PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 22130396-2 2012 Among the leading innovations to the rules are that both 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (peroxisome proliferator-activated receptor-delta [PPAR-delta]-5" adenosine monophosphate-activated protein kinase [AMPK] agonist) and GW1516 (PPAR-delta-agonist) are no longer categorized as gene doping substances in the new 2012 prohibited list but as metabolic modulators in the class "Hormone and metabolic modulators." GW 501516 247-253 peroxisome proliferator activated receptor delta Homo sapiens 113-161 22130396-2 2012 Among the leading innovations to the rules are that both 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (peroxisome proliferator-activated receptor-delta [PPAR-delta]-5" adenosine monophosphate-activated protein kinase [AMPK] agonist) and GW1516 (PPAR-delta-agonist) are no longer categorized as gene doping substances in the new 2012 prohibited list but as metabolic modulators in the class "Hormone and metabolic modulators." GW 501516 247-253 peroxisome proliferator activated receptor delta Homo sapiens 163-173 21896929-9 2011 The latter mimicked the GSIS-amplifying effect of high glucose preexposure and of the PPAR-delta agonist GW501516 in INS-1E cells and isolated rat islets. GW 501516 105-113 peroxisome proliferator-activated receptor delta Rattus norvegicus 86-96 23056264-7 2012 Silencing of Angptl4 blocked the effect of GW501516 and bexarotene on LPL activity. GW 501516 43-51 angiopoietin like 4 Homo sapiens 13-20 23056264-7 2012 Silencing of Angptl4 blocked the effect of GW501516 and bexarotene on LPL activity. GW 501516 43-51 lipoprotein lipase Homo sapiens 70-73 22072715-3 2011 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly attenuated Ang II-induced generation of superoxides and suppressed senescence of VSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 22072715-3 2011 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly attenuated Ang II-induced generation of superoxides and suppressed senescence of VSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 59-68 22072715-4 2011 A marked increase in the levels of p53 and p21 induced by Ang II was blunted by the treatment with GW501516. GW 501516 99-107 tumor protein p53 Homo sapiens 35-38 22072715-4 2011 A marked increase in the levels of p53 and p21 induced by Ang II was blunted by the treatment with GW501516. GW 501516 99-107 H3 histone pseudogene 16 Homo sapiens 43-46 22072715-7 2011 Finally, administration of GW501516 to apoE-deficient mice treated with Ang II significantly reduced the number of senescent cells in the aorta, where up-regulation of PTEN with reduced levels of phosphorylated Akt and ROS was demonstrated. GW 501516 27-35 apolipoprotein E Mus musculus 39-43 22072715-7 2011 Finally, administration of GW501516 to apoE-deficient mice treated with Ang II significantly reduced the number of senescent cells in the aorta, where up-regulation of PTEN with reduced levels of phosphorylated Akt and ROS was demonstrated. GW 501516 27-35 phosphatase and tensin homolog Mus musculus 168-172 22072715-7 2011 Finally, administration of GW501516 to apoE-deficient mice treated with Ang II significantly reduced the number of senescent cells in the aorta, where up-regulation of PTEN with reduced levels of phosphorylated Akt and ROS was demonstrated. GW 501516 27-35 thymoma viral proto-oncogene 1 Mus musculus 211-214 23052247-5 2012 RESULTS: PPARdelta agonist GW501516 upregulated Ski expression in a dose-dependent manner. GW 501516 27-35 Ski proto-oncogene Rattus norvegicus 48-51 23056264-4 2012 Expression of Angptl4 was upregulated during myotubes differentiation and by oleic acid, insulin and PPAR delta agonist GW501516. GW 501516 120-128 angiopoietin like 4 Homo sapiens 14-21 23056264-4 2012 Expression of Angptl4 was upregulated during myotubes differentiation and by oleic acid, insulin and PPAR delta agonist GW501516. GW 501516 120-128 peroxisome proliferator activated receptor delta Homo sapiens 101-111 23056264-5 2012 Treatment with GW501516 or Angptl4 overexpression inhibited both lipoprotein lipase (LPL) activity and LPL-dependent uptake of FAs whereas uptake of BSA-bound FAs was not affected by either treatment. GW 501516 15-23 lipoprotein lipase Homo sapiens 65-83 23056264-5 2012 Treatment with GW501516 or Angptl4 overexpression inhibited both lipoprotein lipase (LPL) activity and LPL-dependent uptake of FAs whereas uptake of BSA-bound FAs was not affected by either treatment. GW 501516 15-23 lipoprotein lipase Homo sapiens 85-88 23056264-5 2012 Treatment with GW501516 or Angptl4 overexpression inhibited both lipoprotein lipase (LPL) activity and LPL-dependent uptake of FAs whereas uptake of BSA-bound FAs was not affected by either treatment. GW 501516 15-23 lipoprotein lipase Homo sapiens 103-106 21615395-7 2011 Treatment of myotubes with a selective high-affinity PPARdelta agonist (GW501516) did not change mean PPARD, but enhanced mean PDK4 and ANGPTL4 expression 13- and 16-fold, respectively (P < 0 0001, both). GW 501516 72-80 peroxisome proliferator activated receptor delta Homo sapiens 53-62 21615395-7 2011 Treatment of myotubes with a selective high-affinity PPARdelta agonist (GW501516) did not change mean PPARD, but enhanced mean PDK4 and ANGPTL4 expression 13- and 16-fold, respectively (P < 0 0001, both). GW 501516 72-80 pyruvate dehydrogenase kinase 4 Homo sapiens 127-131 21615395-7 2011 Treatment of myotubes with a selective high-affinity PPARdelta agonist (GW501516) did not change mean PPARD, but enhanced mean PDK4 and ANGPTL4 expression 13- and 16-fold, respectively (P < 0 0001, both). GW 501516 72-80 angiopoietin like 4 Homo sapiens 136-143 21615395-8 2011 The individual PDK4 and ANGPTL4 expression levels reached upon GW501516 treatment were associated with donors" insulin sensitivity neither (P > 0 2, both). GW 501516 63-71 pyruvate dehydrogenase kinase 4 Homo sapiens 15-19 21615395-8 2011 The individual PDK4 and ANGPTL4 expression levels reached upon GW501516 treatment were associated with donors" insulin sensitivity neither (P > 0 2, both). GW 501516 63-71 angiopoietin like 4 Homo sapiens 24-31 21615395-8 2011 The individual PDK4 and ANGPTL4 expression levels reached upon GW501516 treatment were associated with donors" insulin sensitivity neither (P > 0 2, both). GW 501516 63-71 insulin Homo sapiens 111-118 21615395-9 2011 However, GW501516-mediated fold increments in PDK4 and ANGPTL4 expression, reflecting PPARdelta responsiveness, were positively associated with donors" insulin sensitivity derived from OGTT (P = 0 0182 and P = 0 0231, respectively) and hyperinsulinemic-euglycemic clamp (P = 0 0046 and P = 0 0258, respectively). GW 501516 9-17 pyruvate dehydrogenase kinase 4 Homo sapiens 46-50 21615395-9 2011 However, GW501516-mediated fold increments in PDK4 and ANGPTL4 expression, reflecting PPARdelta responsiveness, were positively associated with donors" insulin sensitivity derived from OGTT (P = 0 0182 and P = 0 0231, respectively) and hyperinsulinemic-euglycemic clamp (P = 0 0046 and P = 0 0258, respectively). GW 501516 9-17 angiopoietin like 4 Homo sapiens 55-62 21615395-9 2011 However, GW501516-mediated fold increments in PDK4 and ANGPTL4 expression, reflecting PPARdelta responsiveness, were positively associated with donors" insulin sensitivity derived from OGTT (P = 0 0182 and P = 0 0231, respectively) and hyperinsulinemic-euglycemic clamp (P = 0 0046 and P = 0 0258, respectively). GW 501516 9-17 peroxisome proliferator activated receptor delta Homo sapiens 86-95 21615395-9 2011 However, GW501516-mediated fold increments in PDK4 and ANGPTL4 expression, reflecting PPARdelta responsiveness, were positively associated with donors" insulin sensitivity derived from OGTT (P = 0 0182 and P = 0 0231, respectively) and hyperinsulinemic-euglycemic clamp (P = 0 0046 and P = 0 0258, respectively). GW 501516 9-17 insulin Homo sapiens 152-159 21896929-11 2011 High glucose, 4-HNE, and GW501516 also induced luciferase expression in a PPAR-delta-mediated transactivation assay. GW 501516 25-33 peroxisome proliferator-activated receptor delta Rattus norvegicus 74-84 21511721-7 2011 Carbaprostacyclin (a stable analogue of PGI(2)) and GW501516 (a PPARdelta selective agonist) significantly accelerated blastocyst hatching but did not increase total cell number of cultured blastocysts. GW 501516 52-60 peroxisome proliferator activator receptor delta Mus musculus 64-73 21816786-12 2011 CONCLUSIONS: GW501516 increased the hepatic removal of VLDL particles, which might have resulted from decreased apoC-III concentration. GW 501516 13-21 apolipoprotein C3 Homo sapiens 112-120 21816786-13 2011 GW501516 increased apoA-II production, resulting in an increased concentration of LpA-I:A-II particles. GW 501516 0-8 apolipoprotein A2 Homo sapiens 19-26 21816786-3 2011 OBJECTIVE: The aim of the study was to examine the effect of GW501516, a PPAR-delta agonist, on lipoprotein metabolism. GW 501516 61-69 peroxisome proliferator activated receptor delta Homo sapiens 73-83 21816786-7 2011 RESULTS: GW501516 decreased plasma triglycerides, fatty acid, apoB-100, and apoB-48 concentrations. GW 501516 9-17 apolipoprotein B Homo sapiens 62-70 21816786-7 2011 RESULTS: GW501516 decreased plasma triglycerides, fatty acid, apoB-100, and apoB-48 concentrations. GW 501516 9-17 apolipoprotein B Homo sapiens 76-83 21816786-8 2011 GW501516 decreased the concentrations of VLDL-apoB by increasing its fractional catabolism and of apoC-III by decreasing its production rate (P < 0.05). GW 501516 0-8 apolipoprotein C3 Homo sapiens 98-106 21816786-10 2011 GW501516 increased HDL-cholesterol, apoA-II, and LpA-I:A-II concentrations by increasing apoA-II and LpA-I:A-II production (P < 0.05). GW 501516 0-8 apolipoprotein A2 Homo sapiens 36-43 21816786-10 2011 GW501516 increased HDL-cholesterol, apoA-II, and LpA-I:A-II concentrations by increasing apoA-II and LpA-I:A-II production (P < 0.05). GW 501516 0-8 apolipoprotein A2 Homo sapiens 89-96 21617181-4 2011 RESULTS: First, we observed that the PPAR-beta/-delta agonist GW501516 prevented both IL-6-dependent reduction in insulin-stimulated Akt phosphorylation and glucose uptake in adipocytes. GW 501516 62-70 peroxisome proliferator activator receptor delta Mus musculus 37-46 21709207-3 2011 Treatment of human EPCs with a selective PPARdelta agonist GW501516 for 24 hours increased the levels of mRNA, protein, and enzymatic activity of GTP cyclohydrolase I (GTPCH I), as well as the production of tetrahydrobiopterin. GW 501516 59-67 peroxisome proliferator activated receptor delta Homo sapiens 41-50 21709207-3 2011 Treatment of human EPCs with a selective PPARdelta agonist GW501516 for 24 hours increased the levels of mRNA, protein, and enzymatic activity of GTP cyclohydrolase I (GTPCH I), as well as the production of tetrahydrobiopterin. GW 501516 59-67 GTP cyclohydrolase 1 Homo sapiens 146-166 21709207-3 2011 Treatment of human EPCs with a selective PPARdelta agonist GW501516 for 24 hours increased the levels of mRNA, protein, and enzymatic activity of GTP cyclohydrolase I (GTPCH I), as well as the production of tetrahydrobiopterin. GW 501516 59-67 GTP cyclohydrolase 1 Homo sapiens 168-175 21709207-4 2011 The effects of GW501516 were mediated by suppression of PTEN expression, thereby increasing phosphorylation of AKT. GW 501516 15-23 phosphatase and tensin homolog Homo sapiens 56-60 21709207-4 2011 The effects of GW501516 were mediated by suppression of PTEN expression, thereby increasing phosphorylation of AKT. GW 501516 15-23 AKT serine/threonine kinase 1 Homo sapiens 111-114 21709207-5 2011 The AKT signaling also mediated GW501516-induced phosphorylation of endothelial NO synthase. GW 501516 32-40 AKT serine/threonine kinase 1 Homo sapiens 4-7 21709207-11 2011 GTPCH I-small interfering RNA transfection significantly inhibited in vivo regenerative capacity of EPCs stimulated with GW501516. GW 501516 121-129 GTP cyclohydrolase 1 Homo sapiens 0-7 21617181-9 2011 Several steps in STAT3 activation require its association with heat shock protein 90 (Hsp90), which was prevented by GW501516 as revealed in immunoprecipitation studies. GW 501516 117-125 signal transducer and activator of transcription 3 Mus musculus 17-22 22466297-0 2011 GW501516 acts as an efficient PPARalpha activator in the mouse liver. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 30-39 22466297-1 2011 The peroxisome proliferator-activated receptor (PPAR) subtype specificity of GW501516, a well-known PPARdelta-specific agonist, was studied by examining its effects on the expression of endogenous genes in primary hepatocytes and the liver of wild-type and PPARalpha-null mice. GW 501516 77-85 peroxisome proliferator activated receptor alpha Mus musculus 4-46 22466297-1 2011 The peroxisome proliferator-activated receptor (PPAR) subtype specificity of GW501516, a well-known PPARdelta-specific agonist, was studied by examining its effects on the expression of endogenous genes in primary hepatocytes and the liver of wild-type and PPARalpha-null mice. GW 501516 77-85 peroxisome proliferator activated receptor alpha Mus musculus 48-52 22466297-1 2011 The peroxisome proliferator-activated receptor (PPAR) subtype specificity of GW501516, a well-known PPARdelta-specific agonist, was studied by examining its effects on the expression of endogenous genes in primary hepatocytes and the liver of wild-type and PPARalpha-null mice. GW 501516 77-85 peroxisome proliferator activator receptor delta Mus musculus 100-109 22466297-1 2011 The peroxisome proliferator-activated receptor (PPAR) subtype specificity of GW501516, a well-known PPARdelta-specific agonist, was studied by examining its effects on the expression of endogenous genes in primary hepatocytes and the liver of wild-type and PPARalpha-null mice. GW 501516 77-85 peroxisome proliferator activated receptor alpha Mus musculus 257-266 22466297-2 2011 GW501516, like the PPARalpha-specific agonist Wy14,643, induced the expression of several PPAR target genes in a dose-dependent manner but this action was mostly absent in the cells and liver of PPARalpha-null mice. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 19-28 22466297-2 2011 GW501516, like the PPARalpha-specific agonist Wy14,643, induced the expression of several PPAR target genes in a dose-dependent manner but this action was mostly absent in the cells and liver of PPARalpha-null mice. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 19-23 22466297-2 2011 GW501516, like the PPARalpha-specific agonist Wy14,643, induced the expression of several PPAR target genes in a dose-dependent manner but this action was mostly absent in the cells and liver of PPARalpha-null mice. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 195-204 22466297-3 2011 Results indicated that GW501516 acts as an efficient PPARalpha activator in the mouse liver. GW 501516 23-31 peroxisome proliferator activated receptor alpha Mus musculus 53-62 21617181-9 2011 Several steps in STAT3 activation require its association with heat shock protein 90 (Hsp90), which was prevented by GW501516 as revealed in immunoprecipitation studies. GW 501516 117-125 heat shock protein, 3 Mus musculus 63-84 21617181-9 2011 Several steps in STAT3 activation require its association with heat shock protein 90 (Hsp90), which was prevented by GW501516 as revealed in immunoprecipitation studies. GW 501516 117-125 heat shock protein, 3 Mus musculus 86-91 21617181-4 2011 RESULTS: First, we observed that the PPAR-beta/-delta agonist GW501516 prevented both IL-6-dependent reduction in insulin-stimulated Akt phosphorylation and glucose uptake in adipocytes. GW 501516 62-70 interleukin 6 Mus musculus 86-90 21617181-4 2011 RESULTS: First, we observed that the PPAR-beta/-delta agonist GW501516 prevented both IL-6-dependent reduction in insulin-stimulated Akt phosphorylation and glucose uptake in adipocytes. GW 501516 62-70 thymoma viral proto-oncogene 1 Mus musculus 133-136 21617181-7 2011 Moreover, GW501516 prevented IL-6-dependent induction of extracellular signal-related kinase (ERK)1/2, a serine-threonine-protein kinase involved in serine STAT3 phosphorylation. GW 501516 10-18 interleukin 6 Mus musculus 29-33 21617181-7 2011 Moreover, GW501516 prevented IL-6-dependent induction of extracellular signal-related kinase (ERK)1/2, a serine-threonine-protein kinase involved in serine STAT3 phosphorylation. GW 501516 10-18 mitogen-activated protein kinase 3 Mus musculus 57-101 21617181-7 2011 Moreover, GW501516 prevented IL-6-dependent induction of extracellular signal-related kinase (ERK)1/2, a serine-threonine-protein kinase involved in serine STAT3 phosphorylation. GW 501516 10-18 signal transducer and activator of transcription 3 Mus musculus 156-161 21363937-0 2011 The PPARbeta/delta activator GW501516 prevents the down-regulation of AMPK caused by a high-fat diet in liver and amplifies the PGC-1alpha-Lipin 1-PPARalpha pathway leading to increased fatty acid oxidation. GW 501516 29-37 peroxisome proliferator activator receptor delta Mus musculus 4-12 21363937-0 2011 The PPARbeta/delta activator GW501516 prevents the down-regulation of AMPK caused by a high-fat diet in liver and amplifies the PGC-1alpha-Lipin 1-PPARalpha pathway leading to increased fatty acid oxidation. GW 501516 29-37 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 128-138 21511987-0 2011 The role played by the peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) activator, GW501516, in control of fatty acid metabolism: a new potential therapeutic target for treating metabolic syndrome. GW 501516 105-113 peroxisome proliferator activated receptor delta Homo sapiens 23-70 21511987-0 2011 The role played by the peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) activator, GW501516, in control of fatty acid metabolism: a new potential therapeutic target for treating metabolic syndrome. GW 501516 105-113 peroxisome proliferator activated receptor delta Homo sapiens 78-86 21363937-0 2011 The PPARbeta/delta activator GW501516 prevents the down-regulation of AMPK caused by a high-fat diet in liver and amplifies the PGC-1alpha-Lipin 1-PPARalpha pathway leading to increased fatty acid oxidation. GW 501516 29-37 lipin 1 Mus musculus 139-146 21363937-0 2011 The PPARbeta/delta activator GW501516 prevents the down-regulation of AMPK caused by a high-fat diet in liver and amplifies the PGC-1alpha-Lipin 1-PPARalpha pathway leading to increased fatty acid oxidation. GW 501516 29-37 peroxisome proliferator activated receptor alpha Mus musculus 147-156 21363937-3 2011 Exposure to the HFD caused hypertriglyceridemia that was accompanied by reduced hepatic mRNA levels of PPAR-gamma coactivator 1 (PGC-1)-alpha and lipin 1, and these effects were prevented by GW501516 treatment. GW 501516 191-199 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 129-141 21363937-3 2011 Exposure to the HFD caused hypertriglyceridemia that was accompanied by reduced hepatic mRNA levels of PPAR-gamma coactivator 1 (PGC-1)-alpha and lipin 1, and these effects were prevented by GW501516 treatment. GW 501516 191-199 lipin 1 Mus musculus 146-153 21363937-4 2011 GW501516 treatment also increased nuclear lipin 1 protein levels, leading to amplification in the PGC-1alpha-PPARalpha signaling system, as demonstrated by the increase in PPARalpha levels and PPARalpha-DNA binding activity and the increased expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 lipin 1 Mus musculus 42-49 21363937-4 2011 GW501516 treatment also increased nuclear lipin 1 protein levels, leading to amplification in the PGC-1alpha-PPARalpha signaling system, as demonstrated by the increase in PPARalpha levels and PPARalpha-DNA binding activity and the increased expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 98-108 21363937-4 2011 GW501516 treatment also increased nuclear lipin 1 protein levels, leading to amplification in the PGC-1alpha-PPARalpha signaling system, as demonstrated by the increase in PPARalpha levels and PPARalpha-DNA binding activity and the increased expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 109-118 21363937-4 2011 GW501516 treatment also increased nuclear lipin 1 protein levels, leading to amplification in the PGC-1alpha-PPARalpha signaling system, as demonstrated by the increase in PPARalpha levels and PPARalpha-DNA binding activity and the increased expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 172-181 21363937-4 2011 GW501516 treatment also increased nuclear lipin 1 protein levels, leading to amplification in the PGC-1alpha-PPARalpha signaling system, as demonstrated by the increase in PPARalpha levels and PPARalpha-DNA binding activity and the increased expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 172-181 21363937-4 2011 GW501516 treatment also increased nuclear lipin 1 protein levels, leading to amplification in the PGC-1alpha-PPARalpha signaling system, as demonstrated by the increase in PPARalpha levels and PPARalpha-DNA binding activity and the increased expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 172-181 21363937-6 2011 Moreover, GW501516 increased the levels of the hepatic endogenous ligand for PPARalpha, 16:0/18:1-phosphatidilcholine and markedly enhanced the expression of the hepatic Vldl receptor. GW 501516 10-18 peroxisome proliferator activated receptor alpha Mus musculus 77-86 21363937-6 2011 Moreover, GW501516 increased the levels of the hepatic endogenous ligand for PPARalpha, 16:0/18:1-phosphatidilcholine and markedly enhanced the expression of the hepatic