PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 33715419-2 2021 Materials & methods: Bioinformatic docking of candidate molecules featuring a wide range of carboxylic acid bioisosteres into complex with GPR40 was performed using TAK-875 and GW9508 templates. GW9508 177-183 free fatty acid receptor 1 Homo sapiens 139-144 33376857-0 2020 GPR120 Agonist GW9508 Ameliorated Cellular Senescence Induced by ox-LDL. GW9508 15-21 free fatty acid receptor 4 Homo sapiens 0-6 33009637-4 2021 GPR120 agonist GW9508 activated the GPR120 pathway. GW9508 15-21 free fatty acid receptor 4 Homo sapiens 0-6 33009637-4 2021 GPR120 agonist GW9508 activated the GPR120 pathway. GW9508 15-21 free fatty acid receptor 4 Homo sapiens 36-42 33376857-8 2020 Typically, 100 mug/mL of ox-LDL- induced 35.2% LDH release, which was reduced to 16.9% by 50 muM GW9508, the agonist of GPR120. GW9508 97-103 free fatty acid receptor 4 Homo sapiens 120-126 33376857-10 2020 Furthermore, we found that GW9508 ameliorated ox-LDL-induced endothelial cell cycle arrest at the G0/G1 phase and the expression of key senescence proteins, including p53 and plasminogen activator inhibitor-1(PAI-1). GW9508 27-33 tumor protein p53 Homo sapiens 167-170 33376857-10 2020 Furthermore, we found that GW9508 ameliorated ox-LDL-induced endothelial cell cycle arrest at the G0/G1 phase and the expression of key senescence proteins, including p53 and plasminogen activator inhibitor-1(PAI-1). GW9508 27-33 serpin family E member 1 Homo sapiens 175-208 33376857-10 2020 Furthermore, we found that GW9508 ameliorated ox-LDL-induced endothelial cell cycle arrest at the G0/G1 phase and the expression of key senescence proteins, including p53 and plasminogen activator inhibitor-1(PAI-1). GW9508 27-33 serpin family E member 1 Homo sapiens 209-214 33376857-11 2020 Mechanistically, we showed that GW9508 promoted ox-LDL-induced transcriptional factor NF-E2-related factor 2 (NRF2) (increase by 47.3%) translocation into the nucleus. GW9508 32-38 NFE2 like bZIP transcription factor 2 Homo sapiens 86-108 33376857-11 2020 Mechanistically, we showed that GW9508 promoted ox-LDL-induced transcriptional factor NF-E2-related factor 2 (NRF2) (increase by 47.3%) translocation into the nucleus. GW9508 32-38 NFE2 like bZIP transcription factor 2 Homo sapiens 110-114 33376857-12 2020 The effect of GW9508 is dependent on its receptor GPR120, the blockage of which by its specific antagonist, AH7614, abolished the antisenescence effect of GW9508. GW9508 14-20 free fatty acid receptor 4 Homo sapiens 50-56 33376857-12 2020 The effect of GW9508 is dependent on its receptor GPR120, the blockage of which by its specific antagonist, AH7614, abolished the antisenescence effect of GW9508. GW9508 155-161 free fatty acid receptor 4 Homo sapiens 50-56 32243091-4 2020 In this study, we found for the first time that stimulation of GPR120 by its agonist GW9508 elevated the expression of ATP-binding cassette transporters (ABC) A1 and ABCG1 in THP-1 macrophage-derived foam cells and Raw264.7 macrophages, and promoted ABCA1- and ABCG1-mediated cholesterol efflux and reduced cellular cholesteryl ester content as well. GW9508 85-91 free fatty acid receptor 4 Homo sapiens 63-69 32243091-4 2020 In this study, we found for the first time that stimulation of GPR120 by its agonist GW9508 elevated the expression of ATP-binding cassette transporters (ABC) A1 and ABCG1 in THP-1 macrophage-derived foam cells and Raw264.7 macrophages, and promoted ABCA1- and ABCG1-mediated cholesterol efflux and reduced cellular cholesteryl ester content as well. GW9508 85-91 ATP binding cassette subfamily A member 1 Homo sapiens 119-161 32243091-4 2020 In this study, we found for the first time that stimulation of GPR120 by its agonist GW9508 elevated the expression of ATP-binding cassette transporters (ABC) A1 and ABCG1 in THP-1 macrophage-derived foam cells and Raw264.7 macrophages, and promoted ABCA1- and ABCG1-mediated cholesterol efflux and reduced cellular cholesteryl ester content as well. GW9508 85-91 ATP binding cassette subfamily G member 1 Homo sapiens 166-171 32243091-4 2020 In this study, we found for the first time that stimulation of GPR120 by its agonist GW9508 elevated the expression of ATP-binding cassette transporters (ABC) A1 and ABCG1 in THP-1 macrophage-derived foam cells and Raw264.7 macrophages, and promoted ABCA1- and ABCG1-mediated cholesterol efflux and reduced cellular cholesteryl ester content as well. GW9508 85-91 GLI family zinc finger 2 Homo sapiens 175-180 32243091-4 2020 In this study, we found for the first time that stimulation of GPR120 by its agonist GW9508 elevated the expression of ATP-binding cassette transporters (ABC) A1 and ABCG1 in THP-1 macrophage-derived foam cells and Raw264.7 macrophages, and promoted ABCA1- and ABCG1-mediated cholesterol efflux and reduced cellular cholesteryl ester content as well. GW9508 85-91 ATP binding cassette subfamily A member 1 Homo sapiens 250-255 32243091-4 2020 In this study, we found for the first time that stimulation of GPR120 by its agonist GW9508 elevated the expression of ATP-binding cassette transporters (ABC) A1 and ABCG1 in THP-1 macrophage-derived foam cells and Raw264.7 macrophages, and promoted ABCA1- and ABCG1-mediated cholesterol efflux and reduced cellular cholesteryl ester content as well. GW9508 85-91 ATP binding cassette subfamily G member 1 Homo sapiens 261-266 32354273-5 2020 NOX2 KO islets were used to measure total cytosolic calcium and insulin secretion.Results: GW9508 and linoleic acid increased superoxide and H2O2 contents at 5.6 and 8.3 mM of glucose. GW9508 91-97 cytochrome b-245 beta chain Rattus norvegicus 0-4 32354273-7 2020 Knockdown of p22phox abolished the increase in superoxide after GW9508 and linoleic acid. GW9508 64-70 cytochrome b-245 alpha chain Rattus norvegicus 13-20 32354273-8 2020 No differences in insulin secretion were found between wild type and NOX2 KO islets treated with GW9508 or linoleic acid.Discussion: We report for the first time that acute activation of GPR40 leads to NADPH oxidase activation in pancreatic beta-cells, without impact on insulin secretion. GW9508 97-103 free fatty acid receptor 1 Rattus norvegicus 187-192 32893672-14 2020 The GW9508 treatment increased leptin levels, without altering UCP-1 downregulation in visceral fat. GW9508 4-10 leptin Mus musculus 31-37 32580167-8 2020 We also show that GW9508 and TUG891 rescue the expression of type II collagen and aggrecan by preventing the reduction of SOX9 expression. GW9508 18-24 SRY-box transcription factor 9 Homo sapiens 122-126 32347098-9 2020 Additionally, GW9508 also restored ox-LDL-induced dephosphorylation of cAMP-responsive element-binding protein (CREB), which was also abolished by compound C. Finally, we found that AMPKalpha and CREB participated in mediating the effects of GW9508 on the expression of peroxisome proliferator-activated receptor gamma coactivator-1alpha (PGC-1alpha) and mitochondrial homeostasis. GW9508 242-248 cAMP responsive element binding protein 1 Homo sapiens 112-116 33133087-0 2020 The GPR40 Agonist GW9508 Enhances Neutrophil Function to Aid Bacterial Clearance During E. coli Infections. GW9508 18-24 free fatty acid receptor 1 Homo sapiens 4-9 33133087-3 2020 In the present study, we demonstrate that GPR40 is upregulated on activated human neutrophils and investigated the functional effects upon treatment with a selective agonist; GW9508. GW9508 175-181 free fatty acid receptor 1 Homo sapiens 42-47 32347098-0 2020 GPR40 agonist GW9508 ameliorates oxidized LDL-induced endothelial dysfunction via the AMPK/CREB/PGC1alpha pathway. GW9508 14-20 free fatty acid receptor 1 Homo sapiens 0-5 32347098-0 2020 GPR40 agonist GW9508 ameliorates oxidized LDL-induced endothelial dysfunction via the AMPK/CREB/PGC1alpha pathway. GW9508 14-20 protein kinase AMP-activated catalytic subunit alpha 2 Homo sapiens 86-90 32347098-0 2020 GPR40 agonist GW9508 ameliorates oxidized LDL-induced endothelial dysfunction via the AMPK/CREB/PGC1alpha pathway. GW9508 14-20 cAMP responsive element binding protein 1 Homo sapiens 91-95 32347098-0 2020 GPR40 agonist GW9508 ameliorates oxidized LDL-induced endothelial dysfunction via the AMPK/CREB/PGC1alpha pathway. GW9508 14-20 PPARG coactivator 1 alpha Homo sapiens 96-105 32347098-5 2020 Interestingly, we found that the activation of GPR40 by its agonist GW9508 ameliorated ox-LDL-induced reduced cell viability of HAECs. GW9508 68-74 free fatty acid receptor 1 Homo sapiens 47-52 32347098-7 2020 Mechanistically, we found that GW9508 mitigated ox-LDL-induced inactivation of adenosine 5"-monophosphate (AMP)-activated protein kinase alpha (AMPKalpha), however, the blockage of GPR40 by its antagonist GW1100 completely abolished the protective effect of GW9508 on AMPKalpha activation. GW9508 31-37 free fatty acid receptor 1 Homo sapiens 181-186 32347098-9 2020 Additionally, GW9508 also restored ox-LDL-induced dephosphorylation of cAMP-responsive element-binding protein (CREB), which was also abolished by compound C. Finally, we found that AMPKalpha and CREB participated in mediating the effects of GW9508 on the expression of peroxisome proliferator-activated receptor gamma coactivator-1alpha (PGC-1alpha) and mitochondrial homeostasis. GW9508 14-20 cAMP responsive element binding protein 1 Homo sapiens 71-110 32347098-9 2020 Additionally, GW9508 also restored ox-LDL-induced dephosphorylation of cAMP-responsive element-binding protein (CREB), which was also abolished by compound C. Finally, we found that AMPKalpha and CREB participated in mediating the effects of GW9508 on the expression of peroxisome proliferator-activated receptor gamma coactivator-1alpha (PGC-1alpha) and mitochondrial homeostasis. GW9508 14-20 cAMP responsive element binding protein 1 Homo sapiens 112-116 32347098-9 2020 Additionally, GW9508 also restored ox-LDL-induced dephosphorylation of cAMP-responsive element-binding protein (CREB), which was also abolished by compound C. Finally, we found that AMPKalpha and CREB participated in mediating the effects of GW9508 on the expression of peroxisome proliferator-activated receptor gamma coactivator-1alpha (PGC-1alpha) and mitochondrial homeostasis. GW9508 14-20 cAMP responsive element binding protein 1 Homo sapiens 196-200 32347098-9 2020 Additionally, GW9508 also restored ox-LDL-induced dephosphorylation of cAMP-responsive element-binding protein (CREB), which was also abolished by compound C. Finally, we found that AMPKalpha and CREB participated in mediating the effects of GW9508 on the