 227-231 G protein-coupled estrogen receptor 1 Homo sapiens 67-71 29382535-6 2018 In addition, the inhibitor of G protein coupled estrogen receptor (GPER), while not estrogen receptor alpha (ERalpha), can abolish MEHP induced phosphorylation of Akt and cell proliferation, suggesting that GPER is involved in MEHP induced activation of Akt. mono-(2-ethylhexyl)phthalate 227-231 G protein-coupled estrogen receptor 1 Homo sapiens 207-211 29608013-0 2018 17beta-Estradiol on the Expression of G-Protein Coupled Estrogen Receptor (GPER/GPR30) Mitophagy, and the PI3K/Akt Signaling Pathway in ATDC5 Chondrocytes In Vitro. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 75-79 29360846-7 2018 GPER antagonist, G-36, significantly inhibited both the G-1-induced relaxation effect and G-1-enhanced ET-1 contraction. G-36 17-21 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 29229551-11 2018 Exemestane also modulates ERK and STAT3 signalling via GPR30. exemestane 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 55-60 28285016-8 2018 This viewpoint changed recently with the discovery that GPER is associated with aging, particularly that of the cardiovascular system, where the GPER antagonist G36 reduced hypertension and GPER deficiency prevented cardiac fibrosis and vascular dysfunction with age, through the downregulation of Nox1 and as a consequence superoxide production. Superoxides 324-334 G protein-coupled estrogen receptor 1 Homo sapiens 56-60 28285016-8 2018 This viewpoint changed recently with the discovery that GPER is associated with aging, particularly that of the cardiovascular system, where the GPER antagonist G36 reduced hypertension and GPER deficiency prevented cardiac fibrosis and vascular dysfunction with age, through the downregulation of Nox1 and as a consequence superoxide production. Superoxides 324-334 G protein-coupled estrogen receptor 1 Homo sapiens 145-149 28285016-8 2018 This viewpoint changed recently with the discovery that GPER is associated with aging, particularly that of the cardiovascular system, where the GPER antagonist G36 reduced hypertension and GPER deficiency prevented cardiac fibrosis and vascular dysfunction with age, through the downregulation of Nox1 and as a consequence superoxide production. Superoxides 324-334 G protein-coupled estrogen receptor 1 Homo sapiens 145-149 28343901-4 2018 However, GPER also has constitutive activity, e.g. in the absence of specific agonists, that was recently shown to promote hypertension and aging-induced tissue damage by promoting Nox1-derived production of ROS. Reactive Oxygen Species 208-211 G protein-coupled estrogen receptor 1 Homo sapiens 9-13 28343901-5 2018 Furthermore, the small molecule GPER blocker (GRB) G36 reduces blood pressure and vascular ROS production by selectively down-regulating Nox1 expression. Reactive Oxygen Species 91-94 G protein-coupled estrogen receptor 1 Homo sapiens 32-36 28343901-7 2018 Here, we will discuss the paradigm shift from selective GPER activation to ligand-independent, constitutive GPER signaling as a key regulator of Nox-derived oxidative stress, and the surprising identification of GRBs as the first Nox downregulators for the treatment of chronic non-communicable diseases. nicotine 1-N-oxide 145-148 G protein-coupled estrogen receptor 1 Homo sapiens 108-112 29229551-5 2018 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. exemestane 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 135-164 29229551-5 2018 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. exemestane 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 166-171 29360846-15 2018 These data demonstrate that activation of GPER induces relaxation via cAMP as well as contraction via a mechanism involving transactivation of EGFR and the phosphorylation of ERK1/2 in porcine coronary arteries. Cyclic AMP 70-74 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 29391778-0 2018 Ipriflavone promotes proliferation and osteogenic differentiation of periodontal ligament cells by activating GPR30/PI3K/AKT signaling pathway. ipriflavone 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 110-115 28924735-21 2018 Interestingly, Raloxifene-a GPER-activating selective estrogen receptor modulator-has recently been demonstrated to be preventive for cervical cancer relapse in mice. Raloxifene Hydrochloride 15-25 G protein-coupled estrogen receptor 1 Homo sapiens 28-32 29745344-5 2018 We included a carboxyl group instead of the acetyl group from G1 to form amides with several moieties to increase affinity on GPER1. Amides 73-79 G protein-coupled estrogen receptor 1 Homo sapiens 126-131 29745344-6 2018 The designed ligands were submitted to ligand-based and structure-based virtual screening to get insights into the binding mechanism of the best designed compound and phenol red on GPER1. Phenolsulfonphthalein 167-177 G protein-coupled estrogen receptor 1 Homo sapiens 181-186 29745344-10 2018 The compound showed better IC50 values without phenol red, suggesting that phenol red interfere with the G1-PABA action at GPER1, as observed through in silico studies, which is present in MCF-7 cells according to PCR studies and explains the cell proliferation effects. Phenolsulfonphthalein 75-85 G protein-coupled estrogen receptor 1 Homo sapiens 123-128 29383185-0 2017 GPER-independent inhibition of adrenocortical cancer growth by G-1 involves ROS/Egr-1/BAX pathway. ros 76-79 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 30029723-9 2018 Our groups have shown that DHEA and many of its oxidative metabolites serve as a low-affinity ligands for hepatic nuclear receptors, such as the pregnane X receptor, the constitutive androstane receptor, and estrogen receptors alpha/beta (ERalpha/ERbeta) as well as G protein-coupled ER (GPER1). Dehydroepiandrosterone 27-31 G protein-coupled estrogen receptor 1 Homo sapiens 288-293 30029731-6 2018 We review our recent study showing DHEA activated GPER1 (G-protein-coupled estrogen receptor 1) in HepG2 cells to stimulate miR-21 transcription. Dehydroepiandrosterone 35-39 G protein-coupled estrogen receptor 1 Homo sapiens 50-55 30029731-6 2018 We review our recent study showing DHEA activated GPER1 (G-protein-coupled estrogen receptor 1) in HepG2 cells to stimulate miR-21 transcription. Dehydroepiandrosterone 35-39 G protein-coupled estrogen receptor 1 Homo sapiens 57-94 29298702-0 2017 Correction to: Calycosin inhibits the in vitro and in vivo growth of breast cancer cells through WDR7-7-GPR30 Signaling. 7,3'-dihydroxy-4'-methoxyisoflavone 15-24 G protein-coupled estrogen receptor 1 Homo sapiens 104-109 28811233-7 2017 The stimulatory effects of TBBPA and BPA on cell proliferation were reversed by pre-treatment with a G protein-coupled receptor 30 (GPR30) antagonist in both cell lines, which possess similar basal GPR30 expression levels. tetrabromobisphenol A 27-32 G protein-coupled estrogen receptor 1 Homo sapiens 101-130 28945888-13 2017 Conclusion: Human CRC favors estradiol synthesis to augment proliferation via GPER stimulation. Estradiol 29-38 G protein-coupled estrogen receptor 1 Homo sapiens 78-82 28811233-7 2017 The stimulatory effects of TBBPA and BPA on cell proliferation were reversed by pre-treatment with a G protein-coupled receptor 30 (GPR30) antagonist in both cell lines, which possess similar basal GPR30 expression levels. tetrabromobisphenol A 27-32 G protein-coupled estrogen receptor 1 Homo sapiens 132-137 28811233-7 2017 The stimulatory effects of TBBPA and BPA on cell proliferation were reversed by pre-treatment with a G protein-coupled receptor 30 (GPR30) antagonist in both cell lines, which possess similar basal GPR30 expression levels. tetrabromobisphenol A 27-32 G protein-coupled estrogen receptor 1 Homo sapiens 198-203 28811233-7 2017 The stimulatory effects of TBBPA and BPA on cell proliferation were reversed by pre-treatment with a G protein-coupled receptor 30 (GPR30) antagonist in both cell lines, which possess similar basal GPR30 expression levels. bisphenol A 29-32 G protein-coupled estrogen receptor 1 Homo sapiens 101-130 28811233-7 2017 The stimulatory effects of TBBPA and BPA on cell proliferation were reversed by pre-treatment with a G protein-coupled receptor 30 (GPR30) antagonist in both cell lines, which possess similar basal GPR30 expression levels. bisphenol A 29-32 G protein-coupled estrogen receptor 1 Homo sapiens 132-137 28811233-8 2017 Taken together, our results show for the first time that TBBPA, which has lower potency than BPA, stimulates ovarian cancer cell proliferation through the GPR30 pathway. tetrabromobisphenol A 57-62 G protein-coupled estrogen receptor 1 Homo sapiens 155-160 28811233-8 2017 Taken together, our results show for the first time that TBBPA, which has lower potency than BPA, stimulates ovarian cancer cell proliferation through the GPR30 pathway. bisphenol A 59-62 G protein-coupled estrogen receptor 1 Homo sapiens 155-160 29096683-0 2017 Calycosin inhibits the in vitro and in vivo growth of breast cancer cells through WDR7-7-GPR30 Signaling. 7,3'-dihydroxy-4'-methoxyisoflavone 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 89-94 29192164-0 2017 Low-dose levels of bisphenol A inhibit telomerase via ER/GPR30-ERK signalling, impair DNA integrity and reduce cell proliferation in primary PBMC. bisphenol A 19-30 G protein-coupled estrogen receptor 1 Homo sapiens 57-62 29192164-8 2017 The results further demonstrate that BPA triggered rapidly an ER/GPR30-ERK transduction pathway that leads to decreased telomerase activity in human PBMC. bisphenol A 37-40 G protein-coupled estrogen receptor 1 Homo sapiens 65-70 29192164-9 2017 This is the first study to demonstrate adverse impact of BPA at levels of current human exposure on telomerase in normal cells, mediated by ER/GPR30-ERK. bisphenol A 57-60 G protein-coupled estrogen receptor 1 Homo sapiens 143-148 29096683-6 2017 Meanwhile, we show that calycosin stimulated the WDR7-7-GPR30 signaling pathway in MCF-7, T47D, MDA-MB-468, and SKBR3 breast cancer cells. 7,3'-dihydroxy-4'-methoxyisoflavone 24-33 G protein-coupled estrogen receptor 1 Homo sapiens 56-61 29096683-8 2017 Additionally, in all four GPR30-positive breast cancer lines, calycosin decreased the phosphorylation levels of SRC, EGFR, ERK1/2 and Akt, but the inhibition of WDR7-7 blocked these changes and increased proliferation. 7,3'-dihydroxy-4'-methoxyisoflavone 62-71 G protein-coupled estrogen receptor 1 Homo sapiens 26-31 29096683-10 2017 CONCLUSIONS: These results suggest the possibility that calycosin inhibited the proliferation of breast cancer cells, at least partially, through WDR7-7-GPR30 signaling, which may explain why calycosin can exert inhibitory effects on ER- breast cancer. 7,3'-dihydroxy-4'-methoxyisoflavone 56-65 G protein-coupled estrogen receptor 1 Homo sapiens 153-158 29096683-10 2017 CONCLUSIONS: These results suggest the possibility that calycosin inhibited the proliferation of breast cancer cells, at least partially, through WDR7-7-GPR30 signaling, which may explain why calycosin can exert inhibitory effects on ER- breast cancer. 7,3'-dihydroxy-4'-methoxyisoflavone 192-201 G protein-coupled estrogen receptor 1 Homo sapiens 153-158 28882636-8 2017 G-15 reversed the effects of E2 on GPR30 and AKT/mTOR, but did not alter the effect of BPA. G-15 0-4 G protein-coupled estrogen receptor 1 Homo sapiens 35-40 28935720-10 2017 The effect of GPER activation to inhibit SOCE is not affected by combined nonphosphorylatable substitutions at serines 486 and 668 on STIM1, but is substantially reduced by similar substitutions at serines 575, 608 and 621. Serine 198-205 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 28902352-5 2017 To understand the mechanism of TAM-resistance in GPER activated ER+ breast cancer, the function of TRIM2 and Bim inducing cell apoptosis was studied. Tamoxifen 31-34 G protein-coupled estrogen receptor 1 Homo sapiens 49-53 28858478-0 2017 Bisphenol AF and Bisphenol B Exert Higher Estrogenic Effects than Bisphenol A via G Protein-Coupled Estrogen Receptor Pathway. bis(4-hydroxyphenyl)sulfone 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 82-117 28858478-0 2017 Bisphenol AF and Bisphenol B Exert Higher Estrogenic Effects than Bisphenol A via G Protein-Coupled Estrogen Receptor Pathway. bisphenol B 17-28 G protein-coupled estrogen receptor 1 Homo sapiens 82-117 28858478-0 2017 Bisphenol AF and Bisphenol B Exert Higher Estrogenic Effects than Bisphenol A via G Protein-Coupled Estrogen Receptor Pathway. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 82-117 28858478-4 2017 Here, using a SKBR3 cell-based fluorescence competitive binding assay, we found six BPA analogues bound to GPER directly, with bisphenol AF (BPAF) and bisphenol B (BPB) displaying much higher (~9-fold) binding affinity than BPA. bisphenol A 84-87 G protein-coupled estrogen receptor 1 Homo sapiens 107-111 28858478-4 2017 Here, using a SKBR3 cell-based fluorescence competitive binding assay, we found six BPA analogues bound to GPER directly, with bisphenol AF (BPAF) and bisphenol B (BPB) displaying much higher (~9-fold) binding affinity than BPA. 4,4'-hexafluorisopropylidene diphenol 141-145 G protein-coupled estrogen receptor 1 Homo sapiens 107-111 28858478-4 2017 Here, using a SKBR3 cell-based fluorescence competitive binding assay, we found six BPA analogues bound to GPER directly, with bisphenol AF (BPAF) and bisphenol B (BPB) displaying much higher (~9-fold) binding affinity than BPA. bisphenol B 151-162 G protein-coupled estrogen receptor 1 Homo sapiens 107-111 28858478-4 2017 Here, using a SKBR3 cell-based fluorescence competitive binding assay, we found six BPA analogues bound to GPER directly, with bisphenol AF (BPAF) and bisphenol B (BPB) displaying much higher (~9-fold) binding affinity than BPA. bisphenol B 164-167 G protein-coupled estrogen receptor 1 Homo sapiens 107-111 28858478-4 2017 Here, using a SKBR3 cell-based fluorescence competitive binding assay, we found six BPA analogues bound to GPER directly, with bisphenol AF (BPAF) and bisphenol B (BPB) displaying much higher (~9-fold) binding affinity than BPA. bisphenol A 141-144 G protein-coupled estrogen receptor 1 Homo sapiens 107-111 28858478-5 2017 Molecular docking also demonstrated the binding of these BPA analogues to GPER. bisphenol A 57-60 G protein-coupled estrogen receptor 1 Homo sapiens 74-78 28858478-6 2017 By measuring calcium mobilization and cAMP production in SKBR3 cells, we found the binding of these BPA analogues to GPER lead to the activation of subsequent signaling pathways. Calcium 13-20 G protein-coupled estrogen receptor 1 Homo sapiens 117-121 28858478-6 2017 By measuring calcium mobilization and cAMP production in SKBR3 cells, we found the binding of these BPA analogues to GPER lead to the activation of subsequent signaling pathways. Cyclic AMP 38-42 G protein-coupled estrogen receptor 1 Homo sapiens 117-121 28858478-6 2017 By measuring calcium mobilization and cAMP production in SKBR3 cells, we found the binding of these BPA analogues to GPER lead to the activation of subsequent signaling pathways. bisphenol A 100-103 G protein-coupled estrogen receptor 1 Homo sapiens 117-121 28858478-8 2017 Moreover, based on the results of Boyden chamber and wound-healing assays, BPAF and BPB displayed higher activity in promoting GPER mediated SKBR3 cell migration than BPA with the LOEC of 100 nM. 4,4'-hexafluorisopropylidene diphenol 75-79 G protein-coupled estrogen receptor 1 Homo sapiens 127-131 28858478-8 2017 Moreover, based on the results of Boyden chamber and wound-healing assays, BPAF and BPB displayed higher activity in promoting GPER mediated SKBR3 cell migration than BPA with the LOEC of 100 nM. bisphenol B 84-87 G protein-coupled estrogen receptor 1 Homo sapiens 127-131 28858478-8 2017 Moreover, based on the results of Boyden chamber and wound-healing assays, BPAF and BPB displayed higher activity in promoting GPER mediated SKBR3 cell migration than BPA with the LOEC of 100 nM. bisphenol A 75-78 G protein-coupled estrogen receptor 1 Homo sapiens 127-131 28858478-9 2017 Overall, we found two BPA analogues BPAF and BPB could exert higher estrogenic effects than BPA via GPER pathway at nanomolar concentrations. bisphenol A 22-25 G protein-coupled estrogen receptor 1 Homo sapiens 100-104 28858478-9 2017 Overall, we found two BPA analogues BPAF and BPB could exert higher estrogenic effects than BPA via GPER pathway at nanomolar concentrations. 4,4'-hexafluorisopropylidene diphenol 36-40 G protein-coupled estrogen receptor 1 Homo sapiens 100-104 28858478-9 2017 Overall, we found two BPA analogues BPAF and BPB could exert higher estrogenic effects than BPA via GPER pathway at nanomolar concentrations. bisphenol B 45-48 G protein-coupled estrogen receptor 1 Homo sapiens 100-104 28858478-9 2017 Overall, we found two BPA analogues BPAF and BPB could exert higher estrogenic effects than BPA via GPER pathway at nanomolar concentrations. bisphenol A 36-39 G protein-coupled estrogen receptor 1 Homo sapiens 100-104 28902352-0 2017 GPER promotes tamoxifen-resistance in ER+ breast cancer cells by reduced Bim proteins through MAPK/Erk-TRIM2 signaling axis. Tamoxifen 14-23 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 28902352-2 2017 Our previous studies find that GPER and its down-stream signaling play a pivotal role in the development of tamoxifen (TAM) resistance. Tamoxifen 108-117 G protein-coupled estrogen receptor 1 Homo sapiens 31-35 28902352-2 2017 Our previous studies find that GPER and its down-stream signaling play a pivotal role in the development of tamoxifen (TAM) resistance. Tamoxifen 119-122 G protein-coupled estrogen receptor 1 Homo sapiens 31-35 28902352-3 2017 cDNA array analysis indicated a set of genes associated with cell apoptosis are aberrant in GPER activated and TAM-resistant MCF-7R cells compared with TAM-sensitive MCF-7 cells. Tamoxifen 152-155 G protein-coupled estrogen receptor 1 Homo sapiens 92-96 29137421-3 2017 This raises questions about the role of signalling through other estrogen receptors such as ERalpha or G-protein coupled estrogen receptor (GPER, GPR30) by the estrogen 17beta-estradiol (E2) under hypoxic conditions after ERbeta is lost in CRC progression. Estradiol 169-185 G protein-coupled estrogen receptor 1 Homo sapiens 140-144 29137421-3 2017 This raises questions about the role of signalling through other estrogen receptors such as ERalpha or G-protein coupled estrogen receptor (GPER, GPR30) by the estrogen 17beta-estradiol (E2) under hypoxic conditions after ERbeta is lost in CRC progression. Estradiol 169-185 G protein-coupled estrogen receptor 1 Homo sapiens 146-151 29137421-3 2017 This raises questions about the role of signalling through other estrogen receptors such as ERalpha or G-protein coupled estrogen receptor (GPER, GPR30) by the estrogen 17beta-estradiol (E2) under hypoxic conditions after ERbeta is lost in CRC progression. Estradiol 169-185 G protein-coupled estrogen receptor 1 Homo sapiens 103-138 28596490-6 2017 We discovered that interfering with N-linked glycosylation of GPER, either by mutation of the predicted glycosylation sites or pharmacologically with tunicamycin, drives GPER into the nucleus. Nitrogen 36-37 G protein-coupled estrogen receptor 1 Homo sapiens 62-66 28645860-4 2017 MAIN METHODS: Third-order mesenteric arteries were isolated, and concentration-response curves were plotted following the cumulative addition of the selective GPER agonist G-1 (1nM-10muM) following induction of contraction with phenylephrine (3muM). coumarin-3-carboxylic acid 172-175 G protein-coupled estrogen receptor 1 Homo sapiens 159-163 28789417-10 2017 In addition, baicalein significantly inhibited G-1, a specific GPR30 agonist, induced invasion, and reduced G-1 promoted expression and activity of MMP-9, consistent with effects of G15. baicalein 13-22 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 28596490-6 2017 We discovered that interfering with N-linked glycosylation of GPER, either by mutation of the predicted glycosylation sites or pharmacologically with tunicamycin, drives GPER into the nucleus. Nitrogen 36-37 G protein-coupled estrogen receptor 1 Homo sapiens 170-174 28596490-6 2017 We discovered that interfering with N-linked glycosylation of GPER, either by mutation of the predicted glycosylation sites or pharmacologically with tunicamycin, drives GPER into the nucleus. Tunicamycin 150-161 G protein-coupled estrogen receptor 1 Homo sapiens 62-66 28466560-0 2017 Bisphenol A triggers proliferation and migration of laryngeal squamous cell carcinoma via GPER mediated upregulation of IL-6. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 90-94 28596490-6 2017 We discovered that interfering with N-linked glycosylation of GPER, either by mutation of the predicted glycosylation sites or pharmacologically with tunicamycin, drives GPER into the nucleus. Tunicamycin 150-161 G protein-coupled estrogen receptor 1 Homo sapiens 170-174 28450397-2 2017 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. Cyclic AMP 246-250 G protein-coupled estrogen receptor 1 Homo sapiens 24-29 28412354-2 2017 In the present study, we demonstrated that estrogen (17beta-estradiol, or E2)-induced activation of the G protein-coupled receptor 30 (GPR30) triggered Ca2+ release from the endoplasmic reticulum, increased the mitochondrial Ca2+ concentration, and thus induced prostate epithelial cell (PEC) apoptosis. Estradiol 53-69 G protein-coupled estrogen receptor 1 Homo sapiens 104-133 28412354-2 2017 In the present study, we demonstrated that estrogen (17beta-estradiol, or E2)-induced activation of the G protein-coupled receptor 30 (GPR30) triggered Ca2+ release from the endoplasmic reticulum, increased the mitochondrial Ca2+ concentration, and thus induced prostate epithelial cell (PEC) apoptosis. Estradiol 53-69 G protein-coupled estrogen receptor 1 Homo sapiens 135-140 28412354-2 2017 In the present study, we demonstrated that estrogen (17beta-estradiol, or E2)-induced activation of the G protein-coupled receptor 30 (GPR30) triggered Ca2+ release from the endoplasmic reticulum, increased the mitochondrial Ca2+ concentration, and thus induced prostate epithelial cell (PEC) apoptosis. Estradiol 74-76 G protein-coupled estrogen receptor 1 Homo sapiens 104-133 28412354-2 2017 In the present study, we demonstrated that estrogen (17beta-estradiol, or E2)-induced activation of the G protein-coupled receptor 30 (GPR30) triggered Ca2+ release from the endoplasmic reticulum, increased the mitochondrial Ca2+ concentration, and thus induced prostate epithelial cell (PEC) apoptosis. Estradiol 74-76 G protein-coupled estrogen receptor 1 Homo sapiens 135-140 28412354-3 2017 Both E2 and the GPR30-specific agonist G1 induced a transient intracellular Ca2+ 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. Inositol 1,4,5-Trisphosphate 127-156 G protein-coupled estrogen receptor 1 Homo sapiens 16-21 28412354-3 2017 Both E2 and the GPR30-specific agonist G1 induced a transient intracellular Ca2+ 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. Inositol 1,4,5-Trisphosphate 158-161 G protein-coupled estrogen receptor 1 Homo sapiens 16-21 28412354-5 2017 Data generated from the analysis of animal models and human clinical samples indicate that treatment with the GPR30 agonist relieves testosterone propionate (TP)-induced prostatic epithelial hyperplasia, and that the abundance of GPR30 is negatively associated with prostate volume. Testosterone Propionate 133-156 G protein-coupled estrogen receptor 1 Homo sapiens 110-115 28412354-5 2017 Data generated from the analysis of animal models and human clinical samples indicate that treatment with the GPR30 agonist relieves testosterone propionate (TP)-induced prostatic epithelial hyperplasia, and that the abundance of GPR30 is negatively associated with prostate volume. Testosterone Propionate 158-160 G protein-coupled estrogen receptor 1 Homo sapiens 110-115 28466560-9 2017 The increased IL-6 can further activate its downstream signal molecule STAT3, which was evidenced by the results of increased phosphorylation and nuclear translocation of STAT3, while si-IL-6 and si-GPER can both reverse BPA-induced activation of STAT3. bisphenol A 221-224 G protein-coupled estrogen receptor 1 Homo sapiens 199-203 28466560-10 2017 Collectively, our present study revealed that BPA can trigger the progression of LSCC via GPER-mediated upregulation of IL-6. bisphenol A 46-49 G protein-coupled estrogen receptor 1 Homo sapiens 90-94 28476123-6 2017 RESULTS: GPER was significantly (p < 0.01) down regulated in CRC tissues compared with their matched adjacent normal tissues in our two cohorts and three independent investigations from Oncomine database. oncomine 189-197 G protein-coupled estrogen receptor 1 Homo sapiens 9-13 28348059-6 2017 Experiments with the PFKFB3 inhibitor 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one showed that PFKFB3 activity was required for estrogen-mediated HUVEC migration via GPER1. 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one 38-84 G protein-coupled estrogen receptor 1 Homo sapiens 168-173 28286086-7 2017 We analyzed the expression levels of GPER1 mRNA variants in MCF-7 and MDA-MB-231 cells by RT-PCR, and the methylation status of two CpG islands in the GPER1 locus by modified COBRA assays and bisulfite sequencing. hydrogen sulfite 192-201 G protein-coupled estrogen receptor 1 Homo sapiens 151-156 28286086-12 2017 5-Azacytidine, a DNA methyltransferase inhibitor, induced the expression levels of GPER1 mRNA variants in MDA-MB-231 cells. Azacitidine 0-13 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 28440394-13 2017 The expression of GPR30 in endothelial cells was significantly increased following treatment with 17-beta-estradiol under H/R conditions. Estradiol 98-115 G protein-coupled estrogen receptor 1 Homo sapiens 18-23 27721408-6 2017 Moreover, the clinical data from 18F-fluorodeoxyglucose positron emission tomography/computed tomography further present a strong association between the GPER/cAMP/PKA/CREB pathway of stromal fibroblasts with tumor metabolic activity and clinical treatment, suggesting that targeting cytoplasmic GPER in CAFs may rescue the drug sensitivity in patients with breast cancer. Fluorodeoxyglucose F18 33-55 G protein-coupled estrogen receptor 1 Homo sapiens 154-158 27837347-5 2017 Both TAM and estradiol (E2) could promote the migration of triple negative (ER-alpha66-/PR-/HER2-) and ER-alpha36+/GPER1+ breast cancer cells MDA-MB-231. Tamoxifen 5-8 G protein-coupled estrogen receptor 1 Homo sapiens 115-120 27837347-5 2017 Both TAM and estradiol (E2) could promote the migration of triple negative (ER-alpha66-/PR-/HER2-) and ER-alpha36+/GPER1+ breast cancer cells MDA-MB-231. Estradiol 13-22 G protein-coupled estrogen receptor 1 Homo sapiens 115-120 28096479-2 2017 We recently demonstrated that G protein-coupled estrogen receptor 1 (GPER1) mediates tamoxifen action in breast cancer cells by inducing insulin-like growth factor-binding protein-1 (IGFBP-1) to inhibit IGF-1-dependent signaling. Tamoxifen 85-94 G protein-coupled estrogen receptor 1 Homo sapiens 30-67 28096479-2 2017 We recently demonstrated that G protein-coupled estrogen receptor 1 (GPER1) mediates tamoxifen action in breast cancer cells by inducing insulin-like growth factor-binding protein-1 (IGFBP-1) to inhibit IGF-1-dependent signaling. Tamoxifen 85-94 G protein-coupled estrogen receptor 1 Homo sapiens 69-74 27721408-0 2017 Cytoplasmic GPER translocation in cancer-associated fibroblasts mediates cAMP/PKA/CREB/glycolytic axis to confer tumor cells with multidrug resistance. Cyclic AMP 73-77 G protein-coupled estrogen receptor 1 Homo sapiens 12-16 27721408-4 2017 Here we first show that the breast tumor cell-activated PI3K/AKT (phosphoinositide 3-kinase/AKT) signaling pathway induces the cytoplasmic GPER translocation of CAFs in a CRM1-dependent pattern, and leads to the activation of a novel estrogen/GPER/cAMP/PKA/CREB signaling axis that triggers the aerobic glycolysis switch in CAFs. Cyclic AMP 248-252 G protein-coupled estrogen receptor 1 Homo sapiens 139-143 27401115-3 2017 MATERIALS AND METHODS: The phosphorylation or expression levels of ERK1/2, Akt, c-Fos and eNOS were evaluated to assess GPR30 activation in response to known agonists (17beta-estradiol and G-1) in MCF-7 and T-47D breast cancer cell lines and in bovine aortic endothelial cells. Estradiol 168-184 G protein-coupled estrogen receptor 1 Homo sapiens 120-125 27721408-6 2017 Moreover, the clinical data from 18F-fluorodeoxyglucose positron emission tomography/computed tomography further present a strong association between the GPER/cAMP/PKA/CREB pathway of stromal fibroblasts with tumor metabolic activity and clinical treatment, suggesting that targeting cytoplasmic GPER in CAFs may rescue the drug sensitivity in patients with breast cancer. Fluorodeoxyglucose F18 33-55 G protein-coupled estrogen receptor 1 Homo sapiens 296-300 27721408-4 2017 Here we first show that the breast tumor cell-activated PI3K/AKT (phosphoinositide 3-kinase/AKT) signaling pathway induces the cytoplasmic GPER translocation of CAFs in a CRM1-dependent pattern, and leads to the activation of a novel estrogen/GPER/cAMP/PKA/CREB signaling axis that triggers the aerobic glycolysis switch in CAFs. Cyclic AMP 248-252 G protein-coupled estrogen receptor 1 Homo sapiens 243-247 27721408-6 2017 Moreover, the clinical data from 18F-fluorodeoxyglucose positron emission tomography/computed tomography further present a strong association between the GPER/cAMP/PKA/CREB pathway of stromal fibroblasts with tumor metabolic activity and clinical treatment, suggesting that targeting cytoplasmic GPER in CAFs may rescue the drug sensitivity in patients with breast cancer. Cyclic AMP 159-163 G protein-coupled estrogen receptor 1 Homo sapiens 154-158 27721408-6 2017 Moreover, the clinical data from 18F-fluorodeoxyglucose positron emission tomography/computed tomography further present a strong association between the GPER/cAMP/PKA/CREB pathway of stromal fibroblasts with tumor metabolic activity and clinical treatment, suggesting that targeting cytoplasmic GPER in CAFs may rescue the drug sensitivity in patients with breast cancer. Cyclic AMP 159-163 G protein-coupled estrogen receptor 1 Homo sapiens 296-300 27814026-0 2017 GPER (GPR30): A Nongenomic Receptor (GPCR) for Steroid Hormones with Implications for Cardiovascular Disease and Cancer. Steroids 47-63 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 28098854-3 2017 In this study, we demonstrate that beta-estradiol (E2) treatment increased LSD1 expression via the GPR30/PI3K/AKT pathway in endometrial cancer cells. Estradiol 35-49 G protein-coupled estrogen receptor 1 Homo sapiens 99-104 27880919-1 2017 Many studies have been shown that environmental estrogen bisphenol A (BPA) can activate nuclear receptor (estrogen receptor alpha, ERalpha) or membrane receptor (G-protein-coupled receptor, GPR30) in breast cancer cells and exerts genomic or nongenomic actions inducing cell proliferation. bisphenol A 57-68 G protein-coupled estrogen receptor 1 Homo sapiens 190-195 27880919-1 2017 Many studies have been shown that environmental estrogen bisphenol A (BPA) can activate nuclear receptor (estrogen receptor alpha, ERalpha) or membrane receptor (G-protein-coupled receptor, GPR30) in breast cancer cells and exerts genomic or nongenomic actions inducing cell proliferation. bisphenol A 70-73 G protein-coupled estrogen receptor 1 Homo sapiens 190-195 27341075-3 2017 In the present study, we demonstrate that zinc chloride (ZnCl2 ) involves GPER in the activation of insulin-like growth factor receptor I (IGF-IR)/epidermal growth factor receptor (EGFR)-mediated signaling, which in turn triggers downstream pathways like ERK and AKT in breast cancer cells, and main components of the tumor microenvironment namely cancer-associated fibroblasts (CAFs). zinc chloride 42-55 G protein-coupled estrogen receptor 1 Homo sapiens 74-78 27341075-3 2017 In the present study, we demonstrate that zinc chloride (ZnCl2 ) involves GPER in the activation of insulin-like growth factor receptor I (IGF-IR)/epidermal growth factor receptor (EGFR)-mediated signaling, which in turn triggers downstream pathways like ERK and AKT in breast cancer cells, and main components of the tumor microenvironment namely cancer-associated fibroblasts (CAFs). zinc chloride 57-62 G protein-coupled estrogen receptor 1 Homo sapiens 74-78 27341075-4 2017 Further corroborating these findings, ZnCl2 stimulates a functional crosstalk of GPER with IGF-IR and EGFR toward the transcription of diverse GPER target genes. zinc chloride 38-43 G protein-coupled estrogen receptor 1 Homo sapiens 81-85 27341075-4 2017 Further corroborating these findings, ZnCl2 stimulates a functional crosstalk of GPER with IGF-IR and EGFR toward the transcription of diverse GPER target genes. zinc chloride 38-43 G protein-coupled estrogen receptor 1 Homo sapiens 143-147 27341075-5 2017 Then, we show that GPER contributes to the stimulatory effects induced by ZnCl2 on cell-cycle progression, proliferation, and migration of breast cancer cells as well as migration of CAFs. zinc chloride 74-79 G protein-coupled estrogen receptor 1 Homo sapiens 19-23 27959426-0 2017 17beta-estradiol-induced growth of triple-negative breast cancer cells is prevented by the reduction of GPER expression after treatment with gefitinib. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 104-108 27959426-0 2017 17beta-estradiol-induced growth of triple-negative breast cancer cells is prevented by the reduction of GPER expression after treatment with gefitinib. Gefitinib 141-150 G protein-coupled estrogen receptor 1 Homo sapiens 104-108 27959426-3 2017 To a certain extent the growth of TNBCs is stimulated by 17beta-estradiol via GPER. Estradiol 57-73 G protein-coupled estrogen receptor 1 Homo sapiens 78-82 27959426-4 2017 We analyzed whether inhibition of EGFR by gefitinib reduces the expression of GPER and subsequent signal transduction in TNBC cells. Gefitinib 42-51 G protein-coupled estrogen receptor 1 Homo sapiens 78-82 27959426-6 2017 Expression of GPR30 and activation of c-src, EGFR and cAMP-responsive element binding (CREB) protein by 17beta-estradiol was analyzed by western blotting. Estradiol 104-120 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 27959426-8 2017 Gefitinib reduced GPER expression concentration- and time-dependently. Gefitinib 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 18-22 27959426-9 2017 In HCC70 cells, GPER expression was reduced to 15+-11% (p<0.05) after treatment with 200 nM gefitinib for four days, and in HCC1806 cells GPER expression was reduced to 39+-5% (p<0.01) of the control. Gefitinib 95-104 G protein-coupled estrogen receptor 1 Homo sapiens 16-20 27959426-9 2017 In HCC70 cells, GPER expression was reduced to 15+-11% (p<0.05) after treatment with 200 nM gefitinib for four days, and in HCC1806 cells GPER expression was reduced to 39+-5% (p<0.01) of the control. Gefitinib 95-104 G protein-coupled estrogen receptor 1 Homo sapiens 141-145 27959426-11 2017 This increase in cell growth was completely prevented in both TNBC cell lines after GPR30 expression was downregulated by treatment with 200 nM gefitinib. Gefitinib 144-153 G protein-coupled estrogen receptor 1 Homo sapiens 84-89 28278256-1 2017 Previously, we reported that cAMP/PKA signaling is involved in GPER-mediated coronary relaxation by activating MLCP via inhibition of RhoA pathway. Cyclic AMP 29-33 G protein-coupled estrogen receptor 1 Homo sapiens 63-67 28278256-2 2017 In the current study, we tested the hypothesis that activation of GPER induces coronary artery relaxation via inhibition of RhoA/Rho kinase pathway by cAMP downstream targets, exchange proteins directly activated by cAMP (Epac) as well as PKA. Cyclic AMP 151-155 G protein-coupled estrogen receptor 1 Homo sapiens 66-70 28278256-2 2017 In the current study, we tested the hypothesis that activation of GPER induces coronary artery relaxation via inhibition of RhoA/Rho kinase pathway by cAMP downstream targets, exchange proteins directly activated by cAMP (Epac) as well as PKA. Cyclic AMP 216-220 G protein-coupled estrogen receptor 1 Homo sapiens 66-70 28278256-3 2017 Our results show that Epac inhibitors, brefeldin A (BFA, 50 muM), or ESI-09 (20 muM), or CE3F4 (100 muM), all partially inhibited porcine coronary artery relaxation response to the selective GPER agonist, G-1 (0.3-3 muM); while concurrent administration of BFA and PKI (5 muM), a PKA inhibitor, almost completely blocked the relaxation effect of G-1. 3-(5-tert-butylisoxazol-3-yl)-2-((3-chlorophenyl)hydrazono)-3-oxopropionitrile 69-75 G protein-coupled estrogen receptor 1 Homo sapiens 191-195 28326039-11 2017 Furthermore, tamoxifen and fulvestrant, known GPER agonist, also increased CRC STS activity, with this effect inhibited by the GPER antagonist G15. Tamoxifen 13-22 G protein-coupled estrogen receptor 1 Homo sapiens 46-50 28326039-11 2017 Furthermore, tamoxifen and fulvestrant, known GPER agonist, also increased CRC STS activity, with this effect inhibited by the GPER antagonist G15. Tamoxifen 13-22 G protein-coupled estrogen receptor 1 Homo sapiens 127-131 28326039-11 2017 Furthermore, tamoxifen and fulvestrant, known GPER agonist, also increased CRC STS activity, with this effect inhibited by the GPER antagonist G15. Fulvestrant 27-38 G protein-coupled estrogen receptor 1 Homo sapiens 46-50 28326039-11 2017 Furthermore, tamoxifen and fulvestrant, known GPER agonist, also increased CRC STS activity, with this effect inhibited by the GPER antagonist G15. Fulvestrant 27-38 G protein-coupled estrogen receptor 1 Homo sapiens 127-131 27940299-0 2017 GPER/ERK&AKT/NF-kappaB pathway is involved in cadmium-induced proliferation, invasion and migration of GPER-positive thyroid cancer cells. Cadmium 50-57 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 27940299-0 2017 GPER/ERK&AKT/NF-kappaB pathway is involved in cadmium-induced proliferation, invasion and migration of GPER-positive thyroid cancer cells. Cadmium 50-57 G protein-coupled estrogen receptor 1 Homo sapiens 107-111 27940299-3 2017 In the present study, we demonstrate that similar to E2 and G1, a specific agonist for G protein-coupled estrogen receptor (GPER), Cd induces the proliferation, invasion and migration of human WRO and FRO thyroid cancer cells that have endogenous GPER. Cadmium 131-133 G protein-coupled estrogen receptor 1 Homo sapiens 87-122 27940299-3 2017 In the present study, we demonstrate that similar to E2 and G1, a specific agonist for G protein-coupled estrogen receptor (GPER), Cd induces the proliferation, invasion and migration of human WRO and FRO thyroid cancer cells that have endogenous GPER. Cadmium 131-133 G protein-coupled estrogen receptor 1 Homo sapiens 124-128 27940299-3 2017 In the present study, we demonstrate that similar to E2 and G1, a specific agonist for G protein-coupled estrogen receptor (GPER), Cd induces the proliferation, invasion and migration of human WRO and FRO thyroid cancer cells that have endogenous GPER. Cadmium 131-133 G protein-coupled estrogen receptor 1 Homo sapiens 247-251 27940299-4 2017 Moreover, like E2 and G1, Cd leads to a rapid activation of ERK/AKT, and then nuclear translocation of NF-kappaB, increased expression of cyclin A and D1, and secretion of IL-8, all of which are significantly attenuated by GPER blockage or knock-down in both WRO and FRO cells. Cadmium 26-28 G protein-coupled estrogen receptor 1 Homo sapiens 223-227 27940299-5 2017 Furthermore, the Cd-induced proliferation, invasion and migration are suppressed either by specific inhibitors for GPER, ERK, AKT and NF-kappaB, or by knock-down of GPER. Cadmium 17-19 G protein-coupled estrogen receptor 1 Homo sapiens 115-119 27940299-5 2017 Furthermore, the Cd-induced proliferation, invasion and migration are suppressed either by specific inhibitors for GPER, ERK, AKT and NF-kappaB, or by knock-down of GPER. Cadmium 17-19 G protein-coupled estrogen receptor 1 Homo sapiens 165-169 27940299-6 2017 These results suggest that GPER/ERK&AKT/NF-kappaB signaling pathway is involved in the Cd-induced proliferation, invasion and migration of GPER-positive thyroid cancer cells. Cadmium 91-93 G protein-coupled estrogen receptor 1 Homo sapiens 27-31 27940299-6 2017 These results suggest that GPER/ERK&AKT/NF-kappaB signaling pathway is involved in the Cd-induced proliferation, invasion and migration of GPER-positive thyroid cancer cells. Cadmium 91-93 G protein-coupled estrogen receptor 1 Homo sapiens 143-147 27796870-0 2017 GPR30 Activation Contributes to the Puerarin-Mediated Neuroprotection in MPP+-Induced SH-SY5Y Cell Death. puerarin 36-44 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 27796870-4 2017 In this study, we investigated whether puerarin prevented against 1-methyl-4-phenylpyridinium (MPP+)-induced cell death via GPR30. puerarin 39-47 G protein-coupled estrogen receptor 1 Homo sapiens 124-129 27796870-5 2017 Our results showed that the GPR30 agonist, G1, exhibited puerarin-mediated neuroprotection against MPP+-induced cell death of SH-SY5Y cells. puerarin 57-65 G protein-coupled estrogen receptor 1 Homo sapiens 28-33 27796870-5 2017 Our results showed that the GPR30 agonist, G1, exhibited puerarin-mediated neuroprotection against MPP+-induced cell death of SH-SY5Y cells. mangion-purified polysaccharide (Candida albicans) 99-103 G protein-coupled estrogen receptor 1 Homo sapiens 28-33 27796870-7 2017 Moreover, a time- and concentration-dependent effect of puerarin on GPR30 expression was verified at the protein level but not at the mRNA level. puerarin 56-64 G protein-coupled estrogen receptor 1 Homo sapiens 68-73 27796870-8 2017 Further, we showed that an mTor-dependent new GPR30 synthesis contributed to the protection conferred by puerarin. puerarin 105-113 G protein-coupled estrogen receptor 1 Homo sapiens 46-51 27796870-10 2017 Taken together, our data strongly suggest that puerarin prevents MPP+-induced cell death via facilitating GPR30 expression and GDNF release. puerarin 47-55 G protein-coupled estrogen receptor 1 Homo sapiens 106-111 27796870-10 2017 Taken together, our data strongly suggest that puerarin prevents MPP+-induced cell death via facilitating GPR30 expression and GDNF release. mangion-purified polysaccharide (Candida albicans) 65-69 G protein-coupled estrogen receptor 1 Homo sapiens 106-111 27760898-7 2017 However, blockade of Gper1 by its antagonist G-15 did not affect the inhibitory action of E2 on IGF-1-induced proliferation. G-15 45-49 G protein-coupled estrogen receptor 1 Homo sapiens 21-26 31988900-9 2017 Results: Human neutrophils express a functional GPER1 which regulates their functions through cAMP/protein kinase A/cAMP response element-binding protein, p38 mitogen-activated protein kinase, and extracellular regulated MAPK signaling pathways. Cyclic AMP 94-98 G protein-coupled estrogen receptor 1 Homo sapiens 48-53 31988900-9 2017 Results: Human neutrophils express a functional GPER1 which regulates their functions through cAMP/protein kinase A/cAMP response element-binding protein, p38 mitogen-activated protein kinase, and extracellular regulated MAPK signaling pathways. Cyclic AMP 116-120 G protein-coupled estrogen receptor 1 Homo sapiens 48-53 27814026-0 2017 GPER (GPR30): A Nongenomic Receptor (GPCR) for Steroid Hormones with Implications for Cardiovascular Disease and Cancer. Steroids 47-63 G protein-coupled estrogen receptor 1 Homo sapiens 6-11 27814026-1 2017 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. Steroids 30-38 G protein-coupled estrogen receptor 1 Homo sapiens 237-264 27814026-1 2017 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. Steroids 30-38 G protein-coupled estrogen receptor 1 Homo sapiens 266-270 27814026-1 2017 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. Steroids 30-38 G protein-coupled estrogen receptor 1 Homo sapiens 392-396 27814026-5 2017 This review provides a summary of relevant findings of the impact of GPER regulation by either estradiol or aldosterone in in vitro model systems and extends those findings to in vivo studies of direct clinical relevance for development of GPER-directed agents for treatment of cancer and cardiovascular diseases associated with cellular proliferation. Estradiol 95-104 G protein-coupled estrogen receptor 1 Homo sapiens 69-73 27814026-5 2017 This review provides a summary of relevant findings of the impact of GPER regulation by either estradiol or aldosterone in in vitro model systems and extends those findings to in vivo studies of direct clinical relevance for development of GPER-directed agents for treatment of cancer and cardiovascular diseases associated with cellular proliferation. Aldosterone 108-119 G protein-coupled estrogen receptor 1 Homo sapiens 69-73 29059676-12 2017 AR activation triggered by DHT suppressed GPER expression, to promote cell growth of TNBC. Dihydrotestosterone 27-30 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 29224098-7 2017 In humans, 17beta-estradiol (E2) is the predominant circulating estrogen and signals through estrogen receptor alpha (ERalpha), estrogen receptor beta (ERbeta), and G-protein-coupled estrogen receptor (GPER). Estradiol 11-27 G protein-coupled estrogen receptor 1 Homo sapiens 165-200 29224098-7 2017 In humans, 17beta-estradiol (E2) is the predominant circulating estrogen and signals through estrogen receptor alpha (ERalpha), estrogen receptor beta (ERbeta), and G-protein-coupled estrogen receptor (GPER). Estradiol 11-27 G protein-coupled estrogen receptor 1 Homo sapiens 202-206 28662498-8 2017 ERs and GPER blockers were able to prevent the effects of 17beta-estradiol and genistein. Estradiol 58-74 G protein-coupled estrogen receptor 1 Homo sapiens 8-12 28662498-8 2017 ERs and GPER blockers were able to prevent the effects of 17beta-estradiol and genistein. Genistein 79-88 G protein-coupled estrogen receptor 1 Homo sapiens 8-12 29059676-13 2017 G-1, a GPER agonist, inhibited DHT-stimulated proliferation. Dihydrotestosterone 31-34 G protein-coupled estrogen receptor 1 Homo sapiens 7-11 27378491-5 2017 Estradiol-induced melanin synthesis and the activation of related signaling pathways were suppressed by inhibiting GPER via antagonist treatment. Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 115-119 28662498-9 2017 CONCLUSION: In Huh7.5 and LX-2, 17beta-estradiol and genistein counteract the effects of peroxidation through the involvement of ERs and GPER and by an intracellular signalling related to Akt and p38MAPK. Estradiol 32-48 G protein-coupled estrogen receptor 1 Homo sapiens 137-141 28662498-9 2017 CONCLUSION: In Huh7.5 and LX-2, 17beta-estradiol and genistein counteract the effects of peroxidation through the involvement of ERs and GPER and by an intracellular signalling related to Akt and p38MAPK. Genistein 53-62 G protein-coupled estrogen receptor 1 Homo sapiens 137-141 27942913-5 2017 Recently, G protein-coupled estrogen receptor-1 (GPER-1) was elegantly shown to mediate some aldosterone-induced rapid effects in several tissues, a fact that strongly places GPER-1 as the unknown receptor. Aldosterone 93-104 G protein-coupled estrogen receptor 1 Homo sapiens 10-47 27942913-5 2017 Recently, G protein-coupled estrogen receptor-1 (GPER-1) was elegantly shown to mediate some aldosterone-induced rapid effects in several tissues, a fact that strongly places GPER-1 as the unknown receptor. Aldosterone 93-104 G protein-coupled estrogen receptor 1 Homo sapiens 49-55 27942913-5 2017 Recently, G protein-coupled estrogen receptor-1 (GPER-1) was elegantly shown to mediate some aldosterone-induced rapid effects in several tissues, a fact that strongly places GPER-1 as the unknown receptor. Aldosterone 93-104 G protein-coupled estrogen receptor 1 Homo sapiens 175-181 27378491-5 2017 Estradiol-induced melanin synthesis and the activation of related signaling pathways were suppressed by inhibiting GPER via antagonist treatment. Melanins 18-25 G protein-coupled estrogen receptor 1 Homo sapiens 115-119 27369115-6 2017 Combined 5nM treatments with specific estrogen and progesterone receptor agonists showed an involvement of membrane progesterone receptor alpha (mPRalpha, also known as PAQR7), G protein-coupled estrogen receptor 1 (GPER), and estrogen receptor alpha (ERalpha), but not ERbeta, in P4+E2 stimulation of NO production. 3-[[5-Bromanyl-1-(3-Methylsulfonylpropyl)benzimidazol-2-Yl]methyl]-1-Cyclopropyl-Imidazo[4,5-C]pyridin-2-One 9-12 G protein-coupled estrogen receptor 1 Homo sapiens 177-214 27369115-6 2017 Combined 5nM treatments with specific estrogen and progesterone receptor agonists showed an involvement of membrane progesterone receptor alpha (mPRalpha, also known as PAQR7), G protein-coupled estrogen receptor 1 (GPER), and estrogen receptor alpha (ERalpha), but not ERbeta, in P4+E2 stimulation of NO production. 3-[[5-Bromanyl-1-(3-Methylsulfonylpropyl)benzimidazol-2-Yl]methyl]-1-Cyclopropyl-Imidazo[4,5-C]pyridin-2-One 9-12 G protein-coupled estrogen receptor 1 Homo sapiens 216-220 27378491-8 2017 GPER activated melanin production via the cAMP-protein kinase (PK) A pathway, suggesting that GPER plays an important role in estrogen-induced melanin synthesis. Melanins 15-22 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 27378491-8 2017 GPER activated melanin production via the cAMP-protein kinase (PK) A pathway, suggesting that GPER plays an important role in estrogen-induced melanin synthesis. Melanins 15-22 G protein-coupled estrogen receptor 1 Homo sapiens 94-98 27378491-8 2017 GPER activated melanin production via the cAMP-protein kinase (PK) A pathway, suggesting that GPER plays an important role in estrogen-induced melanin synthesis. Melanins 143-150 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 27378491-8 2017 GPER activated melanin production via the cAMP-protein kinase (PK) A pathway, suggesting that GPER plays an important role in estrogen-induced melanin synthesis. Melanins 143-150 G protein-coupled estrogen receptor 1 Homo sapiens 94-98 27378491-9 2017 The effect of GPER activation on cAMP-MITF-TYR signaling was also demonstrated in B16 cells. Cyclic AMP 33-37 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 27378491-11 2017 CONCLUSION: GPER enhances melanin synthesis via cAMP-PKA-MITF-TYR signaling and modulates the effects of estrogen in melanogenesis. Melanins 26-33 G protein-coupled estrogen receptor 1 Homo sapiens 12-16 27378491-11 2017 CONCLUSION: GPER enhances melanin synthesis via cAMP-PKA-MITF-TYR signaling and modulates the effects of estrogen in melanogenesis. Cyclic AMP 48-52 G protein-coupled estrogen receptor 1 Homo sapiens 12-16 27822058-6 2016 Interestingly, higher expression of GPER1 was associated with poorer DFS in HER2-positive subtype of breast cancer (P=0.047) but with better DMFS (P=0.040) and DFS (P=0.035) in HER2-negative subtype of breast cancer. dmfs 141-145 G protein-coupled estrogen receptor 1 Homo sapiens 36-41 27222231-0 2017 PI3K/Akt Activated by GPR30 and Src Regulates 17beta-Estradiol-Induced Cultured Immature Boar Sertoli Cells Proliferation. Estradiol 46-62 G protein-coupled estrogen receptor 1 Homo sapiens 22-27 27222231-7 2017 Both G-15 (an antagonist of GPR30, 0.1 mumol/L) and PP2 (an inhibitor of Src, 2.0 mumol/L) inhibited 17beta-estradiol-induced activation of PI3K, reduced SC proliferation, and decreased messenger RNA (mRNA) and protein expression of S-phase kinase-associated protein 2 (Skp2). G-15 5-9 G protein-coupled estrogen receptor 1 Homo sapiens 28-33 27222231-7 2017 Both G-15 (an antagonist of GPR30, 0.1 mumol/L) and PP2 (an inhibitor of Src, 2.0 mumol/L) inhibited 17beta-estradiol-induced activation of PI3K, reduced SC proliferation, and decreased messenger RNA (mRNA) and protein expression of S-phase kinase-associated protein 2 (Skp2). Estradiol 101-117 G protein-coupled estrogen receptor 1 Homo sapiens 28-33 27519631-0 2016 Tamoxifen has a proliferative effect in endometrial carcinoma mediated via the GPER/EGFR/ERK/cyclin D1 pathway: A retrospective study and an in vitro study. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 79-83 27519631-5 2016 In vitro 4-hydroxytamoxifen (OHT) induced cell proliferation and cell cycle promotion in type I and type II endometrial cancer cell lines, and this proliferation was blocked by GPER silencing. hydroxytamoxifen 9-27 G protein-coupled estrogen receptor 1 Homo sapiens 177-181 27519631-5 2016 In vitro 4-hydroxytamoxifen (OHT) induced cell proliferation and cell cycle promotion in type I and type II endometrial cancer cell lines, and this proliferation was blocked by GPER silencing. Tamoxifen 29-32 G protein-coupled estrogen receptor 1 Homo sapiens 177-181 27849354-0 2016 The treatment effects of flaxseed-derived secoisolariciresinol diglycoside and its metabolite enterolactone on benign prostatic hyperplasia involve the G protein-coupled estrogen receptor 1. flaxseed-derived secoisolariciresinol diglycoside 25-74 G protein-coupled estrogen receptor 1 Homo sapiens 152-189 27849354-0 2016 The treatment effects of flaxseed-derived secoisolariciresinol diglycoside and its metabolite enterolactone on benign prostatic hyperplasia involve the G protein-coupled estrogen receptor 1. 2,3-bis(3'-hydroxybenzyl)butyrolactone 94-107 G protein-coupled estrogen receptor 1 Homo sapiens 152-189 27849354-3 2016 The present study showed that enterolactone (ENL), the mammalian metabolite of SDG, shared the similar binding site of G1 on a new type of membranous estrogen receptor, G-protein-coupled estrogen eceptor 1 (GPER), by docking simulations method. 2,3-bis(3'-hydroxybenzyl)butyrolactone 30-43 G protein-coupled estrogen receptor 1 Homo sapiens 169-205 27849354-3 2016 The present study showed that enterolactone (ENL), the mammalian metabolite of SDG, shared the similar binding site of G1 on a new type of membranous estrogen receptor, G-protein-coupled estrogen eceptor 1 (GPER), by docking simulations method. 2,3-bis(3'-hydroxybenzyl)butyrolactone 30-43 G protein-coupled estrogen receptor 1 Homo sapiens 207-211 27849354-4 2016 ENL and G1 (the specific agonist of GPER) inhibited the proliferation of human prostate stromal cell line WPMY-1 as shown by MTT assay and arrested cell cycle at the G0/G1 phase, which was displayed by propidium iodide staining following flow cytometer examination. monooxyethylene trimethylolpropane tristearate 125-128 G protein-coupled estrogen receptor 1 Homo sapiens 36-40 27849354-4 2016 ENL and G1 (the specific agonist of GPER) inhibited the proliferation of human prostate stromal cell line WPMY-1 as shown by MTT assay and arrested cell cycle at the G0/G1 phase, which was displayed by propidium iodide staining following flow cytometer examination. Propidium 202-218 G protein-coupled estrogen receptor 1 Homo sapiens 36-40 27849354-8 2016 Mechanistic studies showed that SDG and ENL increased the expression of GPER both in vitro and in vivo. secoisolariciresinol diglucoside 32-35 G protein-coupled estrogen receptor 1 Homo sapiens 72-76 27222231-12 2017 Both GPR30 and Src are involved in 17beta-estradiol-induced phosphorylation of PI3K/Akt. Estradiol 35-51 G protein-coupled estrogen receptor 1 Homo sapiens 5-10 27448983-1 2016 G protein-coupled estrogen receptor (GPER) plays an important role in mediating the effects of estradiol. Estradiol 95-104 G protein-coupled estrogen receptor 1 Homo sapiens 0-35 27745655-7 2016 BPA had no effects on either cellular distribution or protein expression of ERalpha, however, at 100mumol/L (or 23mumol/L intracellular BPA) increased ERbeta protein levels in the cytoplasmic fractions and GPR30 protein levels in the nuclear fractions. bisphenol A 136-139 G protein-coupled estrogen receptor 1 Homo sapiens 206-211 27448983-1 2016 G protein-coupled estrogen receptor (GPER) plays an important role in mediating the effects of estradiol. Estradiol 95-104 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 27448983-9 2016 However, gene set enrichment analysis (GSEA) showed that GPER signaling is ultra-activated in ER-positive IBC when compared with normal and its activation is positively associated with NHERF1 mRNA levels. gsea 39-43 G protein-coupled estrogen receptor 1 Homo sapiens 57-61 27271044-4 2016 Stimulation of HBE or 16HBE14o- cells with E2 or G1, a specific agonist of GPER, attenuated the nucleotide-evoked increases in [Ca(2+)]i, whereas this effect was reversed by G15, a GPER-specific antagonist. 16hbe14o 22-30 G protein-coupled estrogen receptor 1 Homo sapiens 75-79 27480627-6 2016 Both estrogen receptor alpha (ERalpha) and G protein-coupled estrogen receptor (GPER) were expressed in HA cells; furthermore, BPA treatment can increase the expression of both ERalpha and GPER. bisphenol A 127-130 G protein-coupled estrogen receptor 1 Homo sapiens 43-78 27480627-6 2016 Both estrogen receptor alpha (ERalpha) and G protein-coupled estrogen receptor (GPER) were expressed in HA cells; furthermore, BPA treatment can increase the expression of both ERalpha and GPER. bisphenol A 127-130 G protein-coupled estrogen receptor 1 Homo sapiens 80-84 27480627-6 2016 Both estrogen receptor alpha (ERalpha) and G protein-coupled estrogen receptor (GPER) were expressed in HA cells; furthermore, BPA treatment can increase the expression of both ERalpha and GPER. bisphenol A 127-130 G protein-coupled estrogen receptor 1 Homo sapiens 189-193 27271044-8 2016 These results demonstrated that the inhibitory effects of G1 or E2 on P2Y receptor-mediated Ca(2+) mobilization and cytokine secretion were due to GPER-mediated activation of a cAMP-dependent PKA pathway. Cyclic AMP 177-181 G protein-coupled estrogen receptor 1 Homo sapiens 147-151 27113328-0 2016 GPER1 mediates estrogen-induced neuroprotection against oxygen-glucose deprivation in the primary hippocampal neurons. oxygen-glucose 56-70 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 27113328-3 2016 Here our studies on primary hippocampal neurons have focused on GPER1 in an in vitro model of ischemia using oxygen-glucose deprivation (OGD). oxygen-glucose 109-123 G protein-coupled estrogen receptor 1 Homo sapiens 64-69 27107933-6 2016 Furthermore, used in various treatment regimens anti-estrogens such as tamoxifen, raloxifen and fulvestrant (ICI 182.780), antagonists/modulators of canonical estrogen receptors, were found to be GPER agonists. Tamoxifen 71-80 G protein-coupled estrogen receptor 1 Homo sapiens 196-200 27107933-6 2016 Furthermore, used in various treatment regimens anti-estrogens such as tamoxifen, raloxifen and fulvestrant (ICI 182.780), antagonists/modulators of canonical estrogen receptors, were found to be GPER agonists. Fulvestrant 96-107 G protein-coupled estrogen receptor 1 Homo sapiens 196-200 27107933-6 2016 Furthermore, used in various treatment regimens anti-estrogens such as tamoxifen, raloxifen and fulvestrant (ICI 182.780), antagonists/modulators of canonical estrogen receptors, were found to be GPER agonists. Raloxifen 82-91 G protein-coupled estrogen receptor 1 Homo sapiens 196-200 26921679-4 2016 Many of currently used drugs such as tamoxifen, raloxifene, or faslodex /fulvestrant were discovered targeting GPER many years after they had been introduced to the clinics for entirely different purposes. Tamoxifen 37-46 G protein-coupled estrogen receptor 1 Homo sapiens 111-115 27189345-4 2016 Ligand-induced mER and GPER signalling events are shared with BCR, CD19 mediated intracellular signalling through phospholipase C, PIP2/IP3/PI3 mediated activation of Akt, MAP kinase, and mTOR. Phosphatidylinositol 4,5-Diphosphate 131-135 G protein-coupled estrogen receptor 1 Homo sapiens 23-27 27197110-4 2016 Three ER, ER-alpha, ER-beta and the G protein-coupled ER (GPER; also called GPR30) in tissues are involved in glucose and lipid homeostasis. Glucose 110-117 G protein-coupled estrogen receptor 1 Homo sapiens 36-56 27197110-4 2016 Three ER, ER-alpha, ER-beta and the G protein-coupled ER (GPER; also called GPR30) in tissues are involved in glucose and lipid homeostasis. Glucose 110-117 G protein-coupled estrogen receptor 1 Homo sapiens 58-62 27197110-4 2016 Three ER, ER-alpha, ER-beta and the G protein-coupled ER (GPER; also called GPR30) in tissues are involved in glucose and lipid homeostasis. Glucose 110-117 G protein-coupled estrogen receptor 1 Homo sapiens 76-81 26921679-4 2016 Many of currently used drugs such as tamoxifen, raloxifene, or faslodex /fulvestrant were discovered targeting GPER many years after they had been introduced to the clinics for entirely different purposes. Raloxifene Hydrochloride 48-58 G protein-coupled estrogen receptor 1 Homo sapiens 111-115 26921679-4 2016 Many of currently used drugs such as tamoxifen, raloxifene, or faslodex /fulvestrant were discovered targeting GPER many years after they had been introduced to the clinics for entirely different purposes. Fulvestrant 63-71 G protein-coupled estrogen receptor 1 Homo sapiens 111-115 27071941-6 2016 Inhibitor studies suggest that rapid MAPK phosphorylation by NaAsO2, CdCl2, and E2 involves ER, Src, epidermal growth factor receptor, and G-protein coupled ER (GPER) in a pertussis toxin-sensitive pathway. sodium arsenite 61-67 G protein-coupled estrogen receptor 1 Homo sapiens 139-159 27071941-6 2016 Inhibitor studies suggest that rapid MAPK phosphorylation by NaAsO2, CdCl2, and E2 involves ER, Src, epidermal growth factor receptor, and G-protein coupled ER (GPER) in a pertussis toxin-sensitive pathway. sodium arsenite 61-67 G protein-coupled estrogen receptor 1 Homo sapiens 161-165 27071941-6 2016 Inhibitor studies suggest that rapid MAPK phosphorylation by NaAsO2, CdCl2, and E2 involves ER, Src, epidermal growth factor receptor, and G-protein coupled ER (GPER) in a pertussis toxin-sensitive pathway. Cadmium Chloride 69-74 G protein-coupled estrogen receptor 1 Homo sapiens 139-159 27071941-6 2016 Inhibitor studies suggest that rapid MAPK phosphorylation by NaAsO2, CdCl2, and E2 involves ER, Src, epidermal growth factor receptor, and G-protein coupled ER (GPER) in a pertussis toxin-sensitive pathway. Cadmium Chloride 69-74 G protein-coupled estrogen receptor 1 Homo sapiens 161-165 28757722-12 2016 This suggests that 17beta-estradiol relaxes the human gallbladder via GPER. Estradiol 19-35 G protein-coupled estrogen receptor 1 Homo sapiens 70-74 27071941-8 2016 This study supports the involvement of membrane ER and GPER signaling in mediating cellular responses to environmentally relevant nM concentrations of CdCl2 and NaAsO2 in lung adenocarcinoma cells. Cadmium Chloride 151-156 G protein-coupled estrogen receptor 1 Homo sapiens 55-59 27071941-8 2016 This study supports the involvement of membrane ER and GPER signaling in mediating cellular responses to environmentally relevant nM concentrations of CdCl2 and NaAsO2 in lung adenocarcinoma cells. sodium arsenite 161-167 G protein-coupled estrogen receptor 1 Homo sapiens 55-59 27111051-1 2016 UNLABELLED: Estradiol mediates its actions by binding to classical nuclear receptors, estrogen receptor alpha (ER-alpha) and estrogen receptor beta (ER-beta), and the non-classical G protein-coupled estrogen receptor 1(GPER). Estradiol 12-21 G protein-coupled estrogen receptor 1 Homo sapiens 181-218 27111051-1 2016 UNLABELLED: Estradiol mediates its actions by binding to classical nuclear receptors, estrogen receptor alpha (ER-alpha) and estrogen receptor beta (ER-beta), and the non-classical G protein-coupled estrogen receptor 1(GPER). Estradiol 12-21 G protein-coupled estrogen receptor 1 Homo sapiens 219-223 27080432-7 2016 Binding at membrane-associated ERalpha and GPER1 could account for rapid estrogen-induced decreases in GABA transmission in the striatum, which, in turn, could affect dopamine transmission in this region. gamma-Aminobutyric Acid 103-107 G protein-coupled estrogen receptor 1 Homo sapiens 43-48 27080432-7 2016 Binding at membrane-associated ERalpha and GPER1 could account for rapid estrogen-induced decreases in GABA transmission in the striatum, which, in turn, could affect dopamine transmission in this region. Dopamine 167-175 G protein-coupled estrogen receptor 1 Homo sapiens 43-48 26981789-0 2016 The protective role of G protein-coupled estrogen receptor 1 (GPER-1) on methotrexate-induced nephrotoxicity in human renal epithelium cells. Methotrexate 73-85 G protein-coupled estrogen receptor 1 Homo sapiens 23-60 26981789-0 2016 The protective role of G protein-coupled estrogen receptor 1 (GPER-1) on methotrexate-induced nephrotoxicity in human renal epithelium cells. Methotrexate 73-85 G protein-coupled estrogen receptor 1 Homo sapiens 62-68 27213340-4 2016 GPER is a recently appreciated GPCR that mediates the rapid effects of estrogen and aldosterone. Aldosterone 84-95 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 27213340-8 2016 GPER appears to be an important determinant of the two major risk factors for coronary artery disease-blood pressure and LDL cholesterol. Cholesterol 125-136 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 27115344-4 2016 Utilizing both genetic and pharmacologic approaches, we establish that sex steroid effects on human pigment synthesis are mediated by the membrane-bound, steroid hormone receptors G protein-coupled estrogen receptor (GPER), and progestin and adipoQ receptor 7 (PAQR7). Steroids 75-82 G protein-coupled estrogen receptor 1 Homo sapiens 180-215 27115344-4 2016 Utilizing both genetic and pharmacologic approaches, we establish that sex steroid effects on human pigment synthesis are mediated by the membrane-bound, steroid hormone receptors G protein-coupled estrogen receptor (GPER), and progestin and adipoQ receptor 7 (PAQR7). Steroids 75-82 G protein-coupled estrogen receptor 1 Homo sapiens 217-221 28757722-13 2016 CONCLUSION: These results demonstrate for the first time that 17beta-estradiol and GPER agonist G-1 cause relaxation of the human gallbladder, probably through GPER. Estradiol 62-78 G protein-coupled estrogen receptor 1 Homo sapiens 160-164 26865461-7 2016 Here, we describe the role exerted by GPCR-mediated signaling in low oxygen conditions, discussing, in particular, the involvement of GPER by a hypoxic microenvironment. Oxygen 69-75 G protein-coupled estrogen receptor 1 Homo sapiens 134-138 26914403-0 2016 Bisphenol A Induces Migration through a GPER-, FAK-, Src-, and ERK2-Dependent Pathway in MDA-MB-231 Breast Cancer Cells. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 40-44 26432358-6 2015 In conclusion, Estrogen suppresses breast cancer growth by inhibiting G1/S phase transition through GPER/ROS/p38 MAPK/p21 mediated signaling during hypoxic condition. ros 105-108 G protein-coupled estrogen receptor 1 Homo sapiens 100-104 26690777-0 2016 GPER1-mediated IGFBP-1 induction modulates IGF-1-dependent signaling in tamoxifen-treated breast cancer cells. Tamoxifen 72-81 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 25784559-0 2016 2,2",4,4"-Tetrabromodiphenyl ether promotes human neuroblastoma SH-SY5Y cells migration via the GPER/PI3K/Akt signal pathway. 2,2',4,4'-tetrabromodiphenyl ether 0-34 G protein-coupled estrogen receptor 1 Homo sapiens 96-100 25784559-7 2016 Further, the signals G protein-coupled estrogen receptor 1 (GPER)/phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)/protein kinase B (Akt) mediated the BDE-47-induced upregulation of MMP-9 and in vitro migration of SH-SY5Y cells since G15 (GPER inhibitor) and LY 294002 (PI3K/Akt inhibitor) significantly abolished the effects of BDE-47. phosphatidylinositol-4, 66-89 G protein-coupled estrogen receptor 1 Homo sapiens 21-58 25784559-7 2016 Further, the signals G protein-coupled estrogen receptor 1 (GPER)/phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)/protein kinase B (Akt) mediated the BDE-47-induced upregulation of MMP-9 and in vitro migration of SH-SY5Y cells since G15 (GPER inhibitor) and LY 294002 (PI3K/Akt inhibitor) significantly abolished the effects of BDE-47. phosphatidylinositol-4, 66-89 G protein-coupled estrogen receptor 1 Homo sapiens 60-64 25784559-7 2016 Further, the signals G protein-coupled estrogen receptor 1 (GPER)/phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)/protein kinase B (Akt) mediated the BDE-47-induced upregulation of MMP-9 and in vitro migration of SH-SY5Y cells since G15 (GPER inhibitor) and LY 294002 (PI3K/Akt inhibitor) significantly abolished the effects of BDE-47. phosphatidylinositol-4, 66-89 G protein-coupled estrogen receptor 1 Homo sapiens 244-248 25784559-7 2016 Further, the signals G protein-coupled estrogen receptor 1 (GPER)/phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)/protein kinase B (Akt) mediated the BDE-47-induced upregulation of MMP-9 and in vitro migration of SH-SY5Y cells since G15 (GPER inhibitor) and LY 294002 (PI3K/Akt inhibitor) significantly abolished the effects of BDE-47. 