Vldl receptor. GW 501516 10-18 very low density lipoprotein receptor Mus musculus 170-183 21363937-7 2011 Interestingly, GW501516 prevented the reduction in AMP-activated protein kinase (AMPK) phosphorylation and the increase in phosphorylated levels of ERK1/2 caused by HFD. GW 501516 15-23 mitogen-activated protein kinase 3 Mus musculus 148-154 21363937-9 2011 These findings indicate that the hypotriglyceridemic effect of GW501516 in HFD-fed mice is accompanied by an increase in phospho-AMPK levels and the amplification of the PGC-1alpha-lipin 1-PPARalpha pathway. GW 501516 63-71 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 170-180 21363937-9 2011 These findings indicate that the hypotriglyceridemic effect of GW501516 in HFD-fed mice is accompanied by an increase in phospho-AMPK levels and the amplification of the PGC-1alpha-lipin 1-PPARalpha pathway. GW 501516 63-71 lipin 1 Mus musculus 181-188 21363937-9 2011 These findings indicate that the hypotriglyceridemic effect of GW501516 in HFD-fed mice is accompanied by an increase in phospho-AMPK levels and the amplification of the PGC-1alpha-lipin 1-PPARalpha pathway. GW 501516 63-71 peroxisome proliferator activated receptor alpha Mus musculus 189-198 20221637-7 2011 The PPARbeta/delta agonists GW501516 and PGI(2) caused stimulations of only 1.5-fold in both cell lines. GW 501516 28-36 peroxisome proliferator activated receptor delta Homo sapiens 4-12 21146504-0 2011 The peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) agonist GW501516 prevents TNF-alpha-induced NF-kappaB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1. GW 501516 83-91 peroxisome proliferator activated receptor delta Homo sapiens 4-51 21146504-0 2011 The peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) agonist GW501516 prevents TNF-alpha-induced NF-kappaB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1. GW 501516 83-91 peroxisome proliferator activated receptor delta Homo sapiens 59-67 21146504-0 2011 The peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) agonist GW501516 prevents TNF-alpha-induced NF-kappaB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1. GW 501516 83-91 tumor necrosis factor Homo sapiens 101-110 21146504-0 2011 The peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) agonist GW501516 prevents TNF-alpha-induced NF-kappaB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1. GW 501516 83-91 RELA proto-oncogene, NF-kB subunit Homo sapiens 173-176 21146504-0 2011 The peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) agonist GW501516 prevents TNF-alpha-induced NF-kappaB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1. GW 501516 83-91 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 197-201 21146504-0 2011 The peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) agonist GW501516 prevents TNF-alpha-induced NF-kappaB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1. GW 501516 83-91 sirtuin 1 Homo sapiens 206-211 21146504-3 2011 The PPARbeta/delta agonist GW501516 inhibited the increase caused by TNF-alpha in the mRNA levels of the NF-kappaB target genes interleukin 8 (IL-8), TNF-alpha and thymic stromal lymphopoietin (TSLP). GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 4-12 21146504-3 2011 The PPARbeta/delta agonist GW501516 inhibited the increase caused by TNF-alpha in the mRNA levels of the NF-kappaB target genes interleukin 8 (IL-8), TNF-alpha and thymic stromal lymphopoietin (TSLP). GW 501516 27-35 tumor necrosis factor Homo sapiens 69-78 21146504-3 2011 The PPARbeta/delta agonist GW501516 inhibited the increase caused by TNF-alpha in the mRNA levels of the NF-kappaB target genes interleukin 8 (IL-8), TNF-alpha and thymic stromal lymphopoietin (TSLP). GW 501516 27-35 C-X-C motif chemokine ligand 8 Homo sapiens 128-141 21146504-3 2011 The PPARbeta/delta agonist GW501516 inhibited the increase caused by TNF-alpha in the mRNA levels of the NF-kappaB target genes interleukin 8 (IL-8), TNF-alpha and thymic stromal lymphopoietin (TSLP). GW 501516 27-35 C-X-C motif chemokine ligand 8 Homo sapiens 143-147 21146504-3 2011 The PPARbeta/delta agonist GW501516 inhibited the increase caused by TNF-alpha in the mRNA levels of the NF-kappaB target genes interleukin 8 (IL-8), TNF-alpha and thymic stromal lymphopoietin (TSLP). GW 501516 27-35 tumor necrosis factor Homo sapiens 150-159 21146504-3 2011 The PPARbeta/delta agonist GW501516 inhibited the increase caused by TNF-alpha in the mRNA levels of the NF-kappaB target genes interleukin 8 (IL-8), TNF-alpha and thymic stromal lymphopoietin (TSLP). GW 501516 27-35 thymic stromal lymphopoietin Homo sapiens 194-198 21146504-4 2011 Likewise, GW501516 prevented the increase in NF-kappaB DNA-binding activity observed in cells exposed to TNF-alpha. GW 501516 10-18 tumor necrosis factor Homo sapiens 105-114 21146504-5 2011 The reduction in NF-kappaB activity following GW501516 treatment in cells stimulated with TNF-alpha did not involve either increased IkappaBalpha protein levels or a reduction in the translocation of the p65 subunit of NF-kappaB. GW 501516 46-54 tumor necrosis factor Homo sapiens 90-99 21146504-6 2011 In contrast, GW501516 treatment decreased TNF-alpha-induced p65 acetylation. GW 501516 13-21 tumor necrosis factor Homo sapiens 42-51 21146504-6 2011 In contrast, GW501516 treatment decreased TNF-alpha-induced p65 acetylation. GW 501516 13-21 RELA proto-oncogene, NF-kB subunit Homo sapiens 60-63 21146504-9 2011 GW501516 increased AMPK phosphorylation and the subsequent p300 phosphorylation, leading to a marked reduction in the association between p65 and this transcriptional co-activator. GW 501516 0-8 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 19-23 21146504-9 2011 GW501516 increased AMPK phosphorylation and the subsequent p300 phosphorylation, leading to a marked reduction in the association between p65 and this transcriptional co-activator. GW 501516 0-8 E1A binding protein p300 Homo sapiens 59-63 21146504-9 2011 GW501516 increased AMPK phosphorylation and the subsequent p300 phosphorylation, leading to a marked reduction in the association between p65 and this transcriptional co-activator. GW 501516 0-8 RELA proto-oncogene, NF-kB subunit Homo sapiens 138-141 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 53-61 C-X-C motif chemokine ligand 8 Homo sapiens 26-30 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 53-61 tumor necrosis factor Homo sapiens 75-84 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 53-61 peroxisome proliferator activated receptor delta Homo sapiens 139-147 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 53-61 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 178-182 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 53-61 sirtuin 1 Homo sapiens 212-217 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 53-61 peroxisome proliferator activated receptor delta Homo sapiens 318-326 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 53-61 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 334-338 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 53-61 sirtuin 1 Homo sapiens 343-348 21070867-9 2011 PPARbeta/delta activation by GW501516 enhanced the physical interaction between PPARbeta/delta and p65, which suggests that this mechanism may also interfere NF-kappaB transactivation capacity in the heart. GW 501516 29-37 peroxisome proliferator activated receptor delta Homo sapiens 0-8 21070867-9 2011 PPARbeta/delta activation by GW501516 enhanced the physical interaction between PPARbeta/delta and p65, which suggests that this mechanism may also interfere NF-kappaB transactivation capacity in the heart. GW 501516 29-37 peroxisome proliferator activated receptor delta Homo sapiens 80-88 21070867-9 2011 PPARbeta/delta activation by GW501516 enhanced the physical interaction between PPARbeta/delta and p65, which suggests that this mechanism may also interfere NF-kappaB transactivation capacity in the heart. GW 501516 29-37 RELA proto-oncogene, NF-kB subunit Homo sapiens 99-102 21070867-10 2011 GW501516-induced PPARbeta/delta activation can attenuate the inflammatory response induced in human cardiac AC16 cells exposed to the saturated fatty acid palmitate and in mice fed a high-fat diet. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 17-25 21297860-6 2011 The transgenic mammary gland also expressed higher levels of PPARdelta and a gene expression profile resembling wild-type mice maintained on a diet containing the PPARdelta agonist, GW501516. GW 501516 182-190 peroxisome proliferator activator receptor delta Mus musculus 163-172 21297860-9 2011 GW501516-treated transgenic mice expressed higher levels of fatty acid and phospholipid metabolites than treated wild-type mice, suggesting the involvement of PDK1 in enhancing PPARdelta-driven energy metabolism. GW 501516 0-8 pyruvate dehydrogenase kinase, isoenzyme 1 Mus musculus 159-163 21297860-9 2011 GW501516-treated transgenic mice expressed higher levels of fatty acid and phospholipid metabolites than treated wild-type mice, suggesting the involvement of PDK1 in enhancing PPARdelta-driven energy metabolism. GW 501516 0-8 peroxisome proliferator activator receptor delta Mus musculus 177-186 21300064-7 2011 Treatment of wild-type and ob/ob mice with GW501516 enhanced the increase in plasma GLP-1 level after an oral glucose load and improved glucose tolerance. GW 501516 43-51 glucagon Mus musculus 84-89 21352808-2 2011 Activation of PPARdelta by GW501516, a specific agonist of PPARdelta, significantly inhibited the Ang II-induced premature senescence of hVSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 21352808-2 2011 Activation of PPARdelta by GW501516, a specific agonist of PPARdelta, significantly inhibited the Ang II-induced premature senescence of hVSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 59-68 21352808-4 2011 Notably, GW501516 up-regulated the expression of antioxidant genes, such as glutathione peroxidase 1, thioredoxin 1, manganese superoxide dismutase and heme oxygenase 1. GW 501516 9-17 glutathione peroxidase 1 Homo sapiens 76-100 21352808-4 2011 Notably, GW501516 up-regulated the expression of antioxidant genes, such as glutathione peroxidase 1, thioredoxin 1, manganese superoxide dismutase and heme oxygenase 1. GW 501516 9-17 superoxide dismutase 2 Homo sapiens 117-147 21352808-4 2011 Notably, GW501516 up-regulated the expression of antioxidant genes, such as glutathione peroxidase 1, thioredoxin 1, manganese superoxide dismutase and heme oxygenase 1. GW 501516 9-17 heme oxygenase 1 Homo sapiens 152-168 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 269-277 C-X-C motif chemokine ligand 8 Homo sapiens 26-30 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 269-277 tumor necrosis factor Homo sapiens 75-84 21146504-11 2011 Finally, the reduction in IL-8 mRNA levels following GW501516 treatment in TNF-alpha-stimulated cells was abolished in the presence of the PPARbeta/delta antagonist GSK0660, the AMPK inhibitor compound C and the SIRT1 inhibitor sirtinol, indicating that the effects of GW501516 on NF-kappaB activity were dependent on PPARbeta/delta, AMPK and SIRT1, respectively. GW 501516 269-277 peroxisome proliferator activated receptor delta Homo sapiens 139-147 21215640-2 2011 Incorporation of structurally constrained oxime-ether based linker in the chemotype of a potent PPARdelta selective agonist GW-501516 was adapted as designing strategy. GW 501516 124-133 peroxisome proliferator activated receptor delta Homo sapiens 96-105 21484566-6 2011 PPAR-delta activators increase the capacity for fat oxidation in skeletal muscle.Clinical experience with bezafibrate, which activates PPAR-delta and -alpha, and studies on the PPAR-alpha/delta activator tetradecylthioacetic acid, the PPAR-delta activator GW501516, and combinations of the PPAR-alpha activator fenofibrate with rosiglitazone or pioglitazone have encouraged attempts to develop single molecules that activate two or all three PPARs. GW 501516 256-264 peroxisome proliferator activated receptor delta Homo sapiens 0-10 20571903-4 2010 Our results show that GW501516 treatment promoted generation of mitochondrial ATP, as well as expression levels of PGC-1alpha, NRF-1 and mtTFA, decreased basal insulin secretion, but had no effect on glucose-stimulated insulin secretion (GSIS), increased amounts of UCP2 and changed ATP-to-ADP ratio, improved mitochondrial morphology in palmitate-treated beta-cells. GW 501516 22-30 nuclear respiratory factor 1 Mesocricetus auratus 127-132 21966476-0 2011 GW501516, a PPARdelta agonist, ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition of TAK1-NFkappaB pathway in mice. GW 501516 0-8 peroxisome proliferator activator receptor delta Mus musculus 12-21 21966476-0 2011 GW501516, a PPARdelta agonist, ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition of TAK1-NFkappaB pathway in mice. GW 501516 0-8 mitogen-activated protein kinase kinase kinase 7 Mus musculus 123-127 21966476-0 2011 GW501516, a PPARdelta agonist, ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition of TAK1-NFkappaB pathway in mice. GW 501516 0-8 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 128-136 21966476-3 2011 Thus, we examined the renoprotective effect of GW501516, a PPARdelta agonist, in a protein-overload mouse nephropathy model and identified its molecular mechanism. GW 501516 47-55 peroxisome proliferator activator receptor delta Mus musculus 59-68 21966476-8 2011 In vitro studies using cultured proximal tubular cells showed that GW501516 attenuated both TNFalpha- and FFA (palmitate)-induced, but not albumin-induced, MCP-1 expression via direct inhibition of the TGF-beta activated kinase 1 (TAK1)-NFkappaB pathway, a common downstream signaling pathway to TNFalpha receptor and toll-like receptor-4. GW 501516 67-75 tumor necrosis factor Mus musculus 92-109 21966476-8 2011 In vitro studies using cultured proximal tubular cells showed that GW501516 attenuated both TNFalpha- and FFA (palmitate)-induced, but not albumin-induced, MCP-1 expression via direct inhibition of the TGF-beta activated kinase 1 (TAK1)-NFkappaB pathway, a common downstream signaling pathway to TNFalpha receptor and toll-like receptor-4. GW 501516 67-75 chemokine (C-C motif) ligand 2 Mus musculus 156-161 21966476-8 2011 In vitro studies using cultured proximal tubular cells showed that GW501516 attenuated both TNFalpha- and FFA (palmitate)-induced, but not albumin-induced, MCP-1 expression via direct inhibition of the TGF-beta activated kinase 1 (TAK1)-NFkappaB pathway, a common downstream signaling pathway to TNFalpha receptor and toll-like receptor-4. GW 501516 67-75 mitogen-activated protein kinase kinase kinase 7 Mus musculus 202-229 21966476-8 2011 In vitro studies using cultured proximal tubular cells showed that GW501516 attenuated both TNFalpha- and FFA (palmitate)-induced, but not albumin-induced, MCP-1 expression via direct inhibition of the TGF-beta activated kinase 1 (TAK1)-NFkappaB pathway, a common downstream signaling pathway to TNFalpha receptor and toll-like receptor-4. GW 501516 67-75 mitogen-activated protein kinase kinase kinase 7 Mus musculus 231-235 21966476-8 2011 In vitro studies using cultured proximal tubular cells showed that GW501516 attenuated both TNFalpha- and FFA (palmitate)-induced, but not albumin-induced, MCP-1 expression via direct inhibition of the TGF-beta activated kinase 1 (TAK1)-NFkappaB pathway, a common downstream signaling pathway to TNFalpha receptor and toll-like receptor-4. GW 501516 67-75 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 237-245 21966476-8 2011 In vitro studies using cultured proximal tubular cells showed that GW501516 attenuated both TNFalpha- and FFA (palmitate)-induced, but not albumin-induced, MCP-1 expression via direct inhibition of the TGF-beta activated kinase 1 (TAK1)-NFkappaB pathway, a common downstream signaling pathway to TNFalpha receptor and toll-like receptor-4. GW 501516 67-75 tumor necrosis factor Mus musculus 92-100 21966511-5 2011 The pro-differentiation effect of PPARbeta/delta agonist GW501516 was also abolished when keratinocytes were co-treated with PPARbeta/delta antagonist GSK0660 and similarly in organotypic skin culture incubated with blocking ANGPTL4 monoclonal antibody targeted against the C-terminal fibrinogen-like domain. GW 501516 57-65 peroxisome proliferator activated receptor delta Homo sapiens 34-42 21966511-5 2011 The pro-differentiation effect of PPARbeta/delta agonist GW501516 was also abolished when keratinocytes were co-treated with PPARbeta/delta antagonist GSK0660 and similarly in organotypic skin culture incubated with blocking ANGPTL4 monoclonal antibody targeted against the C-terminal fibrinogen-like domain. GW 501516 57-65 peroxisome proliferator activated receptor delta Homo sapiens 125-133 21966511-5 2011 The pro-differentiation effect of PPARbeta/delta agonist GW501516 was also abolished when keratinocytes were co-treated with PPARbeta/delta antagonist GSK0660 and similarly in organotypic skin culture incubated with blocking ANGPTL4 monoclonal antibody targeted against the C-terminal fibrinogen-like domain. GW 501516 57-65 angiopoietin like 4 Homo sapiens 225-232 20571903-4 2010 Our results show that GW501516 treatment promoted generation of mitochondrial ATP, as well as expression levels of PGC-1alpha, NRF-1 and mtTFA, decreased basal insulin secretion, but had no effect on glucose-stimulated insulin secretion (GSIS), increased amounts of UCP2 and changed ATP-to-ADP ratio, improved mitochondrial morphology in palmitate-treated beta-cells. GW 501516 22-30 insulin Mesocricetus auratus 160-167 20571903-4 2010 Our results show that GW501516 treatment promoted generation of mitochondrial ATP, as well as expression levels of PGC-1alpha, NRF-1 and mtTFA, decreased basal insulin secretion, but had no effect on glucose-stimulated insulin secretion (GSIS), increased amounts of UCP2 and changed ATP-to-ADP ratio, improved mitochondrial morphology in palmitate-treated beta-cells. GW 501516 22-30 mitochondrial uncoupling protein 2 Mesocricetus auratus 266-270 20571903-5 2010 GW501516-induced activation of PPARdelta enhanced mitochondrial energy metabolism, but also promoted a concomitant mitochondrial uncoupling and resulted in decreased basal insulin secretion and restricted GSIS; this observation indicated the possible action of a protective mechanism responding to the alleviation of excessive lipid load and basal insulin secretion in lipotoxic beta-cells. GW 501516 0-8 peroxisome proliferator-activated receptor delta Mesocricetus auratus 31-40 20406305-8 2010 In this study we show that the PPARdelta agonists GW501516 and L165041 ameliorate MOGp35-55-induced EAE in C57BL/6 mice by blocking interferon (IFN)-gamma and interleukin (IL)-17 production by T helper type 1 (Th1) and Th17 cells. GW 501516 50-58 peroxisome proliferator activator receptor delta Mus musculus 31-40 20406305-8 2010 In this study we show that the PPARdelta agonists GW501516 and L165041 ameliorate MOGp35-55-induced EAE in C57BL/6 mice by blocking interferon (IFN)-gamma and interleukin (IL)-17 production by T helper type 1 (Th1) and Th17 cells. GW 501516 50-58 interferon gamma Mus musculus 132-154 20406305-8 2010 In this study we show that the PPARdelta agonists GW501516 and L165041 ameliorate MOGp35-55-induced EAE in C57BL/6 mice by blocking interferon (IFN)-gamma and interleukin (IL)-17 production by T helper type 1 (Th1) and Th17 cells. GW 501516 50-58 interleukin 17A Mus musculus 159-178 20406305-8 2010 In this study we show that the PPARdelta agonists GW501516 and L165041 ameliorate MOGp35-55-induced EAE in C57BL/6 mice by blocking interferon (IFN)-gamma and interleukin (IL)-17 production by T helper type 1 (Th1) and Th17 cells. GW 501516 50-58 negative elongation factor complex member C/D, Th1l Mus musculus 193-213 19946680-0 2010 Characterization of two major urinary metabolites of the PPARdelta-agonist GW1516 and implementation of the drug in routine doping controls. GW 501516 75-81 peroxisome proliferator activated receptor delta Homo sapiens 57-66 20542425-0 2010 Synthesis of isosteric selenium analog of the PPARbeta/delta agonist GW501516 and comparison of biological activity. GW 501516 69-77 peroxisome proliferator activated receptor delta Homo sapiens 46-54 20542425-2 2010 Herein, we describe an efficient synthesis of a novel isosteric selenium analog of the highly specific PPARbeta/delta ligand 2-methyl-4-((4-methyl-2-(4-trifluoromethylphenyl)-1,3-thiazol-5-yl)-methylsulfanyl)phenoxy-acetic acid (GW501516; 1). GW 501516 229-237 peroxisome proliferator activated receptor delta Homo sapiens 103-111 20221783-1 2010 Activation of peroxisome proliferator-activated receptor (PPAR) delta by GW501516, a specific PPARdelta ligand, significantly inhibited interleukin (IL)-1beta-induced proliferation and migration of vascular smooth muscle cells (VSMCs). GW 501516 73-81 peroxisome proliferator activated receptor delta Homo sapiens 58-62 20221783-1 2010 Activation of peroxisome proliferator-activated receptor (PPAR) delta by GW501516, a specific PPARdelta ligand, significantly inhibited interleukin (IL)-1beta-induced proliferation and migration of vascular smooth muscle cells (VSMCs). GW 501516 73-81 peroxisome proliferator activated receptor delta Homo sapiens 94-103 20221783-1 2010 Activation of peroxisome proliferator-activated receptor (PPAR) delta by GW501516, a specific PPARdelta ligand, significantly inhibited interleukin (IL)-1beta-induced proliferation and migration of vascular smooth muscle cells (VSMCs). GW 501516 73-81 