expression of peroxisome proliferator-activated receptor gamma coactivator-1alpha (PGC-1alpha) and mitochondrial homeostasis. GW9508 14-20 PPARG coactivator 1 alpha Homo sapiens 270-337 32347098-9 2020 Additionally, GW9508 also restored ox-LDL-induced dephosphorylation of cAMP-responsive element-binding protein (CREB), which was also abolished by compound C. Finally, we found that AMPKalpha and CREB participated in mediating the effects of GW9508 on the expression of peroxisome proliferator-activated receptor gamma coactivator-1alpha (PGC-1alpha) and mitochondrial homeostasis. GW9508 14-20 PPARG coactivator 1 alpha Homo sapiens 339-349 32347098-9 2020 Additionally, GW9508 also restored ox-LDL-induced dephosphorylation of cAMP-responsive element-binding protein (CREB), which was also abolished by compound C. Finally, we found that AMPKalpha and CREB participated in mediating the effects of GW9508 on the expression of peroxisome proliferator-activated receptor gamma coactivator-1alpha (PGC-1alpha) and mitochondrial homeostasis. GW9508 242-248 cAMP responsive element binding protein 1 Homo sapiens 71-110 32580167-9 2020 Additionally, we demonstrate that the effects of GW9508 on SOX9 expression are mediated through CREB and that GPR120 is indeed required for this effect. GW9508 49-55 SRY-box transcription factor 9 Homo sapiens 59-63 32580167-9 2020 Additionally, we demonstrate that the effects of GW9508 on SOX9 expression are mediated through CREB and that GPR120 is indeed required for this effect. GW9508 49-55 cAMP responsive element binding protein 1 Homo sapiens 96-100 32580167-9 2020 Additionally, we demonstrate that the effects of GW9508 on SOX9 expression are mediated through CREB and that GPR120 is indeed required for this effect. GW9508 49-55 free fatty acid receptor 4 Homo sapiens 110-116 32580167-10 2020 Thus, agonism of GPR120 by GW9508 might be a potential therapeutic strategy to halt or prevent cartilage degradation. GW9508 27-33 free fatty acid receptor 4 Homo sapiens 17-23 32431615-8 2020 Besides, HaCaT cells stimulated with LA or GW9508 increased the activity of MMP-9 and the expression of IL-8. GW9508 43-49 matrix metallopeptidase 9 Homo sapiens 76-81 32606604-5 2020 The purpose of the present study was to determine the impact of the GPR40 agonist GW9508 on AGEs-treated chondrocytes. GW9508 82-88 free fatty acid receptor 1 Homo sapiens 68-73 32606604-11 2020 Treatment with GW9508 plays a beneficial role in protecting type II Collagen and aggrecan from degeneration by attenuating the expression of MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5. GW9508 15-21 matrix metallopeptidase 3 Homo sapiens 141-146 32606604-11 2020 Treatment with GW9508 plays a beneficial role in protecting type II Collagen and aggrecan from degeneration by attenuating the expression of MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5. GW9508 15-21 matrix metallopeptidase 13 Homo sapiens 148-154 32606604-11 2020 Treatment with GW9508 plays a beneficial role in protecting type II Collagen and aggrecan from degeneration by attenuating the expression of MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5. GW9508 15-21 ADAM metallopeptidase with thrombospondin type 1 motif 4 Homo sapiens 156-164 32606604-11 2020 Treatment with GW9508 plays a beneficial role in protecting type II Collagen and aggrecan from degeneration by attenuating the expression of MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5. GW9508 15-21 ADAM metallopeptidase with thrombospondin type 1 motif 5 Homo sapiens 170-178 32606604-12 2020 Additionally, GW9508 reduces the appearance of pro-inflammatory cytokines and suppresses NF-kappaB activation in AGEs-induced chondrocytes. GW9508 14-20 nuclear factor kappa B subunit 1 Homo sapiens 89-98 32606604-13 2020 Notably, co-treatment with GW1100, a specific antagonist of GPR40, abolishes the beneficial role of GW9508 against AGEs, implying that GPR40 mediates these effects of GW9508. GW9508 100-106 free fatty acid receptor 1 Homo sapiens 60-65 32606604-13 2020 Notably, co-treatment with GW1100, a specific antagonist of GPR40, abolishes the beneficial role of GW9508 against AGEs, implying that GPR40 mediates these effects of GW9508. GW9508 167-173 free fatty acid receptor 1 Homo sapiens 60-65 32606604-13 2020 Notably, co-treatment with GW1100, a specific antagonist of GPR40, abolishes the beneficial role of GW9508 against AGEs, implying that GPR40 mediates these effects of GW9508. GW9508 167-173 free fatty acid receptor 1 Homo sapiens 135-140 32606604-14 2020 Conclusion: Our results suggest that GPR40 is a novel therapeutic target for OA and that GPR40 agonists, including GW9508, may have therapeutic potential in preventing and slowing the progression of OA. GW9508 115-121 free fatty acid receptor 1 Homo sapiens 89-94 32431615-8 2020 Besides, HaCaT cells stimulated with LA or GW9508 increased the activity of MMP-9 and the expression of IL-8. GW9508 43-49 C-X-C motif chemokine ligand 8 Homo sapiens 104-108 32431615-12 2020 Furthermore, IL-8 secreted by HaCaT cells stimulated with LA or GW9508, contributed to neutrophil chemotaxis. GW9508 64-70 C-X-C motif chemokine ligand 8 Homo sapiens 13-17 31809762-0 2020 GW9508 ameliorates cognitive impairment via the cAMP-CREB and JNK pathways in APPswe/PS1dE9 mouse model of Alzheimer"s disease. GW9508 0-6 cAMP responsive element binding protein 1 Mus musculus 53-57 31809762-0 2020 GW9508 ameliorates cognitive impairment via the cAMP-CREB and JNK pathways in APPswe/PS1dE9 mouse model of Alzheimer"s disease. GW9508 0-6 mitogen-activated protein kinase 8 Mus musculus 62-65 31809762-3 2020 GPR40 agonist GW9508 and antagonist GW1100 were respectively given by i.c.v. GW9508 14-20 free fatty acid receptor 1 Mus musculus 0-5 31809762-6 2020 The results revealed that treatment with GW9508 could significantly ameliorate cognitive deficits of APP/PS1 mice, upregulate the expression levels of cAMP, p-CREB and neurotrophic factors in vivo, while GW9508 also ameliorate Abeta1-42-induced neuron damage and downregulate the expression levels of pathological protein such as p-JNK, JNK and apoptosis-related proteins such as IL-6, IL-1beta, TNF-alpha and caspase-3 in vitro. GW9508 41-47 amyloid beta (A4) precursor protein Mus musculus 101-108 31809762-6 2020 The results revealed that treatment with GW9508 could significantly ameliorate cognitive deficits of APP/PS1 mice, upregulate the expression levels of cAMP, p-CREB and neurotrophic factors in vivo, while GW9508 also ameliorate Abeta1-42-induced neuron damage and downregulate the expression levels of pathological protein such as p-JNK, JNK and apoptosis-related proteins such as IL-6, IL-1beta, TNF-alpha and caspase-3 in vitro. GW9508 41-47 cAMP responsive element binding protein 1 Mus musculus 159-163 31809762-6 2020 The results revealed that treatment with GW9508 could significantly ameliorate cognitive deficits of APP/PS1 mice, upregulate the expression levels of cAMP, p-CREB and neurotrophic factors in vivo, while GW9508 also ameliorate Abeta1-42-induced neuron damage and downregulate the expression levels of pathological protein such as p-JNK, JNK and apoptosis-related proteins such as IL-6, IL-1beta, TNF-alpha and caspase-3 in vitro. GW9508 41-47 mitogen-activated protein kinase 8 Mus musculus 332-335 31809762-6 2020 The results revealed that treatment with GW9508 could significantly ameliorate cognitive deficits of APP/PS1 mice, upregulate the expression levels of cAMP, p-CREB and neurotrophic factors in vivo, while GW9508 also ameliorate Abeta1-42-induced neuron damage and downregulate the expression levels of pathological protein such as p-JNK, JNK and apoptosis-related proteins such as IL-6, IL-1beta, TNF-alpha and caspase-3 in vitro. GW9508 41-47 mitogen-activated protein kinase 8 Mus musculus 337-340 31809762-6 2020 The results revealed that treatment with GW9508 could significantly ameliorate cognitive deficits of APP/PS1 mice, upregulate the expression levels of cAMP, p-CREB and neurotrophic factors in vivo, while GW9508 also ameliorate Abeta1-42-induced neuron damage and downregulate the expression levels of pathological protein such as p-JNK, JNK and apoptosis-related proteins such as IL-6, IL-1beta, TNF-alpha and caspase-3 in vitro. GW9508 41-47 interleukin 6 Mus musculus 380-384 31809762-6 2020 The results revealed that treatment with GW9508 could significantly ameliorate cognitive deficits of APP/PS1 mice, upregulate the expression levels of cAMP, p-CREB and neurotrophic factors in vivo, while GW9508 also ameliorate Abeta1-42-induced neuron damage and downregulate the expression levels of pathological protein such as p-JNK, JNK and apoptosis-related proteins such as IL-6, IL-1beta, TNF-alpha and caspase-3 in vitro. GW9508 41-47 interleukin 1 beta Mus musculus 386-394 31809762-6 2020 The results revealed that treatment with GW9508 could significantly ameliorate cognitive deficits of APP/PS1 mice, upregulate the expression levels of cAMP, p-CREB and neurotrophic factors in vivo, while GW9508 also ameliorate Abeta1-42-induced neuron damage and downregulate the expression levels of pathological protein such as p-JNK, JNK and apoptosis-related proteins such as IL-6, IL-1beta, TNF-alpha and caspase-3 in vitro. GW9508 41-47 tumor necrosis factor Mus musculus 396-405 31809762-6 2020 The results revealed that treatment with GW9508 could significantly ameliorate cognitive deficits of APP/PS1 mice, upregulate the expression levels of cAMP, p-CREB and neurotrophic factors in vivo, while GW9508 also ameliorate Abeta1-42-induced neuron damage and downregulate the expression levels of pathological protein such as p-JNK, JNK and apoptosis-related proteins such as IL-6, IL-1beta, TNF-alpha and caspase-3 in vitro. GW9508 41-47 caspase 3 Mus musculus 410-419 31214048-6 2019 In endothelin 1-precontracted porcine LES strips, the FFA1 selective agonists, fasiglifam, TUG424, and GW9508, caused marked relaxations in a concentration-dependent manner. GW9508 103-109 endothelin 1 Homo sapiens 3-15 31870843-5 2020 In the present study, we tested the effects of two GPR120 agonists-GW9508 and TUG-891-in mitigating endothelial insult induced by ox-LDL in human aortic endothelial cells (HAECs). GW9508 67-73 free fatty acid receptor 4 Homo sapiens 51-57 31498851-0 2019 G-protein-coupled receptor 40 agonist GW9508 potentiates glucose-stimulated insulin secretion through activation of protein kinase Calpha and epsilon in INS-1 cells. GW9508 38-44 free fatty acid receptor 1 Rattus norvegicus 0-29 31498851-2 2019 We examined