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one 264-273 G protein-coupled estrogen receptor 1 Homo sapiens 21-58 25784559-7 2016 Further, the signals G protein-coupled estrogen receptor 1 (GPER)/phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)/protein kinase B (Akt) mediated the BDE-47-induced upregulation of MMP-9 and in vitro migration of SH-SY5Y cells since G15 (GPER inhibitor) and LY 294002 (PI3K/Akt inhibitor) significantly abolished the effects of BDE-47. 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one 264-273 G protein-coupled estrogen receptor 1 Homo sapiens 60-64 25784559-7 2016 Further, the signals G protein-coupled estrogen receptor 1 (GPER)/phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)/protein kinase B (Akt) mediated the BDE-47-induced upregulation of MMP-9 and in vitro migration of SH-SY5Y cells since G15 (GPER inhibitor) and LY 294002 (PI3K/Akt inhibitor) significantly abolished the effects of BDE-47. 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one 264-273 G protein-coupled estrogen receptor 1 Homo sapiens 244-248 26646587-0 2016 GPER is involved in the stimulatory effects of aldosterone in breast cancer cells and breast tumor-derived endothelial cells. Aldosterone 47-58 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 26646587-4 2016 GPER has been also shown to contribute to certain responses to aldosterone, however the role played by GPER and the molecular mechanisms implicated remain to be fully understood. Aldosterone 63-74 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 26646587-7 2016 Our results demonstrate that aldosterone triggers the EGFR/ERK transduction pathway in a MR- and GPER-dependent manner. Aldosterone 29-40 G protein-coupled estrogen receptor 1 Homo sapiens 97-101 26646587-8 2016 Aldosterone does not bind to GPER, it however induces the direct interaction between MR and GPER as well as between GPER and EGFR. Aldosterone 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 92-96 26646587-8 2016 Aldosterone does not bind to GPER, it however induces the direct interaction between MR and GPER as well as between GPER and EGFR. Aldosterone 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 92-96 26646587-9 2016 Next, we ascertain that the up-regulation of the Na+/H+ exchanger-1 (NHE-1) induced by aldosterone involves MR and GPER. Aldosterone 87-98 G protein-coupled estrogen receptor 1 Homo sapiens 115-119 26646587-10 2016 Biologically, both MR and GPER contribute to the proliferation and migration of breast and endothelial cancer cells mediated by NHE-1 upon aldosterone exposure. Aldosterone 139-150 G protein-coupled estrogen receptor 1 Homo sapiens 26-30 26646587-11 2016 Our data further extend the current knowledge on the molecular mechanisms through which GPER may contribute to the stimulatory action elicited by aldosterone in breast cancer. Aldosterone 146-157 G protein-coupled estrogen receptor 1 Homo sapiens 88-92 26955487-0 2016 Differences in GPR30 Regulation by Chlorotriazine Herbicides in Human Breast Cells. cyanuric chloride 35-49 G protein-coupled estrogen receptor 1 Homo sapiens 15-20 26955487-2 2016 GPR30, a G protein coupled receptor, was identified as a potential orphan receptor that may interact with triazine herbicides such as atrazine, one of the most commonly utilized chlorotriazines in agricultural practices in the United States. Triazines 106-114 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 26955487-2 2016 GPR30, a G protein coupled receptor, was identified as a potential orphan receptor that may interact with triazine herbicides such as atrazine, one of the most commonly utilized chlorotriazines in agricultural practices in the United States. Atrazine 134-142 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 26955487-2 2016 GPR30, a G protein coupled receptor, was identified as a potential orphan receptor that may interact with triazine herbicides such as atrazine, one of the most commonly utilized chlorotriazines in agricultural practices in the United States. cyanuric chloride 178-193 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 26955487-3 2016 Our goal was to identify whether chlorotriazines affected the expression of GPR30. cyanuric chloride 33-48 G protein-coupled estrogen receptor 1 Homo sapiens 76-81 26955487-6 2016 Our results indicate that GPR30 expression increased in breast cancer cells at levels lower than the US EPA drinking water contamination limit. Water 117-122 G protein-coupled estrogen receptor 1 Homo sapiens 26-31 26955487-8 2016 In contrast, treatment with chlorotriazines reduced the expression of GPR30 in noncancerous MCF-10A cells. cyanuric chloride 28-43 G protein-coupled estrogen receptor 1 Homo sapiens 70-75 26585123-2 2016 Recent studies have identified the G-protein-coupled receptor 30 (GPR30, GPER) as a high-affinity membrane receptor for 2-methoxyestradiol. 2-Methoxyestradiol 120-138 G protein-coupled estrogen receptor 1 Homo sapiens 35-64 26585123-2 2016 Recent studies have identified the G-protein-coupled receptor 30 (GPR30, GPER) as a high-affinity membrane receptor for 2-methoxyestradiol. 2-Methoxyestradiol 120-138 G protein-coupled estrogen receptor 1 Homo sapiens 66-71 26585123-2 2016 Recent studies have identified the G-protein-coupled receptor 30 (GPR30, GPER) as a high-affinity membrane receptor for 2-methoxyestradiol. 2-Methoxyestradiol 120-138 G protein-coupled estrogen receptor 1 Homo sapiens 73-77 26253279-0 2015 Action of methyl-, propyl- and butylparaben on GPR30 gene and protein expression, cAMP levels and activation of ERK1/2 and PI3K/Akt signaling pathways in MCF-7 breast cancer cells and MCF-10A non-transformed breast epithelial cells. methyl-, propyl- and butylparaben 10-43 G protein-coupled estrogen receptor 1 Homo sapiens 47-52 26415222-0 2015 Copper activates HIF-1alpha/GPER/VEGF signalling in cancer cells. Copper 0-6 G protein-coupled estrogen receptor 1 Homo sapiens 28-32 26415222-3 2015 Here, we show that copper sulfate (CuSO4) induces the expression of HIF-1alpha as well as GPER and VEGF in breast and hepatic cancer cells through the activation of the EGFR/ERK/c-fos transduction pathway. Copper Sulfate 19-33 G protein-coupled estrogen receptor 1 Homo sapiens 90-94 26415222-3 2015 Here, we show that copper sulfate (CuSO4) induces the expression of HIF-1alpha as well as GPER and VEGF in breast and hepatic cancer cells through the activation of the EGFR/ERK/c-fos transduction pathway. Copper Sulfate 35-40 G protein-coupled estrogen receptor 1 Homo sapiens 90-94 26415222-5 2015 We also ascertained that HIF-1alpha and GPER are required for the transcriptional activation of VEGF induced by CuSO4. Copper Sulfate 112-117 G protein-coupled estrogen receptor 1 Homo sapiens 40-44 26415222-6 2015 In addition, in human endothelial cells, the conditioned medium from breast cancer cells treated with CuSO4 promoted cell migration and tube formation through HIF-1alpha and GPER. Copper Sulfate 102-107 G protein-coupled estrogen receptor 1 Homo sapiens 174-178 26253279-1 2015 In the present study, we examined cAMP levels and activation of the MAPK/ERK1/2 and PI3K/Akt signaling pathways in response to the actions of parabens on GPR30 in MCF-7 and MCF-10A cells. Cyclic AMP 34-38 G protein-coupled estrogen receptor 1 Homo sapiens 154-159 26253279-1 2015 In the present study, we examined cAMP levels and activation of the MAPK/ERK1/2 and PI3K/Akt signaling pathways in response to the actions of parabens on GPR30 in MCF-7 and MCF-10A cells. Parabens 142-150 G protein-coupled estrogen receptor 1 Homo sapiens 154-159 26253279-3 2015 17beta-estradiol and all tested parabens increased GPR30 gene and protein expression in MCF-7 and MCF-10A cells. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 51-56 26253279-3 2015 17beta-estradiol and all tested parabens increased GPR30 gene and protein expression in MCF-7 and MCF-10A cells. Parabens 32-40 G protein-coupled estrogen receptor 1 Homo sapiens 51-56 26253279-7 2015 Collectively, the data presented here point to a nongenomic mechanism of action of parabens in activation GPR30 in both cancer and non-cancer breast cell lines through betagamma dimer-mediated activation of the ERK1/2 pathway, but not the cAMP/PKA pathway. Parabens 83-91 G protein-coupled estrogen receptor 1 Homo sapiens 106-111 26400551-4 2015 Its binding to GPER was achieved by competition assays with [3H]E2 and [5,6-3H] nicotinic acid in ER-negative and GPER-positive SkBr3 breast cancer cells. Tritium 61-63 G protein-coupled estrogen receptor 1 Homo sapiens 15-19 26400551-4 2015 Its binding to GPER was achieved by competition assays with [3H]E2 and [5,6-3H] nicotinic acid in ER-negative and GPER-positive SkBr3 breast cancer cells. [5,6-3h] nicotinic acid 71-94 G protein-coupled estrogen receptor 1 Homo sapiens 15-19 26482875-1 2015 Whether aldosterone activates the G-protein-coupled estrogen receptor (GPER) has been questioned, recently, in the name of Copernicus. Aldosterone 8-19 G protein-coupled estrogen receptor 1 Homo sapiens 34-69 26482875-1 2015 Whether aldosterone activates the G-protein-coupled estrogen receptor (GPER) has been questioned, recently, in the name of Copernicus. Aldosterone 8-19 G protein-coupled estrogen receptor 1 Homo sapiens 71-75 26482875-3 2015 Further, studies in mineralocorticoid receptor (MR)-deficient systems, with pharmacological GPER-selective antagonists or regulation of GPER expression, consistently show that some aldosterone effects can be GPER mediated. Aldosterone 181-192 G protein-coupled estrogen receptor 1 Homo sapiens 92-96 26482875-3 2015 Further, studies in mineralocorticoid receptor (MR)-deficient systems, with pharmacological GPER-selective antagonists or regulation of GPER expression, consistently show that some aldosterone effects can be GPER mediated. Aldosterone 181-192 G protein-coupled estrogen receptor 1 Homo sapiens 136-140 26482875-3 2015 Further, studies in mineralocorticoid receptor (MR)-deficient systems, with pharmacological GPER-selective antagonists or regulation of GPER expression, consistently show that some aldosterone effects can be GPER mediated. Aldosterone 181-192 G protein-coupled estrogen receptor 1 Homo sapiens 136-140 26470790-3 2015 We previously reported that estrogen activates the phosphoinositide 3-kinase (PI3Kinase) pathway via GPER, resulting in phosphatidylinositol (3,4,5)-trisphosphate (PIP3) production within the nucleus of breast cancer cells; however, the mechanisms and consequences of this activity remained unclear. phosphatidylinositol 3,4,5-triphosphate 120-162 G protein-coupled estrogen receptor 1 Homo sapiens 101-105 26470790-3 2015 We previously reported that estrogen activates the phosphoinositide 3-kinase (PI3Kinase) pathway via GPER, resulting in phosphatidylinositol (3,4,5)-trisphosphate (PIP3) production within the nucleus of breast cancer cells; however, the mechanisms and consequences of this activity remained unclear. PIP3 164-168 G protein-coupled estrogen receptor 1 Homo sapiens 101-105 26470790-11 2015 The SERMs tamoxifen and raloxifene, as well as the SERD ICI182,780, were active in mediating FOXO3a inactivation in a GPER-dependent manner. Tamoxifen 10-19 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 26470790-11 2015 The SERMs tamoxifen and raloxifene, as well as the SERD ICI182,780, were active in mediating FOXO3a inactivation in a GPER-dependent manner. Raloxifene Hydrochloride 24-34 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 26200092-5 2015 Raloxifene induced a time-dependent increase in the level of phosphorylated ERK1 and ERK2, by a mechanism blocked by the GPER antagonist. Raloxifene Hydrochloride 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 121-125 26170064-6 2015 Using primary mesencephalic cultures, we found that GPER activation protects dopaminergic neurons from MPP(+) toxicity in an extent similar to the promoted by a 17beta-estradiol. mangion-purified polysaccharide (Candida albicans) 103-109 G protein-coupled estrogen receptor 1 Homo sapiens 52-56 26200092-7 2015 These results reveal a mechanism mediating the regulation of AVP expression by raloxifene, involving the activation of GPER, which in turn activates protein kinase C, MAPK/ERK kinase, and ERK. Raloxifene Hydrochloride 79-89 G protein-coupled estrogen receptor 1 Homo sapiens 119-123 26183213-0 2015 A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models. calixpyrrole 2-14 G protein-coupled estrogen receptor 1 Homo sapiens 51-55 26183213-5 2015 Here, we provide evidence on the molecular mechanisms through which a calixpyrrole derivative acts as a GPER antagonist in different model systems, such as breast tumor cells and cancer-associated fibroblasts (CAFs) obtained from breast cancer patients. calixpyrrole 70-82 G protein-coupled estrogen receptor 1 Homo sapiens 104-108 26183213-7 2015 Moreover, calixpyrrole derivatives could be considered in future anticancer strategies targeting GPER in cancer cells. calixpyrrole 10-22 G protein-coupled estrogen receptor 1 Homo sapiens 97-101 26303299-13 2015 Selective activation of GPER may therefore be considered as a novel strategy to treat increased prostanoid-dependent vasomotor tone or vascular disease in postmenopausal women. Prostaglandins 96-106 G protein-coupled estrogen receptor 1 Homo sapiens 24-28 25847233-4 2015 In primary endothelial cells, GPER/GPR30 agonist G-1 decreases PMCA-mediated Ca(2+) extrusion by promoting PMCA tyrosine phosphorylation. Tyrosine 112-120 G protein-coupled estrogen receptor 1 Homo sapiens 30-34 26131713-3 2015 However, tamoxifen not only exerts antiestrogenic activity, but also acts as full agonist on the G protein-coupled estrogen receptor (GPER). Tamoxifen 9-18 G protein-coupled estrogen receptor 1 Homo sapiens 97-132 26131713-3 2015 However, tamoxifen not only exerts antiestrogenic activity, but also acts as full agonist on the G protein-coupled estrogen receptor (GPER). Tamoxifen 9-18 G protein-coupled estrogen receptor 1 Homo sapiens 134-138 26088671-2 2015 G protein-coupled estrogen receptor (GPER) is activated by 17beta-estradiol and participates in functional crosstalk with other steroid receptors. Estradiol 59-75 G protein-coupled estrogen receptor 1 Homo sapiens 0-35 26088671-2 2015 G protein-coupled estrogen receptor (GPER) is activated by 17beta-estradiol and participates in functional crosstalk with other steroid receptors. Estradiol 59-75 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 26225773-5 2015 Our results show that 17beta-estradiol (E2) and the selective ligand of GPER, namely G-1, induce the expression of SIRT1 through GPER and the subsequent activation of the EGFR/ERK/c-fos/AP-1 transduction pathway. Estradiol 22-38 G protein-coupled estrogen receptor 1 Homo sapiens 72-76 26225773-5 2015 Our results show that 17beta-estradiol (E2) and the selective ligand of GPER, namely G-1, induce the expression of SIRT1 through GPER and the subsequent activation of the EGFR/ERK/c-fos/AP-1 transduction pathway. Estradiol 22-38 G protein-coupled estrogen receptor 1 Homo sapiens 129-133 25885794-9 2015 Results of pharmacological experiments revealed that the cytoprotective actions of estradiol were dependent on ERbeta and IGF1R receptor tyrosine kinase activity and independent of ERalpha and G protein-coupled estrogen receptor 1 (G protein coupled receptor 30). Estradiol 83-92 G protein-coupled estrogen receptor 1 Homo sapiens 232-261 25805831-0 2015 Ca2+ channel subunit alpha 1D promotes proliferation and migration of endometrial cancer cells mediated by 17beta-estradiol via the G protein-coupled estrogen receptor. Estradiol 107-123 G protein-coupled estrogen receptor 1 Homo sapiens 132-167 26030000-4 2015 Here, we demonstrate that in SkBr3 breast cancer and HepG2 hepatocarcinoma cells, 17beta-estradiol (E2) and the selective GPER ligand G-1 induce miR144 expression through GPER and the involvement of the PI3K/ERK1/2/Elk1 transduction pathway. Estradiol 82-98 G protein-coupled estrogen receptor 1 Homo sapiens 171-175 25969534-10 2015 These results suggest that physiological concentrations of DHEA activate a GPER intracellular signaling cascade that increases pri-miR-21 transcription mediated at least in part by AP-1 and androgen receptor miR-21 promoter interaction. Dehydroepiandrosterone 59-63 G protein-coupled estrogen receptor 1 Homo sapiens 75-79 25413376-6 2015 In addition, we show that 17beta-oestradiol induces the ERK1/2 activation and increases c-Fos expression through GPR30 associated with ERbeta down-regulation in TCam-2 cell line. Estradiol 26-43 G protein-coupled estrogen receptor 1 Homo sapiens 113-118 25990368-15 2015 GPER probably contributes to tamoxifen resistance via interaction with the tumor microenvironment in a beta1-integrin-dependent pattern. Tamoxifen 29-38 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 26359098-0 2015 [GPER silence inhibits the stimulation of growth and inhibition of apoptosis induced by tamoxifen in breast cancer-associated fibroblasts]. Tamoxifen 88-97 G protein-coupled estrogen receptor 1 Homo sapiens 1-5 26359098-8 2015 Tamoxifen promoted the growth of BCAFs, which could be attenuated by knockdown of GPER. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 82-86 26359098-9 2015 Moreover, the apoptosis of BCAFs was reduced by tamoxifen, which was also reversed by knockdown of GPER. Tamoxifen 48-57 G protein-coupled estrogen receptor 1 Homo sapiens 99-103 26359098-11 2015 The ability of tamoxifen to accelerate cell proliferation and decrease cell apoptosis could be weakened by knockdown of GPER. Tamoxifen 15-24 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 25969534-4 2015 siRNA, antibody, and inhibitor studies suggest that the rapid DHEA-mediated increase in miR-21 involves a G-protein-coupled estrogen receptor (GPER/GPR30), estrogen receptor alpha-36 (ERalpha36), epidermal growth factor receptor-dependent, pertussis toxin-sensitive pathway requiring activation of c-Src, ERK1/2, and PI3K. Dehydroepiandrosterone 62-66 G protein-coupled estrogen receptor 1 Homo sapiens 143-147 25969534-4 2015 siRNA, antibody, and inhibitor studies suggest that the rapid DHEA-mediated increase in miR-21 involves a G-protein-coupled estrogen receptor (GPER/GPR30), estrogen receptor alpha-36 (ERalpha36), epidermal growth factor receptor-dependent, pertussis toxin-sensitive pathway requiring activation of c-Src, ERK1/2, and PI3K. Dehydroepiandrosterone 62-66 G protein-coupled estrogen receptor 1 Homo sapiens 148-153 25969534-5 2015 GPER antagonist G-15 attenuated DHEA- and BSA-conjugated DHEA-stimulated pri-miR-21 transcription. G-15 16-20 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 25969534-5 2015 GPER antagonist G-15 attenuated DHEA- and BSA-conjugated DHEA-stimulated pri-miR-21 transcription. Dehydroepiandrosterone 32-36 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 25969534-5 2015 GPER antagonist G-15 attenuated DHEA- and BSA-conjugated DHEA-stimulated pri-miR-21 transcription. Dehydroepiandrosterone 57-61 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 25969534-7 2015 DHEA, like G-1, increased GPER and ERalpha36 mRNA and protein levels. Dehydroepiandrosterone 0-4 G protein-coupled estrogen receptor 1 Homo sapiens 26-30 25969534-8 2015 DHEA increased ERK1/2 and c-Src phosphorylation in a GPER-responsive manner. Dehydroepiandrosterone 0-4 G protein-coupled estrogen receptor 1 Homo sapiens 53-57 25990368-0 2015 Acquisition of epithelial-mesenchymal transition phenotype in the tamoxifen-resistant breast cancer cell: a new role for G protein-coupled estrogen receptor in mediating tamoxifen resistance through cancer-associated fibroblast-derived fibronectin and beta1-integrin signaling pathway in tumor cells. Tamoxifen 66-75 G protein-coupled estrogen receptor 1 Homo sapiens 121-156 25990368-0 2015 Acquisition of epithelial-mesenchymal transition phenotype in the tamoxifen-resistant breast cancer cell: a new role for G protein-coupled estrogen receptor in mediating tamoxifen resistance through cancer-associated fibroblast-derived fibronectin and beta1-integrin signaling pathway in tumor cells. Tamoxifen 170-179 G protein-coupled estrogen receptor 1 Homo sapiens 121-156 25990368-2 2015 beta1-integrin was identified as one of the target genes of G protein-coupled estrogen receptor (GPER), a novel estrogen receptor recognized as an initiator of tamoxifen resistance. Tamoxifen 160-169 G protein-coupled estrogen receptor 1 Homo sapiens 60-95 25990368-2 2015 beta1-integrin was identified as one of the target genes of G protein-coupled estrogen receptor (GPER), a novel estrogen receptor recognized as an initiator of tamoxifen resistance. Tamoxifen 160-169 G protein-coupled estrogen receptor 1 Homo sapiens 97-101 25990368-3 2015 Here, we investigated the role of beta1-integrin in GPER-mediated tamoxifen resistance in breast cancer. Tamoxifen 66-75 G protein-coupled estrogen receptor 1 Homo sapiens 52-56 25847233-4 2015 In primary endothelial cells, GPER/GPR30 agonist G-1 decreases PMCA-mediated Ca(2+) extrusion by promoting PMCA tyrosine phosphorylation. Tyrosine 112-120 G protein-coupled estrogen receptor 1 Homo sapiens 35-40 25847233-7 2015 GPER/GPR30 co-immunoprecipitates with PMCA with or without treatment with 17beta-estradiol, thapsigargin, or G-1. Estradiol 74-90 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 25847233-7 2015 GPER/GPR30 co-immunoprecipitates with PMCA with or without treatment with 17beta-estradiol, thapsigargin, or G-1. Estradiol 74-90 G protein-coupled estrogen receptor 1 Homo sapiens 5-10 25847233-7 2015 GPER/GPR30 co-immunoprecipitates with PMCA with or without treatment with 17beta-estradiol, thapsigargin, or G-1. Thapsigargin 92-104 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 25847233-7 2015 GPER/GPR30 co-immunoprecipitates with PMCA with or without treatment with 17beta-estradiol, thapsigargin, or G-1. Thapsigargin 92-104 G protein-coupled estrogen receptor 1 Homo sapiens 5-10 25847233-13 2015 Activation of GPER/GPR30 further inhibits PMCA activity through tyrosine phosphorylation of the pump. Tyrosine 64-72 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 25847233-13 2015 Activation of GPER/GPR30 further inhibits PMCA activity through tyrosine phosphorylation of the pump. Tyrosine 64-72 G protein-coupled estrogen receptor 1 Homo sapiens 19-24 25609836-10 2015 2-OHE2 also antagonized estrogen actions through GPER on cAMP production in zebrafish oocytes, resulting in a reduction in cAMP levels. 2-hydroxyestradiol 0-6 G protein-coupled estrogen receptor 1 Homo sapiens 49-53 26175858-0 2015 G15 sensitizes epithelial breast cancer cells to doxorubicin by preventing epithelial-mesenchymal transition through inhibition of GPR30. Doxorubicin 49-60 G protein-coupled estrogen receptor 1 Homo sapiens 131-136 25928008-0 2015 Estradiol induces HOTAIR levels via GPER-mediated miR-148a inhibition in breast cancer. Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 36-40 25744245-0 2015 G protein-coupled estrogen receptor (GPER) mediates NSCLC progression induced by 17beta-estradiol (E2) and selective agonist G1. Estradiol 81-97 G protein-coupled estrogen receptor 1 Homo sapiens 0-35 25744245-0 2015 G protein-coupled estrogen receptor (GPER) mediates NSCLC progression induced by 17beta-estradiol (E2) and selective agonist G1. Estradiol 81-97 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 25744245-6 2015 Selective agonist G1 and 17beta-estradiol (E2) promoted the GPER-mediated proliferation, invasion, and migration of NSCLC cells. Estradiol 25-41 G protein-coupled estrogen receptor 1 Homo sapiens 60-64 25744245-8 2015 Importantly, the pro-tumorigenic effects of GPER induced by E2 were significantly reduced by co-administering the GPER inhibitor G15 and the ERbeta inhibitor fulvestrant, as compared to administering fulvestrant alone both in vitro and in vivo. Fulvestrant 158-169 G protein-coupled estrogen receptor 1 Homo sapiens 44-48 25823895-0 2015 17beta-estradiol inhibits spreading of metastatic cells from granulosa cell tumors through a non-genomic mechanism involving GPER1. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 125-130 25616260-3 2015 OBJECTIVES: We aimed to evaluate the potential of atrazine to trigger GPER-mediated signaling in cancer cells and cancer-associated fibroblasts (CAFs). Atrazine 50-58 G protein-coupled estrogen receptor 1 Homo sapiens 70-74 25616260-5 2015 Conversely, atrazine was able to bind to GPER to induce ERK activation and the expression of estrogen target genes, which, interestingly, appeared to rely on both GPER and ERalpha expression. Atrazine 12-20 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 25616260-5 2015 Conversely, atrazine was able to bind to GPER to induce ERK activation and the expression of estrogen target genes, which, interestingly, appeared to rely on both GPER and ERalpha expression. Atrazine 12-20 G protein-coupled estrogen receptor 1 Homo sapiens 163-167 25616260-6 2015 As a biological counterpart, atrazine stimulated the proliferation of ovarian cancer cells that depend on GPER and ERalpha, as evidenced by gene silencing experiments and the use of specific signaling inhibitors. Atrazine 29-37 G protein-coupled estrogen receptor 1 Homo sapiens 106-110 25616260-7 2015 Of note, through GPER, atrazine elicited ERK phosphorylation, gene expression, and migration in CAFs, thus extending its stimulatory role to these main players of the tumor microenvironment. Atrazine 23-31 G protein-coupled estrogen receptor 1 Homo sapiens 17-21 25616260-9 2015 On the basis of our data, atrazine should be included among the environmental contaminants that may elicit estrogenic activity through GPER-mediated signaling. Atrazine 26-34 G protein-coupled estrogen receptor 1 Homo sapiens 135-139 25647524-7 2015 Moreover, knockdown of GPER in CAFs suppressed breast cancer cell invasion induced by CAF conditioned media (CM). caf conditioned media 86-107 G protein-coupled estrogen receptor 1 Homo sapiens 23-27 25672442-5 2015 Furthermore, baicalein interfered with E2-induced novel G protein-coupled estrogen receptor (GPR30)-related signaling, including a decrease in tyrosine phosphorylation of epidermal growth factor receptor (EGFR) as well as phosphorylation of extracellular signal-regulated kinase (ERK) and serine/threonine kinase Akt, without affecting GPR30 expression. baicalein 13-22 G protein-coupled estrogen receptor 1 Homo sapiens 93-98 25672442-5 2015 Furthermore, baicalein interfered with E2-induced novel G protein-coupled estrogen receptor (GPR30)-related signaling, including a decrease in tyrosine phosphorylation of epidermal growth factor receptor (EGFR) as well as phosphorylation of extracellular signal-regulated kinase (ERK) and serine/threonine kinase Akt, without affecting GPR30 expression. baicalein 13-22 G protein-coupled estrogen receptor 1 Homo sapiens 336-341 25672442-5 2015 Furthermore, baicalein interfered with E2-induced novel G protein-coupled estrogen receptor (GPR30)-related signaling, including a decrease in tyrosine phosphorylation of epidermal growth factor receptor (EGFR) as well as phosphorylation of extracellular signal-regulated kinase (ERK) and serine/threonine kinase Akt, without affecting GPR30 expression. Tyrosine 143-151 G protein-coupled estrogen receptor 1 Homo sapiens 93-98 25781607-9 2015 Inhibiting GPR30 through treatment with the G-15 antagonist or specific shRNA impaired E2 effects. G-15 44-48 G protein-coupled estrogen receptor 1 Homo sapiens 11-16 25609836-10 2015 2-OHE2 also antagonized estrogen actions through GPER on cAMP production in zebrafish oocytes, resulting in a reduction in cAMP levels. Cyclic AMP 57-61 G protein-coupled estrogen receptor 1 Homo sapiens 49-53 25609836-10 2015 2-OHE2 also antagonized estrogen actions through GPER on cAMP production in zebrafish oocytes, resulting in a reduction in cAMP levels. Cyclic AMP 123-127 G protein-coupled estrogen receptor 1 Homo sapiens 49-53 26416628-3 2015 We incubated them with 17-beta estradiol (E(2)), after blocking, or upregulating, expression of GPER-1 with ICI182,780 (a GPER-1 agonist) and siGPR30, respectively. Estradiol 23-40 G protein-coupled estrogen receptor 1 Homo sapiens 96-102 25395619-10 2015 In the discovery cohort, GPER P16L genotype was associated with a significant increase in LDL cholesterol (mean+-SEM): 3.18+-0.05, 3.25+-0.08, and 4.25+-0.33 mmol/L, respectively, in subjects with CC (homozygous for P16), CT (heterozygotes), and TT (homozygous for L16) genotypes (P<0.05). Cholesterol 94-105 G protein-coupled estrogen receptor 1 Homo sapiens 25-29 25395619-11 2015 In the validation cohort (n=339), the GPER P16L genotype was associated with a similar increase in LDL cholesterol: 2.17+-0.05, 2.34+-0.06, and 2.42+-0.16 mmol/L, respectively, in subjects with CC, CT, and TT genotypes (P<0.05). Cholesterol 103-114 G protein-coupled estrogen receptor 1 Homo sapiens 38-42 25395619-11 2015 In the validation cohort (n=339), the GPER P16L genotype was associated with a similar increase in LDL cholesterol: 2.17+-0.05, 2.34+-0.06, and 2.42+-0.16 mmol/L, respectively, in subjects with CC, CT, and TT genotypes (P<0.05). Carbon Tetrachloride 198-200 G protein-coupled estrogen receptor 1 Homo sapiens 38-42 25395619-15 2015 Furthermore, humans carrying the hypofunctional P16L genetic variant of GPER have increased plasma LDL cholesterol. Cholesterol 103-114 G protein-coupled estrogen receptor 1 Homo sapiens 72-76 25786510-0 2015 (6-bromo-1,4-dimethyl-9H-carbazol-3-yl-methylene)-hydrazine (carbhydraz) acts as a GPER agonist in breast cancer cells. (6-bromo-1,4-dimethyl-9H-carbazol-3-ylmethylene)hydrazine 1-59 G protein-coupled estrogen receptor 1 Homo sapiens 83-87 25786510-0 2015 (6-bromo-1,4-dimethyl-9H-carbazol-3-yl-methylene)-hydrazine (carbhydraz) acts as a GPER agonist in breast cancer cells. (6-bromo-1,4-dimethyl-9H-carbazol-3-ylmethylene)hydrazine 61-71 G protein-coupled estrogen receptor 1 Homo sapiens 83-87 25786510-4 2015 In the present study, we designed and synthesized two novel carbazole derivatives and then investigated their ability to interact with and activate the GPER-mediated transduction pathway in breast cancer cells. carbazole 60-69 G protein-coupled estrogen receptor 1 Homo sapiens 152-156 25875871-0 2015 Identification of two benzopyrroloxazines acting as selective GPER antagonists in breast cancer cells and cancer-associated fibroblasts. benzopyrroloxazines 22-41 G protein-coupled estrogen receptor 1 Homo sapiens 62-66 25875871-3 2015 RESULTS: Two novel selective GPER antagonists, based on a benzo[b]pyrrolo[1,2-d][1,4]oxazin-4-one structure, have been designed and synthesized. benzo[b]pyrrolo[1,2-d][1,4]oxazin-4-one 58-97 G protein-coupled estrogen receptor 1 Homo sapiens 29-33 25666016-4 2015 Tamoxifen resistance is associated with altered estrogen receptor expression especially on the plasma membrane, including the alternative G-protein coupled receptor GPR-30 (GPER) and estrogen receptor splice products, such as ERalpha36. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 165-171 25666016-4 2015 Tamoxifen resistance is associated with altered estrogen receptor expression especially on the plasma membrane, including the alternative G-protein coupled receptor GPR-30 (GPER) and estrogen receptor splice products, such as ERalpha36. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 173-177 26416628-8 2015 ICI182,780 enhanced E(2)-induced proliferation of LC (p < 0.01), while knock down of the GPER-1 gene with GPER-1 small interfering RNA partially inhibited E(2)-induced cell proliferation (p < 0.01). Estradiol 158-162 G protein-coupled estrogen receptor 1 Homo sapiens 92-98 26416628-8 2015 ICI182,780 enhanced E(2)-induced proliferation of LC (p < 0.01), while knock down of the GPER-1 gene with GPER-1 small interfering RNA partially inhibited E(2)-induced cell proliferation (p < 0.01). Estradiol 158-162 G protein-coupled estrogen receptor 1 Homo sapiens 109-115 25496649-0 2014 Inhibition of GPR30 by estriol prevents growth stimulation of triple-negative breast cancer cells by 17beta-estradiol. Estriol 23-30 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 25587872-3 2015 Furthermore, we explored GPER/GPR30"s molecular recognition properties by using reported agonist ligands (G1, estradiol (E2), tamoxifen, and fulvestrant) and the antagonist ligands (G15 and G36) in subsequent docking studies. Estradiol 110-119 G protein-coupled estrogen receptor 1 Homo sapiens 25-29 25587872-3 2015 Furthermore, we explored GPER/GPR30"s molecular recognition properties by using reported agonist ligands (G1, estradiol (E2), tamoxifen, and fulvestrant) and the antagonist ligands (G15 and G36) in subsequent docking studies. Estradiol 110-119 G protein-coupled estrogen receptor 1 Homo sapiens 30-35 25587872-3 2015 Furthermore, we explored GPER/GPR30"s molecular recognition properties by using reported agonist ligands (G1, estradiol (E2), tamoxifen, and fulvestrant) and the antagonist ligands (G15 and G36) in subsequent docking studies. Tamoxifen 126-135 G protein-coupled estrogen receptor 1 Homo sapiens 25-29 25587872-4 2015 Our results identified the E2 binding site on GPER/GPR30, as well as other receptor cavities for accepting large volume ligands, through GPER/GPR30 pi-pi, hydrophobic, and hydrogen bond interactions. Hydrogen 172-180 G protein-coupled estrogen receptor 1 Homo sapiens 46-50 25587872-4 2015 Our results identified the E2 binding site on GPER/GPR30, as well as other receptor cavities for accepting large volume ligands, through GPER/GPR30 pi-pi, hydrophobic, and hydrogen bond interactions. Hydrogen 172-180 G protein-coupled estrogen receptor 1 Homo sapiens 51-56 26281354-3 2015 Effects of GPER include activation of MAPK and PI3K signaling pathways, stimulation of adenyl cyclase, and mobilization of calcium ions from intracellular stores, as well as upregulation of genes such as FOS and CTGF. Calcium 123-130 G protein-coupled estrogen receptor 1 Homo sapiens 11-15 26281354-5 2015 Antiestrogens tamoxifen, raloxifene, or fulvestrant proved,to be agonists of GPER, which undoubtedly is not without significance for the efficacy of the therapy. Tamoxifen 14-23 G protein-coupled estrogen receptor 1 Homo sapiens 77-81 26281354-5 2015 Antiestrogens tamoxifen, raloxifene, or fulvestrant proved,to be agonists of GPER, which undoubtedly is not without significance for the efficacy of the therapy. Raloxifene Hydrochloride 25-35 G protein-coupled estrogen receptor 1 Homo sapiens 77-81 26281354-5 2015 Antiestrogens tamoxifen, raloxifene, or fulvestrant proved,to be agonists of GPER, which undoubtedly is not without significance for the efficacy of the therapy. Fulvestrant 40-51 G protein-coupled estrogen receptor 1 Homo sapiens 77-81 25496649-0 2014 Inhibition of GPR30 by estriol prevents growth stimulation of triple-negative breast cancer cells by 17beta-estradiol. Estradiol 101-117 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 25496649-3 2014 We have recently shown that knock-down of GPR30 expression prevented growth stimulation of TNBC cell lines by 17beta-estradiol. Estradiol 110-126 G protein-coupled estrogen receptor 1 Homo sapiens 42-47 25167221-0 2014 GPER-1 and estrogen receptor-beta ligands modulate aldosterone synthesis. Aldosterone 51-62 G protein-coupled estrogen receptor 1 Homo sapiens 0-33 25030373-3 2014 Here, we developed (99m)Tc-labeled GPER ligands to demonstrate the in vivo status of GPER as an estrogen receptor (ER) and for GPER visualization in whole animals. Technetium 24-26 G protein-coupled estrogen receptor 1 Homo sapiens 35-39 25030373-3 2014 Here, we developed (99m)Tc-labeled GPER ligands to demonstrate the in vivo status of GPER as an estrogen receptor (ER) and for GPER visualization in whole animals. Technetium 24-26 G protein-coupled estrogen receptor 1 Homo sapiens 85-89 25030373-3 2014 Here, we developed (99m)Tc-labeled GPER ligands to demonstrate the in vivo status of GPER as an estrogen receptor (ER) and for GPER visualization in whole animals. Technetium 24-26 G protein-coupled estrogen receptor 1 Homo sapiens 85-89 25030373-9 2014 In conclusion, we synthesized and evaluated a series of first-generation (99m)Tc-labeled GPER-specific radioligands, demonstrating GPER as an estrogen-binding receptor for the first time in vivo using competitive binding principles, and establishing the utility of such ligands as tumor imaging agents. Technetium 78-80 G protein-coupled estrogen receptor 1 Homo sapiens 89-93 25030373-9 2014 In conclusion, we synthesized and evaluated a series of first-generation (99m)Tc-labeled GPER-specific radioligands, demonstrating GPER as an estrogen-binding receptor for the first time in vivo using competitive binding principles, and establishing the utility of such ligands as tumor imaging agents. Technetium 78-80 G protein-coupled estrogen receptor 1 Homo sapiens 131-135 24894716-4 2014 We demonstrated that 17beta-estradiol (E2) and the GPER-selective ligand G-1 triggered a GPER/EGFR/ERK/c-fos signaling pathway that leads to increased VEGF via upregulation of HIF1alpha. Estradiol 21-37 G protein-coupled estrogen receptor 1 Homo sapiens 89-93 25312822-0 2014 Bisphenol A stimulates human lung cancer cell migration via upregulation of matrix metalloproteinases by GPER/EGFR/ERK1/2 signal pathway. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 25012984-5 2014 Moreover, cell migration triggered by insulin occurred through GPER1 and its main target gene CTGF, whereas the insulin-induced expression of GPER1 boosted cell-cycle progression and the glucose uptake stimulated by estrogens. Glucose 187-194 G protein-coupled estrogen receptor 1 Homo sapiens 142-147 24874276-0 2014 GPER mediates enhanced cell viability and motility via non-genomic signaling induced by 17beta-estradiol in triple-negative breast cancer cells. Estradiol 88-104 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 24874276-6 2014 Treatment with 17beta-estradiol (E2), the GPER-specific agonist G-1 and tamoxifen (TAM) led to rapid activation of p-ERK1/2, but not p-Akt. Estradiol 15-31 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 24874276-6 2014 Treatment with 17beta-estradiol (E2), the GPER-specific agonist G-1 and tamoxifen (TAM) led to rapid activation of p-ERK1/2, but not p-Akt. Tamoxifen 72-81 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 25005496-0 2014 G protein-coupled estrogen receptor 1 mediates relaxation of coronary arteries via cAMP/PKA-dependent activation of MLCP. Cyclic AMP 83-87 G protein-coupled estrogen receptor 1 Homo sapiens 0-37 25005496-3 2014 In the current study, we tested the hypothesis that GPER-induced relaxation of porcine coronary arteries is mediated via cAMP/PKA signaling. Cyclic AMP 121-125 G protein-coupled estrogen receptor 1 Homo sapiens 52-56 25005496-4 2014 Our findings revealed that vascular relaxation to the selective GPER agonist G-1 (0.3-3 muM) was associated with increased cAMP production in a concentration-dependent manner. Cyclic AMP 123-127 G protein-coupled estrogen receptor 1 Homo sapiens 64-68 25005496-12 2014 These findings demonstrate that localized cAMP/PKA signaling is involved in GPER-mediated coronary vasodilation by activating MLCP via inhibition of RhoA pathway. Cyclic AMP 42-46 G protein-coupled estrogen receptor 1 Homo sapiens 76-80 25312822-5 2014 G-protein-coupled estrogen receptor (GPER), while not estrogen receptor alpha/beta (ERalpha/beta), mediated the BPA induced up regulation of MMPs. bisphenol A 112-115 G protein-coupled estrogen receptor 1 Homo sapiens 0-35 25312822-5 2014 G-protein-coupled estrogen receptor (GPER), while not estrogen receptor alpha/beta (ERalpha/beta), mediated the BPA induced up regulation of MMPs. bisphenol A 112-115 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 25312822-6 2014 Further, BPA treatment induced rapid activation of ERK1/2 via GPER/EGFR. bisphenol A 9-12 G protein-coupled estrogen receptor 1 Homo sapiens 62-66 25312822-7 2014 GPER/ERFR/ERK1/2 mediated the BPA induced upregulation of MMPs and in vitro migration of lung cancer A549 cells. bisphenol A 30-33 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 25312822-8 2014 In summary, our data presented here revealed for the first time that BPA can promote the in vitro migration and invasion of lung cancer cells via upregulation of MMPs and GPER/EGFR/ERK1/2 signals, which mediated these effects. bisphenol A 69-72 G protein-coupled estrogen receptor 1 Homo sapiens 171-175 24874276-6 2014 Treatment with 17beta-estradiol (E2), the GPER-specific agonist G-1 and tamoxifen (TAM) led to rapid activation of p-ERK1/2, but not p-Akt. Tamoxifen 83-86 G protein-coupled estrogen receptor 1 Homo sapiens 42-46 24928526-0 2014 Tamoxifen through GPER upregulates aromatase expression: a novel mechanism sustaining tamoxifen-resistant breast cancer cell growth. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 18-22 24928526-0 2014 Tamoxifen through GPER upregulates aromatase expression: a novel mechanism sustaining tamoxifen-resistant breast cancer cell growth. Tamoxifen 86-95 G protein-coupled estrogen receptor 1 Homo sapiens 18-22 24928526-8 2014 This is mediated by the G-protein-coupled receptor GPR30/GPER, since knocking-down GPER expression or treatment with a GPER antagonist reversed the enhanced aromatase levels induced by long-term tamoxifen exposure. Tamoxifen 195-204 G protein-coupled estrogen receptor 1 Homo sapiens 51-56 24928526-8 2014 This is mediated by the G-protein-coupled receptor GPR30/GPER, since knocking-down GPER expression or treatment with a GPER antagonist reversed the enhanced aromatase levels induced by long-term tamoxifen exposure. Tamoxifen 195-204 G protein-coupled estrogen receptor 1 Homo sapiens 57-61 24928526-8 2014 This is mediated by the G-protein-coupled receptor GPR30/GPER, since knocking-down GPER expression or treatment with a GPER antagonist reversed the enhanced aromatase levels induced by long-term tamoxifen exposure. Tamoxifen 195-204 G protein-coupled estrogen receptor 1 Homo sapiens 83-87 24928526-8 2014 This is mediated by the G-protein-coupled receptor GPR30/GPER, since knocking-down GPER expression or treatment with a GPER antagonist reversed the enhanced aromatase levels induced by long-term tamoxifen exposure. Tamoxifen 195-204 G protein-coupled estrogen receptor 1 Homo sapiens 83-87 24928526-9 2014 The molecular mechanism was investigated in ER-negative, GPER/aromatase-positive SKBR3 cells, in which tamoxifen acts as a GPER agonist. Tamoxifen 103-112 G protein-coupled estrogen receptor 1 Homo sapiens 57-61 24928526-9 2014 The molecular mechanism was investigated in ER-negative, GPER/aromatase-positive SKBR3 cells, in which tamoxifen acts as a GPER agonist. Tamoxifen 103-112 G protein-coupled estrogen receptor 1 Homo sapiens 123-127 24928526-11 2014 As tamoxifen via GPER induced aromatase expression also in CAFs, this pathway may be involved in promoting aggressive behavior of breast tumors in response to tamoxifen treatment. Tamoxifen 3-12 G protein-coupled estrogen receptor 1 Homo sapiens 17-21 24928526-11 2014 As tamoxifen via GPER induced aromatase expression also in CAFs, this pathway may be involved in promoting aggressive behavior of breast tumors in response to tamoxifen treatment. Tamoxifen 159-168 G protein-coupled estrogen receptor 1 Homo sapiens 17-21 24662263-0 2014 Niacin activates the G protein estrogen receptor (GPER)-mediated signalling. Niacin 0-6 G protein-coupled estrogen receptor 1 Homo sapiens 21-48 24662263-0 2014 Niacin activates the G protein estrogen receptor (GPER)-mediated signalling. Niacin 0-6 G protein-coupled estrogen receptor 1 Homo sapiens 50-54 24662263-4 2014 In the present study, we demonstrate for the first time that nicotinic acid and nicotinamide bind to and activate the GPER-mediated signalling in breast cancer cells and cancer-associated fibroblasts (CAFs). Niacin 61-75 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 24662263-4 2014 In the present study, we demonstrate for the first time that nicotinic acid and nicotinamide bind to and activate the GPER-mediated signalling in breast cancer cells and cancer-associated fibroblasts (CAFs). Niacinamide 80-92 G protein-coupled estrogen receptor 1 Homo sapiens 118-122 24662263-6 2014 As a biological counterpart, nicotinic acid and nicotinamide induce proliferative and migratory effects in breast cancer cells and CAFs in a GPER-dependent fashion. Niacin 29-43 G protein-coupled estrogen receptor 1 Homo sapiens 141-145 24662263-6 2014 As a biological counterpart, nicotinic acid and nicotinamide induce proliferative and migratory effects in breast cancer cells and CAFs in a GPER-dependent fashion. Niacinamide 48-60 G protein-coupled estrogen receptor 1 Homo sapiens 141-145 24662263-7 2014 Moreover, nicotinic acid prevents the up-regulation of ICAM-1 triggered by the pro-inflammatory cytokine TNF-alpha and stimulates the formation of endothelial tubes through GPER in HUVECs. Niacin 10-24 G protein-coupled estrogen receptor 1 Homo sapiens 173-177 24662263-8 2014 Together, our findings concerning the agonist activity for GPER displayed by both nicotinic acid and nicotinamide broaden the mechanisms involved in the biological action of these molecules and further support the potential of a ligand to induce different responses mediated in a promiscuous manner by distinct GPCRs. Niacin 82-96 G protein-coupled estrogen receptor 1 Homo sapiens 59-63 24662263-8 2014 Together, our findings concerning the agonist activity for GPER displayed by both nicotinic acid and nicotinamide broaden the mechanisms involved in the biological action of these molecules and further support the potential of a ligand to induce different responses mediated in a promiscuous manner by distinct GPCRs. Niacinamide 101-113 G protein-coupled estrogen receptor 1 Homo sapiens 59-63 24928526-12 2014 Blocking estrogen production and/or GPER signaling activation may represent a valid option to overcome tamoxifen-resistance in breast cancers. Tamoxifen 103-112 G protein-coupled estrogen receptor 1 Homo sapiens 36-40 24715381-2 2014 Tamoxifen is a partial agonist at GPER in vitro. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 34-38 24718680-0 2014 Icariin and icaritin stimulate the proliferation of SKBr3 cells through the GPER1-mediated modulation of the EGFR-MAPK signaling pathway. icariin 0-7 G protein-coupled estrogen receptor 1 Homo sapiens 76-81 24718680-0 2014 Icariin and icaritin stimulate the proliferation of SKBr3 cells through the GPER1-mediated modulation of the EGFR-MAPK signaling pathway. icaritin 12-20 G protein-coupled estrogen receptor 1 Homo sapiens 76-81 24718680-4 2014 The ICA- and ICT-stimulated cell growth was completely suppressed by the GPER1 antagonist, G-15, indicating that the ICA- and ICT-stimulated cell proliferation was mediated by GPER1 activation. icariin 4-7 G protein-coupled estrogen receptor 1 Homo sapiens 73-78 24718680-4 2014 The ICA- and ICT-stimulated cell growth was completely suppressed by the GPER1 antagonist, G-15, indicating that the ICA- and ICT-stimulated cell proliferation was mediated by GPER1 activation. icariin 4-7 G protein-coupled estrogen receptor 1 Homo sapiens 176-181 24718680-9 2014 Flow cytometric analysis confirmed that the ICA- and ICT-stimulated SKBr3 cell proliferation involved the GPER1-mediated modulation of the EGFR-MAPK signaling pathway. icariin 44-47 G protein-coupled estrogen receptor 1 Homo sapiens 106-111 24796498-4 2014 Vasodilation induced by G-1 (selective GPER-agonist, 3 muM) from HRAs pre-contracted with norepinephrine amounted to 40+-5% in PMW, significantly larger than those obtained from M (20+-5%) or PGW (20+-5%). Norepinephrine 90-104 G protein-coupled estrogen receptor 1 Homo sapiens 39-43 24796498-5 2014 L-NAME (nitric oxide (NO) synthase inhibitor) abolished these relaxations in PGW, attenuated them in PMW and had no effect in M. Immunohistochemical analysis confirmed the presence of GPER in both smooth muscle and endothelial cells of HRA with maximum expression in PGW. NG-Nitroarginine Methyl Ester 0-6 G protein-coupled estrogen receptor 1 Homo sapiens 184-188 24796498-5 2014 L-NAME (nitric oxide (NO) synthase inhibitor) abolished these relaxations in PGW, attenuated them in PMW and had no effect in M. Immunohistochemical analysis confirmed the presence of GPER in both smooth muscle and endothelial cells of HRA with maximum expression in PGW. Nitric Oxide 8-20 G protein-coupled estrogen receptor 1 Homo sapiens 184-188 24704272-1 2014 In this study, we investigated the role of GPR30 in 17beta-estradiol- (E2) mediated neuroprotection after an ischemic injury in an organotypic hippocampal slice culture (OHSC) model. Estradiol 52-68 G protein-coupled estrogen receptor 1 Homo sapiens 43-48 24704272-3 2014 The canonical estrogen receptor (ER) inhibitor ICI 182,780 completely abrogated the therapeutic effect of E2 while the GPR30 antagonist G-15 effected a slight but not significant reduction in neuroprotection. G-15 136-140 G protein-coupled estrogen receptor 1 Homo sapiens 119-124 24834064-3 2014 A wide number of natural and synthetic compounds, including estrogens and anti-estrogens, elicit stimulatory effects in breast cancer through GPER up-regulation and activation, suggesting that GPER function is associated with breast tumor progression and tamoxifen resistance. Tamoxifen 255-264 G protein-coupled estrogen receptor 1 Homo sapiens 193-197 24718936-8 2014 Inhibition of candidate signaling pathways that may link GPER activation to proliferation revealed a dependence on Src, epidermal growth factor receptor transactivation by heparin-bound EGF and subsequent ERK phosphorylation. Heparin 172-179 G protein-coupled estrogen receptor 1 Homo sapiens 57-61 24715381-6 2014 In the tamoxifen-treated ER-positive and progesterone receptor (PgR)-positive patient subgroup, the absence of PM GPER (53 % of all ER-positive tumors) predicted 91 % 20-year distant disease-free survival, compared to 73 % in the presence of GPER (p = 0.001). Tamoxifen 7-16 G protein-coupled estrogen receptor 1 Homo sapiens 114-118 24446390-10 2014 Small interfering RNA targeting GPER or G protein inhibitor pertussin toxin (PTX) inhibited basal cell proliferation and attenuated 17beta-estradiol- or G-1-induced cell proliferation. Estradiol 132-148 G protein-coupled estrogen receptor 1 Homo sapiens 32-36 24715381-9 2014 GPER overexpression and PM localization are critical events in breast cancer progression, and lack of GPER in the PM is associated with excellent long-term prognosis in ER-positive and PgR-positive tamoxifen-treated primary breast cancer. Tamoxifen 198-207 G protein-coupled estrogen receptor 1 Homo sapiens 102-106 24446390-0 2014 A novel estrogen receptor GPER mediates proliferation induced by 17beta-estradiol and selective GPER agonist G-1 in estrogen receptor alpha (ERalpha)-negative ovarian cancer cells. Estradiol 65-81 G protein-coupled estrogen receptor 1 Homo sapiens 26-30 24736568-0 2014 Activation of GPER-1 estradiol receptor downregulates production of testosterone in isolated rat Leydig cells and adult human testis. Testosterone 68-80 G protein-coupled estrogen receptor 1 Homo sapiens 14-20 24908729-0 2014 [Low-dose nonylphenol promotes the proliferation of DU-145 cells and expression of membrane estrogen receptor GPR30 in DU-145 cells]. nonylphenol 10-21 G protein-coupled estrogen receptor 1 Homo sapiens 110-115 24908729-1 2014 OBJECTIVE: To observe the effects of low-dose exogenous estrogen nonylphenol (NP) on the proliferation of human prostate cancer cell lines DU-145 and the expression of the membrane estrogen receptor GPR30 in the DU-145 cells. nonylphenol 65-76 G protein-coupled estrogen receptor 1 Homo sapiens 199-204 24525372-4 2014 Moreover, both anti-collagenogenic and pro-elastogenic effects of tanshinone IIA occurred only after selective activation of the G protein-coupled estrogen receptor (GPER). tanshinone 66-80 G protein-coupled estrogen receptor 1 Homo sapiens 129-164 24525372-4 2014 Moreover, both anti-collagenogenic and pro-elastogenic effects of tanshinone IIA occurred only after selective activation of the G protein-coupled estrogen receptor (GPER). tanshinone 66-80 G protein-coupled estrogen receptor 1 Homo sapiens 166-170 24736568-14 2014 The expression of GPER-1 in human testis, which lack ERalpha, makes it an exciting target for developing new agents affecting testosterone production in men. Testosterone 126-138 G protein-coupled estrogen receptor 1 Homo sapiens 18-24 24440569-6 2014 E2 and ICI also induced phosphorylation of extracellular regulated protein kinases 1 and 2 (ERK1/2), and suppression of ERK1/2 phosphorylation by U0126 profoundly impeded calpain activation triggered by estrogenic and antiestrogenic stimulations indicating implication of ERK1/2 in the GPR30-mediated action. U 0126 146-151 G protein-coupled estrogen receptor 1 Homo sapiens 286-291 24481325-6 2014 Tamoxifen (TAM) in addition to 17beta-estradiol (E2) and the GPER agonist G1 activated GPER, resulting in transient increases in cell index, intracellular calcium, and ERK1/2 phosphorylation. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 87-91 24481325-6 2014 Tamoxifen (TAM) in addition to 17beta-estradiol (E2) and the GPER agonist G1 activated GPER, resulting in transient increases in cell index, intracellular calcium, and ERK1/2 phosphorylation. Tamoxifen 11-14 G protein-coupled estrogen receptor 1 Homo sapiens 87-91 24481325-6 2014 Tamoxifen (TAM) in addition to 17beta-estradiol (E2) and the GPER agonist G1 activated GPER, resulting in transient increases in cell index, intracellular calcium, and ERK1/2 phosphorylation. Estradiol 49-51 G protein-coupled estrogen receptor 1 Homo sapiens 87-91 24481325-6 2014 Tamoxifen (TAM) in addition to 17beta-estradiol (E2) and the GPER agonist G1 activated GPER, resulting in transient increases in cell index, intracellular calcium, and ERK1/2 phosphorylation. Calcium 155-162 G protein-coupled estrogen receptor 1 Homo sapiens 61-65 24481325-7 2014 Furthermore, TAM, E2, and G1 promoted CAF proliferation and cell-cycle progression, both of which were blocked by GPER interference, the selective GPER antagonist G15, the epidermal growth factor receptor (EGFR) inhibitor AG1478, and the ERK1/2 inhibitor U0126. RTKI cpd 222-228 G protein-coupled estrogen receptor 1 Homo sapiens 114-118 24481325-7 2014 Furthermore, TAM, E2, and G1 promoted CAF proliferation and cell-cycle progression, both of which were blocked by GPER interference, the selective GPER antagonist G15, the epidermal growth factor receptor (EGFR) inhibitor AG1478, and the ERK1/2 inhibitor U0126. U 0126 255-260 G protein-coupled estrogen receptor 1 Homo sapiens 114-118 24481325-8 2014 Importantly, TAM as well as G1 increased E2 production in breast CAFs via GPER/EGFR/ERK signaling when the substrate of E2, testosterone, was added to the medium. Tamoxifen 13-16 G protein-coupled estrogen receptor 1 Homo sapiens 74-78 24481325-8 2014 Importantly, TAM as well as G1 increased E2 production in breast CAFs via GPER/EGFR/ERK signaling when the substrate of E2, testosterone, was added to the medium. Testosterone 124-136 G protein-coupled estrogen receptor 1 Homo sapiens 74-78 24481325-9 2014 GPER-induced aromatase upregulation was probably responsible for this phenomenon, as TAM- and G1-induced CYP19A1 gene expression was reduced by GPER knockdown and G15, AG1478, and U0126 administration. U 0126 180-185 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 24481325-10 2014 Accordingly, GPER-mediated CAF-dependent estrogenic effects on the tumor-associated stroma are conceivable, and CAF is likely to contribute to breast cancer progression, especially TAM resistance, via a positive feedback loop involving GPER/EGFR/ERK signaling and E2 production. Tamoxifen 181-184 G protein-coupled estrogen receptor 1 Homo sapiens 236-240 24019118-0 2014 Oleuropein and hydroxytyrosol activate GPER/ GPR30-dependent pathways leading to apoptosis of ER-negative SKBR3 breast cancer cells. 3,4-dihydroxyphenylethanol 15-29 G protein-coupled estrogen receptor 1 Homo sapiens 39-43 24019118-0 2014 Oleuropein and hydroxytyrosol activate GPER/ GPR30-dependent pathways leading to apoptosis of ER-negative SKBR3 breast cancer cells. 3,4-dihydroxyphenylethanol 15-29 G protein-coupled estrogen receptor 1 Homo sapiens 45-50 24019118-5 2014 MTT cell proliferation assays revealed that both phenols reduced SKBR3 cell growth; this effect was abolished silencing GPER. monooxyethylene trimethylolpropane tristearate 0-3 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 24019118-5 2014 MTT cell proliferation assays revealed that both phenols reduced SKBR3 cell growth; this effect was abolished silencing GPER. Phenols 49-56 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 24239983-5 2014 Plasma membrane fractions prepared from whole kidney tissue or HEK293 cells expressing recombinant human GPER-1 (HEK-GPER-1) displayed high-affinity, specific [(3)H]-17beta-estradiol ([(3)H]-E2) binding, but no specific [(3)H]-aldosterone binding. Estradiol 166-182 G protein-coupled estrogen receptor 1 Homo sapiens 105-111 24239983-5 2014 Plasma membrane fractions prepared from whole kidney tissue or HEK293 cells expressing recombinant human GPER-1 (HEK-GPER-1) displayed high-affinity, specific [(3)H]-17beta-estradiol ([(3)H]-E2) binding, but no specific [(3)H]-aldosterone binding. Estradiol 166-182 G protein-coupled estrogen receptor 1 Homo sapiens 113-123 24239983-5 2014 Plasma membrane fractions prepared from whole kidney tissue or HEK293 cells expressing recombinant human GPER-1 (HEK-GPER-1) displayed high-affinity, specific [(3)H]-17beta-estradiol ([(3)H]-E2) binding, but no specific [(3)H]-aldosterone binding. Aldosterone 227-238 G protein-coupled estrogen receptor 1 Homo sapiens 113-123 24239983-5 2014 Plasma membrane fractions prepared from whole kidney tissue or HEK293 cells expressing recombinant human GPER-1 (HEK-GPER-1) displayed high-affinity, specific [(3)H]-17beta-estradiol ([(3)H]-E2) binding, but no specific [(3)H]-aldosterone binding. Aldosterone 227-238 G protein-coupled estrogen receptor 1 Homo sapiens 105-111 24275097-1 2014 The G protein-coupled receptor GPR30/GPER has been shown to mediate rapid effects of 17beta-estradiol (E2) in diverse types of cancer cells. Estradiol 85-101 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 24451139-5 2014 In order to explain this overexpression, we investigated the possible association of polymorphisms in the GPER gene by using allele-specific tetra-primer polymerase chain reaction performed on tissue samples from 150 paraffin-embedded TGCT specimens (131 seminomas, 19 non seminomas). Paraffin 217-225 G protein-coupled estrogen receptor 1 Homo sapiens 106-110 24421881-1 2014 INTRODUCTION: The G protein-coupled estrogen receptor (GPER) is a novel estrogen receptor that mediates proliferative effects induced by estrogen but also by tamoxifen. Tamoxifen 158-167 G protein-coupled estrogen receptor 1 Homo sapiens 18-53 24421881-1 2014 INTRODUCTION: The G protein-coupled estrogen receptor (GPER) is a novel estrogen receptor that mediates proliferative effects induced by estrogen but also by tamoxifen. Tamoxifen 158-167 G protein-coupled estrogen receptor 1 Homo sapiens 55-59 24486480-0 2014 Retraction: G-protein-coupled receptor 30 and estrogen receptor-alpha are involved in the proliferative effects induced by atrazine in ovarian cancer cells. Atrazine 123-131 G protein-coupled estrogen receptor 1 Homo sapiens 12-41 24275097-1 2014 The G protein-coupled receptor GPR30/GPER has been shown to mediate rapid effects of 17beta-estradiol (E2) in diverse types of cancer cells. Estradiol 85-101 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 23902478-5 2013 G-Protein oestrogen receptor (GPER) is a recently recognized G-protein coupled receptor (GPCR) that is activated by steroid hormones. Steroids 116-132 G protein-coupled estrogen receptor 1 Homo sapiens 0-28 23902478-5 2013 G-Protein oestrogen receptor (GPER) is a recently recognized G-protein coupled receptor (GPCR) that is activated by steroid hormones. Steroids 116-132 G protein-coupled estrogen receptor 1 Homo sapiens 30-34 23902478-7 2013 Activation of GPER also mediates at least some of the vascular effects of aldosterone in smooth muscle and endothelial cells. Aldosterone 74-85 G protein-coupled estrogen receptor 1 Homo sapiens 14-18 23907016-0 2013 17beta-estradiol promotes the invasion and migration of nuclear estrogen receptor-negative breast cancer cells through cross-talk between GPER1 and CXCR1. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 138-143 24169358-0 2013 Fulvestrant induces resistance by modulating GPER and CDK6 expression: implication of methyltransferases, deacetylases and the hSWI/SNF chromatin remodelling complex. Fulvestrant 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 45-49 23959105-7 2013 Typical serum BPA concentrations are orders of magnitude lower than levels measurable by modern analytical methods and below concentrations required to occupy more than 0.0009% of Type II Estrogen Binding Sites, GPR30, ERalpha or ERbeta receptors. bisphenol A 14-17 G protein-coupled estrogen receptor 1 Homo sapiens 212-217 24289103-0 2013 GPR30 as an initiator of tamoxifen resistance in hormone-dependent breast cancer. Tamoxifen 25-34 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 24289103-2 2013 Here, we investigated the role of estrogen G-protein coupled receptor 30 (GPR30) on Tamoxifen resistance in breast cancer. Tamoxifen 84-93 G protein-coupled estrogen receptor 1 Homo sapiens 43-72 24289103-2 2013 Here, we investigated the role of estrogen G-protein coupled receptor 30 (GPR30) on Tamoxifen resistance in breast cancer. Tamoxifen 84-93 G protein-coupled estrogen receptor 1 Homo sapiens 74-79 24289103-8 2013 In TAM-R cells, GPR30 cell-surface translocation facilitated crosstalk with EGFR, and reduced cAMP generation, attenuating inhibition of EGFR signaling. Cyclic AMP 94-98 G protein-coupled estrogen receptor 1 Homo sapiens 16-21 23907016-3 2013 In this study, the main aims were focused on the potential role of GPER1 in regulating migration and invasion of nuclear estrogen receptor (ER)-negative breast cancer cells upon 17beta-estradiol (E2) stimulation and the involved signaling pathway. Estradiol 178-194 G protein-coupled estrogen receptor 1 Homo sapiens 67-72 23755949-1 2013 OBJECTIVE: To investigate whether histone deacetylase inhibitors reduce the expression of the G-protein-coupled estrogen receptor (GPER) and whether the functional inhibition of GPER by the antagonist G-15 decreases the proliferation of endometriotic cells. G-15 201-205 G protein-coupled estrogen receptor 1 Homo sapiens 178-182 23602294-0 2013 Calcium supplementation increases circulating cholesterol by reducing its catabolism via GPER and TRPC1-dependent pathway in estrogen deficient women. Calcium 0-7 G protein-coupled estrogen receptor 1 Homo sapiens 89-93 23602294-0 2013 Calcium supplementation increases circulating cholesterol by reducing its catabolism via GPER and TRPC1-dependent pathway in estrogen deficient women. Cholesterol 46-57 G protein-coupled estrogen receptor 1 Homo sapiens 89-93 24039841-0 2013 Estradiol and tamoxifen induce cell migration through GPR30 and activation of focal adhesion kinase (FAK) in endometrial cancers with low or without nuclear estrogen receptor alpha (ERalpha). Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 54-59 24039841-0 2013 Estradiol and tamoxifen induce cell migration through GPR30 and activation of focal adhesion kinase (FAK) in endometrial cancers with low or without nuclear estrogen receptor alpha (ERalpha). Tamoxifen 14-23 G protein-coupled estrogen receptor 1 Homo sapiens 54-59 24039841-2 2013 Previous reports have demonstrated that estradiol and tamoxifen induce proliferation of human endometrial cancer cells through GPR30 (non-genomic ER) signaling pathway. Estradiol 40-49 G protein-coupled estrogen receptor 1 Homo sapiens 127-132 24039841-2 2013 Previous reports have demonstrated that estradiol and tamoxifen induce proliferation of human endometrial cancer cells through GPR30 (non-genomic ER) signaling pathway. Tamoxifen 54-63 G protein-coupled estrogen receptor 1 Homo sapiens 127-132 24039841-3 2013 Herein, we demonstrate that phosphorylation of focal adhesion kinase (FAK) is involved in cell migration induced by estradiol, tamoxifen and G1 (a GPR30 agonist) through the transmembrane ER (GPR30) in endometrial cancer cell lines with or without ERalpha (Ishikawa and RL95-2). Estradiol 116-125 G protein-coupled estrogen receptor 1 Homo sapiens 147-152 24039841-3 2013 Herein, we demonstrate that phosphorylation of focal adhesion kinase (FAK) is involved in cell migration induced by estradiol, tamoxifen and G1 (a GPR30 agonist) through the transmembrane ER (GPR30) in endometrial cancer cell lines with or without ERalpha (Ishikawa and RL95-2). Estradiol 116-125 G protein-coupled estrogen receptor 1 Homo sapiens 192-197 24039841-3 2013 Herein, we demonstrate that phosphorylation of focal adhesion kinase (FAK) is involved in cell migration induced by estradiol, tamoxifen and G1 (a GPR30 agonist) through the transmembrane ER (GPR30) in endometrial cancer cell lines with or without ERalpha (Ishikawa and RL95-2). Tamoxifen 127-136 G protein-coupled estrogen receptor 1 Homo sapiens 147-152 24039841-3 2013 Herein, we demonstrate that phosphorylation of focal adhesion kinase (FAK) is involved in cell migration induced by estradiol, tamoxifen and G1 (a GPR30 agonist) through the transmembrane ER (GPR30) in endometrial cancer cell lines with or without ERalpha (Ishikawa and RL95-2). Tamoxifen 127-136 G protein-coupled estrogen receptor 1 Homo sapiens 192-197 23804203-0 2013 Resveratrol inhibits K(v)2.2 currents through the estrogen receptor GPR30-mediated PKC pathway. Resveratrol 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 68-73 23804203-7 2013 Moreover, the effect of REV on K(v)2.2 was reduced by preincubation with antagonists of GPR30 receptor and shRNA for GPR30 receptor. Resveratrol 24-27 G protein-coupled estrogen receptor 1 Homo sapiens 88-93 23804203-7 2013 Moreover, the effect of REV on K(v)2.2 was reduced by preincubation with antagonists of GPR30 receptor and shRNA for GPR30 receptor. Resveratrol 24-27 G protein-coupled estrogen receptor 1 Homo sapiens 117-122 23755949-5 2013 INTERVENTION(S): Treatment with the histone deacetylase inhibitor romidepsin or suberoylanilide hydroxamic acid (SAHA), or with the GPER antagonist G-15. G-15 148-152 G protein-coupled estrogen receptor 1 Homo sapiens 132-136 23755949-7 2013 Effects of GPER stimulation and inhibition on cell proliferation were investigated by the 93-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide (Sigma) (MTT) assay. 93-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide 90-151 G protein-coupled estrogen receptor 1 Homo sapiens 11-15 23624423-0 2013 4-Hydroxytamoxifen-stimulated processing of cyclin E is mediated via G protein-coupled receptor 30 (GPR30) and accompanied by enhanced migration in MCF-7 breast cancer cells. hydroxytamoxifen 0-18 G protein-coupled estrogen receptor 1 Homo sapiens 69-98 23951246-7 2013 Although GPER was found to be specifically induced by LH/FSH, GPER agonists (4-Hydroxy-Tamoxifen, G1) reduced EOC cell proliferation only in case of LH/FSH unstimulated pathways. 4'-hydroxytamoxifen 77-96 G protein-coupled estrogen receptor 1 Homo sapiens 62-66 23624423-0 2013 4-Hydroxytamoxifen-stimulated processing of cyclin E is mediated via G protein-coupled receptor 30 (GPR30) and accompanied by enhanced migration in MCF-7 breast cancer cells. hydroxytamoxifen 0-18 G protein-coupled estrogen receptor 1 Homo sapiens 100-105 23402905-0 2013 Anti-tumorigenic action of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H-benzo(b)pyran: evidence for involvement of GPR30/EGFR signaling pathway. 