interleukin 1 beta Homo sapiens 136-158 20221783-2 2010 This effect of GW501516 was dependent on transforming growth factor-beta, and was mediated through the up-regulation of IL-1 receptor antagonist. GW 501516 15-23 interleukin 1 receptor antagonist Homo sapiens 120-144 20221783-3 2010 The inhibitory effect of GW501516 on VSMC proliferation was associated with cell cycle arrest at the G1 to S phase transition, which was accompanied by the induction of p21 and p53 along with decreased cyclin-dependent kinase 4 expression. GW 501516 25-33 cyclin dependent kinase inhibitor 1A Homo sapiens 169-172 20221783-3 2010 The inhibitory effect of GW501516 on VSMC proliferation was associated with cell cycle arrest at the G1 to S phase transition, which was accompanied by the induction of p21 and p53 along with decreased cyclin-dependent kinase 4 expression. GW 501516 25-33 tumor protein p53 Homo sapiens 177-180 20221783-3 2010 The inhibitory effect of GW501516 on VSMC proliferation was associated with cell cycle arrest at the G1 to S phase transition, which was accompanied by the induction of p21 and p53 along with decreased cyclin-dependent kinase 4 expression. GW 501516 25-33 cyclin dependent kinase 4 Homo sapiens 202-227 20221783-4 2010 Inhibition of cell migration by GW501516 was associated with the down-regulation of matrix metalloproteinase (MMP)-2 and MMP-9 in IL-1beta-treated VSMCs. GW 501516 32-40 matrix metallopeptidase 2 Homo sapiens 84-116 20221783-4 2010 Inhibition of cell migration by GW501516 was associated with the down-regulation of matrix metalloproteinase (MMP)-2 and MMP-9 in IL-1beta-treated VSMCs. GW 501516 32-40 matrix metallopeptidase 9 Homo sapiens 121-126 20221783-4 2010 Inhibition of cell migration by GW501516 was associated with the down-regulation of matrix metalloproteinase (MMP)-2 and MMP-9 in IL-1beta-treated VSMCs. GW 501516 32-40 interleukin 1 beta Homo sapiens 130-138 20221783-5 2010 Inhibition of extracellular signal-regulated kinase significantly reduced the GW501516-mediated inhibition of IL-1beta-stimulated VSMC proliferation. GW 501516 78-86 interleukin 1 beta Homo sapiens 110-118 19538467-3 2010 Here, we demonstrate that administration of GW501516, a specific PPARdelta ligand, significantly promoted wound closure in the experimental mouse and had a profound effect on the expression of collagen types I and III, alpha-smooth muscle actin, pSmad3 and TGF-beta1, which play a pivotal role in wound healing processes. GW 501516 44-52 peroxisome proliferator activator receptor delta Mus musculus 65-74 19538467-3 2010 Here, we demonstrate that administration of GW501516, a specific PPARdelta ligand, significantly promoted wound closure in the experimental mouse and had a profound effect on the expression of collagen types I and III, alpha-smooth muscle actin, pSmad3 and TGF-beta1, which play a pivotal role in wound healing processes. GW 501516 44-52 transforming growth factor, beta 1 Mus musculus 257-266 19946680-1 2010 Since January 2009, the list of prohibited substances and methods of doping as established by the World Anti-Doping Agency includes new therapeutics such as the peroxisome-proliferator-activated receptor (PPAR)-delta agonist GW1516, which is categorized as a gene doping substance. GW 501516 225-231 peroxisome proliferator activated receptor delta Homo sapiens 161-216 20185762-0 2010 Activation of peroxisome proliferator-activated receptor-{delta} by GW501516 prevents fatty acid-induced nuclear factor-{kappa}B activation and insulin resistance in skeletal muscle cells. GW 501516 68-76 peroxisome proliferator activator receptor delta Mus musculus 14-63 20185762-4 2010 In C2C12 skeletal muscle cells, the PPARdelta agonist GW501516 prevented phosphorylation of insulin receptor substrate-1 at Ser(307) and the inhibition of insulin-stimulated Akt phosphorylation caused by exposure to the saturated fatty acid palmitate. GW 501516 54-62 peroxisome proliferator activator receptor delta Mus musculus 36-45 20185762-7 2010 In agreement with these changes, GW501516 treatment reversed the increase in DAG and PKCtheta activation caused by palmitate. GW 501516 33-41 protein kinase C, theta Mus musculus 85-93 20185762-4 2010 In C2C12 skeletal muscle cells, the PPARdelta agonist GW501516 prevented phosphorylation of insulin receptor substrate-1 at Ser(307) and the inhibition of insulin-stimulated Akt phosphorylation caused by exposure to the saturated fatty acid palmitate. GW 501516 54-62 insulin receptor substrate 1 Mus musculus 92-120 20185762-9 2010 Consistent with these findings, PPARdelta activation by GW501516 blocked palmitate-induced NF-kappaB DNA-binding activity. GW 501516 56-64 peroxisome proliferator activator receptor delta Mus musculus 32-41 20040361-3 2010 After HIT-T15 cells (a beta-cell line) were exposed to high concentrations of palmitate and GW501516 (GW; a selective agonist of PPARdelta), we found that administration of GW increased the expression of PPARdelta mRNA. GW 501516 92-100 peroxisome proliferator-activated receptor delta Mesocricetus auratus 129-138 20066433-5 2010 Specific pharmacological activation of PPARbeta using GW0742 or GW501516 in low concentrations inhibits proliferation of human and murine melanoma cells. GW 501516 64-72 peroxisome proliferator activated receptor delta Homo sapiens 39-47 19903700-5 2010 METHODS AND RESULTS: En face confocal microscopy of murine aortas demonstrated that the PPARdelta-selective ligand GW501516 induced endothelial haem oxygenase-1 expression. GW 501516 115-123 peroxisome proliferator activator receptor delta Mus musculus 88-97 20040361-3 2010 After HIT-T15 cells (a beta-cell line) were exposed to high concentrations of palmitate and GW501516 (GW; a selective agonist of PPARdelta), we found that administration of GW increased the expression of PPARdelta mRNA. GW 501516 92-100 peroxisome proliferator-activated receptor delta Mesocricetus auratus 204-213 20040361-3 2010 After HIT-T15 cells (a beta-cell line) were exposed to high concentrations of palmitate and GW501516 (GW; a selective agonist of PPARdelta), we found that administration of GW increased the expression of PPARdelta mRNA. GW 501516 92-94 peroxisome proliferator-activated receptor delta Mesocricetus auratus 129-138 20040361-3 2010 After HIT-T15 cells (a beta-cell line) were exposed to high concentrations of palmitate and GW501516 (GW; a selective agonist of PPARdelta), we found that administration of GW increased the expression of PPARdelta mRNA. GW 501516 92-94 peroxisome proliferator-activated receptor delta Mesocricetus auratus 204-213 20040361-4 2010 GW-induced activation of PPARdelta up-regulated carnitine palmitoyltransferase 1 (CPT1), long-chain acyl-CoA dehydrogenase (LCAD), pyruvate dehydrogenase kinase 4 (PDK4), and uncoupling protein 2 (UCP2); alleviated mitochondrial swelling; attenuated apoptosis; and reduced basal insulin secretion induced by increased palmitate in HIT cells. GW 501516 0-2 peroxisome proliferator-activated receptor delta Mesocricetus auratus 25-34 20040361-4 2010 GW-induced activation of PPARdelta up-regulated carnitine palmitoyltransferase 1 (CPT1), long-chain acyl-CoA dehydrogenase (LCAD), pyruvate dehydrogenase kinase 4 (PDK4), and uncoupling protein 2 (UCP2); alleviated mitochondrial swelling; attenuated apoptosis; and reduced basal insulin secretion induced by increased palmitate in HIT cells. GW 501516 0-2 pyruvate dehydrogenase kinase, isozyme 4 Mesocricetus auratus 131-162 20040361-4 2010 GW-induced activation of PPARdelta up-regulated carnitine palmitoyltransferase 1 (CPT1), long-chain acyl-CoA dehydrogenase (LCAD), pyruvate dehydrogenase kinase 4 (PDK4), and uncoupling protein 2 (UCP2); alleviated mitochondrial swelling; attenuated apoptosis; and reduced basal insulin secretion induced by increased palmitate in HIT cells. GW 501516 0-2 pyruvate dehydrogenase kinase, isozyme 4 Mesocricetus auratus 164-168 20040361-4 2010 GW-induced activation of PPARdelta up-regulated carnitine palmitoyltransferase 1 (CPT1), long-chain acyl-CoA dehydrogenase (LCAD), pyruvate dehydrogenase kinase 4 (PDK4), and uncoupling protein 2 (UCP2); alleviated mitochondrial swelling; attenuated apoptosis; and reduced basal insulin secretion induced by increased palmitate in HIT cells. GW 501516 0-2 mitochondrial uncoupling protein 2 Mesocricetus auratus 175-195 20040361-4 2010 GW-induced activation of PPARdelta up-regulated carnitine palmitoyltransferase 1 (CPT1), long-chain acyl-CoA dehydrogenase (LCAD), pyruvate dehydrogenase kinase 4 (PDK4), and uncoupling protein 2 (UCP2); alleviated mitochondrial swelling; attenuated apoptosis; and reduced basal insulin secretion induced by increased palmitate in HIT cells. GW 501516 0-2 mitochondrial uncoupling protein 2 Mesocricetus auratus 197-201 21318167-3 2010 In the present study, we describe a new gastric tumor mouse model that is dependent on the potent and highly selective PPARdelta agonist GW501516 following carcinogen administration. GW 501516 137-145 peroxisome proliferator activator receptor delta Mus musculus 119-128 19660859-4 2010 Inhibition of C20 cell proliferation and clonogenicity was observed following treatment with GW0742 or GW501516, two highly specific PPARbeta/delta ligands. GW 501516 103-111 peroxisome proliferator-activated receptor delta Rattus norvegicus 133-141 20086318-7 2009 Incubation with 500 nM GW501516 (PPARdelta activator) for 24 h significantly decreased GLUT-4 mRNA in L6 myotubes. GW 501516 23-31 solute carrier family 2 member 4 Rattus norvegicus 87-93 19744959-5 2009 GW501516, a PPARbeta/delta agonist, was found to stimulate utrophin A mRNA levels in C2C12 muscle cells through an element in the utrophin A promoter. GW 501516 0-8 peroxisome proliferator activator receptor delta Mus musculus 12-20 19696401-6 2009 Studies in human platelets showed that PKCalpha, which can mediate platelet activation, was bound and repressed by PPARbeta/delta after platelets were treated with GW501516. GW 501516 164-172 protein kinase C alpha Homo sapiens 39-47 19696401-6 2009 Studies in human platelets showed that PKCalpha, which can mediate platelet activation, was bound and repressed by PPARbeta/delta after platelets were treated with GW501516. GW 501516 164-172 peroxisome proliferator activated receptor delta Homo sapiens 115-123 19513536-3 2009 The PPARdelta agonist GW501516 exerted similar effects on protein synthesis to IL15. GW 501516 22-30 peroxisome proliferator activator receptor delta Mus musculus 4-13 19667161-8 2009 GW501516 (PPARdelta ligand) and WY14643 (PPARalpha ligand) both had an antiproliferative effect of approximately 10%. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 10-19 19667161-12 2009 Treatment with GW501516 and WY14643 resulted in an increase in the VDR expression (2-fold after 120 h). GW 501516 15-23 vitamin D receptor Homo sapiens 67-70 19512923-5 2009 A couple of recent studies using the specific PPARdelta agonist GW501516 suggest potent hypolipidaemic actions, presumably caused by enhanced fat oxidation in skeletal muscle. GW 501516 64-72 peroxisome proliferator activated receptor delta Homo sapiens 46-55 19435887-3 2009 In this study, we determined the effect of selective PPARdelta agonism with the synthetic ligand, GW501516, on FAO and mitochondrial gene expression in vitro and in vivo. GW 501516 98-106 peroxisome proliferator activator receptor delta Mus musculus 53-62 19435887-4 2009 Our results show that activation of PPARdelta by GW501516 led to a robust increase in mRNA levels of key lipid metabolism genes. GW 501516 49-57 peroxisome proliferator activator receptor delta Mus musculus 36-45 19461048-6 2009 Administration of a PPARdelta ligand GW501516 to mice also suppressed elastase-induced cell death of aortic VSMCs. GW 501516 37-45 peroxisome proliferator activator receptor delta Mus musculus 20-29 19236478-6 2009 By contrast, a PPARbeta/delta activator (GW501516) normalized only the expression of involucrin and filaggrin but not loricrin. GW 501516 41-49 peroxisome proliferator activator receptor delta Mus musculus 15-23 19389799-4 2009 Using intravital microscopy in the mouse cremasteric microcirculation, we have shown that activation of PPARbeta/delta by its selective ligand GW501516 inhibits TNF-alpha-induced leukocyte rolling flux, adhesion, and emigration in a dose-dependant manner. GW 501516 143-151 peroxisome proliferator activator receptor delta Mus musculus 104-112 19389799-4 2009 Using intravital microscopy in the mouse cremasteric microcirculation, we have shown that activation of PPARbeta/delta by its selective ligand GW501516 inhibits TNF-alpha-induced leukocyte rolling flux, adhesion, and emigration in a dose-dependant manner. GW 501516 143-151 tumor necrosis factor Mus musculus 161-170 19389799-5 2009 Moreover, GW501516 reduced the expression of adhesion molecules such as ICAM-1, VCAM-1, and E-selectin in the cremasteric postcapillary venules. GW 501516 10-18 intercellular adhesion molecule 1 Mus musculus 72-78 19389799-5 2009 Moreover, GW501516 reduced the expression of adhesion molecules such as ICAM-1, VCAM-1, and E-selectin in the cremasteric postcapillary venules. GW 501516 10-18 vascular cell adhesion molecule 1 Mus musculus 80-86 19389799-5 2009 Moreover, GW501516 reduced the expression of adhesion molecules such as ICAM-1, VCAM-1, and E-selectin in the cremasteric postcapillary venules. GW 501516 10-18 selectin, endothelial cell Mus musculus 92-102 19389799-6 2009 Similarly, rolling and adhesion of hPMNs under physiological flow on TNF-alpha-activated HUVECs were also inhibited markedly by GW501516. GW 501516 128-136 tumor necrosis factor Mus musculus 69-78 19389799-7 2009 These inhibitory responses of GW501516 on activated endothelium were accompanied by a reduction in TNF-alpha-induced endothelial GRO-alpha release and VCAM-1, E-selectin, and ICAM-1 mRNA expression. GW 501516 30-38 tumor necrosis factor Mus musculus 99-108 19389799-7 2009 These inhibitory responses of GW501516 on activated endothelium were accompanied by a reduction in TNF-alpha-induced endothelial GRO-alpha release and VCAM-1, E-selectin, and ICAM-1 mRNA expression. GW 501516 30-38 vascular cell adhesion molecule 1 Mus musculus 151-157 19389799-7 2009 These inhibitory responses of GW501516 on activated endothelium were accompanied by a reduction in TNF-alpha-induced endothelial GRO-alpha release and VCAM-1, E-selectin, and ICAM-1 mRNA expression. GW 501516 30-38 selectin, endothelial cell Mus musculus 159-169 19389799-7 2009 These inhibitory responses of GW501516 on activated endothelium were accompanied by a reduction in TNF-alpha-induced endothelial GRO-alpha release and VCAM-1, E-selectin, and ICAM-1 mRNA expression. GW 501516 30-38 intercellular adhesion molecule 1 Mus musculus 175-181 19483413-7 2009 The amino acid(s) that predominantly influence the potency and selectivity of TIPP-204 are different from that of the well-known PPARdelta-selective agonist GW-501516, which belongs to a different chemical class. GW 501516 157-166 peroxisome proliferator activated receptor delta Homo sapiens 129-138 19422681-0 2009 Effects of the PPAR-beta agonist GW501516 in an in vitro model of brain inflammation and antibody-induced demyelination. GW 501516 33-41 peroxisome proliferator-activated receptor delta Rattus norvegicus 15-24 19422681-7 2009 GW 501516, a specific PPAR-beta agonist, was examined for its capacity to protect from antibody-mediated demyelination and to prevent inflammatory responses induced by IFN-gamma and LPS. GW 501516 0-9 peroxisome proliferator-activated receptor delta Rattus norvegicus 22-31 19422681-7 2009 GW 501516, a specific PPAR-beta agonist, was examined for its capacity to protect from antibody-mediated demyelination and to prevent inflammatory responses induced by IFN-gamma and LPS. GW 501516 0-9 interferon gamma Rattus norvegicus 168-177 19422681-11 2009 RESULTS: GW 501516 decreased the IFN-gamma-induced up-regulation of TNF-alpha and iNOS in accord with the proposed anti-inflammatory effects of this PPAR-beta agonist. GW 501516 9-18 interferon gamma Rattus norvegicus 33-42 19422681-11 2009 RESULTS: GW 501516 decreased the IFN-gamma-induced up-regulation of TNF-alpha and iNOS in accord with the proposed anti-inflammatory effects of this PPAR-beta agonist. GW 501516 9-18 tumor necrosis factor Rattus norvegicus 68-77 19422681-11 2009 RESULTS: GW 501516 decreased the IFN-gamma-induced up-regulation of TNF-alpha and iNOS in accord with the proposed anti-inflammatory effects of this PPAR-beta agonist. GW 501516 9-18 nitric oxide synthase 2 Rattus norvegicus 82-86 19422681-11 2009 RESULTS: GW 501516 decreased the IFN-gamma-induced up-regulation of TNF-alpha and iNOS in accord with the proposed anti-inflammatory effects of this PPAR-beta agonist. GW 501516 9-18 peroxisome proliferator-activated receptor delta Rattus norvegicus 149-158 18776129-1 2009 We previously demonstrated that a selective agonist of peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta), GW501516, stimulated human non-small cell lung carcinoma (NSCLC) growth, partly through inhibition of phosphatase and tensin homolog deleted on chromosome 10 expression. GW 501516 127-135 peroxisome proliferator activated receptor delta Homo sapiens 55-108 18776129-1 2009 We previously demonstrated that a selective agonist of peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta), GW501516, stimulated human non-small cell lung carcinoma (NSCLC) growth, partly through inhibition of phosphatase and tensin homolog deleted on chromosome 10 expression. GW 501516 127-135 peroxisome proliferator activated receptor delta Homo sapiens 110-118 18776129-5 2009 Instead, we found that GW501516 stimulated peroxisome proliferator-activated receptor coactivator gamma (PGC)-1alpha, which activated the phosphatidylinositol 3 kinase (PI3-K)/Akt mitogenic pathway. GW 501516 23-31 PPARG coactivator 1 alpha Homo sapiens 54-116 18776129-5 2009 Instead, we found that GW501516 stimulated peroxisome proliferator-activated receptor coactivator gamma (PGC)-1alpha, which activated the phosphatidylinositol 3 kinase (PI3-K)/Akt mitogenic pathway. GW 501516 23-31 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta Homo sapiens 138-167 18776129-5 2009 Instead, we found that GW501516 stimulated peroxisome proliferator-activated receptor coactivator gamma (PGC)-1alpha, which activated the phosphatidylinositol 3 kinase (PI3-K)/Akt mitogenic pathway. GW 501516 23-31 AKT serine/threonine kinase 1 Homo sapiens 176-179 18684227-0 2008 Peroxisome proliferator-activated receptor delta-agonist, GW501516, ameliorates insulin resistance, improves dyslipidaemia in monosodium L-glutamate metabolic syndrome mice. GW 501516 58-66 peroxisome proliferator activator receptor delta Mus musculus 0-48 19347285-5 2009 We have shown that NSCLC cells express PPARbeta/delta protein and that treatment with a selective PPARbeta/delta agonist, GW501516, stimulated the expression of EP4 and induced NSCLC cell proliferation. GW 501516 122-130 peroxisome proliferator activated receptor delta Homo sapiens 39-47 19347285-5 2009 We have shown that NSCLC cells express PPARbeta/delta protein and that treatment with a selective PPARbeta/delta agonist, GW501516, stimulated the expression of EP4 and induced NSCLC cell proliferation. GW 501516 122-130 peroxisome proliferator activated receptor delta Homo sapiens 98-106 19347285-5 2009 We have shown that NSCLC cells express PPARbeta/delta protein and that treatment with a selective PPARbeta/delta agonist, GW501516, stimulated the expression of EP4 and induced NSCLC cell proliferation. GW 501516 122-130 prostaglandin E receptor 4 Homo sapiens 161-164 19266055-0 2009 The PPARdelta ligand GW501516 reduces growth but not apoptosis in mouse inner medullary collecting duct cells. GW 501516 21-29 peroxisome proliferator activator receptor delta Mus musculus 4-13 18636547-6 2008 Overexpression of PPARdelta or treatment with the selective PPARdelta ligand, GW501516, also increased beta-catenin binding to TCF/LEF response element and increased its reporter activity. GW 501516 78-86 peroxisome proliferator activated receptor delta Homo sapiens 18-27 18636547-6 2008 Overexpression of PPARdelta or treatment with the selective PPARdelta ligand, GW501516, also increased beta-catenin binding to TCF/LEF response element and increased its reporter activity. GW 501516 78-86 peroxisome proliferator activated receptor delta Homo sapiens 60-69 18636547-6 2008 Overexpression of PPARdelta or treatment with the selective PPARdelta ligand, GW501516, also increased beta-catenin binding to TCF/LEF response element and increased its reporter activity. GW 501516 78-86 catenin beta 1 Homo sapiens 103-115 18636547-6 2008 Overexpression of PPARdelta or treatment with the selective PPARdelta ligand, GW501516, also increased beta-catenin binding to TCF/LEF response element and increased its reporter activity. GW 501516 78-86 hepatocyte nuclear factor 4 alpha Homo sapiens 127-134 18636547-7 2008 Addition of AA and GW501516 to nuclear extracts induced a comparable degree of beta-catenin binding to TCF/LEF response element. GW 501516 19-27 catenin beta 1 Homo sapiens 79-91 18636547-7 2008 Addition of AA and GW501516 to nuclear extracts induced a comparable degree of beta-catenin binding to TCF/LEF response element. GW 501516 19-27 hepatocyte nuclear factor 4 alpha Homo sapiens 103-110 18687807-5 2008 GW0742 and GW501516 increased expression of known PPARbeta/delta target genes, whereas RA did not; RA increased the expression of known retinoic acid receptor/retinoid X receptor target