whether a GPR40 agonist, GW9508, could stimulate conventional and novel isoforms of PKC at two glucose concentrations (3 mM and 20 mM) in INS-1D cells. GW9508 37-43 free fatty acid receptor 1 Rattus norvegicus 22-27 31498851-2 2019 We examined whether a GPR40 agonist, GW9508, could stimulate conventional and novel isoforms of PKC at two glucose concentrations (3 mM and 20 mM) in INS-1D cells. GW9508 37-43 protein kinase C, alpha Rattus norvegicus 96-99 31498851-6 2019 RESULTS: At 3 mM glucose, GW9508 induced sustained MARCKS-GFP translocation to the cytosol, irrespective of changes in [Ca2+]i. GW9508 26-32 myristoylated alanine rich protein kinase C substrate Rattus norvegicus 51-57 31498851-7 2019 At 20 mM glucose, GW9508 induced sustained MARCKS-GFP translocation but also transient translocation that followed sharp increases in [Ca2+]i. GW9508 18-24 myristoylated alanine rich protein kinase C substrate Rattus norvegicus 43-49 31498851-9 2019 At 20 mM glucose, GW9508 induced transient translocation of PKCalpha and sustained translocation as well as transient translocation of PKCepsilon. GW9508 18-24 protein kinase C, alpha Rattus norvegicus 60-68 31498851-10 2019 While the inhibitors (75 muM) of each PKC isotype reduced GW9508-potentiated, glucose-stimulated insulin secretion in INS-1D cells, the PKCepsilon inhibitor had a more potent effect. GW9508 58-64 protein kinase C, alpha Rattus norvegicus 38-41 31129422-4 2019 This study was aimed to investigate the effect of GPR40 stimulation on proinflammatory cytokine (TNFalpha and IL-1beta)-induced tight junction disruption in human airway epithelial Calu-3 cells using GW9508, a GPR40 agonist. GW9508 200-206 free fatty acid receptor 1 Homo sapiens 50-55 31129422-4 2019 This study was aimed to investigate the effect of GPR40 stimulation on proinflammatory cytokine (TNFalpha and IL-1beta)-induced tight junction disruption in human airway epithelial Calu-3 cells using GW9508, a GPR40 agonist. GW9508 200-206 tumor necrosis factor Homo sapiens 97-105 31129422-5 2019 We found that stimulation of GPR40 by GW9508 attenuated the cytokine-induced airway epithelial barrier leakage as analyzed by measurements of transepithelial electrical resistance and transepithelial flux of fluorescently labeled dextran (molecular weight of 4 kDa). GW9508 38-44 free fatty acid receptor 1 Homo sapiens 29-34 31129422-6 2019 Furthermore, GW9508 prevented the cytokine-induced dislocalization of zonula occludens (ZO)-1, occludin and claudin-1. GW9508 13-19 tight junction protein 1 Homo sapiens 70-93 31129422-6 2019 Furthermore, GW9508 prevented the cytokine-induced dislocalization of zonula occludens (ZO)-1, occludin and claudin-1. GW9508 13-19 occludin Homo sapiens 95-103 31129422-6 2019 Furthermore, GW9508 prevented the cytokine-induced dislocalization of zonula occludens (ZO)-1, occludin and claudin-1. GW9508 13-19 claudin 1 Homo sapiens 108-117 31129422-7 2019 The barrier-protective effect of GW9508 was abolished by a GPR40 antagonist, but not a GPR120 antagonist. GW9508 33-39 free fatty acid receptor 1 Homo sapiens 59-64 31129422-9 2019 Intriguingly, GW9508 inhibited cytokine-induced airway epithelial barrier disruption through suppression of extracellular signal-regulated kinase (ERK) phosphorylation in a phospholipase C (PLC) and calcium/calmodulin-dependent protein kinase kinase beta (CaMKKbeta)-dependent manner. GW9508 14-20 mitogen-activated protein kinase 1 Homo sapiens 108-145 31129422-9 2019 Intriguingly, GW9508 inhibited cytokine-induced airway epithelial barrier disruption through suppression of extracellular signal-regulated kinase (ERK) phosphorylation in a phospholipase C (PLC) and calcium/calmodulin-dependent protein kinase kinase beta (CaMKKbeta)-dependent manner. GW9508 14-20 mitogen-activated protein kinase 1 Homo sapiens 147-150 31129422-9 2019 Intriguingly, GW9508 inhibited cytokine-induced airway epithelial barrier disruption through suppression of extracellular signal-regulated kinase (ERK) phosphorylation in a phospholipase C (PLC) and calcium/calmodulin-dependent protein kinase kinase beta (CaMKKbeta)-dependent manner. GW9508 14-20 calcium/calmodulin dependent protein kinase kinase 1 Homo sapiens 256-265 31129318-0 2019 Anti-atherosclerotic action of GW9508 - Free fatty acid receptors activator - In apoE-knockout mice. GW9508 31-37 apolipoprotein E Mus musculus 81-85 31129318-3 2019 METHODS: The present study investigates the influence of prolonged treatment with GW9508 - agonist of FFAR1 and FFAR4 - on the development of atherosclerosis plaque in apoE-knockout mice, using morphometric and molecular methods. GW9508 82-88 free fatty acid receptor 1 Mus musculus 102-107 31129318-3 2019 METHODS: The present study investigates the influence of prolonged treatment with GW9508 - agonist of FFAR1 and FFAR4 - on the development of atherosclerosis plaque in apoE-knockout mice, using morphometric and molecular methods. GW9508 82-88 free fatty acid receptor 4 Mus musculus 112-117 31129318-3 2019 METHODS: The present study investigates the influence of prolonged treatment with GW9508 - agonist of FFAR1 and FFAR4 - on the development of atherosclerosis plaque in apoE-knockout mice, using morphometric and molecular methods. GW9508 82-88 apolipoprotein E Mus musculus 168-172 31129318-4 2019 RESULTS: GW9508 administration has led to the reduction of atheroscletoric plaque size in an apoE-knockout mice model. GW9508 9-15 apolipoprotein E Mus musculus 93-97 31129318-6 2019 CONCLUSIONS: Prolonged administration of GW9508 resulted in significant amelioration of atherogenesis, providing evidence that the strategy based on macrophage phenotype switching toward an M2-like activation state via stimulation of FFAR1/FFAR4 receptors holds promise for a new approach to the prevention or treatment of atherosclerosis. GW9508 41-47 free fatty acid receptor 1 Mus musculus 234-239 31129318-6 2019 CONCLUSIONS: Prolonged administration of GW9508 resulted in significant amelioration of atherogenesis, providing evidence that the strategy based on macrophage phenotype switching toward an M2-like activation state via stimulation of FFAR1/FFAR4 receptors holds promise for a new approach to the prevention or treatment of atherosclerosis. GW9508 41-47 free fatty acid receptor 4 Mus musculus 240-245 31295865-5 2019 In vitro, pretreatment of rat proximal tubular (NRK52E) cells with GW9508, a GPR40 agonist, attenuated the decreased cell viability, increased the Bax/Bcl-2 protein expression ratio, increased protein expression of cleaved caspase-3 and activated the nuclear translocation of nuclear factor-kappaB (NF-kappaB) p65 subunit induced by TNF-alpha treatment. GW9508 67-73 free fatty acid receptor 1 Rattus norvegicus 77-82 31295865-5 2019 In vitro, pretreatment of rat proximal tubular (NRK52E) cells with GW9508, a GPR40 agonist, attenuated the decreased cell viability, increased the Bax/Bcl-2 protein expression ratio, increased protein expression of cleaved caspase-3 and activated the nuclear translocation of nuclear factor-kappaB (NF-kappaB) p65 subunit induced by TNF-alpha treatment. GW9508 67-73 BCL2 associated X, apoptosis regulator Rattus norvegicus 147-150 31295865-5 2019 In vitro, pretreatment of rat proximal tubular (NRK52E) cells with GW9508, a GPR40 agonist, attenuated the decreased cell viability, increased the Bax/Bcl-2 protein expression ratio, increased protein expression of cleaved caspase-3 and activated the nuclear translocation of nuclear factor-kappaB (NF-kappaB) p65 subunit induced by TNF-alpha treatment. GW9508 67-73 BCL2, apoptosis regulator Rattus norvegicus 151-156 31295865-5 2019 In vitro, pretreatment of rat proximal tubular (NRK52E) cells with GW9508, a GPR40 agonist, attenuated the decreased cell viability, increased the Bax/Bcl-2 protein expression ratio, increased protein expression of cleaved caspase-3 and activated the nuclear translocation of nuclear factor-kappaB (NF-kappaB) p65 subunit induced by TNF-alpha treatment. GW9508 67-73 caspase 3 Rattus norvegicus 223-232 31295865-5 2019 In vitro, pretreatment of rat proximal tubular (NRK52E) cells with GW9508, a GPR40 agonist, attenuated the decreased cell viability, increased the Bax/Bcl-2 protein expression ratio, increased protein expression of cleaved caspase-3 and activated the nuclear translocation of nuclear factor-kappaB (NF-kappaB) p65 subunit induced by TNF-alpha treatment. GW9508 67-73 synaptotagmin 1 Rattus norvegicus 310-313 31295865-5 2019 In vitro, pretreatment of rat proximal tubular (NRK52E) cells with GW9508, a GPR40 agonist, attenuated the decreased cell viability, increased the Bax/Bcl-2 protein expression ratio, increased protein expression of cleaved caspase-3 and activated the nuclear translocation of nuclear factor-kappaB (NF-kappaB) p65 subunit induced by TNF-alpha treatment. GW9508 67-73 tumor necrosis factor Rattus norvegicus 333-342 31214048-6 2019 In endothelin 1-precontracted porcine LES strips, the FFA1 selective agonists, fasiglifam, TUG424, and GW9508, caused marked relaxations in a concentration-dependent manner. GW9508 103-109 free fatty acid receptor 1 Homo sapiens 54-58 30981281-10 2019 GW9508 also markedly stimulated gene and protein expression of IL-10 and beta-endorphin in cultured primary spinal microglia and astrocytes but not in neurons, originated from 1-day-old neonatal rats. GW9508 0-6 interleukin 10 Rattus norvegicus 63-68 29777569-2 2018 The FFA1 agonist GW9508 has great potential for the treatment of type 2 diabetes mellitus, but it has been suffering from high plasma clearance probably because the phenylpropanoic acid is vulnerable to beta-oxidation. GW9508 17-23 free fatty acid receptor 1 Mus musculus 4-8 30981281-7 2019 Intrathecal injection of the GPR40 agonist GW9508 dose-dependently attenuated mechanical allodynia and thermal hyperalgesia in neuropathic rats, with Emax values of 80% and 100% MPE and ED50 values of 6.7 and 5.4 mug, respectively. GW9508 43-49 free fatty acid receptor 1 Rattus norvegicus 29-34 30981281-9 2019 Intrathecal GW9508 significantly enhanced IL-10 and beta-endorphin immunostaining in spinal microglia and astrocytes but not in neurons. GW9508 12-18 interleukin 10 Rattus norvegicus 42-47 30981281-11 2019 The IL-10 antibody inhibited GW9508-stimulated gene expression of the beta-endorphin precursor proopiomelanocortin (POMC) but not IL-10, whereas the beta-endorphin antibody did not affect GW9508-stimulated IL-10 or POMC gene expression. GW9508 29-35 interleukin 10 Rattus norvegicus 4-9 30981281-11 2019 The IL-10 antibody inhibited