2-(piperidinoethoxyphenyl)-3-(4-hydroxyphenyl)-2H-benzo(b)pyran 27-90 G protein-coupled estrogen receptor 1 Homo sapiens 120-125 23840305-5 2013 We found that the GPER agonist, G-1, inhibited both human and porcine CASMC proliferation in a concentration- (10(-8) to 10(-5) M) and time-dependent manner. casmc 70-75 G protein-coupled estrogen receptor 1 Homo sapiens 18-22 23840305-9 2013 CONCLUSION: GPER activation inhibits CASMC proliferation by suppressing cell cycle progression via inhibition of ERK1/2 and Akt phosphorylation. casmc 37-42 G protein-coupled estrogen receptor 1 Homo sapiens 12-16 23419549-0 2013 The key involvement of estrogen receptor beta and G-protein-coupled receptor 30 in the neuroprotective action of daidzein. daidzein 113-121 G protein-coupled estrogen receptor 1 Homo sapiens 50-79 23615160-7 2013 Finally, given that certain clinically approved drugs such as SERM or SERDs (thought only to block or downregulate nuclear ERs) actually cause vasodilation through GPER and have been shown in recent clinical studies to provide cardiovascular protection in postmenopausal women, we may have to rethink our current understanding, concepts, and strategies of how to interfere with the increased risk of vascular disease in women with estrogen deficiency or after menopause. serds 70-75 G protein-coupled estrogen receptor 1 Homo sapiens 164-168 23580092-2 2013 It has become apparent that GPER mediates the non-genomic signaling of 17beta-estradiol (E2) in a variety of estrogen-related cancers. Estradiol 71-87 G protein-coupled estrogen receptor 1 Homo sapiens 28-32 23580092-9 2013 Small interfering RNA (siRNA) targeting GPER and G protein inhibitor pertussin toxin (PTX) inhibited the migration and invasion of OVCAR5 cells, and also reduced the expression and activity of MMP-9. ptx 86-89 G protein-coupled estrogen receptor 1 Homo sapiens 40-44 23554355-3 2013 EXPERIMENTAL DESIGN: GPER1 expression was analyzed by immunohistochemistry in breast tumors from 273 pre- and postmenopausal stage II patients, all treated with adjuvant tamoxifen for 2 years (cohort I) and from 208 premenopausal lymph node-negative patients, of which 87% were not subjected to any adjuvant systemic treatment (cohort II). Tamoxifen 170-179 G protein-coupled estrogen receptor 1 Homo sapiens 21-26 23085545-9 2013 GPR30 mediates rapid non-genomic effects to protect neurons against injury by inhibiting p-DAPK1 dephosphorylation, which inhibits NR2B subunit phosphorylation at Ser-1303. Serine 163-166 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 23554355-8 2013 Treating HEK-R with the proteasome inhibitor epoxomicin, to decrease GPER1 degradation, further increases receptor-dependent proapoptotic signaling. epoxomicin 45-55 G protein-coupled estrogen receptor 1 Homo sapiens 69-74 23544495-0 2013 [Influence of pertussis toxin on GPER-mediated activation of phosphatidylinositol 3-kinase/protein kinase B signaling induced by 17beta-estradiol in endometrial carcinoma cells]. Estradiol 129-145 G protein-coupled estrogen receptor 1 Homo sapiens 33-37 23300088-1 2013 The estrogen 17beta-estradiol (E2) modulates dendritic spine plasticity in the cornu ammonis 1 (CA1) region of the hippocampus, and GPR30 (G-protein coupled estrogen receptor 1 (GPER1)) is an estrogen-sensitive G-protein-coupled receptor (GPCR) that is expressed in the mammalian brain and in specific subregions that are responsive to E2, including the hippocampus. Estradiol 13-29 G protein-coupled estrogen receptor 1 Homo sapiens 139-176 23544495-1 2013 OBJECTIVE: To investigate the influence of pertussis toxin (PTX) on G protein-coupled estrogen receptor (GPER)-mediated activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) signaling activated by 17beta-estradiol (17beta-E2) in endometrial carcinoma cells. Estradiol 217-233 G protein-coupled estrogen receptor 1 Homo sapiens 68-103 23544495-1 2013 OBJECTIVE: To investigate the influence of pertussis toxin (PTX) on G protein-coupled estrogen receptor (GPER)-mediated activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) signaling activated by 17beta-estradiol (17beta-E2) in endometrial carcinoma cells. Estradiol 217-233 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 23544495-1 2013 OBJECTIVE: To investigate the influence of pertussis toxin (PTX) on G protein-coupled estrogen receptor (GPER)-mediated activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) signaling activated by 17beta-estradiol (17beta-E2) in endometrial carcinoma cells. 17beta-e2 235-244 G protein-coupled estrogen receptor 1 Homo sapiens 68-103 23544495-1 2013 OBJECTIVE: To investigate the influence of pertussis toxin (PTX) on G protein-coupled estrogen receptor (GPER)-mediated activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) signaling activated by 17beta-estradiol (17beta-E2) in endometrial carcinoma cells. 17beta-e2 235-244 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 23544495-2 2013 METHODS: Expressions of GPER protein were detected by immunohistochemical SP method in Ishikawa and HEC-1A cells. TFF2 protein, human 74-76 G protein-coupled estrogen receptor 1 Homo sapiens 24-28 23544495-4 2013 RESULTS: (1) Immunohistochemical SP method showed that GPER was positive stained in cell cytoplasm of Ishikawa and HEC-1A cell. TFF2 protein, human 33-35 G protein-coupled estrogen receptor 1 Homo sapiens 55-59 23135268-5 2012 In this study, we demonstrate for the first time that 17beta-estradiol (E2) and the selective GPER ligand G-1 regulate FASN expression and activity through the GPER-mediated signaling, which involved the EGF receptor/ERK/c-Fos/AP1 transduction pathway, as ascertained by using specific pharmacological inhibitors, performing gene-silencing experiments and ChIP assays in breast SkBr3, colorectal LoVo, hepatocarcinoma HepG2 cancer cells, and breast cancer-associated fibroblasts. Estradiol 54-70 G protein-coupled estrogen receptor 1 Homo sapiens 160-164 23273253-1 2012 BACKGROUND: G-protein-coupled estrogen receptor (GPER/GPR30) was reported to bind 17beta-estradiol (E2), tamoxifen, and ICI 182,780 (fulvestrant) and promotes activation of epidermal growth factor receptor (EGFR)-mediated signaling in breast, endometrial and thyroid cancer cells. Tamoxifen 105-114 G protein-coupled estrogen receptor 1 Homo sapiens 49-53 23273253-1 2012 BACKGROUND: G-protein-coupled estrogen receptor (GPER/GPR30) was reported to bind 17beta-estradiol (E2), tamoxifen, and ICI 182,780 (fulvestrant) and promotes activation of epidermal growth factor receptor (EGFR)-mediated signaling in breast, endometrial and thyroid cancer cells. Tamoxifen 105-114 G protein-coupled estrogen receptor 1 Homo sapiens 54-59 23043685-10 2013 Treatment with 0.1 muM 17beta-estradiol increased mRNA expression of GPR30 in leiomyoma SMCs but decreased expression in myometrial SMCs. 17beta 23-29 G protein-coupled estrogen receptor 1 Homo sapiens 69-74 22453024-0 2013 Estradiol and raloxifene induce the proliferation of osteoblasts through G-protein-coupled receptor GPR30. Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 100-105 22453024-0 2013 Estradiol and raloxifene induce the proliferation of osteoblasts through G-protein-coupled receptor GPR30. Raloxifene Hydrochloride 14-24 G protein-coupled estrogen receptor 1 Homo sapiens 100-105 22453024-7 2013 CONCLUSION: GPR30 is required for the proliferation of hFOB cells induced by estradiol or raloxifene. Estradiol 77-86 G protein-coupled estrogen receptor 1 Homo sapiens 12-17 22453024-7 2013 CONCLUSION: GPR30 is required for the proliferation of hFOB cells induced by estradiol or raloxifene. Raloxifene Hydrochloride 90-100 G protein-coupled estrogen receptor 1 Homo sapiens 12-17 23273253-1 2012 BACKGROUND: G-protein-coupled estrogen receptor (GPER/GPR30) was reported to bind 17beta-estradiol (E2), tamoxifen, and ICI 182,780 (fulvestrant) and promotes activation of epidermal growth factor receptor (EGFR)-mediated signaling in breast, endometrial and thyroid cancer cells. Estradiol 82-98 G protein-coupled estrogen receptor 1 Homo sapiens 49-53 23273253-1 2012 BACKGROUND: G-protein-coupled estrogen receptor (GPER/GPR30) was reported to bind 17beta-estradiol (E2), tamoxifen, and ICI 182,780 (fulvestrant) and promotes activation of epidermal growth factor receptor (EGFR)-mediated signaling in breast, endometrial and thyroid cancer cells. Estradiol 82-98 G protein-coupled estrogen receptor 1 Homo sapiens 54-59 22552965-0 2012 Bisphenol A induces gene expression changes and proliferative effects through GPER in breast cancer cells and cancer-associated fibroblasts. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 78-82 22899172-11 2012 Pretreatment with "classic" (ERalpha and ERbeta) or "non classic" (GPR30) oestrogen receptor (ER) inhibitors (ICI182,780 and PTX, respectively) counteracted the ability of Apigenin to decrease the TNFalpha-triggered activation of the Akt pathway. ptx 125-128 G protein-coupled estrogen receptor 1 Homo sapiens 67-72 22878119-7 2012 Dydrogesterone and dienogest also significantly suppress ESR1 and ESR2 transcription, whereas medroxyprogestrone acetate and dydrogesterone significantly reduce mRNA levels of GPER. medroxyprogestrone acetate 94-120 G protein-coupled estrogen receptor 1 Homo sapiens 176-180 22878119-7 2012 Dydrogesterone and dienogest also significantly suppress ESR1 and ESR2 transcription, whereas medroxyprogestrone acetate and dydrogesterone significantly reduce mRNA levels of GPER. Dydrogesterone 125-139 G protein-coupled estrogen receptor 1 Homo sapiens 176-180 22552965-2 2012 BPA exerts estrogen-like activity by interacting with the classical estrogen receptors (ERalpha and ERbeta) and through the G protein-coupled receptor (GPR30/GPER). bisphenol A 0-3 G protein-coupled estrogen receptor 1 Homo sapiens 158-162 22552965-3 2012 In this regard, recent studies have shown that GPER was involved in the proliferative effects induced by BPA in both normal and tumor cells. bisphenol A 105-108 G protein-coupled estrogen receptor 1 Homo sapiens 47-51 22552965-2 2012 BPA exerts estrogen-like activity by interacting with the classical estrogen receptors (ERalpha and ERbeta) and through the G protein-coupled receptor (GPR30/GPER). bisphenol A 0-3 G protein-coupled estrogen receptor 1 Homo sapiens 152-157 22552965-6 2012 Specific pharmacological inhibitors and gene-silencing procedures were used to show that BPA induces the expression of the GPER target genes c-FOS, EGR-1, and CTGF through the GPER/EGFR/ERK transduction pathway in SKBR3 breast cancer cells and CAFs. bisphenol A 89-92 G protein-coupled estrogen receptor 1 Homo sapiens 123-127 22858342-10 2012 Cytosolic calcium concentration elevates faster and with higher amplitude following G-1 intracellular microinjections compared to extracellular exposure, suggesting subcellular GPER functionality. Calcium 10-17 G protein-coupled estrogen receptor 1 Homo sapiens 177-181 22552965-6 2012 Specific pharmacological inhibitors and gene-silencing procedures were used to show that BPA induces the expression of the GPER target genes c-FOS, EGR-1, and CTGF through the GPER/EGFR/ERK transduction pathway in SKBR3 breast cancer cells and CAFs. bisphenol A 89-92 G protein-coupled estrogen receptor 1 Homo sapiens 176-180 22552965-8 2012 CONCLUSIONS: Results indicate that GPER is involved in the biological action elicited by BPA in breast cancer cells and CAFs. bisphenol A 89-92 G protein-coupled estrogen receptor 1 Homo sapiens 35-39 21971420-4 2012 Finally, estradiol modulates dendritogenesis by the inhibition of Notch signaling, by a mechanism that, at least in hippocampal neurons, is mediated by G-protein coupled receptor 30. Estradiol 9-18 G protein-coupled estrogen receptor 1 Homo sapiens 152-181 22858342-11 2012 Thus, GPER activation results in spinal nociception, and the downstream mechanisms involve cytosolic calcium increase, ROS accumulation, and neuronal membrane depolarization. Calcium 101-108 G protein-coupled estrogen receptor 1 Homo sapiens 6-10 22858342-11 2012 Thus, GPER activation results in spinal nociception, and the downstream mechanisms involve cytosolic calcium increase, ROS accumulation, and neuronal membrane depolarization. Reactive Oxygen Species 119-122 G protein-coupled estrogen receptor 1 Homo sapiens 6-10 22858342-12 2012 PERSPECTIVE: Our results suggest that GPER modulates pain processing in spinal sensory neurons via cytosolic calcium increase and ROS accumulation. Calcium 109-116 G protein-coupled estrogen receptor 1 Homo sapiens 38-42 22858342-12 2012 PERSPECTIVE: Our results suggest that GPER modulates pain processing in spinal sensory neurons via cytosolic calcium increase and ROS accumulation. Reactive Oxygen Species 130-133 G protein-coupled estrogen receptor 1 Homo sapiens 38-42 22306576-4 2012 In addition to the insulinotropic action of ERbeta, the newly described estrogen receptor, GPR30, is involved in the insulinotropic effects of high doses of E2 (100nM-5muM). Estradiol 157-159 G protein-coupled estrogen receptor 1 Homo sapiens 91-96 22270964-7 2012 RESULTS: Downregulation of GPR30 led to reduced growth and invasion by cells treated with 17beta-estradiol. Estradiol 90-106 G protein-coupled estrogen receptor 1 Homo sapiens 27-32 22525040-5 2012 The combination of Expand High Fidelity(PLUS) and SYTO9 in the presence of 2.0 mM MgCl(2) produced the best separation in melting curves of mutations in all regions of the GPR30 ORF. Magnesium Chloride 82-89 G protein-coupled estrogen receptor 1 Homo sapiens 172-177 22147081-0 2012 GPER mediates the Egr-1 expression induced by 17beta-estradiol and 4-hydroxitamoxifen in breast and endometrial cancer cells. Estradiol 46-62 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 22147081-0 2012 GPER mediates the Egr-1 expression induced by 17beta-estradiol and 4-hydroxitamoxifen in breast and endometrial cancer cells. 4-hydroxitamoxifen 67-85 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 22147081-2 2012 In a microarray analysis performed in breast cancer cells, 17beta-estradiol (E2) and the estrogen receptor antagonist 4-hydroxitamoxifen (OHT) up-regulated Egr-1 through the G protein-coupled receptor named GPR30/GPER. Estradiol 59-75 G protein-coupled estrogen receptor 1 Homo sapiens 207-212 22147081-2 2012 In a microarray analysis performed in breast cancer cells, 17beta-estradiol (E2) and the estrogen receptor antagonist 4-hydroxitamoxifen (OHT) up-regulated Egr-1 through the G protein-coupled receptor named GPR30/GPER. Estradiol 59-75 G protein-coupled estrogen receptor 1 Homo sapiens 213-217 22147081-2 2012 In a microarray analysis performed in breast cancer cells, 17beta-estradiol (E2) and the estrogen receptor antagonist 4-hydroxitamoxifen (OHT) up-regulated Egr-1 through the G protein-coupled receptor named GPR30/GPER. 4-hydroxitamoxifen 118-136 G protein-coupled estrogen receptor 1 Homo sapiens 207-212 22147081-2 2012 In a microarray analysis performed in breast cancer cells, 17beta-estradiol (E2) and the estrogen receptor antagonist 4-hydroxitamoxifen (OHT) up-regulated Egr-1 through the G protein-coupled receptor named GPR30/GPER. 4-hydroxitamoxifen 118-136 G protein-coupled estrogen receptor 1 Homo sapiens 213-217 22147081-2 2012 In a microarray analysis performed in breast cancer cells, 17beta-estradiol (E2) and the estrogen receptor antagonist 4-hydroxitamoxifen (OHT) up-regulated Egr-1 through the G protein-coupled receptor named GPR30/GPER. Tamoxifen 138-141 G protein-coupled estrogen receptor 1 Homo sapiens 207-212 22147081-2 2012 In a microarray analysis performed in breast cancer cells, 17beta-estradiol (E2) and the estrogen receptor antagonist 4-hydroxitamoxifen (OHT) up-regulated Egr-1 through the G protein-coupled receptor named GPR30/GPER. Tamoxifen 138-141 G protein-coupled estrogen receptor 1 Homo sapiens 213-217 22147081-5 2012 In addition, we show that GPER mediates the expression of Egr-1 also in carcinoma-associated fibroblasts (CAFs). cafs 106-110 G protein-coupled estrogen receptor 1 Homo sapiens 26-30 22147081-7 2012 The results obtained in CAFs provide further evidence regarding the potential role exerted by the GPER-dependent Egr-1 up-regulation in tumor development and progression. cafs 24-28 G protein-coupled estrogen receptor 1 Homo sapiens 98-102 22521564-7 2012 This article represents a summary of a lecture given at the 7(th) International Meeting on Rapid Responses to Steroid Hormones in September 2011 in Axos, Crete, and reviews the current knowledge and questions about GPER-dependent signaling and function. Steroids 110-126 G protein-coupled estrogen receptor 1 Homo sapiens 215-219 22495674-3 2012 A broad literature suggests that GPR30 is a Gs-coupled heptahelical transmembrane receptor that promotes specific binding of naturally occurring and man-made estrogens but not cortisol, progesterone, or testosterone. Hydrocortisone 176-184 G protein-coupled estrogen receptor 1 Homo sapiens 33-38 22495674-3 2012 A broad literature suggests that GPR30 is a Gs-coupled heptahelical transmembrane receptor that promotes specific binding of naturally occurring and man-made estrogens but not cortisol, progesterone, or testosterone. Progesterone 186-198 G protein-coupled estrogen receptor 1 Homo sapiens 33-38 22576740-5 2012 In MCF-7 cells, the ErbB2 inhibitor, AG825, the MAPK inhibitor, PD98059, and the MEK1/2 inhibitor, U0126, blocked the HRG-beta1-induced GPR30 expression. tyrphostin AG825 37-42 G protein-coupled estrogen receptor 1 Homo sapiens 136-141 22576740-5 2012 In MCF-7 cells, the ErbB2 inhibitor, AG825, the MAPK inhibitor, PD98059, and the MEK1/2 inhibitor, U0126, blocked the HRG-beta1-induced GPR30 expression. 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one 64-71 G protein-coupled estrogen receptor 1 Homo sapiens 136-141 22576740-5 2012 In MCF-7 cells, the ErbB2 inhibitor, AG825, the MAPK inhibitor, PD98059, and the MEK1/2 inhibitor, U0126, blocked the HRG-beta1-induced GPR30 expression. U 0126 99-104 G protein-coupled estrogen receptor 1 Homo sapiens 136-141 22521737-7 2012 Thus, genistein plays a role in the regulation of MAPK activation via GPR30, and GPR30 represents a novel target regulated by steroid hormones in PDL cells. Genistein 6-15 G protein-coupled estrogen receptor 1 Homo sapiens 70-75 22521737-7 2012 Thus, genistein plays a role in the regulation of MAPK activation via GPR30, and GPR30 represents a novel target regulated by steroid hormones in PDL cells. Steroids 126-142 G protein-coupled estrogen receptor 1 Homo sapiens 81-86 22425989-0 2012 The G protein-coupled receptor GPR30 mediates the proliferative and invasive effects induced by hydroxytamoxifen in endometrial cancer cells. hydroxytamoxifen 96-112 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 22138413-4 2012 We establish that estradiol can activate GPER-cAMP/PKA signalling pathway. Estradiol 18-27 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 22387674-5 2012 17beta-estradiol signaling is mediated via estrogen receptors, including GPER1, but others receptors, such as the IGF-1 receptor, are implicated in the neuroprotective effect. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 73-78 22387674-7 2012 Compounds that stimulate GPER1 such as selective estrogen receptor modulators and phytoestrogens show neuroprotective activity and are alternatives to 17beta-estradiol. Estradiol 151-167 G protein-coupled estrogen receptor 1 Homo sapiens 25-30 22425775-6 2012 Moreover, GPR30 boosts HRG-beta1-induced migration and invasion of SkBr3 cells after combinative treatment with E2, 4-hydroxy-tamoxifen or the specific GPR30 agonist G-1, which are blocked by the specific GPR30 antagonist G-15 or the transfection with the small interfering RNA for GPR30. Estradiol 112-114 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 22425775-6 2012 Moreover, GPR30 boosts HRG-beta1-induced migration and invasion of SkBr3 cells after combinative treatment with E2, 4-hydroxy-tamoxifen or the specific GPR30 agonist G-1, which are blocked by the specific GPR30 antagonist G-15 or the transfection with the small interfering RNA for GPR30. 4'-hydroxytamoxifen 116-135 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 22260839-9 2012 Potentiation occurs at nanomolar steroid levels and depends on GPR30 and EGFR transactivation. Steroids 33-40 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 22342541-8 2012 Data from proliferation assays on the MCF-7, MDA-MB-231 and SKBr3 cell lines suggested that 7beta-OH-EpiA may also act through the membrane GPR30 receptor. 7beta-oh 92-100 G protein-coupled estrogen receptor 1 Homo sapiens 140-145 22781117-0 2012 [Effect of GPER on the activation of PI3K/Akt induced by 17beta-estradiol in endometrial carcinoma cells]. Estradiol 57-73 G protein-coupled estrogen receptor 1 Homo sapiens 11-15 22781117-1 2012 OBJECTIVE: To investigate the expression of G protein-coupled ER (GPER) and ER in the activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) induced by 17beta-estradiol (17beta-E(2))in endometrial carcinoma cells, Ishikawa and HEC-1A. Phosphatidylinositols 100-120 G protein-coupled estrogen receptor 1 Homo sapiens 44-64 22781117-1 2012 OBJECTIVE: To investigate the expression of G protein-coupled ER (GPER) and ER in the activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) induced by 17beta-estradiol (17beta-E(2))in endometrial carcinoma cells, Ishikawa and HEC-1A. Phosphatidylinositols 100-120 G protein-coupled estrogen receptor 1 Homo sapiens 66-70 22781117-1 2012 OBJECTIVE: To investigate the expression of G protein-coupled ER (GPER) and ER in the activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) induced by 17beta-estradiol (17beta-E(2))in endometrial carcinoma cells, Ishikawa and HEC-1A. Estradiol 171-187 G protein-coupled estrogen receptor 1 Homo sapiens 44-64 22781117-1 2012 OBJECTIVE: To investigate the expression of G protein-coupled ER (GPER) and ER in the activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) induced by 17beta-estradiol (17beta-E(2))in endometrial carcinoma cells, Ishikawa and HEC-1A. Estradiol 171-187 G protein-coupled estrogen receptor 1 Homo sapiens 66-70 22781117-1 2012 OBJECTIVE: To investigate the expression of G protein-coupled ER (GPER) and ER in the activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) induced by 17beta-estradiol (17beta-E(2))in endometrial carcinoma cells, Ishikawa and HEC-1A. 17beta-e 189-197 G protein-coupled estrogen receptor 1 Homo sapiens 44-64 22781117-1 2012 OBJECTIVE: To investigate the expression of G protein-coupled ER (GPER) and ER in the activation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) induced by 17beta-estradiol (17beta-E(2))in endometrial carcinoma cells, Ishikawa and HEC-1A. 17beta-e 189-197 G protein-coupled estrogen receptor 1 Homo sapiens 66-70 22138413-4 2012 We establish that estradiol can activate GPER-cAMP/PKA signalling pathway. Cyclic AMP 46-50 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 22251451-0 2012 MIBE acts as antagonist ligand of both estrogen receptor alpha and GPER in breast cancer cells. mibe 0-4 G protein-coupled estrogen receptor 1 Homo sapiens 67-71 22027943-2 2012 The aim of this study was to determine the effects of long-term tibolone (TIB) treatment in comparison with conventional hormone therapy on the expression and distribution of estrogen receptor (ER) alpha, ER-beta, G-protein-coupled ER-1 (GPER), progesterone receptor (PR) A, PRB, androgen receptor (AR), and syndecan-1 in the macaque uterus. tibolone 74-77 G protein-coupled estrogen receptor 1 Homo sapiens 214-236 22027943-2 2012 The aim of this study was to determine the effects of long-term tibolone (TIB) treatment in comparison with conventional hormone therapy on the expression and distribution of estrogen receptor (ER) alpha, ER-beta, G-protein-coupled ER-1 (GPER), progesterone receptor (PR) A, PRB, androgen receptor (AR), and syndecan-1 in the macaque uterus. tibolone 74-77 G protein-coupled estrogen receptor 1 Homo sapiens 238-242 22027943-0 2012 Effects of long-term tibolone treatment on nuclear sex steroid hormone receptors and G-protein-coupled estrogen receptor-1 expression in the macaque uterus. tibolone 21-29 G protein-coupled estrogen receptor 1 Homo sapiens 85-122 22027943-2 2012 The aim of this study was to determine the effects of long-term tibolone (TIB) treatment in comparison with conventional hormone therapy on the expression and distribution of estrogen receptor (ER) alpha, ER-beta, G-protein-coupled ER-1 (GPER), progesterone receptor (PR) A, PRB, androgen receptor (AR), and syndecan-1 in the macaque uterus. tibolone 64-72 G protein-coupled estrogen receptor 1 Homo sapiens 214-236 22027943-2 2012 The aim of this study was to determine the effects of long-term tibolone (TIB) treatment in comparison with conventional hormone therapy on the expression and distribution of estrogen receptor (ER) alpha, ER-beta, G-protein-coupled ER-1 (GPER), progesterone receptor (PR) A, PRB, androgen receptor (AR), and syndecan-1 in the macaque uterus. tibolone 64-72 G protein-coupled estrogen receptor 1 Homo sapiens 238-242 22330739-6 2012 However, activation of GPER protects beta cells from apoptosis, raises glucose-stimulated insulin secretion and lipid homeostasis without affecting insulin biosynthesis. Glucose 71-78 G protein-coupled estrogen receptor 1 Homo sapiens 23-27 22251451-6 2012 We synthesized a novel compound (ethyl 3-[5-(2-ethoxycarbonyl-1-methylvinyloxy)-1-methyl-1H-indol-3-yl]but-2-enoate), referred to as MIBE, and investigated its properties elicited through ERalpha and GPER in breast cancer cells. ethyl 3-[5-(2-ethoxycarbonyl-1-methylvinyloxy)-1-methyl-1h-indol-3-yl]but-2-enoate 33-115 G protein-coupled estrogen receptor 1 Homo sapiens 200-204 23077529-4 2012 We have designed and synthesized a series of organometallic tricarbonyl-rhenium complexes conjugated to a GPER-selective small molecule derived from tetrahydro-3H-cyclopenta[c]quinoline. quinoline 176-185 G protein-coupled estrogen receptor 1 Homo sapiens 106-110 23285198-9 2012 N-3 PUFA treatment initiated the pro-apoptotic signaling of estrogen by increasing GPER1-cAMP-PKA signaling response, and blunting EGFR, Erk 1/2, and AKT activity. Cyclic AMP 89-93 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 23077529-0 2012 Synthesis and characterization of tricarbonyl-Re/Tc(I) chelate probes targeting the G protein-coupled estrogen receptor GPER/GPR30. tricarbonyl-re 34-48 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 21312194-0 2012 Bisphenol A promotes testicular seminoma cell proliferation through GPER/GPR30. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 68-72 21312194-0 2012 Bisphenol A promotes testicular seminoma cell proliferation through GPER/GPR30. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 73-78 21802511-0 2011 Diacylglycerol kinase alpha mediates 17-beta-estradiol-induced proliferation, motility, and anchorage-independent growth of Hec-1A endometrial cancer cell line through the G protein-coupled estrogen receptor GPR30. Estradiol 37-54 G protein-coupled estrogen receptor 1 Homo sapiens 208-213 23077529-0 2012 Synthesis and characterization of tricarbonyl-Re/Tc(I) chelate probes targeting the G protein-coupled estrogen receptor GPER/GPR30. tricarbonyl-re 34-48 G protein-coupled estrogen receptor 1 Homo sapiens 125-130 23077529-0 2012 Synthesis and characterization of tricarbonyl-Re/Tc(I) chelate probes targeting the G protein-coupled estrogen receptor GPER/GPR30. Technetium 49-51 G protein-coupled estrogen receptor 1 Homo sapiens 120-124 23077529-0 2012 Synthesis and characterization of tricarbonyl-Re/Tc(I) chelate probes targeting the G protein-coupled estrogen receptor GPER/GPR30. Technetium 49-51 G protein-coupled estrogen receptor 1 Homo sapiens 125-130 23077529-4 2012 We have designed and synthesized a series of organometallic tricarbonyl-rhenium complexes conjugated to a GPER-selective small molecule derived from tetrahydro-3H-cyclopenta[c]quinoline. tricarbonyl-rhenium 60-79 G protein-coupled estrogen receptor 1 Homo sapiens 106-110 23077529-4 2012 We have designed and synthesized a series of organometallic tricarbonyl-rhenium complexes conjugated to a GPER-selective small molecule derived from tetrahydro-3H-cyclopenta[c]quinoline. tetrahydro-3h-cyclopenta 149-173 G protein-coupled estrogen receptor 1 Homo sapiens 106-110 22295107-5 2012 The treatment with estradiol (E2), anti-estrogenic agents 4-hydroxytamoxifen and ICI 182780, ERbeta specific ligand DPN and GPR30 agonist G1 led to a rapid activation of p-ERK1/2, suggesting the involvement of ERalpha36, ERbeta and GPR30 in the non-genomic signaling pathway in these cells. Estradiol 19-28 G protein-coupled estrogen receptor 1 Homo sapiens 232-237 22295107-5 2012 The treatment with estradiol (E2), anti-estrogenic agents 4-hydroxytamoxifen and ICI 182780, ERbeta specific ligand DPN and GPR30 agonist G1 led to a rapid activation of p-ERK1/2, suggesting the involvement of ERalpha36, ERbeta and GPR30 in the non-genomic signaling pathway in these cells. hydroxytamoxifen 58-76 G protein-coupled estrogen receptor 1 Homo sapiens 232-237 22295107-5 2012 The treatment with estradiol (E2), anti-estrogenic agents 4-hydroxytamoxifen and ICI 182780, ERbeta specific ligand DPN and GPR30 agonist G1 led to a rapid activation of p-ERK1/2, suggesting the involvement of ERalpha36, ERbeta and GPR30 in the non-genomic signaling pathway in these cells. Fulvestrant 81-91 G protein-coupled estrogen receptor 1 Homo sapiens 232-237 22295107-5 2012 The treatment with estradiol (E2), anti-estrogenic agents 4-hydroxytamoxifen and ICI 182780, ERbeta specific ligand DPN and GPR30 agonist G1 led to a rapid activation of p-ERK1/2, suggesting the involvement of ERalpha36, ERbeta and GPR30 in the non-genomic signaling pathway in these cells. NAD 116-119 G protein-coupled estrogen receptor 1 Homo sapiens 232-237 21791623-10 2011 In summary, GPER activation relaxes coronary artery smooth muscle by increasing potassium efflux via BK(Ca) channels and requires an intact cellular signaling mechanism. Potassium 80-89 G protein-coupled estrogen receptor 1 Homo sapiens 12-16 21782022-2 2011 We have previously described both a GPER-selective agonist G-1 and antagonist G15 based on a tetrahydro-3H-cyclopenta[c]quinoline scaffold. SCHEMBL915978 93-129 G protein-coupled estrogen receptor 1 Homo sapiens 36-40 21942929-4 2011 AREAS COVERED: The article aims to review the available evidence relating to the pharmacokinetics, tolerability and efficacy of extended-release gabapentin (GpER). Gabapentin 145-155 G protein-coupled estrogen receptor 1 Homo sapiens 157-161 22031799-3 2011 METHODS: Immunohistochemistry was used to detect GPER in paraffin-embedded tissues of primary breast cancers from 423 patients and GPER expression was correlated with clinicopathological factors. Paraffin 57-65 G protein-coupled estrogen receptor 1 Homo sapiens 49-53 21809103-1 2011 Estradiol and progesterone mediate their actions by binding to classical nuclear receptors, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta) and progesterone receptor A and B (PR-A and PR-B) and the non-classical G protein-coupled estrogen receptor (GPER). Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 234-269 21809103-1 2011 Estradiol and progesterone mediate their actions by binding to classical nuclear receptors, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta) and progesterone receptor A and B (PR-A and PR-B) and the non-classical G protein-coupled estrogen receptor (GPER). Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 271-275 21844907-5 2011 However, 17beta-estradiol also mediates rapid signaling events via pathways that involve transmembrane ERs, such as G-protein-coupled ER 1 (GPER; formerly known as GPR30). Estradiol 9-25 G protein-coupled estrogen receptor 1 Homo sapiens 116-138 21844907-5 2011 However, 17beta-estradiol also mediates rapid signaling events via pathways that involve transmembrane ERs, such as G-protein-coupled ER 1 (GPER; formerly known as GPR30). Estradiol 9-25 G protein-coupled estrogen receptor 1 Homo sapiens 140-144 21844907-5 2011 However, 17beta-estradiol also mediates rapid signaling events via pathways that involve transmembrane ERs, such as G-protein-coupled ER 1 (GPER; formerly known as GPR30). Estradiol 9-25 G protein-coupled estrogen receptor 1 Homo sapiens 164-169 22319655-5 2011 Moreover, it is noteworthy that GPR 30 (a transmembrane ER) induces rapid responses after estradiol binding, which, in turn, modulates cyclins and proapoptotic factors (e.g., BAX) to affect germ cell cycle progression and apoptosis. Estradiol 90-99 G protein-coupled estrogen receptor 1 Homo sapiens 32-38 21607586-1 2011 Recently, we have shown that the new G-protein-coupled estrogen receptor GPR30 plays an important role in the development of tamoxifen resistance in vitro. Tamoxifen 125-134 G protein-coupled estrogen receptor 1 Homo sapiens 73-78 21607586-2 2011 This study was undertaken to evaluate the correlation between GPR30 and tamoxifen resistance in breast cancer patients. Tamoxifen 72-81 G protein-coupled estrogen receptor 1 Homo sapiens 62-67 21607586-4 2011 The association between GPR30 expression and tamoxifen resistance was confirmed in a second cohort of 103 patients treated only with tamoxifen. Tamoxifen 45-54 G protein-coupled estrogen receptor 1 Homo sapiens 24-29 21607586-4 2011 The association between GPR30 expression and tamoxifen resistance was confirmed in a second cohort of 103 patients treated only with tamoxifen. Tamoxifen 133-142 G protein-coupled estrogen receptor 1 Homo sapiens 24-29 21607586-7 2011 In a first cohort, survival analysis showed that GPR30 was negatively correlated with relapse-free survival (RFS) only in patients treated with tamoxifen (tamoxifen with or without chemotherapy). Tamoxifen 144-153 G protein-coupled estrogen receptor 1 Homo sapiens 49-54 21607586-7 2011 In a first cohort, survival analysis showed that GPR30 was negatively correlated with relapse-free survival (RFS) only in patients treated with tamoxifen (tamoxifen with or without chemotherapy). Tamoxifen 155-164 G protein-coupled estrogen receptor 1 Homo sapiens 49-54 21607586-9 2011 In a subset of patients treated only with tamoxifen, multivariate analysis revealed that GPR30 expression is an independent unfavorable factor for RFS (HR = 4.440; 95% CI, 1.408-13.997; P = 0.011). Tamoxifen 42-51 G protein-coupled estrogen receptor 1 Homo sapiens 89-94 21607586-11 2011 In 33 paired biopsies obtained before and after adjuvant therapy, GPR30 expression significantly increased only under tamoxifen treatment (P = 0.001). Tamoxifen 118-127 G protein-coupled estrogen receptor 1 Homo sapiens 66-71 21607586-12 2011 GPR30 expression in breast cancer independently predicts a poor RFS in patients treated with tamoxifen. Tamoxifen 93-102 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 21300668-5 2011 Treatment of cells with pertussis toxin or inhibition of GPR30/epidermal growth factor receptor kinase transactivation prevented equol-induced activation of extracellular signal-regulated kinase 1/2 via c-Src, Akt, and eNOS. Equol 129-134 G protein-coupled estrogen receptor 1 Homo sapiens 57-62 21354433-2 2011 GPER promotes estrogen binding and rapid signaling via membrane-associated enzymes resulting in increased cAMP and release of heparan bound epidermal growth factor (proHB-EGF) from breast cancer cells. Cyclic AMP 106-110 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 21354433-2 2011 GPER promotes estrogen binding and rapid signaling via membrane-associated enzymes resulting in increased cAMP and release of heparan bound epidermal growth factor (proHB-EGF) from breast cancer cells. heparan 126-133 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 21354433-5 2011 Upon ectopic expression in human embryonic kidney HEK-293 cells, functional GPER is generated as these cells acquire the capacity to stimulate cAMP and activate cyclic AMP responsive binding protein in response to estradiol-17 beta stimulation. Cyclic AMP 143-147 G protein-coupled estrogen receptor 1 Homo sapiens 76-80 21354433-5 2011 Upon ectopic expression in human embryonic kidney HEK-293 cells, functional GPER is generated as these cells acquire the capacity to stimulate cAMP and activate cyclic AMP responsive binding protein in response to estradiol-17 beta stimulation. Cyclic AMP 161-171 G protein-coupled estrogen receptor 1 Homo sapiens 76-80 21354433-5 2011 Upon ectopic expression in human embryonic kidney HEK-293 cells, functional GPER is generated as these cells acquire the capacity to stimulate cAMP and activate cyclic AMP responsive binding protein in response to estradiol-17 beta stimulation. Estradiol 214-223 G protein-coupled estrogen receptor 1 Homo sapiens 76-80 21354433-5 2011 Upon ectopic expression in human embryonic kidney HEK-293 cells, functional GPER is generated as these cells acquire the capacity to stimulate cAMP and activate cyclic AMP responsive binding protein in response to estradiol-17 beta stimulation. 17 beta 224-231 G protein-coupled estrogen receptor 1 Homo sapiens 76-80 21545416-5 2011 GPR30, now designated as GPER-1 (http://www.iuphar-db.org/DATABASE/FamilyIntroductionForward?familyId=22), a newly characterized "orphan receptor", has been implicated in mediating the rapid effects of estradiol and most recently those of aldosterone. Estradiol 202-211 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 21545416-5 2011 GPR30, now designated as GPER-1 (http://www.iuphar-db.org/DATABASE/FamilyIntroductionForward?familyId=22), a newly characterized "orphan receptor", has been implicated in mediating the rapid effects of estradiol and most recently those of aldosterone. Estradiol 202-211 G protein-coupled estrogen receptor 1 Homo sapiens 25-31 21545416-5 2011 GPR30, now designated as GPER-1 (http://www.iuphar-db.org/DATABASE/FamilyIntroductionForward?familyId=22), a newly characterized "orphan receptor", has been implicated in mediating the rapid effects of estradiol and most recently those of aldosterone. Aldosterone 239-250 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 21545416-5 2011 GPR30, now designated as GPER-1 (http://www.iuphar-db.org/DATABASE/FamilyIntroductionForward?familyId=22), a newly characterized "orphan receptor", has been implicated in mediating the rapid effects of estradiol and most recently those of aldosterone. Aldosterone 239-250 G protein-coupled estrogen receptor 1 Homo sapiens 25-31 21540189-7 2011 GPER is ubiquitinated at the cell surface, exhibits a short half-life (t1/2;) <1 h), and is protected from degradation by the proteasome inhibitor, MG132. benzyloxycarbonylleucyl-leucyl-leucine aldehyde 151-156 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 21540189-8 2011 Disruption of the TGN by brefeldin A induces the accumulation of endocytosed GPER in Rab11+ perinuclear endosomes and prevents GPER degradation. Brefeldin A 25-36 G protein-coupled estrogen receptor 1 Homo sapiens 77-81 21540189-8 2011 Disruption of the TGN by brefeldin A induces the accumulation of endocytosed GPER in Rab11+ perinuclear endosomes and prevents GPER degradation. Brefeldin A 25-36 G protein-coupled estrogen receptor 1 Homo sapiens 127-131 21493710-5 2011 Genistein can also activate signaling through GPR30, a G-protein-coupled cell surface receptor. Genistein 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 46-51 21493710-7 2011 We show herein that nanomolar concentrations of genistein induce ASAH1 transcription through a GPR30-dependent, pertussis toxin-sensitive pathway that requires the activation of c-Src and extracellular signal regulated kinase 1/2 (ERK1/2). Genistein 48-57 G protein-coupled estrogen receptor 1 Homo sapiens 95-100 21660819-11 2011 Atrazine does not appear to interact strongly with estrogen receptors alpha or beta but may interact with putative estrogen receptor GPR30 (G-protein-coupled receptor). Atrazine 0-8 G protein-coupled estrogen receptor 1 Homo sapiens 133-138 21278053-8 2011 Instead, Akt and ERK1/2 phosphorylation induced by dieldrin in CGC was mediated by multiple activation of ERalpha, ERbeta, and G protein-coupled receptor 30. Dieldrin 51-59 G protein-coupled estrogen receptor 1 Homo sapiens 127-156 21138734-8 2011 We hypothesize that GPR30 plays an important role in mediating direct effects of estradiol on basal forebrain cholinergic neurons, with corresponding effects on cognitive performance. Estradiol 81-90 G protein-coupled estrogen receptor 1 Homo sapiens 20-25 21266576-5 2011 Moreover, we show that HIF-1alpha-responsive elements located within the promoter region of GPER are involved in hypoxia-dependent transcription of GPER, which requires the ROS-induced activation of EGFR/ERK signaling in both SkBr3 and HL-1 and cells. ros 173-176 G protein-coupled estrogen receptor 1 Homo sapiens 92-96 21266576-5 2011 Moreover, we show that HIF-1alpha-responsive elements located within the promoter region of GPER are involved in hypoxia-dependent transcription of GPER, which requires the ROS-induced activation of EGFR/ERK signaling in both SkBr3 and HL-1 and cells. ros 173-176 G protein-coupled estrogen receptor 1 Homo sapiens 148-152 21266576-7 2011 Taken together, our data suggest that the hypoxia-induced expression of GPER may be included among the mechanisms involved in the anti-apoptotic effects elicited by estrogens, particularly in a low oxygen microenvironment. Oxygen 198-204 G protein-coupled estrogen receptor 1 Homo sapiens 72-76 20875696-0 2011 Bisphenol A induces a rapid activation of Erk1/2 through GPR30 in human breast cancer cells. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 57-62 21149639-9 2011 We conclude that GPER1-mediated stimulation of cAMP production and beta-arrestin2 recruitment occur in the PM. Cyclic AMP 47-51 G protein-coupled estrogen receptor 1 Homo sapiens 17-22 21278491-1 2011 GPR30 is a 7-transmembrane G protein-coupled estrogen receptor that functions alongside traditional estrogen receptors to regulate cellular responses to 17beta-estradiol and environmental estrogens. Estradiol 153-169 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 21242460-0 2011 GPR30 expression is required for the mineralocorticoid receptor-independent rapid vascular effects of aldosterone. Aldosterone 102-113 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 21242460-5 2011 The present studies were undertaken to test the hypothesis that the rapid response to aldosterone in smooth muscle is dependent on the availability of a GPR30-dependent signaling pathway. Aldosterone 86-97 G protein-coupled estrogen receptor 1 Homo sapiens 153-158 20875696-7 2011 As a conclusion, GPR30 plays an important role in the BPA-induced activation of Erk1/2 in a manner distinguishable from that in ERalpha-mediated signaling. bisphenol A 54-57 G protein-coupled estrogen receptor 1 Homo sapiens 17-22 20568229-11 2010 We also observed that, CCL18 interferes with the activation of GPR30 by previously identified ligands (17beta-estradiol and chemical agonists). Estradiol 103-119 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 24999376-4 2011 Using knock-out animals or drugs selectively targeting GPER/GPR30, a significant role for this receptor as a mediator of acute estrogen-dependent vasodilation involving nitric oxide (NO) and blood pressure-lowering activity has been demonstrated. Nitric Oxide 169-181 G protein-coupled estrogen receptor 1 Homo sapiens 55-59 24999376-4 2011 Using knock-out animals or drugs selectively targeting GPER/GPR30, a significant role for this receptor as a mediator of acute estrogen-dependent vasodilation involving nitric oxide (NO) and blood pressure-lowering activity has been demonstrated. Nitric Oxide 169-181 G protein-coupled estrogen receptor 1 Homo sapiens 60-65 20508064-11 2010 The cyclic variations of GPER mRNA obviously relate to strong epithelial expression in the proliferative phase, and the expression pattern suggests regulation by ovarian steroids. Steroids 170-178 G protein-coupled estrogen receptor 1 Homo sapiens 25-29 19931550-1 2010 Recent studies by several research groups have shown that G protein estrogen receptor-1 (GPER) formerly known as GPR30, mediates 17beta-estradiol (E2) activation of signal transduction pathways in a variety of human cancer cells and displays E2 binding typical of a membrane estrogen receptor. Estradiol 129-145 G protein-coupled estrogen receptor 1 Homo sapiens 58-87 19911269-0 2010 Role of GPR30 in the mechanisms of tamoxifen resistance in breast cancer MCF-7 cells. Tamoxifen 35-44 G protein-coupled estrogen receptor 1 Homo sapiens 8-13 19911269-4 2010 These tamoxifen-resistant cells (TAM-R) exhibited enhanced sensitivity to 17-ss-estradiol and GPR30 agonist, G1, when compared to the parental cells. Tamoxifen 6-15 G protein-coupled estrogen receptor 1 Homo sapiens 94-99 19911269-4 2010 These tamoxifen-resistant cells (TAM-R) exhibited enhanced sensitivity to 17-ss-estradiol and GPR30 agonist, G1, when compared to the parental cells. tam-r 33-38 G protein-coupled estrogen receptor 1 Homo sapiens 94-99 19911269-6 2010 These effects were abolished by EGFR inhibitor AG1478, GPR30 anti-sense oligonucleotide, and the selective c-Src inhibitor PP2. Oligonucleotides 72-87 G protein-coupled estrogen receptor 1 Homo sapiens 55-60 19911269-9 2010 Continuous treatment of MCF-7 cells with GPR30 agonist G1 mimics the long-term treatment with tamoxifen and increases drastically its agonistic activity. Tamoxifen 94-103 G protein-coupled estrogen receptor 1 Homo sapiens 41-46 19911269-10 2010 This data suggests the important role of GPR30/EGFR receptor signaling in the development of tamoxifen resistance. Tamoxifen 93-102 G protein-coupled estrogen receptor 1 Homo sapiens 41-46 19931550-1 2010 Recent studies by several research groups have shown that G protein estrogen receptor-1 (GPER) formerly known as GPR30, mediates 17beta-estradiol (E2) activation of signal transduction pathways in a variety of human cancer cells and displays E2 binding typical of a membrane estrogen receptor. Estradiol 129-145 G protein-coupled estrogen receptor 1 Homo sapiens 89-93 19931550-1 2010 Recent studies by several research groups have shown that G protein estrogen receptor-1 (GPER) formerly known as GPR30, mediates 17beta-estradiol (E2) activation of signal transduction pathways in a variety of human cancer cells and displays E2 binding typical of a membrane estrogen receptor. Estradiol 129-145 G protein-coupled estrogen receptor 1 Homo sapiens 113-118 19931550-7 2010 The comparisons show that croaker and human GPER have very similar estrogen binding characteristics, typical of estrogen membrane receptors, and activate the same estrogen signaling pathways via stimulatory G proteins (Gs) resulting in increased cAMP production. Cyclic AMP 246-250 G protein-coupled estrogen receptor 1 Homo sapiens 44-48 19472088-5 2010 This effect may be due to up-regulation of G-coupled estrogen receptor, GPR30, which is activated by tamoxifen. Tamoxifen 101-110 G protein-coupled estrogen receptor 1 Homo sapiens 72-77 20551055-0 2010 Nuclear alternate estrogen receptor GPR30 mediates 17beta-estradiol-induced gene expression and migration in breast cancer-associated fibroblasts. 17beta 51-57 G protein-coupled estrogen receptor 1 Homo sapiens 36-41 20551055-0 2010 Nuclear alternate estrogen receptor GPR30 mediates 17beta-estradiol-induced gene expression and migration in breast cancer-associated fibroblasts. Estradiol 58-67 G protein-coupled estrogen receptor 1 Homo sapiens 36-41 20486699-4 2010 Therefore, we developed a series of GPR30-targeted (111/113)In(III)-labeled analogues using macrocyclic and acyclic polyamino-polycarboxylate chelate designs that would render either a net negative or neutral charge. polyamino-polycarboxylate 116-141 G protein-coupled estrogen receptor 1 Homo sapiens 36-41 20456608-12 2010 Third, oestradiol causes rapid, direct, excitatory action in GnRH neurones and this action of oestradiol appears to be mediated through a membrane receptor, such as G-protein coupled receptor 30. Estradiol 7-17 G protein-coupled estrogen receptor 1 Homo sapiens 165-194 20456608-12 2010 Third, oestradiol causes rapid, direct, excitatory action in GnRH neurones and this action of oestradiol appears to be mediated through a membrane receptor, such as G-protein coupled receptor 30. Estradiol 94-104 G protein-coupled estrogen receptor 1 Homo sapiens 165-194 20138962-0 2010 Estriol acts as a GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol 0-7 G protein-coupled estrogen receptor 1 Homo sapiens 18-23 20401403-0 2010 Highly efficient synthesis and characterization of the GPR30-selective agonist G-1 and related tetrahydroquinoline analogs. 1,2,3,4-tetrahydroquinoline 95-114 G protein-coupled estrogen receptor 1 Homo sapiens 55-60 20153348-0 2010 The membrane estrogen receptor GPR30 mediates cadmium-induced proliferation of breast cancer cells. Cadmium 46-53 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 20153348-4 2010 Here, we have investigated whether the newly appreciated transmembrane estrogen receptor, G-protein coupled receptor 30 (GPR30), may be involved in Cd-induced cell proliferation. Cadmium 148-150 G protein-coupled estrogen receptor 1 Homo sapiens 90-119 20153348-4 2010 Here, we have investigated whether the newly appreciated transmembrane estrogen receptor, G-protein coupled receptor 30 (GPR30), may be involved in Cd-induced cell proliferation. Cadmium 148-150 G protein-coupled estrogen receptor 1 Homo sapiens 121-126 20153348-10 2010 These results demonstrate that Cd-induced breast cancer cell proliferation occurs through GPR30-mediated activation in a manner that is similar to that achieved by estrogen in these cells. Cadmium 31-33 G protein-coupled estrogen receptor 1 Homo sapiens 90-95 20401403-1 2010 The GPR30 agonist probe G-1 and structural analogs were efficiently synthesized using multicomponent or stepwise Sc(III)-catalyzed aza-Diels-Alder cyclization. aza-diels 131-140 G protein-coupled estrogen receptor 1 Homo sapiens 4-9 20211987-11 2010 These findings provide insight into the molecular mechanisms of GPER-1/ERRalpha-mediated signaling and may be relevant to what happens in breast cancer cells escaping inhibitory control by TAM. Tamoxifen 189-192 G protein-coupled estrogen receptor 1 Homo sapiens 64-70 19741198-0 2009 Estradiol-mediated ERK phosphorylation and apoptosis in vascular smooth muscle cells requires GPR 30. Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 94-100 20041667-0 2010 Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30. 1,2,3,4-tetrahydroquinoline 44-64 G protein-coupled estrogen receptor 1 Homo sapiens 115-120 20041667-1 2010 A series of iodo-substituted tetrahydro-3H-cyclopenta[c]quinolines was synthesized as potential targeted imaging agents for the G protein-coupled estrogen receptor GPR30. iodo-substituted tetrahydro-3h-cyclopenta[c]quinolines 12-66 G protein-coupled estrogen receptor 1 Homo sapiens 164-169 20041667-3 2010 Selected iodo-substituted tetrahydro-3H-cyclopenta[c]quinolines exhibited IC(50) values lower than 20 nM in competitive binding studies with GPR30-expressing human endometrial cancer cells. iodo-substituted tetrahydro-3h-cyclopenta[c]quinolines 9-63 G protein-coupled estrogen receptor 1 Homo sapiens 141-146 20041667-4 2010 These compounds functioned as antagonists of GPR30 and blocked estrogen-induced PI3K activation and calcium mobilization. Calcium 100-107 G protein-coupled estrogen receptor 1 Homo sapiens 45-50 20086172-6 2010 In Ca(2+) mobilization studies, GPR30, but not ERalpha, mediated E(2)-induced Ca(2+) responses because E(2), 4-hydroxytamoxifen (activates GPR30), and G-1, but not DES, elicited cytosolic Ca(2+) increases not only in MCF-7 cells but also in ER-negative SKBr3 cells. hydroxytamoxifen 109-127 G protein-coupled estrogen receptor 1 Homo sapiens 139-144 20086172-7 2010 Additionally, in MCF-7 cells, GPR30 depletion blocked E(2)-induced and G-1-induced Ca(2+) mobilization, but ERalpha depletion did not. Estradiol 54-58 G protein-coupled estrogen receptor 1 Homo sapiens 30-35 20639684-6 2010 Both GPER agonists attenuated contractions to endothelin-1 (p < 0.05 vs. ethanol), but not to serotonin (n.s.). Ethanol 76-83 G protein-coupled estrogen receptor 1 Homo sapiens 5-9 20197310-5 2010 Both 17beta-estradiol (E2) and G1, a compound reported to be a selective GPR30 agonist, increased the phosphorylation levels of the MAPK/ERK1/2 in SK-BR-3 cells, which could be blocked by an anti-ER-alpha36-specific antibody against its ligand-binding domain. Estradiol 5-21 G protein-coupled estrogen receptor 1 Homo sapiens 73-78 20086172-1 2010 The G protein-coupled receptor GPR30 binds 17beta-estradiol (E(2)) yet differs from classic estrogen receptors (ERalpha and ERbeta). Estradiol 43-59 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 20086172-2 2010 GPR30 can mediate E(2)-induced nongenomic signaling, but its role in ERalpha-positive breast cancer remains unclear. Estradiol 18-22 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 20086172-4 2010 We therefore examined GPR30 in estrogenic activities in ER-positive MCF-7 breast cancer cells using G-1 and diethylstilbestrol (DES), ligands that selectively activate GPR30 and ER, respectively, and small interfering RNAs. Diethylstilbestrol 108-126 G protein-coupled estrogen receptor 1 Homo sapiens 22-27 20086172-4 2010 We therefore examined GPR30 in estrogenic activities in ER-positive MCF-7 breast cancer cells using G-1 and diethylstilbestrol (DES), ligands that selectively activate GPR30 and ER, respectively, and small interfering RNAs. Diethylstilbestrol 128-131 G protein-coupled estrogen receptor 1 Homo sapiens 22-27 20086172-4 2010 We therefore examined GPR30 in estrogenic activities in ER-positive MCF-7 breast cancer cells using G-1 and diethylstilbestrol (DES), ligands that selectively activate GPR30 and ER, respectively, and small interfering RNAs. Diethylstilbestrol 128-131 G protein-coupled estrogen receptor 1 Homo sapiens 168-173 20086172-6 2010 In Ca(2+) mobilization studies, GPR30, but not ERalpha, mediated E(2)-induced Ca(2+) responses because E(2), 4-hydroxytamoxifen (activates GPR30), and G-1, but not DES, elicited cytosolic Ca(2+) increases not only in MCF-7 cells but also in ER-negative SKBr3 cells. Estradiol 65-69 G protein-coupled estrogen receptor 1 Homo sapiens 32-37 20086172-6 2010 In Ca(2+) mobilization studies, GPR30, but not ERalpha, mediated E(2)-induced Ca(2+) responses because E(2), 4-hydroxytamoxifen (activates GPR30), and G-1, but not DES, elicited cytosolic Ca(2+) increases not only in MCF-7 cells but also in ER-negative SKBr3 cells. Estradiol 103-107 G protein-coupled estrogen receptor 1 Homo sapiens 32-37 20086172-6 2010 In Ca(2+) mobilization studies, GPR30, but not ERalpha, mediated E(2)-induced Ca(2+) responses because E(2), 4-hydroxytamoxifen (activates GPR30), and G-1, but not DES, elicited cytosolic Ca(2+) increases not only in MCF-7 cells but also in ER-negative SKBr3 cells. hydroxytamoxifen 109-127 G protein-coupled estrogen receptor 1 Homo sapiens 32-37 19741198-1 2009 Recent studies suggest that the rapid and nongenomic effects of estradiol may be mediated through the G protein-coupled receptor dubbed GPR30 receptor. Estradiol 64-73 G protein-coupled estrogen receptor 1 Homo sapiens 136-141 19741198-2 2009 The present study examines the role of GPR30 versus a classical estrogen receptor (ERalpha) in mediating the growth regulatory effects of estradiol. Estradiol 138-147 G protein-coupled estrogen receptor 1 Homo sapiens 39-44 19741198-6 2009 Transfer of the genes encoding GPR30 led to estradiol stimulation of ERK phosphorylation, which is opposite the effects of estradiol in the primary culture of VSMCs. Estradiol 44-53 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 19741198-6 2009 Transfer of the genes encoding GPR30 led to estradiol stimulation of ERK phosphorylation, which is opposite the effects of estradiol in the primary culture of VSMCs. Estradiol 123-132 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 19741198-6 2009 Transfer of the genes encoding GPR30 led to estradiol stimulation of ERK phosphorylation, which is opposite the effects of estradiol in the primary culture of VSMCs. vsmcs 159-164 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 19741198-8 2009 Estradiol-mediated stimulation of ERK subsequent to heterologous GPR30 expression was pertussis toxin sensitive and phosphoinositide 3-kinase (PI3 kinase) dependent; under these conditions, estradiol also inhibited protein kinase A (PKA). Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 65-70 19741198-8 2009 Estradiol-mediated stimulation of ERK subsequent to heterologous GPR30 expression was pertussis toxin sensitive and phosphoinositide 3-kinase (PI3 kinase) dependent; under these conditions, estradiol also inhibited protein kinase A (PKA). Estradiol 190-199 G protein-coupled estrogen receptor 1 Homo sapiens 65-70 19464786-4 2009 Not only does GPR30 mediate some of the rapid signal transduction events following cell stimulation, such as calcium mobilization and kinase activation, it also appears to regulate rapid transcriptional activation of genes such as c-fos. Calcium 109-116 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 19749156-2 2009 We demonstrate that epidermal growth factor (EGF) and TGF alpha transactivate the GPR30 promoter and accordingly up-regulate GPR30 mRNA and protein levels only in endometrial and tamoxifen-resistant breast cancer cells. Tamoxifen 179-188 G protein-coupled estrogen receptor 1 Homo sapiens 82-87 19749156-2 2009 We demonstrate that epidermal growth factor (EGF) and TGF alpha transactivate the GPR30 promoter and accordingly up-regulate GPR30 mRNA and protein levels only in endometrial and tamoxifen-resistant breast cancer cells. Tamoxifen 179-188 G protein-coupled estrogen receptor 1 Homo sapiens 125-130 19749156-6 2009 Given that EGFR/HER2 overexpression is associated with tamoxifen resistance, our data may suggest that ligand-activated EGFR could contribute to the failure of tamoxifen therapy also by up-regulating GPR30, which in turn could facilitates the action of estrogen. Tamoxifen 55-64 G protein-coupled estrogen receptor 1 Homo sapiens 200-205 19749156-7 2009 In addition, important for resistance is the ability of tamoxifen to bind to and activate GPR30, the expression of which is up-regulated by EGFR activation. Tamoxifen 56-65 G protein-coupled estrogen receptor 1 Homo sapiens 90-95 19549922-0 2009 Stimulating the GPR30 estrogen receptor with a novel tamoxifen analogue activates SF-1 and promotes endometrial cell proliferation. Tamoxifen 53-62 G protein-coupled estrogen receptor 1 Homo sapiens 16-21 19549922-4 2009 Using a novel tamoxifen analogue, STX, which activates GPR30 but not ERs, significant stimulation of the phosphatidylinositol 3-kinase (PI3K) and mitogen-activated protein kinase (MAPK) pathways was observed in H-38 cells and in Ishikawa endometrial cancer cells expressing GPR30; a similar effect was observed in JEG3 choriocarcinoma cells. Tamoxifen 14-23 G protein-coupled estrogen receptor 1 Homo sapiens 55-60 19549922-4 2009 Using a novel tamoxifen analogue, STX, which activates GPR30 but not ERs, significant stimulation of the phosphatidylinositol 3-kinase (PI3K) and mitogen-activated protein kinase (MAPK) pathways was observed in H-38 cells and in Ishikawa endometrial cancer cells expressing GPR30; a similar effect was observed in JEG3 choriocarcinoma cells. Tamoxifen 14-23 G protein-coupled estrogen receptor 1 Homo sapiens 274-279 19549922-6 2009 Consistent with these findings, STX, tamoxifen, and the phytoestrogen genistein were able to increase SF-1 transcription, promote Ishikawa cell proliferation, and induce the SF-1 target gene aromatase in a GPR30-dependent manner. Tamoxifen 37-46 G protein-coupled estrogen receptor 1 Homo sapiens 206-211 19549922-8 2009 We propose that this novel GPR30/SF-1 pathway increases local concentrations of estrogen, and together with classic ER signaling, mediate the proliferative effects of synthetic estrogens such as tamoxifen, in promoting endometriosis and endometrial cancers. Tamoxifen 195-204 G protein-coupled estrogen receptor 1 Homo sapiens 27-32 19428439-5 2009 The increase of bromodeoxyuridine uptake by diosgenin was blocked by an adenylate cyclase inhibitor, but not by antisense oligonucleotides against estrogen receptor alpha, estrogen receptor beta or an orphan G-protein-coupled receptor, GPR30, indicating the involvement of cAMP but not estrogen receptor alpha, estrogen receptor beta or GPR30. Bromodeoxyuridine 16-33 G protein-coupled estrogen receptor 1 Homo sapiens 337-342 19342448-6 2009 Function-blocking antibodies directed against integrin alpha5beta1 or soluble Arg-Gly-Asp peptide fragments derived from FN specifically inhibited GPR30-mediated epidermal growth factor receptor transactivation. Arginine 78-81 G protein-coupled estrogen receptor 1 Homo sapiens 147-152 19342448-6 2009 Function-blocking antibodies directed against integrin alpha5beta1 or soluble Arg-Gly-Asp peptide fragments derived from FN specifically inhibited GPR30-mediated epidermal growth factor receptor transactivation. Glycine 82-85 G protein-coupled estrogen receptor 1 Homo sapiens 147-152 19342448-6 2009 Function-blocking antibodies directed against integrin alpha5beta1 or soluble Arg-Gly-Asp peptide fragments derived from FN specifically inhibited GPR30-mediated epidermal growth factor receptor transactivation. Aspartic Acid 86-89 G protein-coupled estrogen receptor 1 Homo sapiens 147-152 19342448-8 2009 Mutant Shc (317Y/F) blocked GPR30-induced FN matrix assembly and tyrosyl phosphorylation of erbB1. cyclo(tyrosyl-tyrosyl) 65-72 G protein-coupled estrogen receptor 1 Homo sapiens 28-33 19428439-5 2009 The increase of bromodeoxyuridine uptake by diosgenin was blocked by an adenylate cyclase inhibitor, but not by antisense oligonucleotides against estrogen receptor alpha, estrogen receptor beta or an orphan G-protein-coupled receptor, GPR30, indicating the involvement of cAMP but not estrogen receptor alpha, estrogen receptor beta or GPR30. Bromodeoxyuridine 16-33 G protein-coupled estrogen receptor 1 Homo sapiens 236-241 19428439-5 2009 The increase of bromodeoxyuridine uptake by diosgenin was blocked by an adenylate cyclase inhibitor, but not by antisense oligonucleotides against estrogen receptor alpha, estrogen receptor beta or an orphan G-protein-coupled receptor, GPR30, indicating the involvement of cAMP but not estrogen receptor alpha, estrogen receptor beta or GPR30. Diosgenin 44-53 G protein-coupled estrogen receptor 1 Homo sapiens 236-241 19428439-5 2009 The increase of bromodeoxyuridine uptake by diosgenin was blocked by an adenylate cyclase inhibitor, but not by antisense oligonucleotides against estrogen receptor alpha, estrogen receptor beta or an orphan G-protein-coupled receptor, GPR30, indicating the involvement of cAMP but not estrogen receptor alpha, estrogen receptor beta or GPR30. Diosgenin 44-53 G protein-coupled estrogen receptor 1 Homo sapiens 337-342 19207808-3 2009 The results from a series of studies further suggest that the rapid action of E(2) in primate LHRH neurones appears to be mediated by GPR30. Estradiol 78-82 G protein-coupled estrogen receptor 1 Homo sapiens 134-139 19162071-8 2009 We also report that the GPR30 is expressed on cultured sensory neurons, that activation of the receptor elicits signaling to increase calcium accumulation. Calcium 134-141 G protein-coupled estrogen receptor 1 Homo sapiens 24-29 19326083-9 2009 It also increased cellular accumulation of cAMP, a hallmark of GPR30-mediated estrogen signaling. Cyclic AMP 43-47 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 19326083-10 2009 These data imply that tectoridin exerts its estrogenic effect mainly via the GPR30 and ERK-mediated rapid nongenomic estrogen signaling pathway. tectoridin 22-32 G protein-coupled estrogen receptor 1 Homo sapiens 77-82 19326083-11 2009 This property of tectoridin sets it aside from genistein where it exerts the estrogenic effects via both an ER-dependent genomic pathway and a GPR30-dependent nongenomic pathway. tectoridin 17-27 G protein-coupled estrogen receptor 1 Homo sapiens 143-148 19153601-3 2009 We show here for ER-negative human breast cancer cells that the activation of GPR30 signalling by oestrogen or by hydroxytamoxifen (OHT), an ER antagonist but GPR30 agonist, induces a transcription factor network, which resembles that induced by serum in fibroblasts. hydroxytamoxifen 114-130 G protein-coupled estrogen receptor 1 Homo sapiens 78-83 19153601-3 2009 We show here for ER-negative human breast cancer cells that the activation of GPR30 signalling by oestrogen or by hydroxytamoxifen (OHT), an ER antagonist but GPR30 agonist, induces a transcription factor network, which resembles that induced by serum in fibroblasts. hydroxytamoxifen 114-130 G protein-coupled estrogen receptor 1 Homo sapiens 159-164 19395996-7 2009 The nuclear ER antagonists ICI 182780 and tamoxifen, which are GPR30 agonists, as well as the specifically constructed GPR30 agonist G1, mimicked the effect of E(2) on uPAR expression and cell migration. Tamoxifen 42-51 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 19179659-2 2009 Stimulation of GPER blocks vasoconstrictor-induced changes in intracellular calcium concentrations and vascular tone, as well as serum-stimulated cell proliferation of human vascular smooth muscle cells. Calcium 76-83 G protein-coupled estrogen receptor 1 Homo sapiens 15-19 19131510-4 2009 Collectively, E(2) induces a rapid excitatory effect on primate LHRH neurons, and this rapid action of E(2) appears to be mediated, in part, through GPR30. Estradiol 14-18 G protein-coupled estrogen receptor 1 Homo sapiens 149-154 19131510-4 2009 Collectively, E(2) induces a rapid excitatory effect on primate LHRH neurons, and this rapid action of E(2) appears to be mediated, in part, through GPR30. Estradiol 103-107 G protein-coupled estrogen receptor 1 Homo sapiens 149-154 19395996-0 2009 Estradiol attenuates EGF-induced rapid uPAR mobilization and cell migration via the G-protein-coupled receptor 30 in ovarian cancer cells. Estradiol 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 84-113 18566127-4 2008 Recently, an orphan G protein-coupled receptor, GPR30, has been claimed to bind to and to signal in response to estradiol. Estradiol 112-121 G protein-coupled estrogen receptor 1 Homo sapiens 48-53 19395996-3 2009 G-protein-coupled receptor 30 (GPR30) is a newly identified membrane estrogen receptor (ER).The objective of this study was to explore the effects of 17beta-estradiol (E(2)) on uPAR expression and cell migration in ovarian cancer cells and further to identify the ER involved.We used 7 ovarian cancer cell lines, cell migration assay, cellular binding of (125)I-uPA, cellular degradation of (125)I-uPA/PAI-1 complex, enzyme-linked immunosorbent assay for uPAR, solid-phase enzyme immunoassay for ERalpha, and quantitative polymerase chain reaction. Estradiol 150-166 G protein-coupled estrogen receptor 1 Homo sapiens 0-29 19395996-3 2009 G-protein-coupled receptor 30 (GPR30) is a newly identified membrane estrogen receptor (ER).The objective of this study was to explore the effects of 17beta-estradiol (E(2)) on uPAR expression and cell migration in ovarian cancer cells and further to identify the ER involved.We used 7 ovarian cancer cell lines, cell migration assay, cellular binding of (125)I-uPA, cellular degradation of (125)I-uPA/PAI-1 complex, enzyme-linked immunosorbent assay for uPAR, solid-phase enzyme immunoassay for ERalpha, and quantitative polymerase chain reaction. Estradiol 150-166 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 19395996-7 2009 The nuclear ER antagonists ICI 182780 and tamoxifen, which are GPR30 agonists, as well as the specifically constructed GPR30 agonist G1, mimicked the effect of E(2) on uPAR expression and cell migration. Fulvestrant 27-37 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 19079715-0 2008 G-protein-coupled receptor 30 and estrogen receptor-alpha are involved in the proliferative effects induced by atrazine in ovarian cancer cells. Atrazine 111-119 G protein-coupled estrogen receptor 1 Homo sapiens 0-29 19079715-2 2008 Recent investigations have demonstrated that the orphan G-protein-coupled receptor 30 (GPR30), which is structurally unrelated to the ER, mediates rapid actions of 17beta-estradiol and environmental estrogens. Estradiol 164-180 G protein-coupled estrogen receptor 1 Homo sapiens 56-85 19079715-2 2008 Recent investigations have demonstrated that the orphan G-protein-coupled receptor 30 (GPR30), which is structurally unrelated to the ER, mediates rapid actions of 17beta-estradiol and environmental estrogens. Estradiol 164-180 G protein-coupled estrogen receptor 1 Homo sapiens 87-92 19079715-3 2008 OBJECTIVES: Given the ability of atrazine to exert estrogen-like activity in cancer cells, we evaluated the potential of atrazine to signal through GPR30 in stimulating biological responses in cancer cells. Atrazine 121-129 G protein-coupled estrogen receptor 1 Homo sapiens 148-153 19079715-7 2008 Using specific signaling inhibitors and gene silencing, we demonstrated that atrazine stimulated the proliferation of ovarian cancer cells through the GPR30-epidermal growth factor receptor transduction pathway and the involvement of ERalpha. Atrazine 77-85 G protein-coupled estrogen receptor 1 Homo sapiens 151-156 19079715-9 2008 On the basis of the present data, atrazine should be included among the environmental contaminants potentially able to signal via GPR30 in eliciting estrogenic action. Atrazine 34-42 G protein-coupled estrogen receptor 1 Homo sapiens 130-135 18625716-9 2008 We further examined the function of two genes linked to cAMP signaling as follows: Gpr30 that is stimulated and Rgs2 that is down-regulated by Runx2. Cyclic AMP 56-60 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 18625716-11 2008 Notwithstanding its growth-suppressive potential, our results surprisingly indicate that Runx2 may sensitize cAMP-related G protein-coupled receptor signaling by activating Gpr30 and repressing Rgs2 gene expression in osteoblasts to increase responsiveness to mitogenic signals. Cyclic AMP 109-113 G protein-coupled estrogen receptor 1 Homo sapiens 173-178 18768737-0 2008 17-Beta-estradiol inhibits transforming growth factor-beta signaling and function in breast cancer cells via activation of extracellular signal-regulated kinase through the G protein-coupled receptor 30. Estradiol 0-17 G protein-coupled estrogen receptor 1 Homo sapiens 173-202 18768737-6 2008 Silencing of GPR30 in MCF-7 cells completely reduced the ability of 17-beta-estradiol (E2) to inhibit the TGF-beta pathway. Estradiol 68-85 G protein-coupled estrogen receptor 1 Homo sapiens 13-18 18467441-3 2008 Using as a model system SkBr3 and BT20 breast cancer cells lacking the classical ER, the regulation of GPR30 expression by 17beta-estradiol, the selective GPR30 ligand G-1, IGF-I, and epidermal growth factor (EGF) was evaluated. Estradiol 123-139 G protein-coupled estrogen receptor 1 Homo sapiens 103-108 18467434-5 2008 Transient overexpression of GPR30 inhibited 17beta-estradiol (E2)-induced cell proliferation. Estradiol 44-60 G protein-coupled estrogen receptor 1 Homo sapiens 28-33 18467434-5 2008 Transient overexpression of GPR30 inhibited 17beta-estradiol (E2)-induced cell proliferation. Estradiol 62-64 G protein-coupled estrogen receptor 1 Homo sapiens 28-33 17878253-7 2007 Paraffin-embedded sections of the growth plates were used to detect expression of the GPR30 protein. Paraffin 0-8 G protein-coupled estrogen receptor 1 Homo sapiens 86-91 18275979-4 2008 Specifically, treatment of MCF-7 cells, that express ER alpha, ER beta and GPR30, to 0.5-10 microM Cd for only 2.5 min resulted in transient phosphorylation of ERK1/2. Cadmium 99-101 G protein-coupled estrogen receptor 1 Homo sapiens 75-80 18275979-6 2008 In SK-BR-3 cells, that express only GPR30, Cd also caused a transient activation of ERK1/2, but not of AKT. Cadmium 43-45 G protein-coupled estrogen receptor 1 Homo sapiens 36-41 18275979-10 2008 It is concluded that Cd, like estradiol, can cause rapid activation of ERK1/2 and AKT and that these signaling events are mediated by possible interaction with membrane ER alpha and GPR30, but not ER beta. Cadmium 21-23 G protein-coupled estrogen receptor 1 Homo sapiens 182-187 18420744-1 2008 Human G protein-coupled receptor 30 (GPR30) mediates estradiol-17beta (E2) activation of adenylyl cyclase in breast cancer cells and displays E2 binding typical of membrane estrogen receptors (mERs). 