genes, whereas GW0742 did not affect these genes. GW 501516 11-19 peroxisome proliferator activated receptor delta Homo sapiens 50-58 18511850-7 2008 Impaired tube formation and cell proliferation induced by inactivation of COX-1 were rescued by the treatment with iloprost or the selective peroxisome proliferator-activated receptor (PPAR)delta agonist GW501516 but not by the selective PGI(2) receptor agonist cicaprost. GW 501516 204-212 mitochondrially encoded cytochrome c oxidase I Homo sapiens 74-79 18701481-5 2008 The synthetic PPARdelta agonist GW501516 augmented these PPARdelta proliferation effects in a dose-dependent manner. GW 501516 32-40 peroxisome proliferator activated receptor delta Homo sapiens 14-23 18701481-5 2008 The synthetic PPARdelta agonist GW501516 augmented these PPARdelta proliferation effects in a dose-dependent manner. GW 501516 32-40 peroxisome proliferator activated receptor delta Homo sapiens 57-66 18443198-3 2008 RESEARCH DESIGN AND METHODS AND RESULTS: First, we examined whether the PPARbeta/delta agonist GW501516 prevents lipopolysaccharide (LPS)-induced cytokine production in differentiated 3T3-L1 adipocytes. GW 501516 95-103 peroxisome proliferator-activated receptor delta Rattus norvegicus 72-80 18443198-4 2008 Treatment with GW501516 blocked LPS-induced IL-6 expression and secretion by adipocytes and the subsequent activation of the signal transducer and activator of transcription 3 (STAT3)-Suppressor of cytokine signaling 3 (SOCS3) pathway. GW 501516 15-23 interleukin 6 Rattus norvegicus 44-48 18443198-4 2008 Treatment with GW501516 blocked LPS-induced IL-6 expression and secretion by adipocytes and the subsequent activation of the signal transducer and activator of transcription 3 (STAT3)-Suppressor of cytokine signaling 3 (SOCS3) pathway. GW 501516 15-23 signal transducer and activator of transcription 3 Rattus norvegicus 125-175 18443198-4 2008 Treatment with GW501516 blocked LPS-induced IL-6 expression and secretion by adipocytes and the subsequent activation of the signal transducer and activator of transcription 3 (STAT3)-Suppressor of cytokine signaling 3 (SOCS3) pathway. GW 501516 15-23 signal transducer and activator of transcription 3 Rattus norvegicus 177-182 18443198-4 2008 Treatment with GW501516 blocked LPS-induced IL-6 expression and secretion by adipocytes and the subsequent activation of the signal transducer and activator of transcription 3 (STAT3)-Suppressor of cytokine signaling 3 (SOCS3) pathway. GW 501516 15-23 suppressor of cytokine signaling 3 Rattus norvegicus 184-218 18443198-4 2008 Treatment with GW501516 blocked LPS-induced IL-6 expression and secretion by adipocytes and the subsequent activation of the signal transducer and activator of transcription 3 (STAT3)-Suppressor of cytokine signaling 3 (SOCS3) pathway. GW 501516 15-23 suppressor of cytokine signaling 3 Rattus norvegicus 220-225 18443198-9 2008 Interestingly, GW501516 prevented ERK1/2 phosphorylation by LPS. GW 501516 15-23 mitogen activated protein kinase 3 Rattus norvegicus 34-40 18711014-4 2008 PPAR-delta activation with agonist (GW501516 or L-165041) increased the proliferation of human EPCs and protected them from hypoxia-induced apoptosis. GW 501516 36-44 peroxisome proliferator activated receptor delta Homo sapiens 0-10 18390835-7 2008 Conversely, inhibition of PI3K and silencing of p65 by small RNA interference (siRNA) blocked the effect of GW501516 on PTEN expression and on NSCLC cell proliferation. GW 501516 108-116 phosphatase and tensin homolog Homo sapiens 120-124 18390835-2 2008 We previously demonstrated that a selective PPARbeta/delta agonist, GW501516, stimulated human non-small cell lung carcinoma (NSCLC) cell growth. GW 501516 68-76 peroxisome proliferator activated receptor delta Homo sapiens 44-52 18390835-9 2008 Silencing of IKBalpha enhanced the effect of GW501516 on PTEN protein expression and on cell proliferation. GW 501516 45-53 phosphatase and tensin homolog Homo sapiens 57-61 18390835-4 2008 We show that GW501516 decreased phosphate and tensin homolog deleted on chromosome 10 (PTEN), a tumor suppressor known to decrease cell growth and induce apoptosis. GW 501516 13-21 phosphatase and tensin homolog Homo sapiens 87-91 18390835-10 2008 It also augmented the GW501516-induced complex formation of PPARbeta/delta and p65 proteins. GW 501516 22-30 peroxisome proliferator activated receptor delta Homo sapiens 60-68 18390835-6 2008 GW501516 increased NF-kappaB DNA binding activity and p65 protein expression through activation of PPARbeta/delta and PI3K/Akt signals and enhanced the physical interactions between PPARbeta/delta and p65 protein. GW 501516 0-8 nuclear factor kappa B subunit 1 Homo sapiens 19-28 18390835-10 2008 It also augmented the GW501516-induced complex formation of PPARbeta/delta and p65 proteins. GW 501516 22-30 RELA proto-oncogene, NF-kB subunit Homo sapiens 79-82 18390835-6 2008 GW501516 increased NF-kappaB DNA binding activity and p65 protein expression through activation of PPARbeta/delta and PI3K/Akt signals and enhanced the physical interactions between PPARbeta/delta and p65 protein. GW 501516 0-8 RELA proto-oncogene, NF-kB subunit Homo sapiens 54-57 18390835-11 2008 Overexpression of PTEN suppressed NSCLC cell growth and eliminated the effect of GW501516 on phosphorylation of Akt. GW 501516 81-89 phosphatase and tensin homolog Homo sapiens 18-22 18390835-6 2008 GW501516 increased NF-kappaB DNA binding activity and p65 protein expression through activation of PPARbeta/delta and PI3K/Akt signals and enhanced the physical interactions between PPARbeta/delta and p65 protein. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 99-107 18390835-11 2008 Overexpression of PTEN suppressed NSCLC cell growth and eliminated the effect of GW501516 on phosphorylation of Akt. GW 501516 81-89 AKT serine/threonine kinase 1 Homo sapiens 112-115 18390835-6 2008 GW501516 increased NF-kappaB DNA binding activity and p65 protein expression through activation of PPARbeta/delta and PI3K/Akt signals and enhanced the physical interactions between PPARbeta/delta and p65 protein. GW 501516 0-8 AKT serine/threonine kinase 1 Homo sapiens 123-126 18390835-6 2008 GW501516 increased NF-kappaB DNA binding activity and p65 protein expression through activation of PPARbeta/delta and PI3K/Akt signals and enhanced the physical interactions between PPARbeta/delta and p65 protein. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 182-190 18390835-12 2008 Together, our observations suggest that GW501516 induces the proliferation of NSCLC cells by inhibiting the expression of PTEN through activation of PPARbeta/delta, which stimulates PI3K/Akt and NF-kappaB signaling. GW 501516 40-48 phosphatase and tensin homolog Homo sapiens 122-126 18390835-6 2008 GW501516 increased NF-kappaB DNA binding activity and p65 protein expression through activation of PPARbeta/delta and PI3K/Akt signals and enhanced the physical interactions between PPARbeta/delta and p65 protein. GW 501516 0-8 RELA proto-oncogene, NF-kB subunit Homo sapiens 201-204 18390835-12 2008 Together, our observations suggest that GW501516 induces the proliferation of NSCLC cells by inhibiting the expression of PTEN through activation of PPARbeta/delta, which stimulates PI3K/Akt and NF-kappaB signaling. GW 501516 40-48 peroxisome proliferator activated receptor delta Homo sapiens 149-157 18390835-7 2008 Conversely, inhibition of PI3K and silencing of p65 by small RNA interference (siRNA) blocked the effect of GW501516 on PTEN expression and on NSCLC cell proliferation. GW 501516 108-116 RELA proto-oncogene, NF-kB subunit Homo sapiens 48-51 18390835-12 2008 Together, our observations suggest that GW501516 induces the proliferation of NSCLC cells by inhibiting the expression of PTEN through activation of PPARbeta/delta, which stimulates PI3K/Akt and NF-kappaB signaling. GW 501516 40-48 AKT serine/threonine kinase 1 Homo sapiens 187-190 18390835-12 2008 Together, our observations suggest that GW501516 induces the proliferation of NSCLC cells by inhibiting the expression of PTEN through activation of PPARbeta/delta, which stimulates PI3K/Akt and NF-kappaB signaling. GW 501516 40-48 nuclear factor kappa B subunit 1 Homo sapiens 195-204 18506377-4 2008 Treatment of HepG2 cells with the PPARdelta specific agonist GW501516 increased apoA-II mRNA expression. GW 501516 61-69 peroxisome proliferator activated receptor delta Homo sapiens 34-43 18506377-4 2008 Treatment of HepG2 cells with the PPARdelta specific agonist GW501516 increased apoA-II mRNA expression. GW 501516 61-69 apolipoprotein A2 Homo sapiens 80-87 18506377-5 2008 Likewise, reporter gene assays using a construct containing 2.7 kb of the proximal apoA-II promoter showed increased activity after treatment with GW501516, both in HepG2 and in HuH-7 cells. GW 501516 147-155 apolipoprotein A2 Homo sapiens 83-90 18155554-1 2008 Replacement of the methyl-thiazole moiety of GW501516 (a PPARdelta selective agonist) with [1,2,4]thiadiazole gave compound 21 which unexpectedly displayed submicromolar potency as a partial agonist at PPARalpha in addition to the high potency at PPARdelta. GW 501516 45-53 peroxisome proliferator activated receptor delta Homo sapiens 57-66 18155554-1 2008 Replacement of the methyl-thiazole moiety of GW501516 (a PPARdelta selective agonist) with [1,2,4]thiadiazole gave compound 21 which unexpectedly displayed submicromolar potency as a partial agonist at PPARalpha in addition to the high potency at PPARdelta. GW 501516 45-53 peroxisome proliferator activated receptor alpha Homo sapiens 202-211 18155554-1 2008 Replacement of the methyl-thiazole moiety of GW501516 (a PPARdelta selective agonist) with [1,2,4]thiadiazole gave compound 21 which unexpectedly displayed submicromolar potency as a partial agonist at PPARalpha in addition to the high potency at PPARdelta. GW 501516 45-53 peroxisome proliferator activated receptor delta Homo sapiens 247-256 18007025-4 2008 The PPARdelta activator GW501516 upregulates TGF-beta1 expression in a dose- and time-dependent manner. GW 501516 24-32 peroxisome proliferator activator receptor delta Mus musculus 4-13 18048767-4 2008 METHODS AND RESULTS: In human umbilical vein endothelial cells (HUVECs), the synthetic PPAR-delta ligands GW0742 and GW501516 significantly inhibited tumor necrosis factor (TNF)-alpha-induced expression of vascular cell adhesion molecule-1 and E-selectin (assayed by real-time RT-PCR and Northern blotting), as well as the ensuing endothelial-leukocyte adhesion. GW 501516 117-125 peroxisome proliferator activated receptor delta Homo sapiens 87-97 18048767-4 2008 METHODS AND RESULTS: In human umbilical vein endothelial cells (HUVECs), the synthetic PPAR-delta ligands GW0742 and GW501516 significantly inhibited tumor necrosis factor (TNF)-alpha-induced expression of vascular cell adhesion molecule-1 and E-selectin (assayed by real-time RT-PCR and Northern blotting), as well as the ensuing endothelial-leukocyte adhesion. GW 501516 117-125 tumor necrosis factor Homo sapiens 150-183 18048767-4 2008 METHODS AND RESULTS: In human umbilical vein endothelial cells (HUVECs), the synthetic PPAR-delta ligands GW0742 and GW501516 significantly inhibited tumor necrosis factor (TNF)-alpha-induced expression of vascular cell adhesion molecule-1 and E-selectin (assayed by real-time RT-PCR and Northern blotting), as well as the ensuing endothelial-leukocyte adhesion. GW 501516 117-125 vascular cell adhesion molecule 1 Homo sapiens 206-239 18048767-4 2008 METHODS AND RESULTS: In human umbilical vein endothelial cells (HUVECs), the synthetic PPAR-delta ligands GW0742 and GW501516 significantly inhibited tumor necrosis factor (TNF)-alpha-induced expression of vascular cell adhesion molecule-1 and E-selectin (assayed by real-time RT-PCR and Northern blotting), as well as the ensuing endothelial-leukocyte adhesion. GW 501516 117-125 selectin E Homo sapiens 244-254 18007025-4 2008 The PPARdelta activator GW501516 upregulates TGF-beta1 expression in a dose- and time-dependent manner. GW 501516 24-32 transforming growth factor, beta 1 Mus musculus 45-54 18007025-11 2008 Finally, administration of GW501516 to mice upregulated TGF-beta1, whereas the expression of proinflammatory genes including monocyte chemoattractant protein-1 was significantly attenuated in the thoracic aorta. GW 501516 27-35 transforming growth factor, beta 1 Mus musculus 56-65 18054822-5 2008 Culturing cells in the presence of either GW0742 or GW501516 caused upregulation of the known PPARbeta/delta target gene angiopoietin-like protein 4 (ANGPTL4). GW 501516 52-60 peroxisome proliferator activated receptor delta Homo sapiens 94-102 18024853-7 2008 RESULTS: Treatment with GW501516 showed statistically significant reductions in fasting plasma triglycerides (-30%), apolipoprotein B (-26%), LDL cholesterol (-23%), and insulin (-11%), whereas HDL cholesterol was unchanged. GW 501516 24-32 apolipoprotein B Homo sapiens 117-133 18024853-7 2008 RESULTS: Treatment with GW501516 showed statistically significant reductions in fasting plasma triglycerides (-30%), apolipoprotein B (-26%), LDL cholesterol (-23%), and insulin (-11%), whereas HDL cholesterol was unchanged. GW 501516 24-32 insulin Homo sapiens 170-177 18024853-11 2008 CONCLUSIONS: The PPARdelta agonist GW501516 reverses multiple abnormalities associated with the metabolic syndrome without increasing oxidative stress. GW 501516 35-43 peroxisome proliferator activated receptor delta Homo sapiens 17-26 18054822-5 2008 Culturing cells in the presence of either GW0742 or GW501516 caused upregulation of the known PPARbeta/delta target gene angiopoietin-like protein 4 (ANGPTL4). GW 501516 52-60 angiopoietin like 4 Homo sapiens 150-157 17532641-3 2007 The (S)-enantiomer of a representative compound exhibited extremely potent PPARdelta transactivation activity, comparable with or somewhat superior to that of the known PPARdelta-selective agonist, GW-501516. GW 501516 198-207 peroxisome proliferator activated receptor delta Homo sapiens 169-178 17803688-6 2007 The formation of these apparently aberrant complexes, as well as the ubiquitination and destabilization of PPARbeta, were strongly inhibited by GW501516. GW 501516 144-152 peroxisome proliferator activated receptor delta Homo sapiens 107-115 18047848-8 2007 In the first human study using a PPAR-delta agonist, experimental data obtained with GW 501516 (a highly specific PPAR-delta agonist) suggested that upregulated enzymes critical to fatty acid oxidation in human cells enhanced fatty acid and beta-oxidation in skeletal muscle. GW 501516 85-94 peroxisome proliferator activated receptor delta Homo sapiens 33-43 18047848-8 2007 In the first human study using a PPAR-delta agonist, experimental data obtained with GW 501516 (a highly specific PPAR-delta agonist) suggested that upregulated enzymes critical to fatty acid oxidation in human cells enhanced fatty acid and beta-oxidation in skeletal muscle. GW 501516 85-94 peroxisome proliferator activated receptor delta Homo sapiens 114-124 17869249-0 2007 The PPARdelta agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells. GW 501516 23-31 peroxisome proliferator-activated receptor delta Rattus norvegicus 4-13 17869249-2 2007 Recently, GW501516, a selective PPARdelta agonist, was reported to increase glucose uptake in human skeletal myotubes by an AMPK-dependent mechanism that may contribute to the improved glucose tolerance. GW 501516 10-18 peroxisome proliferator activated receptor delta Homo sapiens 32-41 17869249-3 2007 Here, we demonstrate that whilst GW501516 increases expression of PGC-1alpha and CPT-1 and stimulates fatty-acid oxidation in L6 myotubes, it fails to enhance insulin sensitivity, AMPK activity or glucose uptake and storage. GW 501516 33-41 PPARG coactivator 1 alpha Rattus norvegicus 66-76 17461989-6 2007 Depletion of the PPARdelta receptor, but not of PPARalpha or gamma, attenuated the suppressive effect of GW501516 on interleukin-6-induced alpha1-antichymotrypsin mRNA expression, indicating that PPARdelta specifically mediated this effect. GW 501516 105-113 peroxisome proliferator activated receptor delta Homo sapiens 17-26 17543901-5 2007 Only the PPARdelta ligand GW501516, but not PPARalpha ligand Wy-14,643 or PPARgamma ligand rosiglitazone, significantly increased PPAR-dependent promoter activity and expression of the PPAR-responsive gene UCP2 ( approximately 5-fold). GW 501516 26-34 peroxisome proliferator activated receptor delta Homo sapiens 9-18 17543901-5 2007 Only the PPARdelta ligand GW501516, but not PPARalpha ligand Wy-14,643 or PPARgamma ligand rosiglitazone, significantly increased PPAR-dependent promoter activity and expression of the PPAR-responsive gene UCP2 ( approximately 5-fold). GW 501516 26-34 peroxisome proliferator activated receptor alpha Homo sapiens 9-13 17543901-5 2007 Only the PPARdelta ligand GW501516, but not PPARalpha ligand Wy-14,643 or PPARgamma ligand rosiglitazone, significantly increased PPAR-dependent promoter activity and expression of the PPAR-responsive gene UCP2 ( approximately 5-fold). GW 501516 26-34 uncoupling protein 2 Homo sapiens 206-210 17500064-3 2007 We recently demonstrated that the PPARdelta agonist GW501516 activates AMP-activated protein kinase (AMPK) and stimulates glucose uptake in skeletal muscle. GW 501516 52-60 peroxisome proliferator activated receptor delta Homo sapiens 34-43 17500064-6 2007 Using small interfering RNA, we have demonstrated that PPARdelta expression is required for the effect of GW501516 on the intracellular accumulation of fatty acids. GW 501516 106-114 peroxisome proliferator activated receptor delta Homo sapiens 55-64 17500064-7 2007 Furthermore, we have shown that the subsequent increase in fatty acid oxidation induced by GW501516 is dependent on both PPARdelta and AMPK. GW 501516 91-99 peroxisome proliferator activated receptor delta Homo sapiens 121-130 17500064-8 2007 Concomitant with these metabolic changes, we provide evidence that GW501516 increases the expression of key genes involved in lipid metabolism (FABP3, CPT1, and PDK4) by a PPARdelta-dependent mechanism. GW 501516 67-75 fatty acid binding protein 3 Homo sapiens 144-149 17500064-8 2007 Concomitant with these metabolic changes, we provide evidence that GW501516 increases the expression of key genes involved in lipid metabolism (FABP3, CPT1, and PDK4) by a PPARdelta-dependent mechanism. GW 501516 67-75 carnitine palmitoyltransferase 1A Homo sapiens 151-155 17500064-8 2007 Concomitant with these metabolic changes, we provide evidence that GW501516 increases the expression of key genes involved in lipid metabolism (FABP3, CPT1, and PDK4) by a PPARdelta-dependent mechanism. GW 501516 67-75 pyruvate dehydrogenase kinase 4 Homo sapiens 161-165 17500064-8 2007 Concomitant with these metabolic changes, we provide evidence that GW501516 increases the expression of key genes involved in lipid metabolism (FABP3, CPT1, and PDK4) by a PPARdelta-dependent mechanism. GW 501516 67-75 peroxisome proliferator activated receptor delta Homo sapiens 172-181 17500064-10 2007 In conclusion, the PPARdelta agonist GW501516 promotes changes in lipid/glucose metabolism and gene expression in human skeletal muscle cells by PPARdelta- and AMPK-dependent and -independent mechanisms. GW 501516 37-45 peroxisome proliferator activated receptor delta Homo sapiens 19-28 17500064-10 2007 In conclusion, the PPARdelta agonist GW501516 promotes changes in lipid/glucose metabolism and gene expression in human skeletal muscle cells by PPARdelta- and AMPK-dependent and -independent mechanisms. GW 501516 37-45 peroxisome proliferator activated receptor delta Homo sapiens 145-154 17461989-0 2007 The PPARdelta agonist GW501516 suppresses interleukin-6-mediated hepatocyte acute phase reaction via STAT3 inhibition. GW 501516 22-30 peroxisome proliferator activated receptor delta Homo sapiens 4-13 17461989-0 2007 The PPARdelta agonist GW501516 suppresses interleukin-6-mediated hepatocyte acute phase reaction via STAT3 inhibition. GW 501516 22-30 interleukin 6 Homo sapiens 42-55 17461989-0 2007 The PPARdelta agonist GW501516 suppresses interleukin-6-mediated hepatocyte acute phase reaction via STAT3 inhibition. GW 501516 22-30 signal transducer and activator of transcription 3 Homo sapiens 101-106 17461989-3 2007 MATERIALS AND METHODS: We examined the ability of the synthetic PPARdelta agonist GW501516 to suppress interleukin-6-induced expression of acute phase proteins in human hepatoma HepG2 cells and rat primary hepatocytes. GW 501516 82-90 peroxisome proliferator activated receptor delta Homo sapiens 64-73 17461989-3 2007 MATERIALS AND METHODS: We examined the ability of the synthetic PPARdelta agonist GW501516 to suppress interleukin-6-induced expression of acute phase proteins in human hepatoma HepG2 cells and rat primary hepatocytes. GW 501516 82-90 interleukin 6 Homo sapiens 103-116 17461989-4 2007 Results GW501516 dose-dependently suppressed interleukin-6-induced mRNA expression of the acute phase protein alpha1-antichymotrypsin in HepG2 cells. GW 501516 8-16 interleukin 6 Homo sapiens 45-58 17461989-4 2007 Results GW501516 dose-dependently suppressed interleukin-6-induced mRNA expression of the acute phase protein alpha1-antichymotrypsin in HepG2 cells. GW 501516 8-16 serpin family A member 3 Homo sapiens 110-133 17543901-6 2007 GW501516 reduced the proliferation rate of CF (-38%) and CMF (-26%), which was associated with increased expression of the cell cycle inhibitor gene G0/G1 switch gene 2 (G0S2). GW 501516 0-8 G0/G1 switch 2 Homo sapiens 