GW9508-stimulated gene expression of the beta-endorphin precursor proopiomelanocortin (POMC) but not IL-10, whereas the beta-endorphin antibody did not affect GW9508-stimulated IL-10 or POMC gene expression. GW9508 29-35 proopiomelanocortin Rattus norvegicus 116-120 30981281-11 2019 The IL-10 antibody inhibited GW9508-stimulated gene expression of the beta-endorphin precursor proopiomelanocortin (POMC) but not IL-10, whereas the beta-endorphin antibody did not affect GW9508-stimulated IL-10 or POMC gene expression. GW9508 29-35 proopiomelanocortin Rattus norvegicus 215-219 30981281-11 2019 The IL-10 antibody inhibited GW9508-stimulated gene expression of the beta-endorphin precursor proopiomelanocortin (POMC) but not IL-10, whereas the beta-endorphin antibody did not affect GW9508-stimulated IL-10 or POMC gene expression. GW9508 188-194 interleukin 10 Rattus norvegicus 4-9 30981281-12 2019 GW9508 increased phosphorylation of mitogen-activated protein kinases (MAPKs) including p38, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), and its stimulatory effects on IL-10 and POMC expression were blocked by each MAPK isoform inhibitor. GW9508 0-6 mitogen activated protein kinase 14 Rattus norvegicus 88-91 30981281-12 2019 GW9508 increased phosphorylation of mitogen-activated protein kinases (MAPKs) including p38, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), and its stimulatory effects on IL-10 and POMC expression were blocked by each MAPK isoform inhibitor. GW9508 0-6 Eph receptor B1 Rattus norvegicus 93-130 30981281-12 2019 GW9508 increased phosphorylation of mitogen-activated protein kinases (MAPKs) including p38, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), and its stimulatory effects on IL-10 and POMC expression were blocked by each MAPK isoform inhibitor. GW9508 0-6 Eph receptor B1 Rattus norvegicus 132-135 30981281-12 2019 GW9508 increased phosphorylation of mitogen-activated protein kinases (MAPKs) including p38, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), and its stimulatory effects on IL-10 and POMC expression were blocked by each MAPK isoform inhibitor. GW9508 0-6 mitogen-activated protein kinase 8 Rattus norvegicus 142-165 30981281-12 2019 GW9508 increased phosphorylation of mitogen-activated protein kinases (MAPKs) including p38, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), and its stimulatory effects on IL-10 and POMC expression were blocked by each MAPK isoform inhibitor. GW9508 0-6 mitogen-activated protein kinase 8 Rattus norvegicus 167-170 30981281-12 2019 GW9508 increased phosphorylation of mitogen-activated protein kinases (MAPKs) including p38, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), and its stimulatory effects on IL-10 and POMC expression were blocked by each MAPK isoform inhibitor. GW9508 0-6 interleukin 10 Rattus norvegicus 204-209 30981281-12 2019 GW9508 increased phosphorylation of mitogen-activated protein kinases (MAPKs) including p38, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), and its stimulatory effects on IL-10 and POMC expression were blocked by each MAPK isoform inhibitor. GW9508 0-6 proopiomelanocortin Rattus norvegicus 214-218 30981281-13 2019 Spinal GW9508-induced mechanical antiallodynia was completely blocked by intrathecal minocycline, IL-10 neutralizing antibody, beta-endorphin antiserum, and mu-opioid receptor-preferred antagonist naloxone. GW9508 7-13 interleukin 10 Rattus norvegicus 98-103 29981843-5 2018 Next, we demonstrated that chronic treatment with docosahexaenoic acid (DHA) or the synthetic GPR40 agonist, GW9508, significantly alleviates cognitive functions in mice, which correlates with increased BDNF expression in the hippocampus. GW9508 109-115 free fatty acid receptor 1 Mus musculus 94-99 29981843-5 2018 Next, we demonstrated that chronic treatment with docosahexaenoic acid (DHA) or the synthetic GPR40 agonist, GW9508, significantly alleviates cognitive functions in mice, which correlates with increased BDNF expression in the hippocampus. GW9508 109-115 brain derived neurotrophic factor Mus musculus 203-207 29321392-3 2018 We have already demonstrated that the intracerebroventricular administration of DHA or GW9508, a GPR40/FFAR1 agonist, suppresses formalin-induced pain behavior. GW9508 87-93 free fatty acid receptor 1 Homo sapiens 97-102 29750897-6 2018 The cell motile activities of DLD-5FU and DLD-CDDP cells were reduced by GW9508 which is an agonist of FFA1 and FFA4. GW9508 73-79 free fatty acid receptor 1 Homo sapiens 103-107 29777058-3 2018 14,15-EET, 11,12-EET, arachidonic acid, and the GPR40 agonist GW9508 increase intracellular calcium concentrations in human GPR40-overexpressing HEK293 cells (EC50 = 0.58 +- 0.08 mum, 0.91 +- 0.08 mum, 3.9 +- 0.06 mum, and 19 +- 0.37 nm, respectively). GW9508 62-68 free fatty acid receptor 1 Homo sapiens 48-53 29777058-3 2018 14,15-EET, 11,12-EET, arachidonic acid, and the GPR40 agonist GW9508 increase intracellular calcium concentrations in human GPR40-overexpressing HEK293 cells (EC50 = 0.58 +- 0.08 mum, 0.91 +- 0.08 mum, 3.9 +- 0.06 mum, and 19 +- 0.37 nm, respectively). GW9508 62-68 free fatty acid receptor 1 Homo sapiens 124-129 29777058-6 2018 The GPR40 antagonist GW1100 and siRNA-mediated GPR40 silencing blocked the EET- and GW9508-induced calcium increases. GW9508 84-90 free fatty acid receptor 1 Homo sapiens 4-9 29777058-6 2018 The GPR40 antagonist GW1100 and siRNA-mediated GPR40 silencing blocked the EET- and GW9508-induced calcium increases. GW9508 84-90 free fatty acid receptor 1 Homo sapiens 47-52 29321392-3 2018 We have already demonstrated that the intracerebroventricular administration of DHA or GW9508, a GPR40/FFAR1 agonist, suppresses formalin-induced pain behavior. GW9508 87-93 free fatty acid receptor 1 Homo sapiens 103-108 29568424-2 2017 Herein, we describe the design and synthesis of FAAzo-10, a light-controllable GPR40 agonist based on Gw-9508. GW9508 102-109 free fatty acid receptor 1 Mus musculus 79-84 29913106-3 2018 This study aimed to investigate the function of GPR40 in regulating tight junction assembly in human airway epithelial cells (Calu-3 cells) using GW9508, a GPR40 agonist. GW9508 146-152 free fatty acid receptor 1 Homo sapiens 48-53 29913106-3 2018 This study aimed to investigate the function of GPR40 in regulating tight junction assembly in human airway epithelial cells (Calu-3 cells) using GW9508, a GPR40 agonist. GW9508 146-152 free fatty acid receptor 1 Homo sapiens 156-161 29913106-5 2018 Intracellular Ca2+ measurements confirmed that GW9508 stimulated GPR40, but not GPR120. GW9508 47-53 free fatty acid receptor 1 Homo sapiens 65-70 29913106-10 2018 Our results indicate that GPR40 stimulation by GW9508 leads to AMPK activation via calcium/calmodulin-dependent protein kinase kinase beta (CaMKKbeta). GW9508 47-53 free fatty acid receptor 1 Homo sapiens 26-31 29913106-10 2018 Our results indicate that GPR40 stimulation by GW9508 leads to AMPK activation via calcium/calmodulin-dependent protein kinase kinase beta (CaMKKbeta). GW9508 47-53 calcium/calmodulin dependent protein kinase kinase 2 Homo sapiens 140-149 28159555-6 2017 The cell motile activity of MG63-R7 cells was stimulated by GW9508, which is an agonist of GPR120 and GPR40. GW9508 60-66 free fatty acid receptor 4 Homo sapiens 91-97 28446241-11 2017 Reducing GPR120 hypothalamic expression using a lentivirus-based approach resulted in the loss of the anti-inflammatory effect of GW9508 and increased energy efficiency. GW9508 130-136 free fatty acid receptor 4 Mus musculus 9-15 28446241-12 2017 Intracerebroventricular treatment with the GPR120- and GPR40-specific agonists TUG1197 and TUG905, respectively, resulted in milder effects than those produced by GW9508. GW9508 163-169 free fatty acid receptor 4 Mus musculus 43-49 28446241-12 2017 Intracerebroventricular treatment with the GPR120- and GPR40-specific agonists TUG1197 and TUG905, respectively, resulted in milder effects than those produced by GW9508. GW9508 163-169 free fatty acid receptor 1 Mus musculus 55-60 28731171-6 2017 In addition, PTF enhanced the protein expression of GPR40 and to a certain extent strengthened the protein expression of PKC, increased cellular levels of triphosphoinositide (IP3) and diacylglycerol (DAG), and promoted GW9508-stimulated activity of PLC and PKC reduced by PA in INS-1 cells, which were blocked by PLC inhibitor U-73122 and PKC inhibitor staurosporine, respectively. GW9508 220-226 free fatty acid receptor 1 Rattus norvegicus 52-57 28159555-6 2017 The cell motile activity of MG63-R7 cells was stimulated by GW9508, which is an agonist of GPR120 and GPR40. GW9508 60-66 free fatty acid receptor 1 Homo sapiens 102-107 28159555-7 2017 Moreover, a GPR40 antagonist GW1100 elevated the cell motile activity of MG63-R7 cells in the presence of GW9508. GW9508 106-112 free fatty acid receptor 1 Homo sapiens 12-17 28154332-7 2017 Furthermore, the intracerebroventricular injection of DHA or GW9508, which is a selective GPR40/FFA1 agonist, attenuates formalin-induced inflammatory pain behavior through increasing beta-endorphin release in the hypothalamus. GW9508 61-67 free fatty acid receptor 1 Homo sapiens 90-95 27611773-1 2017 SCOPE: The stimulation of the free fatty acid receptor G-protein coupled receptor (GPR) 40 by GW9508 prevents bone loss by inhibiting osteoclast activity, both in vitro and in vivo. GW9508 94-100 G protein-coupled receptor 34 Mus musculus 55-81 27611773-1 2017 SCOPE: The stimulation of the free fatty acid receptor G-protein coupled receptor (GPR) 40 by GW9508 prevents bone loss by inhibiting osteoclast activity, both in vitro and in vivo. GW9508 94-100 G protein-coupled receptor 34 Mus musculus 83-86 28154332-7 2017 Furthermore, the intracerebroventricular injection of DHA or GW9508, which is a selective GPR40/FFA1 agonist, attenuates formalin-induced inflammatory pain behavior through increasing beta-endorphin release in the hypothalamus. GW9508 61-67 proopiomelanocortin Homo sapiens 184-198 26331585-9 2016 In addition, GW9508 which is an agonist of GPR40 and GPR120 suppressed the cell motile and invasive activities of HT1080 cells treated with CDDP as well as the MMP activation. GW9508 13-19 free fatty acid receptor 1 Homo sapiens 43-48 26331585-9 2016 In addition, GW9508 which is an agonist of GPR40 and GPR120 suppressed the cell motile and invasive activities of HT1080 cells treated with CDDP as well as the MMP activation. GW9508 13-19 free fatty acid receptor 4 Homo sapiens 53-59 26331585-9 2016 In addition, GW9508 which is an agonist of