17beta 63-69 G protein-coupled estrogen receptor 1 Homo sapiens 37-42 18420744-6 2008 Consistent with previous findings with human GPR30, estrogen treatment of plasma membranes from both croaker ovaries and GPR30-transfected cells caused activation of a stimulatory G protein (Gs) resulting in increased cAMP production. Cyclic AMP 218-222 G protein-coupled estrogen receptor 1 Homo sapiens 121-126 18434348-5 2008 GPR30 protein expression was studied by immunohistochemistry in paraffin-embedded sections. Paraffin 64-72 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 18406603-3 2008 Although estrogen"s transcriptional effects occur through classical nuclear steroid receptors (ERs), recent studies reveal the existence of a novel 7-transmembrane G protein-coupled receptor, GPR30, which responds to estrogen and tamoxifen stimulation with rapid cellular signaling including ERK activation, PI3K activation, calcium mobilization and cAMP production. Tamoxifen 230-239 G protein-coupled estrogen receptor 1 Homo sapiens 192-197 18406603-3 2008 Although estrogen"s transcriptional effects occur through classical nuclear steroid receptors (ERs), recent studies reveal the existence of a novel 7-transmembrane G protein-coupled receptor, GPR30, which responds to estrogen and tamoxifen stimulation with rapid cellular signaling including ERK activation, PI3K activation, calcium mobilization and cAMP production. Calcium 325-332 G protein-coupled estrogen receptor 1 Homo sapiens 192-197 18406603-3 2008 Although estrogen"s transcriptional effects occur through classical nuclear steroid receptors (ERs), recent studies reveal the existence of a novel 7-transmembrane G protein-coupled receptor, GPR30, which responds to estrogen and tamoxifen stimulation with rapid cellular signaling including ERK activation, PI3K activation, calcium mobilization and cAMP production. Cyclic AMP 350-354 G protein-coupled estrogen receptor 1 Homo sapiens 192-197 17379646-6 2007 Stimulation of GPR30-expressing HEK-293 cells with 17beta-E2 caused sequestration of GPR30 from the cell surface and resulted in its codistribution with clathrin and mobilization of intracellular calcium stores. Calcium 196-203 G protein-coupled estrogen receptor 1 Homo sapiens 15-20 17379646-6 2007 Stimulation of GPR30-expressing HEK-293 cells with 17beta-E2 caused sequestration of GPR30 from the cell surface and resulted in its codistribution with clathrin and mobilization of intracellular calcium stores. Calcium 196-203 G protein-coupled estrogen receptor 1 Homo sapiens 85-90 17379646-7 2007 Evidence that GPR30 signals from the cell surface was obtained from experiments demonstrating that the cell-impermeable E2-protein conjugates E2-BSA and E2-horseradish peroxidase promote GPR30-dependent elevation of intracellular cAMP concentrations. Cyclic AMP 230-234 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 17379646-7 2007 Evidence that GPR30 signals from the cell surface was obtained from experiments demonstrating that the cell-impermeable E2-protein conjugates E2-BSA and E2-horseradish peroxidase promote GPR30-dependent elevation of intracellular cAMP concentrations. Cyclic AMP 230-234 G protein-coupled estrogen receptor 1 Homo sapiens 187-192 17379646-8 2007 Subcellular fractionation studies further support the plasma membrane as a site of GPR30 action with specific [3H]17beta-E2 binding and G protein activation associated with plasma membrane but not microsomal, or other fractions, prepared from HEK-293 or SKBR3 breast cancer cells. Tritium 111-113 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 17379646-8 2007 Subcellular fractionation studies further support the plasma membrane as a site of GPR30 action with specific [3H]17beta-E2 binding and G protein activation associated with plasma membrane but not microsomal, or other fractions, prepared from HEK-293 or SKBR3 breast cancer cells. 17beta-e2 114-123 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 17403429-4 2007 RESULTS: GPR30 correlated positively with epidermal growth factor receptor (P = .005), but negatively with progesterone (P = .05) receptor expression. Progesterone 107-119 G protein-coupled estrogen receptor 1 Homo sapiens 9-14 17452498-0 2007 Differential effects of 17beta-estradiol on function and expression of estrogen receptor alpha, estrogen receptor beta, and GPR30 in arteries and veins of patients with atherosclerosis. Estradiol 24-40 G protein-coupled estrogen receptor 1 Homo sapiens 124-129 17452498-10 2007 In summary, this is the first study to report that, in human arteries but not in veins, 17beta-estradiol acutely affects vascular tone, estrogen receptor expression, including GPR30, and extracellular signal-regulated kinase phosphorylation. Estradiol 88-104 G protein-coupled estrogen receptor 1 Homo sapiens 176-181 16835357-0 2006 17beta-estradiol, genistein, and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the g protein-coupled receptor GPR30. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 140-145 17308128-0 2007 G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells. Estradiol 94-110 G protein-coupled estrogen receptor 1 Homo sapiens 0-29 17308128-0 2007 G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells. Estradiol 94-110 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 17308128-2 2007 The orphan G protein-coupled receptor 30 (GPR30) mediates the nongenomic signaling of 17beta-estradiol (E2) in a variety of estrogen-sensitive cancer cells through activation of the epidermal growth factor receptor (EGFR) pathway. Estradiol 86-102 G protein-coupled estrogen receptor 1 Homo sapiens 11-40 17308128-2 2007 The orphan G protein-coupled receptor 30 (GPR30) mediates the nongenomic signaling of 17beta-estradiol (E2) in a variety of estrogen-sensitive cancer cells through activation of the epidermal growth factor receptor (EGFR) pathway. Estradiol 86-102 G protein-coupled estrogen receptor 1 Homo sapiens 42-47 17088055-4 2006 Bisphenol A, zearalonone, and nonylphenol also had relatively high binding affinities for GPR30 with RBAs of 2-3%. bisphenol A 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 90-95 17203231-6 2007 GPR30 mRNA expression was significantly reduced in a serum/phenol-free medium. Phenol 59-65 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 17203231-11 2007 Our results suggest that the expression of ERalpha, ERbeta and GPR30 are influenced by sex steroids and might play a role in the response of cells to 17beta-estradiol and antiestrogens but are not the only factors involved in this process. Steroids 91-99 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 17203231-11 2007 Our results suggest that the expression of ERalpha, ERbeta and GPR30 are influenced by sex steroids and might play a role in the response of cells to 17beta-estradiol and antiestrogens but are not the only factors involved in this process. Estradiol 150-166 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 17088055-4 2006 Bisphenol A, zearalonone, and nonylphenol also had relatively high binding affinities for GPR30 with RBAs of 2-3%. zearalonone 13-24 G protein-coupled estrogen receptor 1 Homo sapiens 90-95 17088055-4 2006 Bisphenol A, zearalonone, and nonylphenol also had relatively high binding affinities for GPR30 with RBAs of 2-3%. nonylphenol 30-41 G protein-coupled estrogen receptor 1 Homo sapiens 90-95 17088055-7 2006 Environmental estrogens with relatively high binding affinities for GPR30 (genestein, bisphenol A, nonylphenol and Kepone) also displayed estrogen agonist activities in an in vitro assay of membrane-bound adenylyl cyclase activity, a GPR30-dependent signaling pathway activated by estrogens. bisphenol A 86-97 G protein-coupled estrogen receptor 1 Homo sapiens 68-73 17088055-7 2006 Environmental estrogens with relatively high binding affinities for GPR30 (genestein, bisphenol A, nonylphenol and Kepone) also displayed estrogen agonist activities in an in vitro assay of membrane-bound adenylyl cyclase activity, a GPR30-dependent signaling pathway activated by estrogens. nonylphenol 99-110 G protein-coupled estrogen receptor 1 Homo sapiens 68-73 17088055-7 2006 Environmental estrogens with relatively high binding affinities for GPR30 (genestein, bisphenol A, nonylphenol and Kepone) also displayed estrogen agonist activities in an in vitro assay of membrane-bound adenylyl cyclase activity, a GPR30-dependent signaling pathway activated by estrogens. Chlordecone 115-121 G protein-coupled estrogen receptor 1 Homo sapiens 68-73 17088055-7 2006 Environmental estrogens with relatively high binding affinities for GPR30 (genestein, bisphenol A, nonylphenol and Kepone) also displayed estrogen agonist activities in an in vitro assay of membrane-bound adenylyl cyclase activity, a GPR30-dependent signaling pathway activated by estrogens. Chlordecone 115-121 G protein-coupled estrogen receptor 1 Homo sapiens 234-239 17090028-0 2006 Linkage effects on binding affinity and activation of GPR30 and estrogen receptors ERalpha/beta with tridentate pyridin-2-yl hydrazine tricarbonyl-Re/(99m)Tc(I) chelates. tridentate pyridin-2-yl hydrazine tricarbonyl-re/(99m)tc 101-157 G protein-coupled estrogen receptor 1 Homo sapiens 54-59 17090028-1 2006 We describe a new structural class of neutral tridentate pyridin-2-yl hydrazine chelates for labeling with tricarbonyl Re/99mTc(I) under aqueous conditions and investigate the receptor binding of synthetic estradiol derivatives with the novel G-protein-coupled receptor GPR30 and estrogen receptors ERalpha/beta. 2-hydrazinopyridine 57-79 G protein-coupled estrogen receptor 1 Homo sapiens 270-275 17085646-1 2006 PURPOSE: The seven transmembrane receptor, GPR30, is linked to estrogen binding and heparan-bound epidermal growth factor release. heparan 84-91 G protein-coupled estrogen receptor 1 Homo sapiens 43-48 16835357-0 2006 17beta-estradiol, genistein, and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the g protein-coupled receptor GPR30. Genistein 18-27 G protein-coupled estrogen receptor 1 Homo sapiens 140-145 16835357-0 2006 17beta-estradiol, genistein, and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the g protein-coupled receptor GPR30. hydroxytamoxifen 33-51 G protein-coupled estrogen receptor 1 Homo sapiens 140-145 16835357-5 2006 It is noteworthy that we have demonstrated that the G protein-coupled receptor 30 (GPR30) and the mitogen-activated protein kinase (MAPK) pathway mediate both the up-regulation of c-fos and the growth response to E2, G, and OHT in TC cells studied, because these stimulatory effects were prevented by silencing GPR30 and using the MEK inhibitor 2"-amino-3"-methoxyflavone (PD 98059). 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one 345-371 G protein-coupled estrogen receptor 1 Homo sapiens 52-81 16835357-5 2006 It is noteworthy that we have demonstrated that the G protein-coupled receptor 30 (GPR30) and the mitogen-activated protein kinase (MAPK) pathway mediate both the up-regulation of c-fos and the growth response to E2, G, and OHT in TC cells studied, because these stimulatory effects were prevented by silencing GPR30 and using the MEK inhibitor 2"-amino-3"-methoxyflavone (PD 98059). 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one 345-371 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 16835357-5 2006 It is noteworthy that we have demonstrated that the G protein-coupled receptor 30 (GPR30) and the mitogen-activated protein kinase (MAPK) pathway mediate both the up-regulation of c-fos and the growth response to E2, G, and OHT in TC cells studied, because these stimulatory effects were prevented by silencing GPR30 and using the MEK inhibitor 2"-amino-3"-methoxyflavone (PD 98059). 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one 373-381 G protein-coupled estrogen receptor 1 Homo sapiens 52-81 16835357-5 2006 It is noteworthy that we have demonstrated that the G protein-coupled receptor 30 (GPR30) and the mitogen-activated protein kinase (MAPK) pathway mediate both the up-regulation of c-fos and the growth response to E2, G, and OHT in TC cells studied, because these stimulatory effects were prevented by silencing GPR30 and using the MEK inhibitor 2"-amino-3"-methoxyflavone (PD 98059). 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one 373-381 G protein-coupled estrogen receptor 1 Homo sapiens 83-88 16239258-0 2006 The G protein-coupled receptor GPR30 mediates the proliferative effects induced by 17beta-estradiol and hydroxytamoxifen in endometrial cancer cells. Estradiol 83-99 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 16780796-4 2006 Treatment with estrogen (17beta-estradiol or E2) causes an elevation in the intracellular Ca2+ concentration ([Ca2+]i) within 10 s in HeLa cells expressing FLAG-GPR30. Estradiol 25-41 G protein-coupled estrogen receptor 1 Homo sapiens 161-166 16780796-4 2006 Treatment with estrogen (17beta-estradiol or E2) causes an elevation in the intracellular Ca2+ concentration ([Ca2+]i) within 10 s in HeLa cells expressing FLAG-GPR30. Estradiol 45-47 G protein-coupled estrogen receptor 1 Homo sapiens 161-166 16239258-0 2006 The G protein-coupled receptor GPR30 mediates the proliferative effects induced by 17beta-estradiol and hydroxytamoxifen in endometrial cancer cells. hydroxytamoxifen 104-120 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 15705806-4 2005 Activating GPR30 by estrogen resulted in intracellular calcium mobilization and synthesis of phosphatidylinositol 3,4,5-trisphosphate in the nucleus. Calcium 55-62 G protein-coupled estrogen receptor 1 Homo sapiens 11-16 16125968-5 2005 Identification of GPR30 as a Gs-coupled 7TM receptor that triggers release of heparin-binding EGF establishes its role in cell signaling cascades initiated by estrogens, and explains their capacity to activate second messengers and promote EGF-like effects. Heparin 78-85 G protein-coupled estrogen receptor 1 Homo sapiens 18-23 15705806-4 2005 Activating GPR30 by estrogen resulted in intracellular calcium mobilization and synthesis of phosphatidylinositol 3,4,5-trisphosphate in the nucleus. phosphatidylinositol 3,4,5-triphosphate 93-133 G protein-coupled estrogen receptor 1 Homo sapiens 11-16 11773440-5 2002 We show that 17beta-E2 represses EGF-induced activation of the Raf-to-Erk pathway in human breast carcinoma cells that express GPR30, including MCF-7 and SKBR3 cells which express both or neither, ER, respectively. 17beta-e2 13-22 G protein-coupled estrogen receptor 1 Homo sapiens 127-132 15539556-4 2005 Progesterone-induced increases and small interfering RNA-induced decreases in GPR30 expression in SKBR3 cells were accompanied by parallel changes in specific estradiol-17beta (E2) binding. Estradiol 159-175 G protein-coupled estrogen receptor 1 Homo sapiens 78-83 15511221-1 2004 G protein-coupled receptor 30 (GPR30) has previously been described to be important in steroid-mediated growth and to inhibit cell proliferation. Steroids 87-94 G protein-coupled estrogen receptor 1 Homo sapiens 0-29 15511221-1 2004 G protein-coupled receptor 30 (GPR30) has previously been described to be important in steroid-mediated growth and to inhibit cell proliferation. Steroids 87-94 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 15511221-8 2004 In COS cells, transient transfection of GPR30 with glucocorticoid receptor alpha resulted in an abrogation of the MMTV-luc and GRE-luc reporter activities induced by dexamethasone. Dexamethasone 166-179 G protein-coupled estrogen receptor 1 Homo sapiens 40-45 15245432-9 2004 Antisense oligonucleotide against G-protein-coupled receptor GPR30 suppressed the E2-induced increases of phosphorylated CREB, cyclin D2 level, proliferation, and bromodeoxyuridine incorporation in keratinocytes. Oligonucleotides 10-25 G protein-coupled estrogen receptor 1 Homo sapiens 61-66 15245432-9 2004 Antisense oligonucleotide against G-protein-coupled receptor GPR30 suppressed the E2-induced increases of phosphorylated CREB, cyclin D2 level, proliferation, and bromodeoxyuridine incorporation in keratinocytes. Bromodeoxyuridine 163-180 G protein-coupled estrogen receptor 1 Homo sapiens 61-66 15090535-0 2004 The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells. Estradiol 69-85 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 15090535-3 2004 The c-fos response is repressed in GPR30-expressing SKBR3 cells transfected with an antisense oligonucleotide against GPR30 and reconstituted in GPR30-deficient MDA-MB 231 and BT-20 breast cancer cells transfected with a GPR30 expression vector. Oligonucleotides 94-109 G protein-coupled estrogen receptor 1 Homo sapiens 35-40 15090535-3 2004 The c-fos response is repressed in GPR30-expressing SKBR3 cells transfected with an antisense oligonucleotide against GPR30 and reconstituted in GPR30-deficient MDA-MB 231 and BT-20 breast cancer cells transfected with a GPR30 expression vector. Oligonucleotides 94-109 G protein-coupled estrogen receptor 1 Homo sapiens 118-123 15090535-3 2004 The c-fos response is repressed in GPR30-expressing SKBR3 cells transfected with an antisense oligonucleotide against GPR30 and reconstituted in GPR30-deficient MDA-MB 231 and BT-20 breast cancer cells transfected with a GPR30 expression vector. Oligonucleotides 94-109 G protein-coupled estrogen receptor 1 Homo sapiens 118-123 15090535-3 2004 The c-fos response is repressed in GPR30-expressing SKBR3 cells transfected with an antisense oligonucleotide against GPR30 and reconstituted in GPR30-deficient MDA-MB 231 and BT-20 breast cancer cells transfected with a GPR30 expression vector. Oligonucleotides 94-109 G protein-coupled estrogen receptor 1 Homo sapiens 118-123 14675202-15 2003 These effects of 17beta-estradiol may be mediated via membrane GPR30. Estradiol 17-33 G protein-coupled estrogen receptor 1 Homo sapiens 63-68 14632195-8 2003 Antisense oligonucleotide against guanine nucleotide-binding protein-coupled receptor, GPR30 suppressed the E2-induced cyclic adenosine monophosphate signal, c-Fos expression, and nerve growth factor secretion in both types of macrophages. Oligonucleotides 10-25 G protein-coupled estrogen receptor 1 Homo sapiens 87-92 14632195-8 2003 Antisense oligonucleotide against guanine nucleotide-binding protein-coupled receptor, GPR30 suppressed the E2-induced cyclic adenosine monophosphate signal, c-Fos expression, and nerve growth factor secretion in both types of macrophages. Cyclic AMP 119-149 G protein-coupled estrogen receptor 1 Homo sapiens 87-92 12193550-9 2002 Interestingly, GPR30 antisense abrogated the growth inhibitory effect of progestin and progesterone. Progesterone 87-99 G protein-coupled estrogen receptor 1 Homo sapiens 15-20 11773440-9 2002 Moreover, GPR30-dependent, cAMP-mediated attenuation of EGF-induced Erk-1/-2 activity was achieved by ER antagonists such as tamoxifen or ICI 182, 780; yet not by 17alpha-E2 or progesterone. Tamoxifen 125-134 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 11773440-9 2002 Moreover, GPR30-dependent, cAMP-mediated attenuation of EGF-induced Erk-1/-2 activity was achieved by ER antagonists such as tamoxifen or ICI 182, 780; yet not by 17alpha-E2 or progesterone. ici 138-141 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 11773440-9 2002 Moreover, GPR30-dependent, cAMP-mediated attenuation of EGF-induced Erk-1/-2 activity was achieved by ER antagonists such as tamoxifen or ICI 182, 780; yet not by 17alpha-E2 or progesterone. Progesterone 177-189 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 33818655-0 2021 "Metalloestrogenic" effects of cadmium downstream of G protein-coupled estrogen receptor and mitogen-activated protein kinase pathways in human uterine fibroid cells. Cadmium 31-38 G protein-coupled estrogen receptor 1 Homo sapiens 53-88 33818655-2 2021 We have reported that Cd stimulates proliferation of estrogen-responsive human uterine leiomyoma (ht-UtLM; fibroid) cells through nongenomic signaling involving the G protein-coupled estrogen receptor (GPER), with activation of epidermal growth factor receptor (EGFR) and mitogen-activated protein kinase (pMAPK44/42). Cadmium 22-24 G protein-coupled estrogen receptor 1 Homo sapiens 165-200 33818655-2 2021 We have reported that Cd stimulates proliferation of estrogen-responsive human uterine leiomyoma (ht-UtLM; fibroid) cells through nongenomic signaling involving the G protein-coupled estrogen receptor (GPER), with activation of epidermal growth factor receptor (EGFR) and mitogen-activated protein kinase (pMAPK44/42). Cadmium 22-24 G protein-coupled estrogen receptor 1 Homo sapiens 202-206 26638889-0 2015 MicroRNA-424 suppresses estradiol-induced cell proliferation via targeting GPER in endometrial cancer cells. Estradiol 24-33 G protein-coupled estrogen receptor 1 Homo sapiens 75-79 33799631-0 2021 The G-Protein-Coupled Estrogen Receptor (GPER) Regulates Trimethylation of Histone H3 at Lysine 4 and Represses Migration and Proliferation of Ovarian Cancer Cells In Vitro. Lysine 89-95 G protein-coupled estrogen receptor 1 Homo sapiens 41-45 32796699-5 2020 BPA may also affect metabolism and cancer progression, by interacting with GPR30, and may impair male reproductive function, by binding to androgen receptors. bisphenol A 0-3 G protein-coupled estrogen receptor 1 Homo sapiens 75-80 34328988-9 2021 Based on the obtained knowledge, GPER affinity and relevant toxicity of BPA alternatives can be easily predicted, and the calculated binding free energies are consistent with the available experimental observations. bisphenol A 72-75 G protein-coupled estrogen receptor 1 Homo sapiens 33-37 34821461-3 2022 The expression changes of four ER subtypes (ERalpha66, ERbeta, ERalpha36 and GPR30) were found to bring about tamoxifen resistance. Tamoxifen 110-119 G protein-coupled estrogen receptor 1 Homo sapiens 77-82 34821461-5 2022 Interestingly, E2 at environmental concentrations (0.1-10 nM) could activate the expression of both ERalpha36 and GPR30, and then stimulate the phosphorylation of ERK1/2 and Akt, resulting in cell growth promotion. Estradiol 15-17 G protein-coupled estrogen receptor 1 Homo sapiens 114-119 34821461-7 2022 Conversely, the application of specific antagonists of ERalpha36 and GPR30 could restore tamoxifen"s sensitivity as well as partially offset E2-mediated proliferation. Tamoxifen 89-98 G protein-coupled estrogen receptor 1 Homo sapiens 69-74 34821461-7 2022 Conversely, the application of specific antagonists of ERalpha36 and GPR30 could restore tamoxifen"s sensitivity as well as partially offset E2-mediated proliferation. Estradiol 141-143 G protein-coupled estrogen receptor 1 Homo sapiens 69-74 34821461-8 2022 In short, overexpression of ERalpha36 and GPR30 not only ablate tamoxifen responsiveness but also could promote tumor progression of TamR breast cancer under estrogen conditions. Tamoxifen 64-73 G protein-coupled estrogen receptor 1 Homo sapiens 42-47 34943948-0 2021 GPER Agonist G-1 Disrupts Tubulin Dynamics and Potentiates Temozolomide to Impair Glioblastoma Cell Proliferation. Temozolomide 59-71 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 34714484-0 2021 Saikosaponin-d alleviates hepatic fibrosis through regulating GPER1/autophagy signaling. saikosaponin D 0-14 G protein-coupled estrogen receptor 1 Homo sapiens 62-67 34403325-0 2021 Kaempferol-induced GPER upregulation attenuates atherosclerosis via the PI3K/AKT/Nrf2 pathway. kaempferol 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 19-23 34403325-10 2021 Kaempferol (5, 10 or 20 muM) induced-GPER activation increased cell viability to nearly 10%, 19.8%, 30%, and the decreased cellular reactive oxygen species (ROS) generation (16.7%, 25.6%, 31.1%), respectively, consequently attenuating postmenopausal AS. kaempferol 0-10 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 34403325-10 2021 Kaempferol (5, 10 or 20 muM) induced-GPER activation increased cell viability to nearly 10%, 19.8%, 30%, and the decreased cellular reactive oxygen species (ROS) generation (16.7%, 25.6%, 31.1%), respectively, consequently attenuating postmenopausal AS. Reactive Oxygen Species 132-155 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 34403325-10 2021 Kaempferol (5, 10 or 20 muM) induced-GPER activation increased cell viability to nearly 10%, 19.8%, 30%, and the decreased cellular reactive oxygen species (ROS) generation (16.7%, 25.6%, 31.1%), respectively, consequently attenuating postmenopausal AS. Reactive Oxygen Species 157-160 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 34403325-11 2021 However, the protective effects of kaempferol were blocked through co-treatment with si-GPER. kaempferol 35-45 G protein-coupled estrogen receptor 1 Homo sapiens 88-92 34403325-12 2021 CONCLUSIONS: The beneficial effects of kaempferol against postmenopausal AS are associated with the PI3K/AKT/Nrf2 pathways, mediated by the activation of GPER. kaempferol 39-49 G protein-coupled estrogen receptor 1 Homo sapiens 154-158 34773076-6 2021 Treatment of trophoblast cells with G1 or 17beta-estradiol (E2) activated Yes-associated protein (YAP), the major downstream effector of the Hippo pathway, via GPER but in a mammalian STE20-like protein kinase 1 (MST1)-independent manner. Estradiol 42-58 G protein-coupled estrogen receptor 1 Homo sapiens 160-164 34773076-6 2021 Treatment of trophoblast cells with G1 or 17beta-estradiol (E2) activated Yes-associated protein (YAP), the major downstream effector of the Hippo pathway, via GPER but in a mammalian STE20-like protein kinase 1 (MST1)-independent manner. Estradiol 60-62 G protein-coupled estrogen receptor 1 Homo sapiens 160-164 34328988-6 2021 Bulky substituents and structural rigidity of the connecting C dramatically impair hydrogen bonding between GPER and the bisphenols, which results in decreased contribution of both favorable intermolecular hydrogen bonds and unfavorable polar solvation effect to complex stability of BPB and BPC since decreased number of key residues is expected. S-(4-bromophenyl)cysteine sulfoxide 292-295 G protein-coupled estrogen receptor 1 Homo sapiens 108-112 34600017-7 2022 Results verified that TPP could damage the structures of cell membranes and exert an agonistic effect of GPER as the molecular initiating event. tetraphenylporphine sulfonate 22-25 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 34890987-6 2022 However, both TPhP and TDCIPP activated the estrogen pathway by GPER in SKBR3 cells which were lack of ERalpha. triphenyl phosphate 14-18 G protein-coupled estrogen receptor 1 Homo sapiens 64-68 34890987-7 2022 Although molecular docking results revealed that both TPhP and TDCIPP could dock into ERalpha and GPER, their substituent groups and combination mode might affect the receptor activation. triphenyl phosphate 54-58 G protein-coupled estrogen receptor 1 Homo sapiens 98-102 34571396-4 2021 Our study showed that 17beta-estradiol (E2) significantly reduced cyclic guanosine monophosphate (cGMP) synthesis in COCs and accelerated the meiotic resumption of goat oocytes via GPER. Estradiol 22-38 G protein-coupled estrogen receptor 1 Homo sapiens 181-185 34571396-4 2021 Our study showed that 17beta-estradiol (E2) significantly reduced cyclic guanosine monophosphate (cGMP) synthesis in COCs and accelerated the meiotic resumption of goat oocytes via GPER. Estradiol 40-42 G protein-coupled estrogen receptor 1 Homo sapiens 181-185 34571396-6 2021 In addition, we found that E2 significantly upregulated the mRNA levels of epidermal growth (EGF)-like factors in goat cumulus cells through GPER, and activated the downstream EGF receptor (EGFR) and extracellular signal-regulated kinase 1/2 (ERK1/2) signaling pathways. Estradiol 27-29 G protein-coupled estrogen receptor 1 Homo sapiens 141-145 34571396-8 2021 These results indicate that, through GPER, E2 upregulates the mRNA levels of EGF-like factors in goat cumulus cells and activates the downstream EGF signaling network to suppress the expression of NPR2 protein, which results in a decrease in cGMP synthesis and acceleration of meiotic resumption in goat oocytes. Estradiol 43-45 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 34571396-8 2021 These results indicate that, through GPER, E2 upregulates the mRNA levels of EGF-like factors in goat cumulus cells and activates the downstream EGF signaling network to suppress the expression of NPR2 protein, which results in a decrease in cGMP synthesis and acceleration of meiotic resumption in goat oocytes. Cyclic GMP 242-246 G protein-coupled estrogen receptor 1 Homo sapiens 37-41 34781165-0 2021 The sex steroid precursor dehydroepiandrosterone prevents nonalcoholic steatohepatitis by activating the AMPK pathway mediated by GPR30. Steroids 8-15 G protein-coupled estrogen receptor 1 Homo sapiens 130-135 34781165-0 2021 The sex steroid precursor dehydroepiandrosterone prevents nonalcoholic steatohepatitis by activating the AMPK pathway mediated by GPR30. Dehydroepiandrosterone 26-48 G protein-coupled estrogen receptor 1 Homo sapiens 130-135 34781165-6 2021 Mechanistically, in vitro and in vivo studies showed that the anti-NASH function of DHEA depended on its biotransformation into estrogen rather than androgen, and which up-regulates the expression of G protein-coupled estrogen receptor (GPR30), a non-classical estrogen receptor. Dehydroepiandrosterone 84-88 G protein-coupled estrogen receptor 1 Homo sapiens 237-242 34781165-7 2021 The activation of GPR30-mediated AMP-activated protein kinase signaling is a necessary prerequisite for the alleviative effects of DHEA on NASH. Dehydroepiandrosterone 131-135 G protein-coupled estrogen receptor 1 Homo sapiens 18-23 34781165-8 2021 Collectively, our data show the mechanisms of DHEA treatment and its effects on NASH that were