149-168 17543901-6 2007 GW501516 reduced the proliferation rate of CF (-38%) and CMF (-26%), which was associated with increased expression of the cell cycle inhibitor gene G0/G1 switch gene 2 (G0S2). GW 501516 0-8 G0/G1 switch 2 Homo sapiens 170-174 17461989-6 2007 Depletion of the PPARdelta receptor, but not of PPARalpha or gamma, attenuated the suppressive effect of GW501516 on interleukin-6-induced alpha1-antichymotrypsin mRNA expression, indicating that PPARdelta specifically mediated this effect. GW 501516 105-113 interleukin 6 Homo sapiens 117-130 17461989-6 2007 Depletion of the PPARdelta receptor, but not of PPARalpha or gamma, attenuated the suppressive effect of GW501516 on interleukin-6-induced alpha1-antichymotrypsin mRNA expression, indicating that PPARdelta specifically mediated this effect. GW 501516 105-113 serpin family A member 3 Homo sapiens 139-162 17461989-8 2007 Overexpression of PPARdelta enhanced the suppressive effect of GW501516 on STAT3-activated transcriptional activity of the alpha1-antichymotrypsin promoter, while GW501516 suppressed interleukin-6-induced binding of this transcription factor to this promoter. GW 501516 63-71 peroxisome proliferator activated receptor delta Homo sapiens 18-27 17461989-8 2007 Overexpression of PPARdelta enhanced the suppressive effect of GW501516 on STAT3-activated transcriptional activity of the alpha1-antichymotrypsin promoter, while GW501516 suppressed interleukin-6-induced binding of this transcription factor to this promoter. GW 501516 63-71 signal transducer and activator of transcription 3 Homo sapiens 75-80 17461989-8 2007 Overexpression of PPARdelta enhanced the suppressive effect of GW501516 on STAT3-activated transcriptional activity of the alpha1-antichymotrypsin promoter, while GW501516 suppressed interleukin-6-induced binding of this transcription factor to this promoter. GW 501516 63-71 serpin family A member 3 Homo sapiens 123-146 17461989-8 2007 Overexpression of PPARdelta enhanced the suppressive effect of GW501516 on STAT3-activated transcriptional activity of the alpha1-antichymotrypsin promoter, while GW501516 suppressed interleukin-6-induced binding of this transcription factor to this promoter. GW 501516 163-171 interleukin 6 Homo sapiens 183-196 17346664-4 2007 GW501516, a selective PPARbeta/delta agonist, depressed Ang II-stimulated collagen type I expression and collagen synthesis in cardiac fibroblasts in a concentration-dependent manner. GW 501516 0-8 peroxisome proliferator-activated receptor delta Rattus norvegicus 22-30 17140817-8 2007 PPAR agonists inhibited the stimulating effect of TGF-beta1 by 24-44% on PGs" synthesis and over 75% on aggrecan, GAGs" content and deposition with the following rank order of potency: ROSI>GW501516> or =Wy14643. GW 501516 193-201 peroxisome proliferator activated receptor alpha Rattus norvegicus 0-4 17140817-8 2007 PPAR agonists inhibited the stimulating effect of TGF-beta1 by 24-44% on PGs" synthesis and over 75% on aggrecan, GAGs" content and deposition with the following rank order of potency: ROSI>GW501516> or =Wy14643. GW 501516 193-201 transforming growth factor, beta 1 Rattus norvegicus 50-59 17140817-9 2007 TGF-beta1-induced phosphorylation of Smad2/3 and ERK1/2 was reduced by ROSI over GW501516 but not by Wy14643 whereas stimulated PGE2 production was inhibited by Wy14643 over GW501516 but not by ROSI. GW 501516 81-89 transforming growth factor, beta 1 Rattus norvegicus 0-9 17140817-9 2007 TGF-beta1-induced phosphorylation of Smad2/3 and ERK1/2 was reduced by ROSI over GW501516 but not by Wy14643 whereas stimulated PGE2 production was inhibited by Wy14643 over GW501516 but not by ROSI. GW 501516 174-182 transforming growth factor, beta 1 Rattus norvegicus 0-9 17346664-4 2007 GW501516, a selective PPARbeta/delta agonist, depressed Ang II-stimulated collagen type I expression and collagen synthesis in cardiac fibroblasts in a concentration-dependent manner. GW 501516 0-8 angiotensinogen Rattus norvegicus 56-62 17346664-5 2007 Furthermore, these inhibitory effects of GW501516 were completely reversed by the knockdown of PPARbeta/delta via RNA interference. GW 501516 41-49 peroxisome proliferator-activated receptor delta Rattus norvegicus 95-103 17068288-2 2007 Interestingly, the selective PPARbeta/delta ligand GW501516 is in phase II clinical trials for dyslipidemia. GW 501516 51-59 peroxisome proliferator activated receptor delta Homo sapiens 29-37 17167170-4 2007 In the SH-SY5Y studies, treatment with L-165041 or GW501516 significantly and concentration-dependently attenuated cell death following thapsigargin, 1-methyl-4-phenylpyridinium, or staurosporine exposure, with the extent of damage correlated with the level of caspase-3 inhibition. GW 501516 51-59 caspase 3 Homo sapiens 261-270 17339402-9 2007 In cellular transfection assays, ssPPARbeta1A is activated by monounsaturated fatty acids, 2-bromopalmitate, and mammalian PPARbeta-specific ligand GW501516. GW 501516 148-156 peroxisomal proliferator-activated receptor beta1A Salmo salar 33-45 17339402-9 2007 In cellular transfection assays, ssPPARbeta1A is activated by monounsaturated fatty acids, 2-bromopalmitate, and mammalian PPARbeta-specific ligand GW501516. GW 501516 148-156 peroxisome proliferator activated receptor delta Homo sapiens 35-43 17339402-11 2007 Furthermore, ssPPARbeta2A repressed both the basal reporter gene activity and the GW501516-induced activity of ssPPARbeta1A. GW 501516 82-90 peroxisomal proliferator-activated receptor beta1A Salmo salar 111-123 17243659-5 2007 Modification of the selective PPARdelta agonist 1 (GW501516) so as to incorporate the 2-aryl-2-methylpropionic acid group of the fibrates led to a marked shift in potency and selectivity toward PPARalpha agonism. GW 501516 51-59 peroxisome proliferator activated receptor delta Homo sapiens 30-39 17243659-5 2007 Modification of the selective PPARdelta agonist 1 (GW501516) so as to incorporate the 2-aryl-2-methylpropionic acid group of the fibrates led to a marked shift in potency and selectivity toward PPARalpha agonism. GW 501516 51-59 peroxisome proliferator activated receptor alpha Homo sapiens 194-203 17068288-6 2007 GW501516 induced vascular endothelial cell growth factor mRNA and peptide release, as well as adipose differentiation-related protein (ADRP), a PPARbeta/delta target gene. GW 501516 0-8 perilipin 2 Homo sapiens 135-139 17068288-6 2007 GW501516 induced vascular endothelial cell growth factor mRNA and peptide release, as well as adipose differentiation-related protein (ADRP), a PPARbeta/delta target gene. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 144-158 17068288-7 2007 GW501516-induced proliferation, morphogenesis, vascular endothelial growth factor (VEGF), and ADRP were absent in endothelial cells transfected with dominant-negative PPARbeta/delta. GW 501516 0-8 vascular endothelial growth factor A Homo sapiens 47-81 17068288-7 2007 GW501516-induced proliferation, morphogenesis, vascular endothelial growth factor (VEGF), and ADRP were absent in endothelial cells transfected with dominant-negative PPARbeta/delta. GW 501516 0-8 vascular endothelial growth factor A Homo sapiens 83-87 17068288-7 2007 GW501516-induced proliferation, morphogenesis, vascular endothelial growth factor (VEGF), and ADRP were absent in endothelial cells transfected with dominant-negative PPARbeta/delta. GW 501516 0-8 perilipin 2 Homo sapiens 94-98 17068288-7 2007 GW501516-induced proliferation, morphogenesis, vascular endothelial growth factor (VEGF), and ADRP were absent in endothelial cells transfected with dominant-negative PPARbeta/delta. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 167-175 17068288-8 2007 Furthermore, treatment of cells with cyclo-VEGFI, a VEGF receptor1/2 antagonist, abolished GW501516-induced endothelial cell proliferation and tube formation. GW 501516 91-99 vascular endothelial growth factor A Homo sapiens 43-47 16797985-2 2006 Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARbeta/delta ligand GW501516, the conception of new ligands showing good affinity for PPARbeta/delta is reported. GW 501516 104-112 sarcosine dehydrogenase Homo sapiens 33-36 17178883-3 2006 Activation of PPARdelta by its pharmacologic ligand, GW501516, enhanced the growth of three human HCC cell lines (HuH7, HepG2, and Hep3B), whereas inhibition of PPARdelta by small interfering RNA prevented growth. GW 501516 53-61 peroxisome proliferator activated receptor delta Homo sapiens 14-23 16930961-7 2006 GW501516 and linoleic acid, the well-known ligands of PPARdelta, increased the binding between PPARdelta and co-activators in a ligand dose-dependent manner. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 54-63 16930961-7 2006 GW501516 and linoleic acid, the well-known ligands of PPARdelta, increased the binding between PPARdelta and co-activators in a ligand dose-dependent manner. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 95-104 16960684-1 2006 AIMS/HYPOTHESIS: GW501516, an agonist of peroxisome proliferator-activated receptor-delta (PPAR-delta), increases lipid combustion and exerts antidiabetic action in animals, effects which are attributed mainly to direct effects on skeletal muscle. GW 501516 17-25 peroxisome proliferator-activated receptor delta Rattus norvegicus 41-89 16960684-1 2006 AIMS/HYPOTHESIS: GW501516, an agonist of peroxisome proliferator-activated receptor-delta (PPAR-delta), increases lipid combustion and exerts antidiabetic action in animals, effects which are attributed mainly to direct effects on skeletal muscle. GW 501516 17-25 peroxisome proliferator-activated receptor delta Rattus norvegicus 91-101 16960684-9 2006 CONCLUSIONS/INTERPRETATION: GW501516-induced activation of PPAR-delta reduces glucose utilisation by skeletal muscle through a switch in mitochondrial substrate preference from carbohydrate to lipid. GW 501516 28-36 peroxisome proliferator-activated receptor delta Rattus norvegicus 59-69 17148604-4 2006 Here, we present genetic and pharmacologic evidence demonstrating that deletion of PPARdelta decreases intestinal adenoma growth in Apc(Min/+) mice and inhibits tumor-promoting effects of a PPARdelta agonist GW501516. GW 501516 208-216 peroxisome proliferator activator receptor delta Mus musculus 83-92 17148604-4 2006 Here, we present genetic and pharmacologic evidence demonstrating that deletion of PPARdelta decreases intestinal adenoma growth in Apc(Min/+) mice and inhibits tumor-promoting effects of a PPARdelta agonist GW501516. GW 501516 208-216 peroxisome proliferator activator receptor delta Mus musculus 190-199 16966336-3 2006 Overexpression of PPARdelta or activation of PPARdelta by its pharmacological ligand, GW501516, at low doses (0.5-50 nM) promoted the growth of three human cholangiocarcinoma cell lines (CCLP1, HuCCT1, and SG231). GW 501516 86-94 peroxisome proliferator activated receptor delta Homo sapiens 18-27 16966336-3 2006 Overexpression of PPARdelta or activation of PPARdelta by its pharmacological ligand, GW501516, at low doses (0.5-50 nM) promoted the growth of three human cholangiocarcinoma cell lines (CCLP1, HuCCT1, and SG231). GW 501516 86-94 peroxisome proliferator activated receptor delta Homo sapiens 45-54 16966336-3 2006 Overexpression of PPARdelta or activation of PPARdelta by its pharmacological ligand, GW501516, at low doses (0.5-50 nM) promoted the growth of three human cholangiocarcinoma cell lines (CCLP1, HuCCT1, and SG231). GW 501516 86-94 PPFIA binding protein 2 Homo sapiens 187-192 16797985-2 2006 Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARbeta/delta ligand GW501516, the conception of new ligands showing good affinity for PPARbeta/delta is reported. GW 501516 104-112 peroxisome proliferator activated receptor delta Homo sapiens 82-90 16797985-2 2006 Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARbeta/delta ligand GW501516, the conception of new ligands showing good affinity for PPARbeta/delta is reported. GW 501516 104-112 peroxisome proliferator activated receptor delta Homo sapiens 170-178 16278250-0 2006 PPARdelta activator GW-501516 has no acute effect on glucose transport in skeletal muscle. GW 501516 20-29 peroxisome proliferator activated receptor delta Homo sapiens 0-9 16574099-7 2006 These results suggest that (a) bezafibrate (especially) and GW501516 might improve hepatic steatosis via an improvement in fatty acid beta-oxidation and a direct prevention of inflammation, (b) treatment with a PPARdelta agonist might improve non-alcholic steatohepatitis, (c) bezafibrate may improve non-alcholic steatohepatitis via activation not only of PPARalpha but also of PPARdelta, because bezafibrate is a PPAR pan-agonist. GW 501516 60-68 peroxisome proliferator activator receptor delta Mus musculus 211-220 16574099-7 2006 These results suggest that (a) bezafibrate (especially) and GW501516 might improve hepatic steatosis via an improvement in fatty acid beta-oxidation and a direct prevention of inflammation, (b) treatment with a PPARdelta agonist might improve non-alcholic steatohepatitis, (c) bezafibrate may improve non-alcholic steatohepatitis via activation not only of PPARalpha but also of PPARdelta, because bezafibrate is a PPAR pan-agonist. GW 501516 60-68 peroxisome proliferator activated receptor alpha Mus musculus 211-215 16278250-1 2006 It has been reported that treatment of cultured human skeletal muscle myotubes with the peroxisome proliferator-activated receptor-delta (PPARdelta) activator GW-501516 directly stimulates glucose transport and enhances insulin action. GW 501516 159-168 peroxisome proliferator activated receptor delta Homo sapiens 88-136 16278250-1 2006 It has been reported that treatment of cultured human skeletal muscle myotubes with the peroxisome proliferator-activated receptor-delta (PPARdelta) activator GW-501516 directly stimulates glucose transport and enhances insulin action. GW 501516 159-168 peroxisome proliferator activated receptor delta Homo sapiens 138-147 16278250-8 2006 Treatment of epitrochlearis muscles with GW-501516 for 24 h induced a threefold increase in uncoupling protein-3 mRNA, providing evidence that the GW-501516 compound that we used gets into and is active in skeletal muscle. GW 501516 41-50 uncoupling protein 3 Homo sapiens 92-112 15917308-5 2005 WY14643 (PPARalpha agonist), GW501516 (PPARdelta agonist) and ciglitazone (PPARgamma agonist) were tested for their ability to modulate the behaviour of p53-immortalized liver (PIL) progenitor cell lines in vitro. GW 501516 29-37 transformation related protein 53, pseudogene Mus musculus 153-156 16242326-0 2006 Synthesis of the PPARbeta/delta-selective agonist GW501516 and C4-thiazole-substituted analogs. GW 501516 50-58 peroxisome proliferator activated receptor delta Homo sapiens 17-25 16242326-1 2006 Sequential, position-selective, Pd-catalyzed cross-coupling reactions of 2,4-dibromo-5-hydroxymethylthiazole provided the scaffold for the synthesis of GW501516, the most potent PPARbeta/delta agonist yet described, and equally selective analogs at the thiazole-C4 position. GW 501516 152-160 peroxisome proliferator activated receptor delta Homo sapiens 178-186 16542871-5 2006 Moreover, in the present study, we demonstrated that PPAR beta/delta agonist (GW501516) could inhibit both apoM and apoB expression in the HepG2 cells. GW 501516 78-86 peroxisome proliferator activated receptor delta Homo sapiens 53-62 16542871-5 2006 Moreover, in the present study, we demonstrated that PPAR beta/delta agonist (GW501516) could inhibit both apoM and apoB expression in the HepG2 cells. GW 501516 78-86 apolipoprotein M Homo sapiens 107-111 16542871-5 2006 Moreover, in the present study, we demonstrated that PPAR beta/delta agonist (GW501516) could inhibit both apoM and apoB expression in the HepG2 cells. GW 501516 78-86 apolipoprotein B Homo sapiens 116-120 16337160-5 2006 By performing cell viability assays, we also showed that the selective PPARdelta agonist GW501516 protected cells from H(2)O(2)-induced cell death. GW 501516 89-97 peroxisome proliferator-activated receptor delta Rattus norvegicus 71-80 16337160-6 2006 The protective effect of GW501516 was due to an inhibition of H(2)O(2)-triggered apoptosis as shown by annexin-V labeling, DNA fragmentation analysis, and caspase-3 activity measurement. GW 501516 25-33 annexin A5 Rattus norvegicus 103-112 16337160-6 2006 The protective effect of GW501516 was due to an inhibition of H(2)O(2)-triggered apoptosis as shown by annexin-V labeling, DNA fragmentation analysis, and caspase-3 activity measurement. GW 501516 25-33 caspase 3 Rattus norvegicus 155-164 16337160-7 2006 We demonstrated by transient transfection of a dominant negative mutant of PPARdelta that the protection induced by GW501516 was totally dependent on PPARdelta. GW 501516 116-124 peroxisome proliferator-activated receptor delta Rattus norvegicus 75-84 16337160-7 2006 We demonstrated by transient transfection of a dominant negative mutant of PPARdelta that the protection induced by GW501516 was totally dependent on PPARdelta. GW 501516 116-124 peroxisome proliferator-activated receptor delta Rattus norvegicus 150-159 16337160-8 2006 Semi-quantitative RT-PCR and Western blotting analysis demonstrated that GW501516 treatment upregulated catalase. GW 501516 73-81 catalase Rattus norvegicus 104-112 16061473-5 2005 GW501516 induced NSCLC cell proliferation, and this effect was prevented by PPARbeta/delta antisense or EP4 short interfering RNA (siRNA). GW 501516 0-8 prostaglandin E receptor 4 Homo sapiens 104-107 16061473-4 2005 Our studies show that NSCLC cells express peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) protein and that treatment with a selective PPARbeta/delta agonist (GW501516) increases EP4 mRNA and protein levels. GW 501516 181-189 peroxisome proliferator activated receptor delta Homo sapiens 42-111 16061473-4 2005 Our studies show that NSCLC cells express peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) protein and that treatment with a selective PPARbeta/delta agonist (GW501516) increases EP4 mRNA and protein levels. GW 501516 181-189 peroxisome proliferator activated receptor delta Homo sapiens 97-105 16061473-4 2005 Our studies show that NSCLC cells express peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) protein and that treatment with a selective PPARbeta/delta agonist (GW501516) increases EP4 mRNA and protein levels. GW 501516 181-189 prostaglandin E receptor 4 Homo sapiens 201-204 16061473-5 2005 GW501516 induced NSCLC cell proliferation, and this effect was prevented by PPARbeta/delta antisense or EP4 short interfering RNA (siRNA). GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 76-84 16061473-6 2005 GW501516 increased the phosphorylation of Akt and decreased PTEN expression. GW 501516 0-8 AKT serine/threonine kinase 1 Homo sapiens 42-45 16061473-6 2005 GW501516 increased the phosphorylation of Akt and decreased PTEN expression. GW 501516 0-8 phosphatase and tensin homolog Homo sapiens 60-64 16061473-7 2005 The selective inhibitor of phosphatidylinositol 3-kinase (PI3-K), wortmannin, and PPARbeta/delta antisense, abrogated the effect of GW501516 on EP4 expression, whereas that of the inhibitor of Erk did not. GW 501516 132-140 peroxisome proliferator activated receptor delta Homo sapiens 82-90 16061473-7 2005 The selective inhibitor of phosphatidylinositol 3-kinase (PI3-K), wortmannin, and PPARbeta/delta antisense, abrogated the effect of GW501516 on EP4 expression, whereas that of the inhibitor of Erk did not. GW 501516 132-140 prostaglandin E receptor 4 Homo sapiens 144-147 16061473-8 2005 GW501516 also increased EP4 promoter activity through effects on the region between -1555 and -992 bp in the EP4 promoter, and mutation of the CCAAT/enhancer-binding protein (C/EBP) site in this region abrogated the effect of GW501516. GW 501516 0-8 prostaglandin E receptor 4 Homo sapiens 24-27 16061473-8 2005 GW501516 also increased EP4 promoter activity through effects on the region between -1555 and -992 bp in the EP4 promoter, and mutation of the CCAAT/enhancer-binding protein (C/EBP) site in this region abrogated the effect of GW501516. GW 501516 0-8 prostaglandin E receptor 4 Homo sapiens 109-112 16061473-8 2005 GW501516 also increased EP4 promoter activity through effects on the region between -1555 and -992 bp in the EP4 promoter, and mutation of the CCAAT/enhancer-binding protein (C/EBP) site in this region abrogated the effect of GW501516. GW 501516 226-234 CCAAT enhancer binding protein alpha Homo sapiens 175-180 16061473-9 2005 GW501516 increased not only the binding activity of C/EBP to the NF-IL6 site in the EP4 promoter, which was prevented by the inhibitor of PI3-K, but also increased C/EBPbeta protein in a dose- and PPARbeta/delta-dependent manner. GW 501516 0-8 CCAAT enhancer binding protein alpha Homo sapiens 52-57 16061473-9 2005 GW501516 increased not only the binding activity of C/EBP to the NF-IL6 site in the EP4 promoter, which was prevented by the inhibitor of PI3-K, but also increased C/EBPbeta protein in a dose- and PPARbeta/delta-dependent manner. GW 501516 0-8 prostaglandin E receptor 4 Homo sapiens 84-87 16061473-9 2005 GW501516 increased not only the binding activity of C/EBP to the NF-IL6 site in the EP4 promoter, which was prevented by the inhibitor of PI3-K, but also increased C/EBPbeta protein in a dose- and PPARbeta/delta-dependent manner. GW 501516 0-8 CCAAT enhancer binding protein beta Homo sapiens 164-173 16061473-9 2005 GW501516 increased not only the binding activity of C/EBP to the NF-IL6 site in the EP4 promoter, which was prevented by the inhibitor of PI3-K, but also increased C/EBPbeta protein in a dose- and PPARbeta/delta-dependent manner. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 197-205 16061473-10 2005 The effect of GW501516 on EP4 protein was eliminated in the presence of C/EBPbeta siRNA. GW 501516 14-22 prostaglandin E receptor 4 Homo sapiens 26-29 16061473-10 2005 The effect of GW501516 on EP4 protein was eliminated in the presence of C/EBPbeta siRNA. GW 501516 14-22 CCAAT enhancer binding protein beta Homo sapiens 72-81 16061473-11 2005 Finally, we showed that pretreatment of NSCLC with GW501516 further increased NSCLC cell proliferation in response to exogenous dimethyl-prostaglandin E2 (PGE2) that was diminished in the presence of PPARbeta/delta antisense and EP4 siRNA. GW 501516 51-59 peroxisome proliferator activated receptor delta Homo sapiens 200-208 16061473-11 2005 Finally, we showed that pretreatment of NSCLC with GW501516 further increased NSCLC cell proliferation in response to exogenous dimethyl-prostaglandin E2 (PGE2) that was diminished in the presence of PPARbeta/delta antisense and EP4 siRNA. GW 501516 51-59 prostaglandin E receptor 4 Homo sapiens 229-232 15821150-9 2005 The PPAR-delta ligand GW501516 also inhibited IL-1beta-stimulated PGE(2) production but only at high concentrations (1 microM). GW 501516 22-30 peroxisome proliferator activated receptor delta Homo sapiens 4-14 16115476-9 2005 The considered PPARdelta activator GW501516 and the considered PPARalpha activator fenofibrate also inhibited TNF-alpha-induced VCAM-1 expression, whereas pioglitazone and rosiglitazone did not. GW 501516 35-43 tumor necrosis factor Homo sapiens 110-119 16115476-9 2005 The considered PPARdelta activator GW501516 and the considered PPARalpha activator fenofibrate also inhibited TNF-alpha-induced VCAM-1 expression, whereas pioglitazone and rosiglitazone did not. GW 501516 35-43 vascular cell adhesion molecule 1 Homo sapiens 128-134 15821150-9 2005 The PPAR-delta ligand GW501516 also inhibited IL-1beta-stimulated PGE(2) production but only at high concentrations (1 microM). GW 501516 22-30 interleukin 1 beta Homo sapiens 46-54 15821150-10 2005 IL-1beta-induced nuclear factor-kappaB (NF-kappaB) DNA binding activity was significantly inhibited by 15d-PGJ(2) (10 microM) and GW501516 (1 microM) but increased with 10 microM rosiglitazone. GW 501516 130-138 interleukin 1 beta Homo sapiens 0-8 15821150-10 2005 IL-1beta-induced nuclear factor-kappaB (NF-kappaB) DNA binding activity was significantly inhibited by 15d-PGJ(2) (10 microM) and GW501516 (1 microM) but increased with 10 microM rosiglitazone. GW 501516 130-138 nuclear factor kappa B subunit 1 Homo sapiens 40-49 15764152-5 2005 PPARs were activated by ligands for PPAR alpha (Wy-14643), PPAR delta (GW-501516) and PPAR gamma (rosiglitazone or troglitazone). GW 501516 71-80 peroxisome proliferator activated receptor delta Homo sapiens 59-69 15867396-5 2005 In contrast, animals treated with the PPARdelta agonist GW501516 showed accelerated tumor formation. GW 501516 56-64 peroxisome proliferator activator receptor delta Mus musculus 38-47 15793256-2 2005 Recently, a specific PPARdelta activator (GW501516) was reported to attenuate plasma glucose and insulin levels when administered to genetically obese ob/ob mice. GW 501516 42-50 peroxisome proliferator activator receptor delta Mus musculus 21-30 15793256-2 2005 Recently, a specific PPARdelta activator (GW501516) was reported to attenuate plasma glucose and insulin levels when administered to genetically obese ob/ob mice. GW 501516 42-50 insulin Homo sapiens 97-104 15793256-4 2005 Specific activation of PPARdelta using two pharmacological agonists (GW501516 and GW0742) increased glucose uptake independently of insulin in differentiated C2C12 myotubes. GW 501516 69-77 peroxisome proliferator activated receptor delta Homo sapiens 23-32 15793256-5 2005 In cultured primary human skeletal myotubes, GW501516 increased glucose uptake independently of insulin and enhanced subsequent insulin stimulation. GW 501516 45-53 insulin Homo sapiens 96-103 15793256-5 2005 In cultured primary human skeletal myotubes, GW501516 increased glucose uptake independently of insulin and enhanced subsequent insulin stimulation. GW 501516 45-53 insulin Homo sapiens 128-135 15751073-4 2005 The potency of PPARgamma agonists and the PPARbeta/delta agonist GW-501516 on IL-1Ra levels was tested in the range of 1-10 microM and at 100 pM, respectively. GW 501516 65-74 interleukin 1 receptor antagonist Rattus norvegicus 78-84 15126355-5 2004 Conversely, we have found that several steroid-independent cell lines, including colon lines, were unresponsive to compound F. These findings were confirmed with an additional high-affinity PPARdelta agonist, GW501516. GW 501516 209-217 peroxisome proliferator activated receptor delta Homo sapiens 190-199 15126355-6 2004 Conditional expression of PPARdelta in MCF7 Tet-On cells resulted in a doxycycline-enhanced response to GW501516, thus providing direct genetic evidence for the role of PPARdelta in the proliferative response to this drug. GW 501516 104-112 peroxisome proliferator activated receptor delta Homo sapiens 26-35 15126355-6 2004 Conditional expression of PPARdelta in MCF7 Tet-On cells resulted in a doxycycline-enhanced response to GW501516, thus providing direct genetic evidence for the role of PPARdelta in the proliferative response to this drug. GW 501516 104-112 peroxisome proliferator activated receptor delta Homo sapiens 169-178 15126355-8 2004 Consistent with this hypothesis, we demonstrated a pro-proliferative effect of GW501516 on human umbilical vein endothelial cell cultures and found that GW501516 also regulated the expression of VEGFalpha and FLT-1 in these cells. GW 501516 153-161 vascular endothelial growth factor A Homo sapiens 195-204 15126355-8 2004 Consistent with this hypothesis, we demonstrated a pro-proliferative effect of GW501516 on human umbilical vein endothelial cell cultures and found that GW501516 also regulated the expression of VEGFalpha and FLT-1 in these cells. GW 501516 153-161 fms related receptor tyrosine kinase 1 Homo sapiens 209-214 12699745-3 2003 Optimization of these hits by structure-guided design led to 7k (GW501516) and 7l (GW0742), which shows an EC(50) of 1.1 nM against PPARdelta with 1000-fold selectivity over the other human subtypes. GW 501516 65-73 peroxisome proliferator activated receptor delta Homo sapiens 132-141 14676330-2 2003 Analysis of rat L6 myotubes treated with the PPARdelta subtype-selective agonist, GW501516, by the Affymetrix oligonucleotide microarrays revealed that PPARdelta controls fatty acid oxidation by regulating genes involved in fatty acid transport, beta-oxidation, and mitochondrial respiration. GW 501516 82-90 peroxisome proliferator activator receptor delta Mus musculus 45-54 14676330-2 2003 Analysis of rat L6 myotubes treated with the PPARdelta subtype-selective agonist, GW501516, by the Affymetrix oligonucleotide microarrays revealed that PPARdelta controls fatty acid oxidation by regulating genes involved in fatty acid transport, beta-oxidation, and mitochondrial respiration. GW 501516 82-90 peroxisome proliferator activator receptor delta Mus musculus 152-161 14676330-3 2003 Similar PPARdelta-mediated gene activation was observed in the skeletal muscle of GW501516-treated mice. GW 501516 82-90 peroxisome proliferator activator receptor delta Mus musculus 8-17 12901877-4 2003 In this work, we have studied the effect of PPARdelta activation on COX-2 expression using a selective agonist (GW501516) in human hepatocellular carcinoma (HepG2) cells. GW 501516 112-120 peroxisome proliferator activated receptor delta Homo sapiens 44-53 12901877-4 2003 In this work, we have studied the effect of PPARdelta activation on COX-2 expression using a selective agonist (GW501516) in human hepatocellular carcinoma (HepG2) cells. GW 501516 112-120 prostaglandin-endoperoxide synthase 2 Homo sapiens 68-73 12901877-7 2003 The increased COX-2 protein expression and promoter activity induced by the GW501516 was also confirmed in the monocytic cell line THP-1. GW 501516 76-84 prostaglandin-endoperoxide synthase 2 Homo sapiens 14-19 12901877-7 2003 The increased COX-2 protein expression and promoter activity induced by the GW501516 was also confirmed in the monocytic cell line THP-1. GW 501516 76-84 GLI family zinc finger 2 Homo sapiens 131-136 12901877-10 2003 The levels of PCNA, used as an indicator of cell division were induced, and the cell survival promoting complex p65 (NF-kappaB) was phosphorylated under GW501516 treatment. GW 501516 153-161 proliferating cell nuclear antigen Homo sapiens 14-18 12901877-10 2003 The levels of PCNA, used as an indicator of cell division were induced, and the cell survival promoting complex p65 (NF-kappaB) was phosphorylated under GW501516 treatment. GW 501516 153-161 RELA proto-oncogene, NF-kB subunit Homo sapiens 112-115 12901877-10 2003 The levels of PCNA, used as an indicator of cell division were induced, and the cell survival promoting complex p65 (NF-kappaB) was phosphorylated under GW501516 treatment. GW 501516 153-161 nuclear factor kappa B subunit 1 Homo sapiens 117-126 14758356-2 2004 Exposure of Apc(min) mice to the PPAR-delta ligand GW501516 resulted in a significant increase in the number and size of intestinal polyps. GW 501516 51-59 APC, WNT signaling pathway regulator Mus musculus 12-15 14758356-2 2004 Exposure of Apc(min) mice to the PPAR-delta ligand GW501516 resulted in a significant increase in the number and size of intestinal polyps. GW 501516 51-59 peroxisome proliferator activator receptor delta Mus musculus 33-43 14525954-0 2003 The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. GW 501516 67-75 peroxisome proliferator activated receptor delta Homo sapiens 4-51 14525954-10 2003 Activation of PPARbeta/delta by GW501516 in skeletal muscle cells induces the expression of genes involved in preferential lipid utilization, beta-oxidation, cholesterol efflux, and energy uncoupling. GW 501516 32-40 peroxisome proliferator activated receptor delta Homo sapiens 14-22 14525954-11 2003 Furthermore, we show that treatment of muscle cells with GW501516 increases apolipoprotein-A1 specific efflux of intracellular cholesterol, thus identifying this tissue as an important target of PPARbeta/delta agonists. GW 501516 57-65 apolipoprotein A1 Homo sapiens 76-93 14525954-11 2003 Furthermore, we show that treatment of muscle cells with GW501516 increases apolipoprotein-A1 specific efflux of intracellular cholesterol, thus identifying this tissue as an important target of PPARbeta/delta agonists. GW 501516 57-65 peroxisome proliferator activated receptor delta Homo sapiens 195-203 14604391-0 2003 A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. GW 501516 69-77 peroxisome proliferator activated receptor delta Homo sapiens 86-134 14604391-1 2003 The most potent and selective peroxisome proliferator-activated receptor delta (PPARdelta) agonist GW501516 (1) was synthesized in 4 steps and 78% overall yield starting from o-cresol by using a one-pot regiocontrolled dialkylation of mercaptophenol 5 as the key step. GW 501516 99-107 peroxisome proliferator activated receptor delta Homo sapiens 30-78 14604391-1 2003 The most potent and selective peroxisome proliferator-activated receptor delta (PPARdelta) agonist GW501516 (1) was synthesized in 4 steps and 78% overall yield starting from o-cresol by using a one-pot regiocontrolled dialkylation of mercaptophenol 5 as the key step. GW 501516 99-107 peroxisome proliferator activated receptor delta Homo sapiens 80-89 35624674-5 2022 PPARdelta activation with GW501516, a specific PPARdelta agonist, mitigated 6-OHDA-induced neuronal damage. GW 501516 26-34 peroxisome proliferator activated receptor delta Homo sapiens 0-9 34649350-3 2021 Activation of PPARdelta by the specific ligand GW501516 led to a dose-dependent decrease in ferroptotic cell death triggered by xCT deficiency, along with decreased levels of intracellular iron accumulation and lipid peroxidation. GW 501516 47-55 peroxisome proliferator activator receptor delta Mus musculus 14-23 34649350-4 2021 These effects of GW501516 were abolished by PPARdelta-targeting small interfering RNA (siRNA) and the PPARdelta inhibitor GSK0660, indicating that PPARdelta inhibits xCT deficiency-induced ferroptosis. GW 501516 17-25 peroxisome proliferator activator receptor delta Mus musculus 44-53 34649350-4 2021 These effects of GW501516 were abolished by PPARdelta-targeting small interfering RNA (siRNA) and the PPARdelta inhibitor GSK0660, indicating that PPARdelta inhibits xCT deficiency-induced ferroptosis. GW 501516 17-25 peroxisome proliferator activator receptor delta Mus musculus 102-111 34649350-4 2021 These effects of GW501516 were abolished by PPARdelta-targeting small interfering RNA (siRNA) and the PPARdelta inhibitor GSK0660, indicating that PPARdelta inhibits xCT deficiency-induced ferroptosis. GW 501516 17-25 peroxisome proliferator activator receptor delta Mus musculus 147-156 34649350-5 2021 In addition, GW501516-activated PPARdelta time- and dose-dependently upregulated catalase expression at both the mRNA and protein levels. GW 501516 13-21 peroxisome proliferator activator receptor delta Mus musculus 32-41 34649350-5 2021 In addition, GW501516-activated PPARdelta time- and dose-dependently upregulated catalase expression at both the mRNA and protein levels. GW 501516 13-21 catalase Mus musculus 81-89 34649350-7 2021 Consistently, the effects of GW501516 on ferroptosis of xCT-deficient MEFs were counteracted in the presence of 3-amino-1,2,4-triazole, a specific inhibitor of catalase, suggesting that catalase is essential for the effect of PPARdelta on ferroptosis triggered by xCT deficiency. GW 501516 29-37 catalase Mus musculus 160-168 34649350-7 2021 Consistently, the effects of GW501516 on ferroptosis of xCT-deficient MEFs were counteracted in the presence of 3-amino-1,2,4-triazole, a specific inhibitor of catalase, suggesting that catalase is essential for the effect of PPARdelta on ferroptosis triggered by xCT deficiency. GW 501516 29-37 catalase Mus musculus 186-194 34649350-7 2021 Consistently, the effects of GW501516 on ferroptosis of xCT-deficient MEFs were counteracted in the presence of 3-amino-1,2,4-triazole, a specific inhibitor of catalase, suggesting that catalase is essential for the effect of PPARdelta on ferroptosis triggered by xCT deficiency. GW 501516 29-37 peroxisome proliferator activator receptor delta Mus musculus 226-235 34649350-8 2021 GW501516-activated PPARdelta stabilized peroxisomes through catalase upregulation by targeting peroxisomal hydrogen peroxide-mediated lysosomal rupture, which led to ferroptosis of xCT-deficient MEFs. GW 501516 0-8 peroxisome proliferator activator receptor delta Mus musculus 19-28 34649350-8 2021 GW501516-activated PPARdelta stabilized peroxisomes through catalase upregulation by targeting peroxisomal hydrogen peroxide-mediated lysosomal rupture, which led to ferroptosis of xCT-deficient MEFs. GW 501516 0-8 catalase Mus musculus 60-68 11309497-4 2001 We have used combinatorial chemistry and structure-based drug design to develop a potent and subtype-selective PPARdelta agonist, GW501516. GW 501516 130-138 peroxisome proliferator activated receptor delta Homo sapiens 111-120 11309497-5 2001 In macrophages, fibroblasts, and intestinal cells, GW501516 increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux. GW 501516 51-59 apolipoprotein A1 Homo sapiens 156-173 11309497-6 2001 When dosed to insulin-resistant middle-aged obese rhesus monkeys, GW501516 causes a dramatic dose-dependent rise in serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin. GW 501516 66-74 insulin Macaca mulatta 14-21 11309497-6 2001 When dosed to insulin-resistant middle-aged obese rhesus monkeys, GW501516 causes a dramatic dose-dependent rise in serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin. GW 501516 66-74 insulin Macaca mulatta 260-267 22550474-3 2012 In this paper, treatment of mice conditionally expressing human PPARdelta with GW501516 resulted in a marked loss in body weight that was not evident in nontransgenic animals or animals expressing a dominant negative derivative of PPARdelta. GW 501516 79-87 peroxisome proliferator activated receptor delta Homo sapiens 64-73 22550474-3 2012 In this paper, treatment of mice conditionally expressing human PPARdelta with GW501516 resulted in a marked loss in body weight that was not evident in nontransgenic animals or animals expressing a dominant negative derivative of PPARdelta. GW 501516 79-87 peroxisome proliferator activated receptor delta Homo sapiens 231-240 34678947-0 2021 Peroxisome Proliferator-Activated Receptor Delta Agonist (PPAR- delta) and Selective Androgen Receptor Modulator (SARM) Abuse: Clinical, Analytical and Biological Data in a Case Involving a Poisonous Combination of GW1516 (Cardarine) and MK2866 (Ostarine). GW 501516 215-221 peroxisome proliferator activated receptor delta Homo sapiens 58-69 34678947-0 2021 Peroxisome Proliferator-Activated Receptor Delta Agonist (PPAR- delta) and Selective Androgen Receptor Modulator (SARM) Abuse: Clinical, Analytical and Biological Data in a Case Involving a Poisonous Combination of GW1516 (Cardarine) and MK2866 (Ostarine). GW 501516 223-232 peroxisome proliferator activated receptor delta Homo sapiens 58-69 34678947-2 2021 He claimed having used for some days a combination of GW1516 (cardarine), a peroxisome proliferator-activated receptor delta agonist (PPAR- delta) and MK2866 (ostarine), a selective androgen receptor modulator (SARM) to gain skeletal muscles. GW 501516 54-60 peroxisome proliferator activated receptor delta Homo sapiens 76-124 34678947-2 2021 He claimed having used for some days a combination of GW1516 (cardarine), a peroxisome proliferator-activated receptor delta agonist (PPAR- delta) and MK2866 (ostarine), a selective androgen receptor modulator (SARM) to gain skeletal muscles. GW 501516 54-60 peroxisome proliferator activated receptor delta Homo sapiens 134-145 34420848-4 2021 RESULTS: The PPAR-delta activator GW501516 upregulated expression of catalase and this upregulation was attenuated by PPAR-delta-targeting siRNA. GW 501516 34-42 peroxisome proliferator activated receptor delta Homo sapiens 13-23 34420848-4 2021 RESULTS: The PPAR-delta activator GW501516 upregulated expression of catalase and this upregulation was attenuated by PPAR-delta-targeting siRNA. GW 501516 34-42 catalase Homo sapiens 69-77 34420848-4 2021 RESULTS: The PPAR-delta activator GW501516 upregulated expression of catalase and this upregulation was attenuated by PPAR-delta-targeting siRNA. GW 501516 34-42 peroxisome proliferator activated receptor delta Homo sapiens 118-128 34420848-5 2021 GW501516-activated PPAR-delta induced catalase promoter activity through a direct repeat 1 response element. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 19-29 34420848-5 2021 GW501516-activated PPAR-delta induced catalase promoter activity through a direct repeat 1 response element. GW 501516 0-8 catalase Homo sapiens 38-46 34420848-7 2021 In addition, GW501516-activated PPAR-delta counteracted the reductions in activity and expression of catalase induced by UVB irradiation. GW 501516 13-21 peroxisome proliferator activated receptor delta Homo sapiens 32-42 34420848-7 2021 In addition, GW501516-activated PPAR-delta counteracted the reductions in activity and expression of catalase induced by UVB irradiation. GW 501516 13-21 catalase Homo sapiens 101-109 34420848-9 2021 GW501516-activated PPAR-delta also protected HDFs from cellular damage triggered by UVB irradiation, and this PPAR-delta-mediated reduction of cellular damage was reversed by the catalase inhibitor or catalase-targeting siRNA. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 19-29 34420848-9 2021 GW501516-activated PPAR-delta also protected HDFs from cellular damage triggered by UVB irradiation, and this PPAR-delta-mediated reduction of cellular damage was reversed by the catalase inhibitor or catalase-targeting siRNA. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 110-120 34420848-9 2021 GW501516-activated PPAR-delta also protected HDFs from cellular damage triggered by UVB irradiation, and this PPAR-delta-mediated reduction of cellular damage was reversed by the catalase inhibitor or catalase-targeting siRNA. GW 501516 0-8 catalase Homo sapiens 179-187 34420848-9 2021 GW501516-activated PPAR-delta also protected HDFs from cellular damage triggered by UVB irradiation, and this PPAR-delta-mediated reduction of cellular damage was reversed by the catalase inhibitor or catalase-targeting siRNA. GW 501516 0-8 catalase Homo sapiens 201-209 34420848-11 2021 Furthermore, GW501516-activated PPAR-delta targeted peroxisomal hydrogen peroxide through catalase in UVB-irradiated HDFs. GW 501516 13-21 peroxisome proliferator activated receptor delta Homo sapiens 32-42 34420848-11 2021 Furthermore, GW501516-activated PPAR-delta targeted peroxisomal hydrogen peroxide through catalase in UVB-irradiated HDFs. GW 501516 13-21 catalase Homo sapiens 90-98 34439471-4 2021 Activation of PPARdelta by a specific ligand GW501516 significantly inhibited Ang II-induced hypertrophy and the generation of reactive oxygen species (ROS) in H9c2 cardiomyocytes. GW 501516 45-53 peroxisome proliferator activated receptor delta Homo sapiens 14-23 34439471-4 2021 Activation of PPARdelta by a specific ligand GW501516 significantly inhibited Ang II-induced hypertrophy and the generation of reactive oxygen species (ROS) in H9c2 cardiomyocytes. GW 501516 45-53 angiotensinogen Homo sapiens 78-84 34439471-5 2021 These effects of GW501516 were almost completely abolished in cells stably expressing small hairpin (sh)RNA targeting PPARdelta, indicating that PPARdelta mediates these effects. GW 501516 17-25 peroxisome proliferator activated receptor delta Homo sapiens 118-127 34439471-5 2021 These effects of GW501516 were almost completely abolished in cells stably expressing small hairpin (sh)RNA targeting PPARdelta, indicating that PPARdelta mediates these effects. GW 501516 17-25 peroxisome proliferator activated receptor delta Homo sapiens 145-154 34439471-6 2021 Significant concentration and time-dependent increases in catalase at both mRNA and protein levels were observed in GW501516-treated H9c2 cardiomyocytes. GW 501516 116-124 catalase Homo sapiens 58-66 34439471-7 2021 In addition, GW501516-activated PPARdelta significantly enhanced catalase promoter activity and protein expression, even in the presence of Ang II. GW 501516 13-21 peroxisome proliferator activated receptor delta Homo sapiens 32-41 34439471-7 2021 In addition, GW501516-activated PPARdelta significantly enhanced catalase promoter activity and protein expression, even in the presence of Ang II. GW 501516 13-21 catalase Homo sapiens 65-73 34439471-8 2021 GW501516-activated PPARdelta also inhibited the expression of atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP), which are both marker proteins for hypertrophy. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 19-28 34439471-8 2021 GW501516-activated PPARdelta also inhibited the expression of atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP), which are both marker proteins for hypertrophy. GW 501516 0-8 natriuretic peptide A Homo sapiens 62-88 34439471-8 2021 GW501516-activated PPARdelta also inhibited the expression of atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP), which are both marker proteins for hypertrophy. GW 501516 0-8 natriuretic peptide A Homo sapiens 90-93 34439471-8 2021 GW501516-activated PPARdelta also inhibited the expression of atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP), which are both marker proteins for hypertrophy. GW 501516 0-8 natriuretic peptide B Homo sapiens 99-125 34439471-8 2021 GW501516-activated PPARdelta also inhibited the expression of atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP), which are both marker proteins for hypertrophy. GW 501516 0-8 natriuretic peptide B Homo sapiens 127-130 34439471-9 2021 The effects of GW501516 on the expression of ANP and BNP were reversed by 3-amino-1,2,4-triazole (3-AT), a catalase inhibitor. GW 501516 15-23 natriuretic peptide A Homo sapiens 45-48 34439471-9 2021 The effects of GW501516 on the expression of ANP and BNP were reversed by 3-amino-1,2,4-triazole (3-AT), a catalase inhibitor. GW 501516 15-23 natriuretic peptide B Homo sapiens 53-56 34439471-9 2021 The effects of GW501516 on the expression of ANP and BNP were reversed by 3-amino-1,2,4-triazole (3-AT), a catalase inhibitor. GW 501516 15-23 catalase Homo sapiens 107-115 34439471-11 2021 Furthermore, GW501516-activated PPARdelta exerted catalase-dependent inhibitory effects on Ang II-induced hypertrophy by blocking p38 mitogen-activated protein kinase. GW 501516 13-21 peroxisome proliferator activated receptor delta Homo sapiens 32-41 34439471-11 2021 Furthermore, GW501516-activated PPARdelta exerted catalase-dependent inhibitory effects on Ang II-induced hypertrophy by blocking p38 mitogen-activated protein kinase. GW 501516 13-21 catalase Homo sapiens 50-58 34439471-11 2021 Furthermore, GW501516-activated PPARdelta exerted catalase-dependent inhibitory effects on Ang II-induced hypertrophy by blocking p38 mitogen-activated protein kinase. GW 501516 13-21 angiotensinogen Homo sapiens 91-97 34439471-11 2021 Furthermore, GW501516-activated PPARdelta exerted catalase-dependent inhibitory effects on Ang II-induced hypertrophy by blocking p38 mitogen-activated protein kinase. GW 501516 13-21 mitogen-activated protein kinase 14 Homo sapiens 130-166 35562376-5 2022 Furthermore, PPARdelta ligand activation by a high-fat diet or GW501516 (a highly selective, synthetic PPARdelta ligand) in mutant KRASG12D (KRASmu) pancreatic epithelial cells strongly accelerates PanIN progression to PDAC. GW 501516 63-71 peroxisome proliferator activator receptor delta Mus musculus 13-22 35562376-5 2022 Furthermore, PPARdelta ligand activation by a high-fat diet or GW501516 (a highly selective, synthetic PPARdelta ligand) in mutant KRASG12D (KRASmu) pancreatic epithelial cells strongly accelerates PanIN progression to PDAC. GW 501516 63-71 peroxisome proliferator activator receptor delta Mus musculus 103-112 35624674-5 2022 PPARdelta activation with GW501516, a specific PPARdelta agonist, mitigated 6-OHDA-induced neuronal damage. GW 501516 26-34 peroxisome proliferator activated receptor delta Homo sapiens 47-56 35624674-10 2022 The effects of GW501516 were abrogated by shRNA knockdown of PPARdelta, indicating that the effects of GW501516 were PPARdelta-dependent. GW 501516 15-23 peroxisome proliferator activated receptor delta Homo sapiens 61-70 35624674-10 2022 The effects of GW501516 were abrogated by shRNA knockdown of PPARdelta, indicating that the effects of GW501516 were PPARdelta-dependent. GW 501516 15-23 peroxisome proliferator activated receptor delta Homo sapiens 117-126 35624674-10 2022 The effects of GW501516 were abrogated by shRNA knockdown of PPARdelta, indicating that the effects of GW501516 were PPARdelta-dependent. GW 501516 103-111 peroxisome proliferator activated receptor delta Homo sapiens 61-70 35624674-10 2022 The effects of GW501516 were abrogated by shRNA knockdown of PPARdelta, indicating that the effects of GW501516 were PPARdelta-dependent. GW 501516 103-111 peroxisome proliferator activated receptor delta Homo sapiens 117-126 33319421-1 2021 RATIONALE: The use of GW1516, a peroxisome proliferator-activated receptor delta (PPAR delta) agonist, is strictly prohibited in both horseracing and equestrian competitions. GW 501516 22-28 peroxisome proliferator activated receptor delta Equus caballus 32-80 32703610-4 2021 PPARdelta ligand-activation via oleic acid and GW501516, or overexpression of PPARdelta, elicits profound antitumor actions in neuroblastoma and melanoma. GW 501516 47-55 peroxisome proliferator activator receptor delta Mus musculus 0-9 33470485-1 2021 RATIONALE: GW1516 is a peroxisome proliferator-activated receptor-delta (PPAR-delta) agonist and is banned in horseracing and equestrian sports. GW 501516 11-17 peroxisome proliferator activated receptor delta Equus caballus 23-71 33470485-1 2021 RATIONALE: GW1516 is a peroxisome proliferator-activated receptor-delta (PPAR-delta) agonist and is banned in horseracing and equestrian sports. GW 501516 11-17 peroxisome proliferator activated receptor delta Equus caballus 73-83 32703610-10 2021 In the rotenone PD model in rats, PPARdelta ligand GW501516 saves dopaminergic neurons during injury induced by chemical toxins and improves behavioral functioning in PD via alleviation of endoplasmic reticulum stress. GW 501516 51-59 peroxisome proliferator activator receptor delta Mus musculus 34-43 33319421-1 2021 RATIONALE: The use of GW1516, a peroxisome proliferator-activated receptor delta (PPAR delta) agonist, is strictly prohibited in both horseracing and equestrian competitions. GW 501516 22-28 peroxisome proliferator activated receptor delta Equus caballus 82-92 32776613-1 2020 RATIONALE: GW1516 is a peroxisome proliferator-activated receptor-delta (PPAR-delta) agonist in the class of hormones and metabolic modulators. GW 501516 11-17 peroxisome proliferator activated receptor delta Equus caballus 23-71 33339154-7 2020 The PPARbeta agonist, GW501516 is a strong inducer of pro-resolution substances, derivatives of DHA: 4-HDoHE, 11-HDoHE, 17-HDoHE. GW 501516 22-30 peroxisome proliferator activated receptor alpha Rattus norvegicus 4-12 33339154-9 2020 The PPARbeta agonist GW501516 and the PPARgamma agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFalpha) was more for GW501516. GW 501516 21-29 peroxisome proliferator activated receptor alpha Rattus norvegicus 4-12 33339154-9 2020 The PPARbeta agonist GW501516 and the PPARgamma agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFalpha) was more for GW501516. GW 501516 21-29 interleukin 10 Rattus norvegicus 83-88 33339154-9 2020 The PPARbeta agonist GW501516 and the PPARgamma agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFalpha) was more for GW501516. GW 501516 21-29 interleukin 10 Rattus norvegicus 132-137 33339154-9 2020 The PPARbeta agonist GW501516 and the PPARgamma agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFalpha) was more for GW501516. GW 501516 21-29 interleukin 10 Rattus norvegicus 132-137 33339154-9 2020 The PPARbeta agonist GW501516 and the PPARgamma agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFalpha) was more for GW501516. GW 501516 21-29 tumor necrosis factor Rattus norvegicus 166-174 33339154-9 2020 The PPARbeta agonist GW501516 and the PPARgamma agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFalpha) was more for GW501516. GW 501516 189-197 peroxisome proliferator activated receptor alpha Rattus norvegicus 4-12 33339154-9 2020 The PPARbeta agonist GW501516 and the PPARgamma agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFalpha) was more for GW501516. GW 501516 189-197 peroxisome proliferator-activated receptor gamma Rattus norvegicus 38-47 33339154-9 2020 The PPARbeta agonist GW501516 and the PPARgamma agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFalpha) was more for GW501516. GW 501516 189-197 interleukin 10 Rattus norvegicus 83-88 33339154-10 2020 The PPARbeta ligands, GW501516 and GSK0660, are also the strongest inhibitors of LPS-induced phosphorylation of p38, JNK, ERK MAPKs. GW 501516 22-30 peroxisome proliferator activated receptor alpha Rattus norvegicus 4-12 33339154-10 2020 The PPARbeta ligands, GW501516 and GSK0660, are also the strongest inhibitors of LPS-induced phosphorylation of p38, JNK, ERK MAPKs. GW 501516 22-30 mitogen activated protein kinase 14 Rattus norvegicus 112-115 33339154-10 2020 The PPARbeta ligands, GW501516 and GSK0660, are also the strongest inhibitors of LPS-induced phosphorylation of p38, JNK, ERK MAPKs. GW 501516 22-30 mitogen-activated protein kinase 8 Rattus norvegicus 117-120 33339154-10 2020 The PPARbeta ligands, GW501516 and GSK0660, are also the strongest inhibitors of LPS-induced phosphorylation of p38, JNK, ERK MAPKs. GW 501516 22-30 Eph receptor B1 Rattus norvegicus 122-125 32776613-1 2020 RATIONALE: GW1516 is a peroxisome proliferator-activated receptor-delta (PPAR-delta) agonist in the class of hormones and metabolic modulators. GW 501516 11-17 peroxisome proliferator activated receptor delta Equus caballus 73-83 32669864-0 2020 The Role of PPARdelta Agosnist GW501516 in Rats with Gestational Diabetes Mellitus. GW 501516 31-39 peroxisome proliferator activated receptor delta Homo sapiens 12-21 33308300-4 2020 Calpain-3-deficient mice were also treated with PPAR-delta agonist (GW501516) to assess mitochondrial function and membrane repair. GW 501516 68-76 peroxisome proliferator activator receptor delta Mus musculus 48-58 33308300-11 2020 We used GW501516 to improve mitochondrial biogenesis in vivo in 7-month-old calpain-3-deficient mice. GW 501516 8-16 calpain 3 Mus musculus 76-85 32697599-7 2020 Treatment of primary mouse skeletal muscle cells or C2C12 cells with PPARdelta activators GW501516 and AICAR increased Lin28a expression. GW 501516 90-98 peroxisome proliferator activator receptor delta Mus musculus 69-78 32697599-7 2020 Treatment of primary mouse skeletal muscle cells or C2C12 cells with PPARdelta activators GW501516 and AICAR increased Lin28a expression. GW 501516 90-98 lin-28 homolog A Mus musculus 119-125 32519230-0 2020 Molecular and nanoscale evaluation of N-cadherin expression in invasive bladder cancer cells under control conditions or GW501516 exposure. GW 501516 121-129 cadherin 2 Homo sapiens 38-48 32519230-7 2020 For the first time, we demonstrated by RTqPCR and Western blotting analyses that the peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) agonist GW501516 significantly decreased N-cadherin expression in T24 cells. GW 501516 164-172 peroxisome proliferator activated receptor delta Homo sapiens 85-154 32519230-7 2020 For the first time, we demonstrated by RTqPCR and Western blotting analyses that the peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) agonist GW501516 significantly decreased N-cadherin expression in T24 cells. GW 501516 164-172 cadherin 2 Homo sapiens 197-207 32519230-10 2020 We observed a greater decrease of N-cadherin upon GW501516 exposure with AFM than that detected with molecular biology techniques. GW 501516 50-58 cadherin 2 Homo sapiens 34-44 32519230-12 2020 Taken together, our data suggest that GW501516 could be an interesting therapeutic strategy to avoid bladder cancer cell spreading through N-cadherin decrease. GW 501516 38-46 cadherin 2 Homo sapiens 139-149 32722564-2 2020 After alkali injury, GW501516 (PPARbeta/delta agonist) or vehicle ophthalmic solution was topically instilled onto the rat"s cornea twice a day until day 7. GW 501516 21-29 peroxisome proliferator activated receptor alpha Rattus norvegicus 31-39 32722564-4 2020 GW501516 strongly suppressed infiltration of neutrophils and pan-macrophages, and reduced the mRNA expression of interleukin-6, interleukin-1beta, tumor necrosis factor alpha, and nuclear factor-kappa B. GW 501516 0-8 interleukin 6 Rattus norvegicus 113-126 32722564-4 2020 GW501516 strongly suppressed infiltration of neutrophils and pan-macrophages, and reduced the mRNA expression of interleukin-6, interleukin-1beta, tumor necrosis factor alpha, and nuclear factor-kappa B. GW 501516 0-8 interleukin 1 beta Rattus norvegicus 128-145 32722564-4 2020 GW501516 strongly suppressed infiltration of neutrophils and pan-macrophages, and reduced the mRNA expression of interleukin-6, interleukin-1beta, tumor necrosis factor alpha, and nuclear factor-kappa B. GW 501516 0-8 tumor necrosis factor Rattus norvegicus 147-174 32722564-5 2020 On the other hand, GW501516 promoted infiltration of M2 macrophages, infiltration of vascular endothelial cells associated with neovascularization in the wounded area, and expression of vascular endothelial growth factor A mRNA. GW 501516 19-27 vascular endothelial growth factor A Rattus norvegicus 186-222 32298044-1 2020 GW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-delta) agonist. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 65-113 32298044-1 2020 GW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-delta) agonist. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 115-125 32298044-1 2020 GW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-delta) agonist. GW 501516 24-31 peroxisome proliferator activated receptor delta Homo sapiens 65-113 32298044-1 2020 GW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-delta) agonist. GW 501516 24-31 peroxisome proliferator activated receptor delta Homo sapiens 115-125 32298044-1 2020 GW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-delta) agonist. GW 501516 35-44 peroxisome proliferator activated receptor delta Homo sapiens 65-113 32298044-1 2020 GW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-delta) agonist. GW 501516 35-44 peroxisome proliferator activated receptor delta Homo sapiens 115-125 32669864-10 2020 The biochemical kits were used to detect the expression of lipid metabolism-related factors in blood of GDM rats after the PPARdelta agonist GW501516 treatment. GW 501516 141-149 peroxisome proliferator activated receptor delta Homo sapiens 123-132 32669864-12 2020 Results: The PPARdelta agonist GW501516 decreased the expression of FGB, FINS and HOMA-IR in GDM rats, and we found that GW501516 decreased ISI in GDM rats. GW 501516 31-39 peroxisome proliferator activated receptor delta Homo sapiens 13-22 32669864-12 2020 Results: The PPARdelta agonist GW501516 decreased the expression of FGB, FINS and HOMA-IR in GDM rats, and we found that GW501516 decreased ISI in GDM rats. GW 501516 121-129 peroxisome proliferator activated receptor delta Homo sapiens 13-22 32669864-14 2020 In GDM rats, the expression of PPARdelta in islet decreased and the expression of Angptl8 increased, which was reversed by GW501516. GW 501516 123-131 peroxisome proliferator activated receptor delta Homo sapiens 31-40 32669864-14 2020 In GDM rats, the expression of PPARdelta in islet decreased and the expression of Angptl8 increased, which was reversed by GW501516. GW 501516 123-131 angiopoietin-like 8 Rattus norvegicus 82-89 32669864-16 2020 Finally, we found that GW501516 inhibited the expression of SREBP-1c and promoted the expression of GLUT2 in the islet tissue. GW 501516 23-31 sterol regulatory element binding transcription factor 1 Rattus norvegicus 60-68 32669864-16 2020 Finally, we found that GW501516 inhibited the expression of SREBP-1c and promoted the expression of GLUT2 in the islet tissue. GW 501516 23-31 solute carrier family 2 member 2 Rattus norvegicus 100-105 32669864-17 2020 Conclusion: The PPARdelta agonist GW501516 could improve the blood glucose level, damaged islet tissue and increase the insulin content in the rats with GDM, possibly by regulating the SREBP-1c/GLUT2 pathway. GW 501516 34-42 peroxisome proliferator activated receptor delta Homo sapiens 16-25 32669864-17 2020 Conclusion: The PPARdelta agonist GW501516 could improve the blood glucose level, damaged islet tissue and increase the insulin content in the rats with GDM, possibly by regulating the SREBP-1c/GLUT2 pathway. GW 501516 34-42 sterol regulatory element binding transcription factor 1 Rattus norvegicus 185-193 32669864-17 2020 Conclusion: The PPARdelta agonist GW501516 could improve the blood glucose level, damaged islet tissue and increase the insulin content in the rats with GDM, possibly by regulating the SREBP-1c/GLUT2 pathway. GW 501516 34-42 solute carrier family 2 member 2 Rattus norvegicus 194-199 32669864-18 2020 Our study provided a new basis for clinical treatment of GDM in pregnant women with PPARdelta agonist GW501516. GW 501516 102-110 peroxisome proliferator activated receptor delta Homo sapiens 84-93 31364177-1 2019 GW501516-activated peroxisome proliferator-activated receptor (PPAR) beta/delta and G-protein-coupled receptor (GPR) 40 were shown to protect pancreatic beta cells against lipoapoptosis. GW 501516 0-8 peroxisome proliferator-activated receptor delta Rattus norvegicus 19-79 33318871-9 2021 PPARdelta agonist GW501516 offered protections similar to NaHS in PPG treated VSMCs. GW 501516 18-26 peroxisome proliferator activator receptor delta Mus musculus 0-9 33318871-10 2021 Aggravated active and passive contraction in PPG mice aortas, upregulated p-STAT3 and inflammatory molecules, downregulated SOCS3 and phenotype transformation in PPG treated VSMCs could be corrected by PPARdelta agonist GW501516 treatment. GW 501516 220-228 suppressor of cytokine signaling 3 Mus musculus 124-129 33318871-10 2021 Aggravated active and passive contraction in PPG mice aortas, upregulated p-STAT3 and inflammatory molecules, downregulated SOCS3 and phenotype transformation in PPG treated VSMCs could be corrected by PPARdelta agonist GW501516 treatment. GW 501516 220-228 peroxisome proliferator activator receptor delta Mus musculus 202-211 33318871-11 2021 On the contrary, PPARdelta antagonist GSK0660 exhibited opposite effects on vascular contraction in aortas, expressions of p-STAT3 and SOCS3 in VSMCs compared with GW501516. GW 501516 164-172 peroxisome proliferator activator receptor delta Mus musculus 17-26 32143325-4 2020 Using PPARbeta/delta agonist GW501516 upregulates FoxA2, which in turn, attenuates the production of proinflammatory cytokines and reduces the infiltration of CD45+ immune cells in two mouse models of muscle inflammation, systemic LPS and intramuscular injection of carrageenan, which mimic localized exercise-induced inflammation. GW 501516 29-37 peroxisome proliferator activated receptor alpha Mus musculus 6-20 32143325-4 2020 Using PPARbeta/delta agonist GW501516 upregulates FoxA2, which in turn, attenuates the production of proinflammatory cytokines and reduces the infiltration of CD45+ immune cells in two mouse models of muscle inflammation, systemic LPS and intramuscular injection of carrageenan, which mimic localized exercise-induced inflammation. GW 501516 29-37 forkhead box A2 Mus musculus 50-55 32143325-6 2020 In line with these results, a deficiency in either PPARbeta/delta or FoxA2 diminishes the action of the PPARbeta/delta agonist GW501516 to suppress an aggravated inflammatory response. GW 501516 127-135 peroxisome proliferator activated receptor alpha Mus musculus 51-65 32143325-6 2020 In line with these results, a deficiency in either PPARbeta/delta or FoxA2 diminishes the action of the PPARbeta/delta agonist GW501516 to suppress an aggravated inflammatory response. GW 501516 127-135 forkhead box A2 Mus musculus 69-74 32143325-6 2020 In line with these results, a deficiency in either PPARbeta/delta or FoxA2 diminishes the action of the PPARbeta/delta agonist GW501516 to suppress an aggravated inflammatory response. GW 501516 127-135 peroxisome proliferator activated receptor alpha Mus musculus 51-59 31796534-2 2020 Here, we demonstrate that SOX9 was dramatically induced by stably expressing PPARdelta and