GPR40 and GPR120 suppressed the cell motile and invasive activities of HT1080 cells treated with CDDP as well as the MMP activation. GW9508 13-19 matrix metallopeptidase 2 Homo sapiens 160-163 27764222-7 2016 Moreover, GW9508, a specific ligand for G-protein coupled receptor (Gpr)-120/Free fatty acid receptor (Ffar)-4, mimicked the effects of EPA. GW9508 10-16 G protein-coupled receptor 34 Mus musculus 40-66 27489163-7 2016 Treatment of Ffar4 agonist (GW9508) recapitulated the thermogenic activation of EPA by increasing oxygen consumption rate, brown-specific marker genes, and miR-30b and 378, which were abrogated in Ffar4-silenced cells. GW9508 28-34 free fatty acid receptor 4 Mus musculus 13-18 27489163-7 2016 Treatment of Ffar4 agonist (GW9508) recapitulated the thermogenic activation of EPA by increasing oxygen consumption rate, brown-specific marker genes, and miR-30b and 378, which were abrogated in Ffar4-silenced cells. GW9508 28-34 microRNA 30b Mus musculus 156-163 27489163-7 2016 Treatment of Ffar4 agonist (GW9508) recapitulated the thermogenic activation of EPA by increasing oxygen consumption rate, brown-specific marker genes, and miR-30b and 378, which were abrogated in Ffar4-silenced cells. GW9508 28-34 free fatty acid receptor 4 Mus musculus 197-202 26869446-4 2016 The Cx HC activity of these cells increased after 5 min of treatment with LA or GW9508, an agonist of GPR40/GPR120; or exposure to extracellular divalent cation-free solution (DCFS), known to increase the open probability of Cx HCs, yields an immediate increase in Cx HC activity of similar intensity and additive with LA-induced change. GW9508 80-86 free fatty acid receptor 1 Homo sapiens 102-107 27363707-4 2016 Our results showed that natural (oleic and linoleic acid) and synthetic (GW9508) FFAR1/GPR40 agonists increased ERK1/2, p38 MAPK and Akt phosphorylation, and that the FFAR1/GPR40 antagonist GW1100 reduced these responses. GW9508 73-79 free fatty acid receptor 1 Bos taurus 81-86 27363707-4 2016 Our results showed that natural (oleic and linoleic acid) and synthetic (GW9508) FFAR1/GPR40 agonists increased ERK1/2, p38 MAPK and Akt phosphorylation, and that the FFAR1/GPR40 antagonist GW1100 reduced these responses. GW9508 73-79 mitogen-activated protein kinase 3 Bos taurus 112-118 27363707-4 2016 Our results showed that natural (oleic and linoleic acid) and synthetic (GW9508) FFAR1/GPR40 agonists increased ERK1/2, p38 MAPK and Akt phosphorylation, and that the FFAR1/GPR40 antagonist GW1100 reduced these responses. GW9508 73-79 free fatty acid receptor 1 Bos taurus 167-172 26869446-4 2016 The Cx HC activity of these cells increased after 5 min of treatment with LA or GW9508, an agonist of GPR40/GPR120; or exposure to extracellular divalent cation-free solution (DCFS), known to increase the open probability of Cx HCs, yields an immediate increase in Cx HC activity of similar intensity and additive with LA-induced change. GW9508 80-86 free fatty acid receptor 4 Homo sapiens 108-114 27121981-4 2016 In the present study, we found that activation of GPR40 by its agonist GW9508 attenuated Liver X receptor (LXR)-induced hepatic lipid accumulation. GW9508 71-77 free fatty acid receptor 1 Homo sapiens 50-55 26976092-9 2016 All GPR40 receptor agonist GW9508, treatment groups enhanced the learning and memory ability in Step-through passive test, Morris water maze test, Hole board discrimination test, Novel object recognition test. GW9508 27-33 free fatty acid receptor 1 Mus musculus 4-9 27121981-4 2016 In the present study, we found that activation of GPR40 by its agonist GW9508 attenuated Liver X receptor (LXR)-induced hepatic lipid accumulation. GW9508 71-77 nuclear receptor subfamily 1, group H, member 3 Mus musculus 107-110 27121981-6 2016 All these effects of LXR were dramatically downregulated after GW9508 supplementation. GW9508 63-69 nuclear receptor subfamily 1, group H, member 3 Mus musculus 21-24 27121981-8 2016 Taken together, our results demonstrated that GW9508 exerts a beneficial effect to ameliorate LXR-induced hepatic steatosis through regulation of AMPK signaling pathway. GW9508 46-52 nuclear receptor subfamily 1, group H, member 3 Mus musculus 94-97 26853521-1 2016 Here, we assessed the effects of long-chain fatty acids (LCFAs) and the LCFA receptor agonist GW9508 on the transcription of the gonadotropin subunit genes Cga, Lhb and Fshb because LCFA receptor GPR120 was observed in mouse gonadotropes in our recent study. GW9508 94-100 chromogranin A Mus musculus 156-159 26853521-1 2016 Here, we assessed the effects of long-chain fatty acids (LCFAs) and the LCFA receptor agonist GW9508 on the transcription of the gonadotropin subunit genes Cga, Lhb and Fshb because LCFA receptor GPR120 was observed in mouse gonadotropes in our recent study. GW9508 94-100 luteinizing hormone beta Mus musculus 161-164 26853521-1 2016 Here, we assessed the effects of long-chain fatty acids (LCFAs) and the LCFA receptor agonist GW9508 on the transcription of the gonadotropin subunit genes Cga, Lhb and Fshb because LCFA receptor GPR120 was observed in mouse gonadotropes in our recent study. GW9508 94-100 follicle stimulating hormone beta Mus musculus 169-173 26853521-1 2016 Here, we assessed the effects of long-chain fatty acids (LCFAs) and the LCFA receptor agonist GW9508 on the transcription of the gonadotropin subunit genes Cga, Lhb and Fshb because LCFA receptor GPR120 was observed in mouse gonadotropes in our recent study. GW9508 94-100 free fatty acid receptor 4 Mus musculus 196-202 26791484-5 2016 In Caco-2 cells, GPR120 was internalized, bound to beta-arrestin-2, and attenuated NF-kappaB activation in response to 30-min exposure to the agonists GW9508, TUG-891, or docosahexaenoic acid. GW9508 151-157 free fatty acid receptor 4 Homo sapiens 17-23 26342087-6 2015 The long-chain free fatty acids (oleic acid and linoleic acid) and GW9508 (FFAR1/FFAR4 dual agonist) dose-dependently stimulated transient intracellular Ca(2+) concentration ([Ca(2+)]i) increases and inositol phosphate synthesis in HASM cells. GW9508 67-73 free fatty acid receptor 1 Homo sapiens 75-80 26280807-4 2016 Activation of GPR120 by its ligand GW9508 suppressed receptor activator of NF- kappaB ligand (RANKL)-induced osteoclast differentiation and the expression of nuclear factor of activated T cells c1 (NFATc1), a key modulator of osteoclastogenesis. GW9508 35-41 free fatty acid receptor 4 Homo sapiens 14-20 26280807-4 2016 Activation of GPR120 by its ligand GW9508 suppressed receptor activator of NF- kappaB ligand (RANKL)-induced osteoclast differentiation and the expression of nuclear factor of activated T cells c1 (NFATc1), a key modulator of osteoclastogenesis. GW9508 35-41 TNF superfamily member 11 Homo sapiens 94-99 26280807-4 2016 Activation of GPR120 by its ligand GW9508 suppressed receptor activator of NF- kappaB ligand (RANKL)-induced osteoclast differentiation and the expression of nuclear factor of activated T cells c1 (NFATc1), a key modulator of osteoclastogenesis. GW9508 35-41 nuclear factor of activated T cells 1 Homo sapiens 198-204 26821052-8 2016 Two synthetic FFAR agonists, GW9508 and TUG-891, likewise inhibited LPA- and EGF-induced proliferation. GW9508 29-35 epidermal growth factor Homo sapiens 77-80 26699911-4 2016 To further investigate this hypothesis, biological effects of GW9508, a synthetic agonist for GPR40, was first tested on osteoblast differentiation parameters. GW9508 62-68 free fatty acid receptor 1 Mus musculus 94-99 26699911-10 2016 Nevertheless, a significant increase in OPG expression was observed upon GW9508 treatment that contribute to explain the GPR40-related osteoporosis prevention. GW9508 73-79 tumor necrosis factor receptor superfamily, member 11b (osteoprotegerin) Mus musculus 40-43 26699911-10 2016 Nevertheless, a significant increase in OPG expression was observed upon GW9508 treatment that contribute to explain the GPR40-related osteoporosis prevention. GW9508 73-79 free fatty acid receptor 1 Mus musculus 121-126 26342087-6 2015 The long-chain free fatty acids (oleic acid and linoleic acid) and GW9508 (FFAR1/FFAR4 dual agonist) dose-dependently stimulated transient intracellular Ca(2+) concentration ([Ca(2+)]i) increases and inositol phosphate synthesis in HASM cells. GW9508 67-73 free fatty acid receptor 4 Homo sapiens 81-86 26134561-7 2015 DHA and GW9508, a GPR120 agonist, increased GPR120 expression. GW9508 8-14 free fatty acid receptor 4 Homo sapiens 18-24 26071852-1 2015 Previous studies have shown that the administration of docosahexaenoic acid (DHA) or GW9508, a GPR40/FFA1 (free fatty acid receptor) agonist, facilitates beta-endorphin release in the arcuate nucleus of the hypothalamus in mice. GW9508 85-91 free fatty acid receptor 1 Mus musculus 95-100 26071852-4 2015 The intracerebroventricular injection of DHA or GW9508 significantly increased PC2 protein expression in the hypothalamus. GW9508 48-54 proprotein convertase subtilisin/kexin type 2 Mus musculus 79-82 26134561-7 2015 DHA and GW9508, a GPR120 agonist, increased GPR120 expression. GW9508 8-14 free fatty acid receptor 4 Homo sapiens 44-50 25790291-5 2015 Stimulation with a synthetic GPR120 agonist, GW9508, induced rapid down-regulation of cell surface expression of GPR120, suggesting ligand-dependent receptor internalization. GW9508 45-51 free fatty acid receptor 4 Homo sapiens 29-35 25790291-5 2015 Stimulation with a synthetic GPR120 agonist, GW9508, induced rapid down-regulation of cell surface expression of GPR120, suggesting ligand-dependent receptor internalization. GW9508 45-51 free fatty acid receptor 4 Homo sapiens 113-119 25576830-7 2015 Furthermore, in vivo GW9508 administration rescued estrogen-deficient bone loss, indicating the essential role of the GPR40 receptor. GW9508 21-27 free fatty acid receptor 1 Mus musculus 118-123 25281202-10 2014 BCAO-induced mechanical hyperalgesia was significantly decreased by intracerebroventricular injection of docosahexaenoic acid or GW9508, a GPR40 agonist; furthermore, these effects were reversed by GW1100, a GPR40 antagonist. GW9508 129-135 free fatty acid receptor 1 Mus musculus 139-144 25447053-8 2015 Dual agonists of GPR40 and GPR120, GW9508 and linoleic acid, respectively, increased GLP-2 production from L cells, but these agonists decreased it in the presence of TNF-alpha. GW9508 35-41 glucagon Homo sapiens 85-90 25447053-8 2015 Dual agonists of GPR40 and GPR120, GW9508 and linoleic acid, respectively, increased GLP-2 production from L cells, but these agonists decreased it in the presence