previously overlooked; the data also show that GPR30 can be used as a target for treating lipid metabolism disorders and related diseases, such as NASH. Dehydroepiandrosterone 46-50 G protein-coupled estrogen receptor 1 Homo sapiens 142-147 34877243-3 2021 Different studies show that down regulation of estrogen receptor beta (ERbeta) associates with GPR30 over-expression both in human testicular carcinoma in situ (CIS) and seminomas and that the mitogenic role exerted by 17beta-oestradiol induces the activation of extracellular signal-regulated kinase 1/2 (ERK1/2) through GPR30. Estradiol 219-236 G protein-coupled estrogen receptor 1 Homo sapiens 95-100 34877243-3 2021 Different studies show that down regulation of estrogen receptor beta (ERbeta) associates with GPR30 over-expression both in human testicular carcinoma in situ (CIS) and seminomas and that the mitogenic role exerted by 17beta-oestradiol induces the activation of extracellular signal-regulated kinase 1/2 (ERK1/2) through GPR30. Estradiol 219-236 G protein-coupled estrogen receptor 1 Homo sapiens 322-327 34328988-0 2021 Structural basis for molecular recognition of G protein-coupled estrogen receptor by selected bisphenols. bis(4-hydroxyphenyl)sulfone 94-104 G protein-coupled estrogen receptor 1 Homo sapiens 46-81 34328988-1 2021 Complicated ligand-dependent signaling pathways of bisphenol A (BPA) and its analogues involve not only intranuclear estrogen receptor but also membrane receptor G protein-coupled estrogen receptor (GPER). bisphenol A 51-62 G protein-coupled estrogen receptor 1 Homo sapiens 162-197 34328988-1 2021 Complicated ligand-dependent signaling pathways of bisphenol A (BPA) and its analogues involve not only intranuclear estrogen receptor but also membrane receptor G protein-coupled estrogen receptor (GPER). bisphenol A 51-62 G protein-coupled estrogen receptor 1 Homo sapiens 199-203 34328988-1 2021 Complicated ligand-dependent signaling pathways of bisphenol A (BPA) and its analogues involve not only intranuclear estrogen receptor but also membrane receptor G protein-coupled estrogen receptor (GPER). bisphenol A 64-67 G protein-coupled estrogen receptor 1 Homo sapiens 162-197 34328988-1 2021 Complicated ligand-dependent signaling pathways of bisphenol A (BPA) and its analogues involve not only intranuclear estrogen receptor but also membrane receptor G protein-coupled estrogen receptor (GPER). bisphenol A 64-67 G protein-coupled estrogen receptor 1 Homo sapiens 199-203 34328988-3 2021 To reveal the structural dependence of GPER recognition by bisphenols, a systematic molecular dynamics simulation study was performed for selected bisphenols with different electron hybrid orbitals and substituents on their C atoms connecting two phenol rings. bis(4-hydroxyphenyl)sulfone 59-69 G protein-coupled estrogen receptor 1 Homo sapiens 39-43 34328988-3 2021 To reveal the structural dependence of GPER recognition by bisphenols, a systematic molecular dynamics simulation study was performed for selected bisphenols with different electron hybrid orbitals and substituents on their C atoms connecting two phenol rings. bis(4-hydroxyphenyl)sulfone 147-157 G protein-coupled estrogen receptor 1 Homo sapiens 39-43 34328988-3 2021 To reveal the structural dependence of GPER recognition by bisphenols, a systematic molecular dynamics simulation study was performed for selected bisphenols with different electron hybrid orbitals and substituents on their C atoms connecting two phenol rings. Phenol 247-253 G protein-coupled estrogen receptor 1 Homo sapiens 39-43 34328988-5 2021 All the tested bisphenols can bind with GPER at its classic orthosteric site to obtain GPER-ligand complexes, while van der Waals interactions and direct inter-molecular electrostatic energies provide the driving forces for ligand binding. bis(4-hydroxyphenyl)sulfone 15-25 G protein-coupled estrogen receptor 1 Homo sapiens 40-44 34328988-5 2021 All the tested bisphenols can bind with GPER at its classic orthosteric site to obtain GPER-ligand complexes, while van der Waals interactions and direct inter-molecular electrostatic energies provide the driving forces for ligand binding. bis(4-hydroxyphenyl)sulfone 15-25 G protein-coupled estrogen receptor 1 Homo sapiens 87-91 34328988-6 2021 Bulky substituents and structural rigidity of the connecting C dramatically impair hydrogen bonding between GPER and the bisphenols, which results in decreased contribution of both favorable intermolecular hydrogen bonds and unfavorable polar solvation effect to complex stability of BPB and BPC since decreased number of key residues is expected. Hydrogen 83-91 G protein-coupled estrogen receptor 1 Homo sapiens 108-112 34328988-6 2021 Bulky substituents and structural rigidity of the connecting C dramatically impair hydrogen bonding between GPER and the bisphenols, which results in decreased contribution of both favorable intermolecular hydrogen bonds and unfavorable polar solvation effect to complex stability of BPB and BPC since decreased number of key residues is expected. bis(4-hydroxyphenyl)sulfone 121-131 G protein-coupled estrogen receptor 1 Homo sapiens 108-112 34328988-6 2021 Bulky substituents and structural rigidity of the connecting C dramatically impair hydrogen bonding between GPER and the bisphenols, which results in decreased contribution of both favorable intermolecular hydrogen bonds and unfavorable polar solvation effect to complex stability of BPB and BPC since decreased number of key residues is expected. Hydrogen 206-214 G protein-coupled estrogen receptor 1 Homo sapiens 108-112 34768896-11 2021 This result proved that the promotional effect of BBR on the GPER1/NF-kappaB pathway was closely related to its inhibitory effect on autophagy, which may serve as a new mechanism by which to explain the inhibitory effect of BBR on MDA-MB-231 cells and expand our understanding of the function of both BBR and GPER1. Berberine 50-53 G protein-coupled estrogen receptor 1 Homo sapiens 61-66 34768896-11 2021 This result proved that the promotional effect of BBR on the GPER1/NF-kappaB pathway was closely related to its inhibitory effect on autophagy, which may serve as a new mechanism by which to explain the inhibitory effect of BBR on MDA-MB-231 cells and expand our understanding of the function of both BBR and GPER1. Berberine 50-53 G protein-coupled estrogen receptor 1 Homo sapiens 309-314 34768896-9 2021 BBR could bind to GPER1 directly and change the secondary structure of GPER1, as in the case of 17beta-estradiol (E2). Estradiol 96-112 G protein-coupled estrogen receptor 1 Homo sapiens 18-23 34768896-9 2021 BBR could bind to GPER1 directly and change the secondary structure of GPER1, as in the case of 17beta-estradiol (E2). Estradiol 96-112 G protein-coupled estrogen receptor 1 Homo sapiens 71-76 34768896-9 2021 BBR could bind to GPER1 directly and change the secondary structure of GPER1, as in the case of 17beta-estradiol (E2). Estradiol 114-116 G protein-coupled estrogen receptor 1 Homo sapiens 18-23 34768896-11 2021 This result proved that the promotional effect of BBR on the GPER1/NF-kappaB pathway was closely related to its inhibitory effect on autophagy, which may serve as a new mechanism by which to explain the inhibitory effect of BBR on MDA-MB-231 cells and expand our understanding of the function of both BBR and GPER1. Berberine 224-227 G protein-coupled estrogen receptor 1 Homo sapiens 61-66 34363795-2 2021 It has been reported that G-1, an agonist of GPER, increases nitric oxide (NO) production through the phosphorylation of endothelial nitric oxide synthase (eNOS). Nitric Oxide 61-73 G protein-coupled estrogen receptor 1 Homo sapiens 45-49 34768896-9 2021 BBR could bind to GPER1 directly and change the secondary structure of GPER1, as in the case of 17beta-estradiol (E2). Estradiol 114-116 G protein-coupled estrogen receptor 1 Homo sapiens 71-76 34768896-10 2021 In addition, BBR induced not only a high degree of co-localization of GPER1 and microtubule-associated protein 1 light chain 3 (MAP1LC3), but also the accumulation of sequestosome 1 (SQSTM1/p62) by the inhibition of the nuclear translocation of the nuclear factor-kappa B (NF-kappaB) subunit (RELA/p65), which indicates NF-kappaB inhibition and anti-cancer effects. Berberine 13-16 G protein-coupled estrogen receptor 1 Homo sapiens 70-75 34671265-0 2021 Corrigendum: Bazi Bushen Capsule Alleviates Post-Menopausal Atherosclerosis via GPER1-Dependent Anti-Inflammatory and Anti-Apoptotic Effects. bazi bushen 13-24 G protein-coupled estrogen receptor 1 Homo sapiens 80-85 34621174-8 2021 Therefore, additional molecular effects of BPA and BPAF were unmasked after treatment with different inhibitors of well-known pivotal players of GPER-mediated signaling. bisphenol A 43-46 G protein-coupled estrogen receptor 1 Homo sapiens 145-149 34631701-4 2021 We found that E2 rapidly decreased the surface movement of AMPAR via membrane G protein-coupled estrogen receptor 1 (GPER1) in neurites in a dose-dependent manner. Estradiol 14-16 G protein-coupled estrogen receptor 1 Homo sapiens 78-115 34631701-4 2021 We found that E2 rapidly decreased the surface movement of AMPAR via membrane G protein-coupled estrogen receptor 1 (GPER1) in neurites in a dose-dependent manner. Estradiol 14-16 G protein-coupled estrogen receptor 1 Homo sapiens 117-122 34631701-5 2021 The cortical actin network played a pivotal role in the GPER1 mediated effects of E2 on the surface mobility of AMPAR. Estradiol 82-84 G protein-coupled estrogen receptor 1 Homo sapiens 56-61 34621174-8 2021 Therefore, additional molecular effects of BPA and BPAF were unmasked after treatment with different inhibitors of well-known pivotal players of GPER-mediated signaling. 4-boronophenylalanine-fructose 51-55 G protein-coupled estrogen receptor 1 Homo sapiens 145-149 34621174-11 2021 Indeed, a biased agonism profile for BPA and BPAF for GPER was suggested based on their different binding modes revealed by our molecular docking. bisphenol A 37-40 G protein-coupled estrogen receptor 1 Homo sapiens 54-58 34621174-11 2021 Indeed, a biased agonism profile for BPA and BPAF for GPER was suggested based on their different binding modes revealed by our molecular docking. 4-boronophenylalanine-fructose 45-49 G protein-coupled estrogen receptor 1 Homo sapiens 54-58 34575683-5 2021 GPR30 activation by 17beta-estradiol elicited the SRC/EGFR/PI3K/Akt/mTOR signaling pathway. Estradiol 20-36 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 34534372-5 2022 17beta-estradiol is the predominant and most biologically active endogenous estrogen, which signals through estrogen receptor alpha, estrogen receptor beta, and G protein-coupled estrogen receptor 1. Estradiol 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 161-198 34575683-11 2021 Collectively, our results indicate that 17beta-estradiol-mediated GPR30 activation elicits the SRC/EGFR/PI3K/Akt/mTOR signaling pathway and promotes p62 phosphorylation. Estradiol 40-56 G protein-coupled estrogen receptor 1 Homo sapiens 66-71 34575683-0 2021 GPR30 Activation by 17beta-Estradiol Promotes p62 Phosphorylation and Increases Estrogen Receptor alpha Protein Expression by Inducing Its Release from a Complex Formed with KEAP1. Estradiol 20-36 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 34330822-1 2021 GPR30 is a membrane receptor reported to bind 17beta-estradiol (E2) and mediate rapid non-genomic estrogen responses, hence also named G protein-coupled estrogen receptor (GPER). Estradiol 46-62 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 34329471-6 2021 In 157 paired breast cancer and adjacent normal samples, tumour suppressor gene GPER1 and miR-339 are both downregulated in Luminal A/B and Triple Negative Breast Cancer subtypes. Phenobarbital 124-131 G protein-coupled estrogen receptor 1 Homo sapiens 80-85 34330822-1 2021 GPR30 is a membrane receptor reported to bind 17beta-estradiol (E2) and mediate rapid non-genomic estrogen responses, hence also named G protein-coupled estrogen receptor (GPER). Estradiol 46-62 G protein-coupled estrogen receptor 1 Homo sapiens 135-170 34330822-1 2021 GPR30 is a membrane receptor reported to bind 17beta-estradiol (E2) and mediate rapid non-genomic estrogen responses, hence also named G protein-coupled estrogen receptor (GPER). Estradiol 46-62 G protein-coupled estrogen receptor 1 Homo sapiens 172-176 34330822-1 2021 GPR30 is a membrane receptor reported to bind 17beta-estradiol (E2) and mediate rapid non-genomic estrogen responses, hence also named G protein-coupled estrogen receptor (GPER). Estradiol 64-66 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 34330822-1 2021 GPR30 is a membrane receptor reported to bind 17beta-estradiol (E2) and mediate rapid non-genomic estrogen responses, hence also named G protein-coupled estrogen receptor (GPER). Estradiol 64-66 G protein-coupled estrogen receptor 1 Homo sapiens 135-170 34330822-1 2021 GPR30 is a membrane receptor reported to bind 17beta-estradiol (E2) and mediate rapid non-genomic estrogen responses, hence also named G protein-coupled estrogen receptor (GPER). Estradiol 64-66 G protein-coupled estrogen receptor 1 Homo sapiens 172-176 34330822-9 2021 Significance Statement Much controversy surrounds E2 and G-1 as GPR30 agonists. Estradiol 50-52 G protein-coupled estrogen receptor 1 Homo sapiens 64-69 34085740-10 2021 GPER was significantly increased in active patients and correlated with BPA levels. bisphenol A 72-75 G protein-coupled estrogen receptor 1 Homo sapiens 0-4 34646075-8 2021 GPER-1 knockdown by siRNA reduced the cells number to 60% of siRNA-control-treated cells (P < .05), and GPER-1 antagonist, G-15 inhibited two HGSC cell lines proliferation (KF and UWB1.289) in a dose-dependent manner. G-15 123-127 G protein-coupled estrogen receptor 1 Homo sapiens 104-110 34244306-7 2021 Through multiplexed RNA profiling analysis of 4-OHT-treated ER+ and ER- cells, we identified increased activation of apoptotic and death receptor signaling pathways and identified G protein-coupled receptor for estrogen (GPR30) engagement as a putative mechanism for immunogenic modulation. 4,17 beta-dihydroxy-4-androstene-3-one 46-51 G protein-coupled estrogen receptor 1 Homo sapiens 221-226 34182538-0 2021 GPR30-mediated HMGB1 upregulation in CAFs induces autophagy and tamoxifen resistance in ERalpha-positive breast cancer cells. Tamoxifen 64-73 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 34182538-5 2021 GPR30-induced HMGB1 upregulation triggered MEK/ERK signaling, leading to increased autophagic behavior to protect cancer cells from TAM-induced apoptosis, mimicking the recombinant HMGB1-mediated increase in cancer cell resistance potential to TAM. Tamoxifen 244-247 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 34182538-2 2021 G-protein-coupled estrogen receptor (GPR30/GPER), which reportedly initiates TAM resistance in ERalpha+/ GPR30+ breast cancers, is detected in the breast cancer microenvironment, especially cancer associated fibroblasts (CAFs). Tamoxifen 77-80 G protein-coupled estrogen receptor 1 Homo sapiens 37-42 34182538-7 2021 CAF-expressed GPR30 induced TAM resistance via HMGB1 in vivo. Tamoxifen 28-31 G protein-coupled estrogen receptor 1 Homo sapiens 14-19 34182538-8 2021 Overall, TAM upregulated HMGB1 expression and secretion in CAFs via GPR30/PI3K/AKT signaling, and the secreted HMGB1 induced autophagy to enhance TAM resistance in MCF-7 cells in an ERK-dependent manner. Tamoxifen 9-12 G protein-coupled estrogen receptor 1 Homo sapiens 68-73 34182538-2 2021 G-protein-coupled estrogen receptor (GPR30/GPER), which reportedly initiates TAM resistance in ERalpha+/ GPR30+ breast cancers, is detected in the breast cancer microenvironment, especially cancer associated fibroblasts (CAFs). Tamoxifen 77-80 G protein-coupled estrogen receptor 1 Homo sapiens 43-47 34182538-2 2021 G-protein-coupled estrogen receptor (GPR30/GPER), which reportedly initiates TAM resistance in ERalpha+/ GPR30+ breast cancers, is detected in the breast cancer microenvironment, especially cancer associated fibroblasts (CAFs). Tamoxifen 77-80 G protein-coupled estrogen receptor 1 Homo sapiens 105-110 34182538-3 2021 Herein, considering that GPR30 mediates transcriptional regulation in different cell backgrounds, a microarray strategy was applied in immortalized CAFs derived from primary breast cancer samples, resulting in the identification of 165 GPR30 target genes, among which HMGB1 was confirmed to be upregulated by 17-beta estradiol(E2)- and TAM-triggered GPR30 activation in CAFs. Estradiol 309-326 G protein-coupled estrogen receptor 1 Homo sapiens 25-30 34182538-3 2021 Herein, considering that GPR30 mediates transcriptional regulation in different cell backgrounds, a microarray strategy was applied in immortalized CAFs derived from primary breast cancer samples, resulting in the identification of 165 GPR30 target genes, among which HMGB1 was confirmed to be upregulated by 17-beta estradiol(E2)- and TAM-triggered GPR30 activation in CAFs. Estradiol 309-326 G protein-coupled estrogen receptor 1 Homo sapiens 236-241 34182538-3 2021 Herein, considering that GPR30 mediates transcriptional regulation in different cell backgrounds, a microarray strategy was applied in immortalized CAFs derived from primary breast cancer samples, resulting in the identification of 165 GPR30 target genes, among which HMGB1 was confirmed to be upregulated by 17-beta estradiol(E2)- and TAM-triggered GPR30 activation in CAFs. Estradiol 309-326 G protein-coupled estrogen receptor 1 Homo sapiens 350-355 34182538-3 2021 Herein, considering that GPR30 mediates transcriptional regulation in different cell backgrounds, a microarray strategy was applied in immortalized CAFs derived from primary breast cancer samples, resulting in the identification of 165 GPR30 target genes, among which HMGB1 was confirmed to be upregulated by 17-beta estradiol(E2)- and TAM-triggered GPR30 activation in CAFs. Estradiol 327-329 G protein-coupled estrogen receptor 1 Homo sapiens 25-30 34182538-3 2021 Herein, considering that GPR30 mediates transcriptional regulation in different cell backgrounds, a microarray strategy was applied in immortalized CAFs derived from primary breast cancer samples, resulting in the identification of 165 GPR30 target genes, among which HMGB1 was confirmed to be upregulated by 17-beta estradiol(E2)- and TAM-triggered GPR30 activation in CAFs. Estradiol 327-329 G protein-coupled estrogen receptor 1 Homo sapiens 236-241 34182538-3 2021 Herein, considering that GPR30 mediates transcriptional regulation in different cell backgrounds, a microarray strategy was applied in immortalized CAFs derived from primary breast cancer samples, resulting in the identification of 165 GPR30 target genes, among which HMGB1 was confirmed to be upregulated by 17-beta estradiol(E2)- and TAM-triggered GPR30 activation in CAFs. Tamoxifen 336-339 G protein-coupled estrogen receptor 1 Homo sapiens 25-30 34182538-3 2021 Herein, considering that GPR30 mediates transcriptional regulation in different cell backgrounds, a microarray strategy was applied in immortalized CAFs derived from primary breast cancer samples, resulting in the identification of 165 GPR30 target genes, among which HMGB1 was confirmed to be upregulated by 17-beta estradiol(E2)- and TAM-triggered GPR30 activation in CAFs. Tamoxifen 336-339 G protein-coupled estrogen receptor 1 Homo sapiens 236-241 34182538-3 2021 Herein, considering that GPR30 mediates transcriptional regulation in different cell backgrounds, a microarray strategy was applied in immortalized CAFs derived from primary breast cancer samples, resulting in the identification of 165 GPR30 target genes, among which HMGB1 was confirmed to be upregulated by 17-beta estradiol(E2)- and TAM-triggered GPR30 activation in CAFs. Tamoxifen 336-339 G protein-coupled estrogen receptor 1 Homo sapiens 350-355 34182538-4 2021 Activated GPR30 increased extracellular HMGB1 secretion by CAFs, which was reduced by blocking PI3K/AKT signaling using G15 or LY294002. 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one 127-135 G protein-coupled estrogen receptor 1 Homo sapiens 10-15 34182538-5 2021 GPR30-induced HMGB1 upregulation triggered MEK/ERK signaling, leading to increased autophagic behavior to protect cancer cells from TAM-induced apoptosis, mimicking the recombinant HMGB1-mediated increase in cancer cell resistance potential to TAM. Tamoxifen 132-135 G protein-coupled estrogen receptor 1 Homo sapiens 0-5 34239558-6 2021 Suppression of MR did not influence GPER1 expression, and GPER1 was capable of mediating part of aldosterone-induced endothelial inflammatory response. Aldosterone 97-108 G protein-coupled estrogen receptor 1 Homo sapiens 58-63 34248622-6 2021 In si-GPER1-treated HUVECs, the anti-apoptotic effect of BZBS was decreased. bzbs 57-61 G protein-coupled estrogen receptor 1 Homo sapiens 6-11 34248622-7 2021 This study revealed that BZBS exhibited a clear effect against atherogenesis via GPER1-dependent anti-inflammatory and anti-apoptotic mechanisms. bzbs 25-29 G protein-coupled estrogen receptor 1 Homo sapiens 81-86 34248622-0 2021 Bazi Bushen Capsule Alleviates Post-Menopausal Atherosclerosis via GPER1-Dependent Anti-Inflammatory and Anti-Apoptotic Effects. bazi bushen 0-11 G protein-coupled estrogen receptor 1 Homo sapiens 67-72 34205363-4 2021 In addition to the MR, aldosterone can bind and stimulate other receptors, such as the plasma membrane-residing G protein-coupled estrogen receptor (GPER), further complicating it signaling properties in the myocardium. Aldosterone 23-34 G protein-coupled estrogen receptor 1 Homo sapiens 112-147 34205363-4 2021 In addition to the MR, aldosterone can bind and stimulate other receptors, such as the plasma membrane-residing G protein-coupled estrogen receptor (GPER), further complicating it signaling properties in the myocardium. Aldosterone 23-34 G protein-coupled estrogen receptor 1 Homo sapiens 149-153 34239558-0 2021 G Protein-Coupled Estrogen Receptor 1 (GPER1) Mediates Aldosterone-Induced Endothelial Inflammation in a Mineralocorticoid Receptor-Independent Manner. Aldosterone 55-66 G protein-coupled estrogen receptor 1 Homo sapiens 0-37 34239558-0 2021 G Protein-Coupled Estrogen Receptor 1 (GPER1) Mediates Aldosterone-Induced Endothelial Inflammation in a Mineralocorticoid Receptor-Independent Manner. Aldosterone 55-66 G protein-coupled estrogen receptor 1 Homo sapiens 39-44 34239558-3 2021 However, whether GPER1 mediates aldosterone-induced inflammation response in endothelial cells and its relationship with MR are yet undetermined and therefore require further explanation. Aldosterone 32-43 G protein-coupled estrogen receptor 1 Homo sapiens 17-22 34239558-8 2021 Conclusion: These findings not only demonstrated the role of GPER1 in aldosterone-induced vascular inflammation but also suggested an alternative for pharmaceutical treatment of hyperaldosteronism considering the unsatisfying effect on cardiovascular risks with MR antagonists. Aldosterone 70-81 G protein-coupled estrogen receptor 1 Homo sapiens 61-66 34602561-4 2021 However, the effects of BPA/MBP on GPER1, have not yet been fully resolved. bisphenol A 24-27 G protein-coupled estrogen receptor 1 Homo sapiens 35-40 35245871-7 2022 Therefore, TCS acts on GPER to activate the downstream PKC/MAPK signaling pathway, further up-regulating miR-144 expression and causing abnormal modulation of these nerve-related genes to trigger neurodevelopmental toxicity. Triclosan 11-14 G protein-coupled estrogen receptor 1 Homo sapiens 23-27 34602561-0 2021 4-Methyl-2,4-bis(4-hydroxyphenyl)pent-1-ene (MBP) Targets Estrogen Receptor beta, to Evoke the Resistance of Human Breast Cancer MCF-7 Cells to G-1, an Agonist for G Protein-Coupled Estrogen Receptor 1. 4-methyl-2,4-bis(4-hydroxyphenyl)pent-1-ene 0-43 G protein-coupled estrogen receptor 1 Homo sapiens 164-201 35245871-1 2022 Although the previous research confirmed that triclosan (TCS) induced an estrogen effect by acting on a novel G-protein coupled estrogen-membrane receptor (GPER), the underlying mechanisms by which downstream pathways induce neurotoxicity remain unclear after TCS activation of GPER. Triclosan 46-55 G protein-coupled estrogen receptor 1 Homo sapiens 110-154 35245871-1 2022 Although the previous research confirmed that triclosan (TCS) induced an estrogen effect by acting on a novel G-protein coupled estrogen-membrane receptor (GPER), the underlying mechanisms by which downstream pathways induce neurotoxicity remain unclear after TCS activation of GPER. Triclosan 46-55 G protein-coupled estrogen receptor 1 Homo sapiens 156-160 35245871-1 2022 Although the previous research confirmed that triclosan (TCS) induced an estrogen effect by acting on a novel G-protein coupled estrogen-membrane receptor (GPER), the underlying mechanisms by which downstream pathways induce neurotoxicity remain unclear after TCS activation of GPER. Triclosan 46-55 G protein-coupled estrogen receptor 1 Homo sapiens 278-282 35537249-6 2022 We demonstrated that GPER1 and OXTR aggregates might be formed due to interactions with GAGs rather than arising from changes of levels of these proteins in cells. Glycosaminoglycans 88-92 G protein-coupled estrogen receptor 1 Homo sapiens 21-26 35245871-1 2022 Although the previous research confirmed that triclosan (TCS) induced an estrogen effect by acting on a novel G-protein coupled estrogen-membrane receptor (GPER), the underlying mechanisms by which downstream pathways induce neurotoxicity remain unclear after TCS activation of GPER. Triclosan 57-60 G protein-coupled estrogen receptor 1 Homo sapiens 110-154 35245871-1 2022 Although the previous research confirmed that triclosan (TCS) induced an estrogen effect by acting on a novel G-protein coupled estrogen-membrane receptor (GPER), the underlying mechanisms by which downstream pathways induce neurotoxicity remain unclear after TCS activation of GPER. Triclosan 57-60 G protein-coupled estrogen receptor 1 Homo sapiens 156-160 35245871-1 2022 Although the previous research confirmed that triclosan (TCS) induced an estrogen effect by acting on a novel G-protein coupled estrogen-membrane receptor (GPER), the underlying mechanisms by which downstream pathways induce neurotoxicity remain unclear after TCS activation of GPER. Triclosan 57-60 G protein-coupled estrogen receptor 1 Homo sapiens 278-282 35326671-0 2022 27-Hydroxycholesterol Binds GPER and Induces Progression of Estrogen Receptor-Negative Breast Cancer. 27-hydroxycholesterol 0-21 G protein-coupled estrogen receptor 1 Homo sapiens 28-32 35440074-0 2022 Dehydroepiandrosterone exacerbates nigericin-induced abnormal autophagy and pyroptosis via GPER activation in LPS-primed macrophages. Dehydroepiandrosterone 0-22 G protein-coupled estrogen receptor 1 Homo sapiens 91-95 35440074-0 2022 Dehydroepiandrosterone exacerbates nigericin-induced abnormal autophagy and pyroptosis via GPER activation in LPS-primed macrophages. Nigericin 35-44 G protein-coupled estrogen receptor 1 Homo sapiens 91-95 35326671-10 2022 Collectively, these data demonstrate that cholesterol conversion into 27HC promotes ER- BC growth and progression, and the expression of GPER is required for its effects. Cholesterol 42-53 G protein-coupled estrogen receptor 1 Homo sapiens 137-141 35446883-8 2022 Additionally, using gene ontology enrichment analysis, we demonstrated for timolol a significant enrichment in 23 pathways, 19 of them including either GPER1 or PDE4B. Timolol 75-82 G protein-coupled estrogen receptor 1 Homo sapiens 152-157 35446883-9 2022 In the case of carvedilol, we showed that, beside genes with well-established association with hypertension (GPER1, PDE4B and TNFAIP3), the drug also affects genes that are only indirectly linked to hypertension due to their effects on artery walls or their role in lipid biosynthesis. Carvedilol 15-25 G protein-coupled estrogen receptor 1 Homo sapiens 109-114 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Dehydroepiandrosterone 153-157 G protein-coupled estrogen receptor 1 Homo sapiens 68-103 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Dehydroepiandrosterone 153-157 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Dehydroepiandrosterone 153-157 G protein-coupled estrogen receptor 1 Homo sapiens 205-209 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Nigericin 161-164 G protein-coupled estrogen receptor 1 Homo sapiens 68-103 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Nigericin 161-164 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Nigericin 161-164 G protein-coupled estrogen receptor 1 Homo sapiens 205-209 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Dehydroepiandrosterone 347-351 G protein-coupled estrogen receptor 1 Homo sapiens 68-103 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Dehydroepiandrosterone 347-351 G protein-coupled estrogen receptor 1 Homo sapiens 105-109 35440074-8 2022 Mechanistically, the present study certified that the activation of G protein-coupled estrogen receptor (GPER) signal mediated the cell death induced by DHEA in Nig-stimulated inflammatory macrophages, as GPER specific inhibitor G15 alleviated the abnormal autophagy and ultimately prevented the gasdermin D (GSDMD)-mediated pyroptosis induced by DHEA. Dehydroepiandrosterone 347-351 G protein-coupled estrogen receptor 1 Homo sapiens 205-209 35440074-9 2022 Collectively, DHEA can exacerbate Nig-induced abnormal autophagy and pyroptosis via activation of GPER in LPS-primed macrophages, which prompts us the potential application value of DHEA in anti-infection or anti-tumor immunity. Dehydroepiandrosterone 14-18 G protein-coupled estrogen receptor 1 Homo sapiens 98-102 35440074-9 2022 Collectively, DHEA can exacerbate Nig-induced abnormal autophagy and pyroptosis via activation of GPER in LPS-primed macrophages, which prompts us the potential application value of DHEA in anti-infection or anti-tumor immunity. Nigericin 34-37 G protein-coupled estrogen receptor 1 Homo sapiens 98-102 35440074-9 2022 Collectively, DHEA can exacerbate Nig-induced abnormal autophagy and pyroptosis via activation of GPER in LPS-primed macrophages, which prompts us the potential application value of DHEA in anti-infection or anti-tumor immunity. Dehydroepiandrosterone 182-186 G protein-coupled estrogen receptor 1 Homo sapiens 98-102 35519261-3 2022 The biosensor is made by an 18 TFBG with a 50 nm-thick gold nanofilm coating over the surface of the fiber, further immobilized with a specific antibody against GPR30, which is a membrane receptor expressed in many breast cancers, serving as bait. TFBG 32-36 G protein-coupled estrogen receptor 1 Homo sapiens 162-167 35122788-10 2022 In addition, DHEA may interact with the G-protein coupled receptor GPER for stimulation of miR-21 and subsequent activation of the MAPK pathway. Dehydroepiandrosterone 13-17 G protein-coupled estrogen receptor 1 Homo sapiens 67-71 35337112-7 2022 Tamoxifen is a known agonist of GPER1, a receptor that can promote tumor progression. Tamoxifen 0-9 G protein-coupled estrogen receptor 1 Homo sapiens 32-37 35237599-9 2022 The observed cytotoxic effects, apparently, were not triggered by the interaction of G-1 with the GPER as pre-incubation with the highly selective GPER antagonist G-36 was ineffective in preventing the cytotoxicity of G-1. G-36 163-167 G protein-coupled estrogen receptor 1 Homo sapiens 147-151 35170266-3 2022 The role of G protein-coupled estrogen receptor (GPR30), which mediates the non-genomic effects of E2, is mostly unexplored. Estradiol 99-101 G protein-coupled estrogen receptor 1 Homo sapiens 49-54 35242036-9 2022 Ovarian cancer tumor tissues chronically (30 days) treated with JWH-133 in comparison to vehicle treated groups showed an increase in endocannabinoid (AEA and 2-AG) and protein (CB2 and TNFalpha) levels with a decrease in GPER protein levels. 1,1-dimethylbutyl-1-deoxy-Delta(9)-THC 64-71 G protein-coupled estrogen receptor 1 Homo sapiens 222-226 35061800-0 2022 Cryptotanshinone inhibits proliferation and induces apoptosis of breast cancer MCF-7 cells via GPER mediated PI3K/AKT signaling pathway. cryptotanshinone 0-16 G protein-coupled estrogen receptor 1 Homo sapiens 95-99 35061800-2 2022 This study aimed to illuminate the function of GPER and its mediated PI3K/AKT pathway in cryptotanshinone (CPT) inducing cell apoptosis and antiproliferation effect on GPER positive breast cancer MCF-7 cells. cryptotanshinone 89-105 G protein-coupled estrogen receptor 1 Homo sapiens 47-51 35061800-2 2022 This study aimed to illuminate the function of GPER and its mediated PI3K/AKT pathway in cryptotanshinone (CPT) inducing cell apoptosis and antiproliferation effect on GPER positive breast cancer MCF-7 cells. cryptotanshinone 107-110 G protein-coupled estrogen receptor 1 Homo sapiens 47-51 35061800-2 2022 This study aimed to illuminate the function of GPER and its mediated PI3K/AKT pathway in cryptotanshinone (CPT) inducing cell apoptosis and antiproliferation effect on GPER positive breast cancer MCF-7 cells. cryptotanshinone 89-105 G protein-coupled estrogen receptor 1 Homo sapiens 168-172 35061800-2 2022 This study aimed to illuminate the function of GPER and its mediated PI3K/AKT pathway in cryptotanshinone (CPT) inducing cell apoptosis and antiproliferation effect on GPER positive breast cancer MCF-7 cells. cryptotanshinone 107-110 G protein-coupled estrogen receptor 1 Homo sapiens 168-172 35061800-5 2022 Autodock vina was applied to make molecular docking between CPT or estradiol and GPER. Estradiol 67-76 G protein-coupled estrogen receptor 1 Homo sapiens 81-85 35096058-4 2022 In this study, we aim to evaluate the clinical relevance of GPR30 expression in GC patients and the role of the GPR30/PI3K/AKT signalling pathway in the anti-GC effect of NEH. neh 171-174 G protein-coupled estrogen receptor 1 Homo sapiens 112-117 35096058-13 2022 Furthermore, NEH inhibited the proliferation, migration, and invasion in GC cells in a concentration-dependent manner through inhibiting the GPR30-mediated PI3K/AKT signalling pathway in vitro. neh 13-16 G protein-coupled estrogen receptor 1 Homo sapiens 141-146