of TNF-alpha. GW9508 35-41 tumor necrosis factor Homo sapiens 167-176 25447053-9 2015 The GPR40 antagonist, GW1100, inhibited the GW9508-induced increase in GLP-2 production, and silencing GPR120 resulted in further elevation of GLP-2 production. GW9508 44-50 free fatty acid receptor 1 Homo sapiens 4-9 25447053-9 2015 The GPR40 antagonist, GW1100, inhibited the GW9508-induced increase in GLP-2 production, and silencing GPR120 resulted in further elevation of GLP-2 production. GW9508 44-50 glucagon Homo sapiens 71-76 25889021-3 2015 RESULTS: Intrathecal injection of GPR40 agonist (MEDICA16 or GW9508) dose-dependently reduced ipsilateral mechanical allodynia in CFA and SNL models and thermal hyperalgesia in carrageenan model. GW9508 61-67 free fatty acid receptor 1 Mus musculus 34-39 25281202-10 2014 BCAO-induced mechanical hyperalgesia was significantly decreased by intracerebroventricular injection of docosahexaenoic acid or GW9508, a GPR40 agonist; furthermore, these effects were reversed by GW1100, a GPR40 antagonist. GW9508 129-135 free fatty acid receptor 1 Mus musculus 208-213 25092426-12 2014 The cisplatin-induced generation of reactive oxygen species (ROS) and the activation of the Src/epidermal growth factor receptor (EGFR)/extracellular signal-regulated kinase (ERK) pathway were also counteracted by pre-treatment with GW9508. GW9508 233-239 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 92-95 25092426-12 2014 The cisplatin-induced generation of reactive oxygen species (ROS) and the activation of the Src/epidermal growth factor receptor (EGFR)/extracellular signal-regulated kinase (ERK) pathway were also counteracted by pre-treatment with GW9508. GW9508 233-239 epidermal growth factor receptor Homo sapiens 96-128 25092426-12 2014 The cisplatin-induced generation of reactive oxygen species (ROS) and the activation of the Src/epidermal growth factor receptor (EGFR)/extracellular signal-regulated kinase (ERK) pathway were also counteracted by pre-treatment with GW9508. GW9508 233-239 epidermal growth factor receptor Homo sapiens 130-134 25008074-3 2014 In this study, a high fat diet (HFD)-induced hepatic steatosis animal model was utilized to evaluate the effects of an FFAR1 agonist, GW9508, on hepatic lipid accumulation, and HepG2 hepatoma cells were also used to clarify the possible mechanisms. GW9508 134-140 free fatty acid receptor 1 Homo sapiens 119-124 25008074-5 2014 Knockdown of hepatic Ffar1 by lentiviral vectors containing short hairpin RNA targeted to Ffar1 diminished the effect of GW9508 in HFD mice. GW9508 121-127 free fatty acid receptor 1 Mus musculus 21-26 25008074-5 2014 Knockdown of hepatic Ffar1 by lentiviral vectors containing short hairpin RNA targeted to Ffar1 diminished the effect of GW9508 in HFD mice. GW9508 121-127 free fatty acid receptor 1 Mus musculus 90-95 25008074-7 2014 Moreover, GW9508 downregulated the expression of sterol regulatory element-binding protein 1 (SREBP1) through a p38-dependent pathway, whereas knockdown of Ffar1 in HepG2 cells diminished the effect of GW9508 on the decrease in SREBP1. GW9508 10-16 sterol regulatory element binding transcription factor 1 Homo sapiens 49-92 25008074-7 2014 Moreover, GW9508 downregulated the expression of sterol regulatory element-binding protein 1 (SREBP1) through a p38-dependent pathway, whereas knockdown of Ffar1 in HepG2 cells diminished the effect of GW9508 on the decrease in SREBP1. GW9508 10-16 sterol regulatory element binding transcription factor 1 Homo sapiens 94-100 25008074-7 2014 Moreover, GW9508 downregulated the expression of sterol regulatory element-binding protein 1 (SREBP1) through a p38-dependent pathway, whereas knockdown of Ffar1 in HepG2 cells diminished the effect of GW9508 on the decrease in SREBP1. GW9508 10-16 mitogen-activated protein kinase 14 Homo sapiens 112-115 25008074-7 2014 Moreover, GW9508 downregulated the expression of sterol regulatory element-binding protein 1 (SREBP1) through a p38-dependent pathway, whereas knockdown of Ffar1 in HepG2 cells diminished the effect of GW9508 on the decrease in SREBP1. GW9508 10-16 sterol regulatory element binding transcription factor 1 Homo sapiens 228-234 25008074-7 2014 Moreover, GW9508 downregulated the expression of sterol regulatory element-binding protein 1 (SREBP1) through a p38-dependent pathway, whereas knockdown of Ffar1 in HepG2 cells diminished the effect of GW9508 on the decrease in SREBP1. GW9508 202-208 free fatty acid receptor 1 Homo sapiens 156-161 25008074-8 2014 Considering all these results together, GW9508 exerts a therapeutic effect to improve hepatic steatosis through a p38-dependent pathway. GW9508 40-46 mitogen-activated protein kinase 14 Homo sapiens 114-117 24734983-7 2014 The results showed that DHA, PD98059 (an ERK1/2 inhibitor), and GW9508 (a GPR120 agonist) inhibited VEGF-induced cell migration. GW9508 64-70 free fatty acid receptor 4 Homo sapiens 74-80 24673159-4 2014 DHA and GW9508 activate cPLA2 via GPR120 receptor, G protein Galphaq and scaffold protein beta-arrestin 2. GW9508 8-14 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 24-29 24673159-4 2014 DHA and GW9508 activate cPLA2 via GPR120 receptor, G protein Galphaq and scaffold protein beta-arrestin 2. GW9508 8-14 free fatty acid receptor 4 Mus musculus 34-40 24673159-5 2014 Extracellular signal-regulated kinase 1/2 activation is involved in DHA- and GW9508-induced cPLA2 activation, but not p38 mitogen-activated protein kinase. GW9508 77-83 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 92-97 24673159-6 2014 The anti-inflammatory role of DHA and GW9508 is in part via activation of cPLA2 , COX-2 and production of PGE2 as a cPLA2 inhibitor or a COX-2 inhibitor partially reverses the DHA- and GW9508-induced inhibition of lipopolysaccharide-induced interleukin-6 secretion. GW9508 38-44 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 74-79 24673159-6 2014 The anti-inflammatory role of DHA and GW9508 is in part via activation of cPLA2 , COX-2 and production of PGE2 as a cPLA2 inhibitor or a COX-2 inhibitor partially reverses the DHA- and GW9508-induced inhibition of lipopolysaccharide-induced interleukin-6 secretion. GW9508 38-44 prostaglandin-endoperoxide synthase 2 Mus musculus 82-87 24673159-6 2014 The anti-inflammatory role of DHA and GW9508 is in part via activation of cPLA2 , COX-2 and production of PGE2 as a cPLA2 inhibitor or a COX-2 inhibitor partially reverses the DHA- and GW9508-induced inhibition of lipopolysaccharide-induced interleukin-6 secretion. GW9508 38-44 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 116-121 24673159-6 2014 The anti-inflammatory role of DHA and GW9508 is in part via activation of cPLA2 , COX-2 and production of PGE2 as a cPLA2 inhibitor or a COX-2 inhibitor partially reverses the DHA- and GW9508-induced inhibition of lipopolysaccharide-induced interleukin-6 secretion. GW9508 38-44 prostaglandin-endoperoxide synthase 2 Mus musculus 137-142 24760994-7 2014 GW9508 (40 muM), an agonist of the FA receptor, G protein-coupled receptor 40 (GPR40), also increased calcium levels almost exclusively in FA-responsive neurons. GW9508 0-6 free fatty acid receptor 1 Rattus norvegicus 48-77 24760994-7 2014 GW9508 (40 muM), an agonist of the FA receptor, G protein-coupled receptor 40 (GPR40), also increased calcium levels almost exclusively in FA-responsive neurons. GW9508 0-6 free fatty acid receptor 1 Rattus norvegicus 79-84 24673159-3 2014 We report here that DHA and the GPR120 agonist, GW9508, activate cPLA2 and cyclooxygenase 2 (COX-2), and cause prostaglandin E2 (PGE2) release in a murine macrophage cell line RAW264.7 and in human primary monocyte-derived macrophages. GW9508 48-54 free fatty acid receptor 4 Mus musculus 32-38 24673159-3 2014 We report here that DHA and the GPR120 agonist, GW9508, activate cPLA2 and cyclooxygenase 2 (COX-2), and cause prostaglandin E2 (PGE2) release in a murine macrophage cell line RAW264.7 and in human primary monocyte-derived macrophages. GW9508 48-54 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 65-70 24673159-3 2014 We report here that DHA and the GPR120 agonist, GW9508, activate cPLA2 and cyclooxygenase 2 (COX-2), and cause prostaglandin E2 (PGE2) release in a murine macrophage cell line RAW264.7 and in human primary monocyte-derived macrophages. GW9508 48-54 prostaglandin-endoperoxide synthase 2 Mus musculus 75-91 24673159-3 2014 We report here that DHA and the GPR120 agonist, GW9508, activate cPLA2 and cyclooxygenase 2 (COX-2), and cause prostaglandin E2 (PGE2) release in a murine macrophage cell line RAW264.7 and in human primary monocyte-derived macrophages. GW9508 48-54 prostaglandin-endoperoxide synthase 2 Mus musculus 93-98 24734983-7 2014 The results showed that DHA, PD98059 (an ERK1/2 inhibitor), and GW9508 (a GPR120 agonist) inhibited VEGF-induced cell migration. GW9508 64-70 vascular endothelial growth factor A Homo sapiens 100-104 16702987-3 2006 Here, we present the first description of GW9508, a small-molecule agonist of the fatty acid receptors GPR40 and GPR120. GW9508 42-48 free fatty acid receptor 1 Mus musculus 103-108 24758921-3 2014 A repeated but not a single intracerebroventricular administration of the GPR40 agonist, GW9508, reduced the duration of immobility behavior. GW9508 89-95 free fatty acid receptor 1 Mus musculus 74-79 24349089-9 2013 The intracerebroventricular injection of DHA (50 microg) and GW9508 (1.0 microg), a GPR40-selective agonist, significantly reduced mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. GW9508 61-67 free fatty acid receptor 1 Mus musculus 84-89 24349089-11 2013 The protein expression of GPR40 was colocalized with that of beta-endorphin and proopiomelanocortin, and a single intracerebroventricular injection of GW9508 (1.0 microg) significantly increased the number of neurons double-stained for c-Fos and proopiomelanocortin in the arcuate nucleus of the hypothalamus. GW9508 151-157 free fatty acid receptor 1 Mus musculus 26-31 24349089-11 2013 The protein expression of GPR40 was colocalized with that of beta-endorphin and proopiomelanocortin, and a single intracerebroventricular injection of GW9508 (1.0 microg) significantly increased the number of neurons double-stained for c-Fos and proopiomelanocortin in the arcuate nucleus of the hypothalamus. GW9508 151-157 pro-opiomelanocortin-alpha Mus musculus 61-75 24349089-11 2013 The protein expression of GPR40 was colocalized with that of beta-endorphin and proopiomelanocortin, and a single intracerebroventricular injection of GW9508 (1.0 microg) significantly increased the number of neurons double-stained for c-Fos and proopiomelanocortin in the arcuate nucleus of the hypothalamus. GW9508 151-157 FBJ osteosarcoma oncogene Mus musculus 236-241 23341496-0 2013 Multiple mechanisms of GW-9508, a selective G protein-coupled receptor 40 agonist, in the regulation of glucose homeostasis and insulin sensitivity. GW9508 23-30 free fatty acid receptor 1 Homo sapiens 44-73 23341496-3 2013 Therefore, we used a selective GPR40 agonist, GW-9508, to clarify the role of GPR40 in the regulation of blood glucose. GW9508 46-53 free fatty acid receptor 1 Homo sapiens 31-36 23341496-4 2013 Bolus intraperitoneal injection of GW-9508 in mice showed a slight decrease in blood glucose, with an increase in plasma insulin levels under glucose stimuli. GW9508 35-42 insulin Homo sapiens 121-128 23341496-5 2013 However, long-term treatment with low doses of GW-9508 in high-fat diet-induced (HFD) diabetic mice decreased blood glucose with decreased plasma insulin significantly and improved glucose intolerance and insulin resistance. GW9508 47-54 insulin Homo sapiens 146-153 23341496-5 2013 However, long-term treatment with low doses of GW-9508 in high-fat diet-induced (HFD) diabetic mice decreased blood glucose with decreased plasma insulin significantly and improved glucose intolerance and insulin resistance. GW9508 47-54 insulin Homo sapiens 205-212 23341496-6 2013 Using small interfering ribonucleic acid to delete GPR40 in HepG2 cells, we demonstrated that GW-9508 reversed palmitate-induced insulin signaling impairment through a GPR40-dependent pathway. GW9508 94-101 free fatty acid receptor 1 Homo sapiens 51-56 23341496-6 2013 Using small interfering ribonucleic acid to delete GPR40 in HepG2 cells, we demonstrated that GW-9508 reversed palmitate-induced insulin signaling impairment through a GPR40-dependent pathway. GW9508 94-101 free fatty acid receptor 1 Homo sapiens 168-173 23341496-7 2013 We also found that GW-9508 activates the Akt/GSK-3beta pathway to increase glycogen levels in HepG2 cells. GW9508 19-26 AKT serine/threonine kinase 1 Homo sapiens 41-44 23341496-7 2013 We also found that GW-9508 activates the Akt/GSK-3beta pathway to increase glycogen levels in HepG2 cells. GW9508 19-26 glycogen synthase kinase 3 beta Homo sapiens 45-54 23341496-8 2013 Furthermore, administration of GW-9508 decreased the hepatic expression of fetuin-A in HFD mice significantly and regulated high-glucose- or palmitate-induced fetuin-A expression to increase insulin sensitivity through a GPR40/PLC/PKC pathway in HepG2 cells. GW9508 31-38 alpha-2-HS-glycoprotein Mus musculus 75-83 23341496-8 2013 Furthermore, administration of GW-9508 decreased the hepatic expression of fetuin-A in HFD mice significantly and regulated high-glucose- or palmitate-induced fetuin-A expression to increase insulin sensitivity through a GPR40/PLC/PKC pathway in HepG2 cells. GW9508 31-38 alpha-2-HS-glycoprotein Mus musculus 159-167 23341496-8 2013 Furthermore, administration of GW-9508 decreased the hepatic expression of fetuin-A in HFD mice significantly and regulated high-glucose- or palmitate-induced fetuin-A expression to increase insulin sensitivity through a GPR40/PLC/PKC pathway in HepG2 cells. GW9508 31-38 insulin Homo sapiens 191-198 23341496-8 2013 Furthermore, administration of GW-9508 decreased the hepatic expression of fetuin-A in HFD mice significantly and regulated high-glucose- or palmitate-induced fetuin-A expression to increase insulin sensitivity through a GPR40/PLC/PKC pathway in HepG2 cells. GW9508 31-38 free fatty acid receptor 1 Mus musculus 221-226 23341496-8 2013 Furthermore, administration of GW-9508 decreased the hepatic expression of fetuin-A in HFD mice significantly and regulated high-glucose- or palmitate-induced fetuin-A expression to increase insulin sensitivity through a GPR40/PLC/PKC pathway in HepG2 cells. GW9508 31-38 perlecan (heparan sulfate proteoglycan 2) Mus musculus 227-230 23335512-7 2013 In addition, in vivo administration of GW9508 counteracted ovariectomy-induced bone loss in wild-type but not GPR40(-/-) mice, enlightening the obligatory role of the GPR40 receptor. GW9508 39-45 free fatty acid receptor 1 Mus musculus 167-172 23649389-13 2013 The beta-endorphin immunoreactivity in the brain increased at 10 and 20 min after intracerebroventricular injection of DHA and GW9508. GW9508 127-133 proopiomelanocortin Homo sapiens 4-18 21593768-0 2011 A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. GW9508 16-22 free fatty acid receptor 1 Homo sapiens 2-7 21593768-0 2011 A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. GW9508 16-22 C-C motif chemokine ligand 5 Homo sapiens 34-38 21593768-0 2011 A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. GW9508 16-22 C-C motif chemokine ligand 17 Homo sapiens 40-45 21593768-0 2011 A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. GW9508 16-22 C-X-C motif chemokine ligand 10 Homo sapiens 51-57 21593768-5 2011 Agonists for Gi-coupled receptors, particularly GW9508 for GPR40, inhibited CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 48-54 free fatty acid receptor 1 Homo sapiens 59-64 21593768-5 2011 Agonists for Gi-coupled receptors, particularly GW9508 for GPR40, inhibited CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 48-54 C-C motif chemokine ligand 17 Homo sapiens 76-81 21593768-5 2011 Agonists for Gi-coupled receptors, particularly GW9508 for GPR40, inhibited CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 48-54 C-C motif chemokine ligand 5 Homo sapiens 86-90 21593768-6 2011 The inhibitory effect by GW9508 was abrogated by depletion of GPR40 with RNA interference. GW9508 25-31 free fatty acid receptor 1 Homo sapiens 62-67 21593768-7 2011 GW9508 further suppressed expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-alpha and IFN-gamma. GW9508 0-6 interleukin 11 Homo sapiens 40-45 21593768-7 2011 GW9508 further suppressed expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-alpha and IFN-gamma. GW9508 0-6 interleukin 24 Homo sapiens 47-52 21593768-7 2011 GW9508 further suppressed expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-alpha and IFN-gamma. GW9508 0-6 interleukin 33 Homo sapiens 58-63 21593768-7 2011 GW9508 further suppressed expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-alpha and IFN-gamma. GW9508 0-6 tumor necrosis factor Homo sapiens 90-99 21593768-7 2011 GW9508 further suppressed expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-alpha and IFN-gamma. GW9508 0-6 interferon gamma Homo sapiens 104-113 21593768-8 2011 GW9508 also inhibited CCL5 and CXCL10 production by normal human epidermal keratinocytes. GW9508 0-6 C-C motif chemokine ligand 5 Homo sapiens 22-26 21593768-8 2011 GW9508 also inhibited CCL5 and CXCL10 production by normal human epidermal keratinocytes. GW9508 0-6 C-X-C motif chemokine ligand 10 Homo sapiens 31-37 21593768-9 2011 Administration of GW9508 topically to the skin in the challenging phase suppressed ear swelling in a repeated hapten application model and contact hypersensitivity with downregulation of CCL5 and CXCL10, respectively. GW9508 18-24 C-C motif chemokine ligand 5 Homo sapiens 187-191 21593768-9 2011 Administration of GW9508 topically to the skin in the challenging phase suppressed ear swelling in a repeated hapten application model and contact hypersensitivity with downregulation of CCL5 and CXCL10, respectively. GW9508 18-24 C-X-C motif chemokine ligand 10 Homo sapiens 196-202 21575602-9 2011 The selective agonist of GPR40, GW9508, induced intracellular calcium mobilization and ERK2 phosphorylation. GW9508 32-38 free fatty acid receptor 1 Homo sapiens 25-30 21575602-9 2011 The selective agonist of GPR40, GW9508, induced intracellular calcium mobilization and ERK2 phosphorylation. GW9508 32-38 mitogen-activated protein kinase 1 Bos taurus 87-91 21334233-0 2011 Insight into analysis of interactions of GW9508 to wild-type and H86F and H137F GPR40: a combined QM/MM study and pharmacophore modeling. GW9508 41-47 free fatty acid receptor 1 Homo sapiens 80-85 21334233-2 2011 In this work, a two-layered ONIOM based QM/MM approach was employed to study the interactions between GW9508 and GPR40: wild-type, H86F, and H137F mutated systems. GW9508 102-108 free fatty acid receptor 1 Homo sapiens 113-118 19815053-3 2010 GW9508, a specific agonist of GPR40, significantly enhanced insulin secretion in the presence of high concentrations of glucose. GW9508 0-6 free fatty acid receptor 1 Rattus norvegicus 30-35 24222669-5 2014 Addition of GW-9508 (a GPR120 chemical agonist) and alpha-linolenic acid (a natural ligand for GPR120) inhibited the secretion of ghrelin by ~50 and 70%, respectively. GW9508 12-19 free fatty acid receptor 4 Mus musculus 23-29 24222669-5 2014 Addition of GW-9508 (a GPR120 chemical agonist) and alpha-linolenic acid (a natural ligand for GPR120) inhibited the secretion of ghrelin by ~50 and 70%, respectively. GW9508 12-19 ghrelin Mus musculus 130-137 24222669-8 2014 Moreover, we observed that the inhibitory effect of GW-9508 on ghrelin secretion was blocked by a small interfering RNA (siRNA) targeting the sequence of GPR120. GW9508 52-59 ghrelin Mus musculus 63-70 24222669-8 2014 Moreover, we observed that the inhibitory effect of GW-9508 on ghrelin secretion was blocked by a small interfering RNA (siRNA) targeting the sequence of GPR120. GW9508 52-59 free fatty acid receptor 4 Mus musculus 154-160 24222669-9 2014 Furthermore, pretreatment with GW-9508 blocked the effect of the norepinephrine (NE)-induced ghrelin elevation in ghrelin cell lines. GW9508 31-38 ghrelin Mus musculus 93-100 24222669-9 2014 Furthermore, pretreatment with GW-9508 blocked the effect of the norepinephrine (NE)-induced ghrelin elevation in ghrelin cell lines. GW9508 31-38 ghrelin Mus musculus 114-121 24222669-10 2014 In addition, we showed that GW-9508 inhibited ghrelin secretion via extracellular signal-regulated kinase activity in ghrelin cell lines. GW9508 28-35 ghrelin Mus musculus 46-53 24222669-10 2014 In addition, we showed that GW-9508 inhibited ghrelin secretion via extracellular signal-regulated kinase activity in ghrelin cell lines. GW9508 28-35 ghrelin Mus musculus 118-125 23628491-1 2013 GW9508 is an agonist of G protein-coupled receptor 40 (GPR40) that is expressed in pancreatic beta-cells and is reported to regulate insulin secretion. GW9508 0-6 free fatty acid receptor 1 Rattus norvegicus 24-53 23628491-1 2013 GW9508 is an agonist of G protein-coupled receptor 40 (GPR40) that is expressed in pancreatic beta-cells and is reported to regulate insulin secretion. GW9508 0-6 free fatty acid receptor 1 Rattus norvegicus 55-60 23335512-6 2013 The GPR40-dependent effect of GW9508 was confirmed using shRNA interference in osteoclast precursors and GPR40(-/-) primary cell cultures. GW9508 30-36 free fatty acid receptor 1 Mus musculus 4-9 23335512-6 2013 The GPR40-dependent effect of GW9508 was confirmed using shRNA interference in osteoclast precursors and GPR40(-/-) primary cell cultures. GW9508 30-36 free fatty acid receptor 1 Mus musculus 105-110 22137657-7 2012 injection of DHA (25 and 50mug/mouse) and GW9508 (a GPR40- and GPR120-selective agonist; 0.1 and 1.0mug/mouse) significantly reduced formalin-induced pain behavior. GW9508 42-48 free fatty acid receptor 1 Mus musculus 52-57 22137657-7 2012 injection of DHA (25 and 50mug/mouse) and GW9508 (a GPR40- and GPR120-selective agonist; 0.1 and 1.0mug/mouse) significantly reduced formalin-induced pain behavior. GW9508 42-48 free fatty acid receptor 4 Mus musculus 63-69 21570468-6 2011 This resulted in a significant increase in the intracellular Ca2+ level, similar to the effect seen after treatment with the synthetic GPR40 agonist GW9508. GW9508 149-155 free fatty acid receptor 1 Homo sapiens 135-140 19723586-9 2009 GW9508 had similar efficacy at the cynomolgus monkey and at the BC101175 human GPR120 receptors. GW9508 0-6 free fatty acid receptor 4 Homo sapiens 79-85 17699519-9 2007 The greater number of putative interactions between GPR40 and GW9508 compared with linoleic acid may explain the higher potency of GW9508. GW9508 131-137 free fatty acid receptor 1 Homo sapiens 52-57 16702987-3 2006 Here, we present the first description of GW9508, a small-molecule agonist of the fatty acid receptors GPR40 and GPR120. GW9508 42-48 free fatty acid receptor 4 Mus musculus 113-119 16702987-7 2006 GW9508 and linoleic acid both stimulated intracellular Ca2+ mobilization in human embryonic kidney (HEK)293 cells expressing GPR40 (pEC50 values of 7.32+/-0.03 and 5.65+/-0.06, respectively) or GPR120 (pEC50 values of 5.46+/-0.09 and 5.89+/-0.04, respectively), but not in the parent HEK-293 cell line. GW9508 0-6 free fatty acid receptor 1 Homo sapiens 125-130 16702987-7 2006 GW9508 and linoleic acid both stimulated intracellular Ca2+ mobilization in human embryonic kidney (HEK)293 cells expressing GPR40 (pEC50 values of 7.32+/-0.03 and 5.65+/-0.06, respectively) or GPR120 (pEC50 values of 5.46+/-0.09 and 5.89+/-0.04, respectively), but not in the parent HEK-293 cell line. GW9508 0-6 free fatty acid receptor 4 Homo sapiens 194-200 16702987-9 2006 GW1100 dose dependently inhibited GPR40-mediated Ca2+ elevations stimulated by GW9508 and linoleic acid (pIC50 values of 5.99+/-0.03 and 5.99+/-0.06, respectively). GW9508 79-85 free fatty acid receptor 1 Mus musculus 34-39 34297968-5 2021 The results revealed that intragastric administrated GW9508 could significantly ameliorate cognitive deficits of AD mouse, up-regulate the expression levels of gut-brain peptides both in blood circulation and hypothalamus thus up-regulate the expression levels of alpha-MSH in hypothalamus, while the negative autophagy-related proteins and inflammation-related proteins were down-regulated correspondingly. GW9508 53-59 STAM binding protein Mus musculus 264-273 34297968-3 2021 GPR40 agonist GW9508 and antagonist GW1100 were given by i.g injection to activate/inhibit the GPR40 receptor respectively in the gut of AD mouse which illustrated the function and mechanism of GPR40 receptor in ameliorating AD symptoms by external treatment of encephalopathy. GW9508 14-20 free fatty acid receptor 1 Mus musculus 0-5 25362997-9 2015 injection of GW9508, a FFA1 receptor agonist, increased the number of c-Fos-positive cells and the number of neurons double-labelled for c-Fos and TPH and/or DBH. GW9508 13-19 FBJ osteosarcoma oncogene Mus musculus 70-75 25362997-9 2015 injection of GW9508, a FFA1 receptor agonist, increased the number of c-Fos-positive cells and the number of neurons double-labelled for c-Fos and TPH and/or DBH. GW9508 13-19 FBJ osteosarcoma oncogene Mus musculus 137-142 25362997-9 2015 injection of GW9508, a FFA1 receptor agonist, increased the number of c-Fos-positive cells and the number of neurons double-labelled for c-Fos and TPH and/or DBH. GW9508 13-19 tryptophan hydroxylase 1 Mus musculus 147-150 25362997-9 2015 injection of GW9508, a FFA1 receptor agonist, increased the number of c-Fos-positive cells and the number of neurons double-labelled for c-Fos and TPH and/or DBH. GW9508 13-19 dopamine beta hydroxylase Mus musculus 158-161 34297968-3 2021 GPR40 agonist GW9508 and antagonist GW1100 were given by i.g injection to activate/inhibit the GPR40 receptor respectively in the gut of AD mouse which illustrated the function and mechanism of GPR40 receptor in ameliorating AD symptoms by external treatment of encephalopathy. GW9508 14-20 free fatty acid receptor 1 Mus musculus 95-100 34297968-3 2021 GPR40 agonist GW9508 and antagonist GW1100 were given by i.g injection to activate/inhibit the GPR40 receptor respectively in the gut of AD mouse which illustrated the function and mechanism of GPR40 receptor in ameliorating AD symptoms by external treatment of encephalopathy. GW9508 14-20 free fatty acid receptor 1 Mus musculus 194-199 34489696-6 2021 Interestingly, local application of a FFAR1 agonist, GW9508, markedly augmented the striatal 5-HT release in FFAR1 wild-type (+/+) mice, whereas topical application of a FFAR1 antagonist, GW1100, significantly reduced the 5-HT release. GW9508 53-59 free fatty acid receptor 1 Mus musculus 38-43 34275493-6 2021 GPR40 agonist, GW9508, was administered intranasally 1 h, 25 h, and 49 h after GMH induction. GW9508 15-21 free fatty acid receptor 1 Rattus norvegicus 0-5 34275493-12 2021 GW9508 upregulated the phosphorylation of PAK4, CREB, and protein level of KDM6B, CD206, IL-10, which was also met with the downregulation of inflammatory markers IL-1beta and TNF-alpha. GW9508 0-6 p21 (RAC1) activated kinase 4 Rattus norvegicus 42-46 34275493-12 2021 GW9508 upregulated the phosphorylation of PAK4, CREB, and protein level of KDM6B, CD206, IL-10, which was also met with the downregulation of inflammatory markers IL-1beta and TNF-alpha. GW9508 0-6 cAMP responsive element binding protein 1 Rattus norvegicus 48-52 34275493-12 2021 GW9508 upregulated the phosphorylation of PAK4, CREB, and protein level of KDM6B, CD206, IL-10, which was also met with the downregulation of inflammatory markers IL-1beta and TNF-alpha. GW9508 0-6 lysine demethylase 6B Rattus norvegicus 75-80 34275493-12 2021 GW9508 upregulated the phosphorylation of PAK4, CREB, and protein level of KDM6B, CD206, IL-10, which was also met with the downregulation of inflammatory markers IL-1beta and TNF-alpha. GW9508 0-6 interleukin 10 Rattus norvegicus 89-94 34275493-12 2021 GW9508 upregulated the phosphorylation of PAK4, CREB, and protein level of KDM6B, CD206, IL-10, which was also met with the downregulation of inflammatory markers IL-1beta and TNF-alpha. GW9508 0-6 interleukin 1 alpha Rattus norvegicus 163-171 34275493-12 2021 GW9508 upregulated the phosphorylation of PAK4, CREB, and protein level of KDM6B, CD206, IL-10, which was also met with the downregulation of inflammatory markers IL-1beta and TNF-alpha. GW9508 0-6 tumor necrosis factor Rattus norvegicus 176-185 34275493-13 2021 The mechanism study demonstrated that the knockdown of GPR40, PAK4, and KDM6B reversed the neuroprotective effects brought on by GW9508. GW9508 129-135 free fatty acid receptor 1 Rattus norvegicus 55-60 34275493-13 2021 The mechanism study demonstrated that the knockdown of GPR40, PAK4, and KDM6B reversed the neuroprotective effects brought on by GW9508. GW9508 129-135 p21 (RAC1) activated kinase 4 Rattus norvegicus 62-66 34275493-13 2021 The mechanism study demonstrated that the knockdown of GPR40, PAK4, and KDM6B reversed the neuroprotective effects brought on by GW9508. GW9508 129-135 lysine demethylase 6B Rattus norvegicus 72-77 34489696-6 2021 Interestingly, local application of a FFAR1 agonist, GW9508, markedly augmented the striatal 5-HT release in FFAR1 wild-type (+/+) mice, whereas topical application of a FFAR1 antagonist, GW1100, significantly reduced the 5-HT release. GW9508 53-59 free fatty acid receptor 1 Mus musculus 109-114 35584771-10 2022 GW9508 can attenuate inflammation by reducing the expression of NLRP3, ASC, caspase-1, IL-1beta, and IL-18 under HG. GW9508 0-6 NLR family pyrin domain containing 3 Homo sapiens 64-69 35584771-10 2022 GW9508 can attenuate inflammation by reducing the expression of NLRP3, ASC, caspase-1, IL-1beta, and IL-18 under HG. GW9508 0-6 PYD and CARD domain containing Homo sapiens 71-74 35584771-10 2022 GW9508 can attenuate inflammation by reducing the expression of NLRP3, ASC, caspase-1, IL-1beta, and IL-18 under HG. GW9508 0-6 caspase 1 Homo sapiens 76-85 35584771-10 2022 GW9508 can attenuate inflammation by reducing the expression of NLRP3, ASC, caspase-1, IL-1beta, and IL-18 under HG. GW9508 0-6 interleukin 1 alpha Homo sapiens 87-95 35584771-10 2022 GW9508 can attenuate inflammation by reducing the expression of NLRP3, ASC, caspase-1, IL-1beta, and IL-18 under HG. GW9508 0-6 interleukin 18 Homo sapiens 101-106 35584771-11 2022 GW9508 rescues the viability of HRMCs and reduces cell apoptosis by preventing an increase in Bax expression and the reduction in Bcl-2 expression. GW9508 0-6 BCL2 associated X, apoptosis regulator Homo sapiens 94-97 35584771-11 2022 GW9508 rescues the viability of HRMCs and reduces cell apoptosis by preventing an increase in Bax expression and the reduction in Bcl-2 expression. GW9508 0-6 BCL2 apoptosis regulator Homo sapiens 130-135 35584771-12 2022 Additionally, knockdown of GPR120 by siRNA weakened the effects of GW9508 on NLRP3 inflammasome expression. GW9508 67-73 free fatty acid receptor 4 Homo sapiens 27-33 35584771-12 2022 Additionally, knockdown of GPR120 by siRNA weakened the effects of GW9508 on NLRP3 inflammasome expression. GW9508 67-73 NLR family pyrin domain containing 3 Homo sapiens 77-82 35061031-9 2022 Importantly, the GPR40 agonist GW9508 reverted established diabetesinduced hypersensitivity, an effect which was blocked by VEGF-A administration. GW9508 31-37 free fatty acid receptor 1 Homo sapiens 17-22 35061031-9 2022 Importantly, the GPR40 agonist GW9508 reverted established diabetesinduced hypersensitivity, an effect which was blocked by VEGF-A administration. GW9508 31-37 vascular endothelial growth factor A Homo sapiens 124-130