by its agonist GW501516 in human GC cell lines. GW 501516 106-114 SRY-box transcription factor 9 Homo sapiens 26-30 31364177-5 2019 HFD aggravated GK rats" poorer INSR30, lower mass, greater apoptosis of beta cells, lower mass, and lower expression of GPR40, which were similarly improved by GW501516 at 3 or 6 mg/kg day and pioglitazone. GW 501516 160-168 free fatty acid receptor 1 Rattus norvegicus 120-125 31364177-7 2019 GW501516 protected INS-1 cells from PAM-induced apoptosis by upregulating GPR40 and activating Akt/Bcl-2/caspase-3. GW 501516 0-8 free fatty acid receptor 1 Rattus norvegicus 74-79 31364177-7 2019 GW501516 protected INS-1 cells from PAM-induced apoptosis by upregulating GPR40 and activating Akt/Bcl-2/caspase-3. GW 501516 0-8 AKT serine/threonine kinase 1 Rattus norvegicus 95-98 32238697-8 2020 CBDA inhibits PPARbeta/delta-mediated transcriptional activation stimulated by the PPARbeta/delta-specific agonist, GW501516. GW 501516 116-124 peroxisome proliferator activated receptor alpha Homo sapiens 14-22 32238697-8 2020 CBDA inhibits PPARbeta/delta-mediated transcriptional activation stimulated by the PPARbeta/delta-specific agonist, GW501516. GW 501516 116-124 peroxisome proliferator activated receptor alpha Homo sapiens 14-28 32238697-9 2020 Furthermore, the disappearance of cellular actin stress fibers, a hallmark of PPARbeta/delta and COX-2 pathway activation, as evoked by the GW501516, was effectively reversed by CBDA. GW 501516 140-148 peroxisome proliferator activated receptor alpha Homo sapiens 78-92 32238697-9 2020 Furthermore, the disappearance of cellular actin stress fibers, a hallmark of PPARbeta/delta and COX-2 pathway activation, as evoked by the GW501516, was effectively reversed by CBDA. GW 501516 140-148 prostaglandin-endoperoxide synthase 2 Homo sapiens 97-102 31063584-4 2019 The activation of PPARdelta by GW501516, a specific PPARdelta agonist, inhibited expression of BACE1. GW 501516 31-39 peroxisome proliferator activated receptor delta Homo sapiens 18-27 31063584-4 2019 The activation of PPARdelta by GW501516, a specific PPARdelta agonist, inhibited expression of BACE1. GW 501516 31-39 peroxisome proliferator activated receptor delta Homo sapiens 52-61 31063584-4 2019 The activation of PPARdelta by GW501516, a specific PPARdelta agonist, inhibited expression of BACE1. GW 501516 31-39 beta-secretase 1 Homo sapiens 95-100 31063584-5 2019 This effect was abrogated by shRNA-mediated knockdown of PPARdelta and by treatment with the PPARdelta antagonist GSK0660, indicating that PPARdelta is involved in GW501516-mediated suppression of BACE1 expression. GW 501516 164-172 peroxisome proliferator activated receptor delta Homo sapiens 57-66 31063584-5 2019 This effect was abrogated by shRNA-mediated knockdown of PPARdelta and by treatment with the PPARdelta antagonist GSK0660, indicating that PPARdelta is involved in GW501516-mediated suppression of BACE1 expression. GW 501516 164-172 peroxisome proliferator activated receptor delta Homo sapiens 93-102 31063584-5 2019 This effect was abrogated by shRNA-mediated knockdown of PPARdelta and by treatment with the PPARdelta antagonist GSK0660, indicating that PPARdelta is involved in GW501516-mediated suppression of BACE1 expression. GW 501516 164-172 peroxisome proliferator activated receptor delta Homo sapiens 93-102 31063584-5 2019 This effect was abrogated by shRNA-mediated knockdown of PPARdelta and by treatment with the PPARdelta antagonist GSK0660, indicating that PPARdelta is involved in GW501516-mediated suppression of BACE1 expression. GW 501516 164-172 beta-secretase 1 Homo sapiens 197-202 31063584-6 2019 On the other hand, GW501516-activated PPARdelta induced expression of SOCS1, which is a negative regulator of cytokine signal transduction, at the transcriptional level by binding to a PPAR response element in its promoter. GW 501516 19-27 peroxisome proliferator activated receptor delta Homo sapiens 38-47 31063584-6 2019 On the other hand, GW501516-activated PPARdelta induced expression of SOCS1, which is a negative regulator of cytokine signal transduction, at the transcriptional level by binding to a PPAR response element in its promoter. GW 501516 19-27 suppressor of cytokine signaling 1 Homo sapiens 70-75 31063584-6 2019 On the other hand, GW501516-activated PPARdelta induced expression of SOCS1, which is a negative regulator of cytokine signal transduction, at the transcriptional level by binding to a PPAR response element in its promoter. GW 501516 19-27 peroxisome proliferator activated receptor alpha Homo sapiens 38-42 31063584-7 2019 This GW501516-mediated induction of SOCS1 expression led to down-regulation of BACE1 expression via inactivation of signal transducer and activator of transcription 1. GW 501516 5-13 suppressor of cytokine signaling 1 Homo sapiens 36-41 31063584-7 2019 This GW501516-mediated induction of SOCS1 expression led to down-regulation of BACE1 expression via inactivation of signal transducer and activator of transcription 1. GW 501516 5-13 beta-secretase 1 Homo sapiens 79-84 31063584-7 2019 This GW501516-mediated induction of SOCS1 expression led to down-regulation of BACE1 expression via inactivation of signal transducer and activator of transcription 1. GW 501516 5-13 signal transducer and activator of transcription 1 Homo sapiens 116-166 31063584-8 2019 GW501516-activated PPARdelta suppressed the generation of neurotoxic amyloid beta (Abeta) in accordance with the decrease in BACE1 expression. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 19-28 31063584-8 2019 GW501516-activated PPARdelta suppressed the generation of neurotoxic amyloid beta (Abeta) in accordance with the decrease in BACE1 expression. GW 501516 0-8 amyloid beta precursor protein Homo sapiens 69-81 31063584-8 2019 GW501516-activated PPARdelta suppressed the generation of neurotoxic amyloid beta (Abeta) in accordance with the decrease in BACE1 expression. GW 501516 0-8 beta-secretase 1 Homo sapiens 125-130 31364177-7 2019 GW501516 protected INS-1 cells from PAM-induced apoptosis by upregulating GPR40 and activating Akt/Bcl-2/caspase-3. GW 501516 0-8 BCL2, apoptosis regulator Rattus norvegicus 99-104 31364177-7 2019 GW501516 protected INS-1 cells from PAM-induced apoptosis by upregulating GPR40 and activating Akt/Bcl-2/caspase-3. GW 501516 0-8 caspase 3 Rattus norvegicus 105-114 31364177-9 2019 These results showed that the PPARbeta/delta agonist GW501516 protected beta cells from lipoapoptosis and improved beta cell mass by upregulating GPR40 and activating the Akt/Bcl-2/caspase-3 pathway, but not the ERK-signaling pathway. GW 501516 53-61 peroxisome proliferator activated receptor alpha Rattus norvegicus 30-44 31364177-9 2019 These results showed that the PPARbeta/delta agonist GW501516 protected beta cells from lipoapoptosis and improved beta cell mass by upregulating GPR40 and activating the Akt/Bcl-2/caspase-3 pathway, but not the ERK-signaling pathway. GW 501516 53-61 free fatty acid receptor 1 Rattus norvegicus 146-151 31364177-9 2019 These results showed that the PPARbeta/delta agonist GW501516 protected beta cells from lipoapoptosis and improved beta cell mass by upregulating GPR40 and activating the Akt/Bcl-2/caspase-3 pathway, but not the ERK-signaling pathway. GW 501516 53-61 AKT serine/threonine kinase 1 Rattus norvegicus 171-174 31364177-9 2019 These results showed that the PPARbeta/delta agonist GW501516 protected beta cells from lipoapoptosis and improved beta cell mass by upregulating GPR40 and activating the Akt/Bcl-2/caspase-3 pathway, but not the ERK-signaling pathway. GW 501516 53-61 BCL2, apoptosis regulator Rattus norvegicus 175-180 31364177-9 2019 These results showed that the PPARbeta/delta agonist GW501516 protected beta cells from lipoapoptosis and improved beta cell mass by upregulating GPR40 and activating the Akt/Bcl-2/caspase-3 pathway, but not the ERK-signaling pathway. GW 501516 53-61 caspase 3 Rattus norvegicus 181-190 31364177-9 2019 These results showed that the PPARbeta/delta agonist GW501516 protected beta cells from lipoapoptosis and improved beta cell mass by upregulating GPR40 and activating the Akt/Bcl-2/caspase-3 pathway, but not the ERK-signaling pathway. GW 501516 53-61 Eph receptor B1 Rattus norvegicus 212-215 31364177-1 2019 GW501516-activated peroxisome proliferator-activated receptor (PPAR) beta/delta and G-protein-coupled receptor (GPR) 40 were shown to protect pancreatic beta cells against lipoapoptosis. GW 501516 0-8 free fatty acid receptor 1 Rattus norvegicus 84-119 31150647-2 2019 Here we found that PPARdelta agonist GW501516 significantly increased Glut1 (Glucose transporter 1) and SLC1A5 (solutecarrier family 1 member 5) gene and protein expressions in HCT-116, SW480, HeLa, and MCF-7 cancer cell lines, while metformin inhibited this event, which was associated with metformin-mediated inhibition of PPARdelta activity in response to GW501516. GW 501516 37-45 peroxisome proliferator activated receptor delta Homo sapiens 19-28 31150647-2 2019 Here we found that PPARdelta agonist GW501516 significantly increased Glut1 (Glucose transporter 1) and SLC1A5 (solutecarrier family 1 member 5) gene and protein expressions in HCT-116, SW480, HeLa, and MCF-7 cancer cell lines, while metformin inhibited this event, which was associated with metformin-mediated inhibition of PPARdelta activity in response to GW501516. GW 501516 37-45 solute carrier family 2 member 1 Homo sapiens 70-75 31150647-5 2019 These findings suggest that metformin inhibited PPARdelta agonist GW501516-induced cancer cell metabolism and tumor growth. GW 501516 66-74 peroxisome proliferator activated receptor delta Homo sapiens 48-57 31150647-2 2019 Here we found that PPARdelta agonist GW501516 significantly increased Glut1 (Glucose transporter 1) and SLC1A5 (solutecarrier family 1 member 5) gene and protein expressions in HCT-116, SW480, HeLa, and MCF-7 cancer cell lines, while metformin inhibited this event, which was associated with metformin-mediated inhibition of PPARdelta activity in response to GW501516. GW 501516 37-45 solute carrier family 2 member 1 Homo sapiens 77-98 31150647-2 2019 Here we found that PPARdelta agonist GW501516 significantly increased Glut1 (Glucose transporter 1) and SLC1A5 (solutecarrier family 1 member 5) gene and protein expressions in HCT-116, SW480, HeLa, and MCF-7 cancer cell lines, while metformin inhibited this event, which was associated with metformin-mediated inhibition of PPARdelta activity in response to GW501516. GW 501516 37-45 solute carrier family 1 member 5 Homo sapiens 104-110 31150647-2 2019 Here we found that PPARdelta agonist GW501516 significantly increased Glut1 (Glucose transporter 1) and SLC1A5 (solutecarrier family 1 member 5) gene and protein expressions in HCT-116, SW480, HeLa, and MCF-7 cancer cell lines, while metformin inhibited this event, which was associated with metformin-mediated inhibition of PPARdelta activity in response to GW501516. GW 501516 37-45 solute carrier family 1 member 5 Homo sapiens 112-143 31150647-2 2019 Here we found that PPARdelta agonist GW501516 significantly increased Glut1 (Glucose transporter 1) and SLC1A5 (solutecarrier family 1 member 5) gene and protein expressions in HCT-116, SW480, HeLa, and MCF-7 cancer cell lines, while metformin inhibited this event, which was associated with metformin-mediated inhibition of PPARdelta activity in response to GW501516. GW 501516 37-45 peroxisome proliferator activated receptor delta Homo sapiens 325-334 31150647-2 2019 Here we found that PPARdelta agonist GW501516 significantly increased Glut1 (Glucose transporter 1) and SLC1A5 (solutecarrier family 1 member 5) gene and protein expressions in HCT-116, SW480, HeLa, and MCF-7 cancer cell lines, while metformin inhibited this event, which was associated with metformin-mediated inhibition of PPARdelta activity in response to GW501516. GW 501516 359-367 peroxisome proliferator activated receptor delta Homo sapiens 19-28 31150647-3 2019 Importantly, GW501516 inhibited the binding of PPARdelta to AMPK, while metformin reversed this process. GW 501516 13-21 peroxisome proliferator activated receptor delta Homo sapiens 47-56 30982495-0 2019 PPARbeta/delta Agonist GW501516 Inhibits Tumorigenesis and Promotes Apoptosis of the Undifferentiated Nasopharyngeal Carcinoma C666-1 Cells by Regulating miR-206. GW 501516 23-31 peroxisome proliferator activated receptor delta Homo sapiens 0-8 30982495-0 2019 PPARbeta/delta Agonist GW501516 Inhibits Tumorigenesis and Promotes Apoptosis of the Undifferentiated Nasopharyngeal Carcinoma C666-1 Cells by Regulating miR-206. GW 501516 23-31 microRNA 206 Homo sapiens 154-161 30982495-1 2019 In previous investigations, we reported that peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) activation by GW501516 inhibits proliferation and promotes apoptosis in the undifferentiated C666-1 nasopharyngeal carcinoma (NPC) cells by modulating caspase-dependent apoptotic pathway. GW 501516 130-138 peroxisome proliferator activated receptor delta Homo sapiens 45-98 30982495-1 2019 In previous investigations, we reported that peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta) activation by GW501516 inhibits proliferation and promotes apoptosis in the undifferentiated C666-1 nasopharyngeal carcinoma (NPC) cells by modulating caspase-dependent apoptotic pathway. GW 501516 130-138 peroxisome proliferator activated receptor delta Homo sapiens 100-108 30982495-3 2019 Among the assayed miRNAs that were involved in regulating the expression of antiapoptotic protein Bcl-2, miR-206 was increased significantly and specifically by GW501516 in C666-1 cells at both the in vitro level and at the in vivo xenograft samples. GW 501516 161-169 BCL2 apoptosis regulator Homo sapiens 98-103 30982495-3 2019 Among the assayed miRNAs that were involved in regulating the expression of antiapoptotic protein Bcl-2, miR-206 was increased significantly and specifically by GW501516 in C666-1 cells at both the in vitro level and at the in vivo xenograft samples. GW 501516 161-169 microRNA 206 Homo sapiens 105-112 30982495-4 2019 The induction on miR-206 expression caused by GW501516 was capable of being antagonized by the PPARbeta/delta antagonist GSK3787 and AMPK antagonist dorsomorphin in C666-1 cells. GW 501516 46-54 microRNA 206 Homo sapiens 17-24 30982495-4 2019 The induction on miR-206 expression caused by GW501516 was capable of being antagonized by the PPARbeta/delta antagonist GSK3787 and AMPK antagonist dorsomorphin in C666-1 cells. GW 501516 46-54 peroxisome proliferator activated receptor delta Homo sapiens 95-103 30982495-4 2019 The induction on miR-206 expression caused by GW501516 was capable of being antagonized by the PPARbeta/delta antagonist GSK3787 and AMPK antagonist dorsomorphin in C666-1 cells. GW 501516 46-54 protein kinase AMP-activated non-catalytic subunit beta 1 Homo sapiens 133-137 30982495-5 2019 GW501516"s suppression on the growth and apoptosis of C666-1 cells was found to be dependent on the presence of miR-206. GW 501516 0-8 microRNA 206 Homo sapiens 112-119 30982495-9 2019 Taken together, the current data demonstrated that miR-206 plays a critical role in the direct apoptosis-promoting effect induced by GW501516 in C666-1 cells. GW 501516 133-141 microRNA 206 Homo sapiens 51-58 30739791-7 2019 GW501516 treatment increased the expression of insulin receptor and inhibited TNFalpha-mediated repression of insulin receptor. GW 501516 0-8 insulin receptor Homo sapiens 110-126 31384284-5 2019 Results: Our data showed that palmitate and PPAR agonists including WY14643 (PPARalpha), GW501516 (PPARbeta/delta), rosiglitazone (PPARgamma) in vitro all induced PLIN5 expression in INS-1 cells. GW 501516 89-97 peroxisome proliferator activated receptor alpha Rattus norvegicus 44-48 31384284-5 2019 Results: Our data showed that palmitate and PPAR agonists including WY14643 (PPARalpha), GW501516 (PPARbeta/delta), rosiglitazone (PPARgamma) in vitro all induced PLIN5 expression in INS-1 cells. GW 501516 89-97 peroxisome proliferator-activated receptor delta Rattus norvegicus 99-107 31384284-5 2019 Results: Our data showed that palmitate and PPAR agonists including WY14643 (PPARalpha), GW501516 (PPARbeta/delta), rosiglitazone (PPARgamma) in vitro all induced PLIN5 expression in INS-1 cells. GW 501516 89-97 perilipin 5 Rattus norvegicus 163-168 30739791-0 2019 PPARbeta/delta agonist GW501516 inhibits TNFalpha-induced repression of adiponectin and insulin receptor in 3T3-L1 adipocytes. GW 501516 23-31 peroxisome proliferator activated receptor delta Homo sapiens 0-8 31144304-9 2019 KEY RESULTS: The PPARdelta agonist GW501516 increased DHFR and BH4 levels in endothelial cells (ECs). GW 501516 35-43 peroxisome proliferator activator receptor delta Mus musculus 17-26 31144304-9 2019 KEY RESULTS: The PPARdelta agonist GW501516 increased DHFR and BH4 levels in endothelial cells (ECs). GW 501516 35-43 dihydrofolate reductase Mus musculus 54-58 31153636-7 2019 PPAR-delta agonist GW501516 partially rescued the insulin resistance induced by miR-29a. GW 501516 19-27 peroxisome proliferator activator receptor delta Mus musculus 0-10 31153636-7 2019 PPAR-delta agonist GW501516 partially rescued the insulin resistance induced by miR-29a. GW 501516 19-27 microRNA 29a Mus musculus 80-87 30739791-8 2019 Our results showed that GW501516 abrogated TNFalpha-induced insulin resistance. GW 501516 24-32 tumor necrosis factor Homo sapiens 43-51 30739791-0 2019 PPARbeta/delta agonist GW501516 inhibits TNFalpha-induced repression of adiponectin and insulin receptor in 3T3-L1 adipocytes. GW 501516 23-31 tumor necrosis factor Homo sapiens 41-49 30739791-0 2019 PPARbeta/delta agonist GW501516 inhibits TNFalpha-induced repression of adiponectin and insulin receptor in 3T3-L1 adipocytes. GW 501516 23-31 adiponectin, C1Q and collagen domain containing Homo sapiens 72-83 30739791-0 2019 PPARbeta/delta agonist GW501516 inhibits TNFalpha-induced repression of adiponectin and insulin receptor in 3T3-L1 adipocytes. GW 501516 23-31 insulin Homo sapiens 88-95 30739791-3 2019 GW501516 induced adipocyte differentiation and the expression of adiponectin in a dose-dependent manner in differentiated adipocytes. GW 501516 0-8 adiponectin, C1Q and collagen domain containing Homo sapiens 65-76 30739791-5 2019 This effect was reversed by GW501516 co-treatment with TNFalpha. GW 501516 28-36 tumor necrosis factor Homo sapiens 55-63 30739791-8 2019 Our results showed that GW501516 abrogated TNFalpha-induced insulin resistance. GW 501516 24-32 insulin Homo sapiens 60-67 30739791-9 2019 In summary, our study demonstrated that the PPARbeta/delta agonist, GW501516 reversed TNFalpha-induced decreases in adipocyte differentiation and adiponectin expression, and improved insulin sensitivity by increasing the expression of insulin receptor. GW 501516 68-76 peroxisome proliferator activated receptor delta Homo sapiens 44-52 30739791-9 2019 In summary, our study demonstrated that the PPARbeta/delta agonist, GW501516 reversed TNFalpha-induced decreases in adipocyte differentiation and adiponectin expression, and improved insulin sensitivity by increasing the expression of insulin receptor. GW 501516 68-76 tumor necrosis factor Homo sapiens 86-94 30739791-9 2019 In summary, our study demonstrated that the PPARbeta/delta agonist, GW501516 reversed TNFalpha-induced decreases in adipocyte differentiation and adiponectin expression, and improved insulin sensitivity by increasing the expression of insulin receptor. GW 501516 68-76 adiponectin, C1Q and collagen domain containing Homo sapiens 146-157 30739791-9 2019 In summary, our study demonstrated that the PPARbeta/delta agonist, GW501516 reversed TNFalpha-induced decreases in adipocyte differentiation and adiponectin expression, and improved insulin sensitivity by increasing the expression of insulin receptor. GW 501516 68-76 insulin Homo sapiens 183-190 30739791-7 2019 GW501516 treatment increased the expression of insulin receptor and inhibited TNFalpha-mediated repression of insulin receptor. GW 501516 0-8 insulin receptor Homo sapiens 47-63 30739791-9 2019 In summary, our study demonstrated that the PPARbeta/delta agonist, GW501516 reversed TNFalpha-induced decreases in adipocyte differentiation and adiponectin expression, and improved insulin sensitivity by increasing the expression of insulin receptor. GW 501516 68-76 insulin receptor Homo sapiens 235-251 30739791-7 2019 GW501516 treatment increased the expression of insulin receptor and inhibited TNFalpha-mediated repression of insulin receptor. GW 501516 0-8 tumor necrosis factor Homo sapiens 78-86 30391747-3 2019 In addition, PPARdelta agonist GW501516 enhanced pro-inflammatory gene expressions (COX-2, IL-6, IL-8 and MCP-1) in inflamed colon. GW 501516 31-39 peroxisome proliferator activator receptor delta Mus musculus 13-22 30679176-7 2019 Treatment with PPARD agonist GW501516 enhanced colorectal cancer tumorigenesis in ApcDelta580 mice, whereas treatment with PPARD antagonist GSK3787 suppressed tumorigenesis. GW 501516 29-37 peroxisome proliferator activator receptor delta Mus musculus 15-20 30620754-2 2019 Activation of PPARdelta by GW501516, a specific ligand of PPARdelta, significantly inhibited Ang II-stimulated protein synthesis in a concentration-dependent manner, as determined by [3H]-leucine incorporation. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 30620754-2 2019 Activation of PPARdelta by GW501516, a specific ligand of PPARdelta, significantly inhibited Ang II-stimulated protein synthesis in a concentration-dependent manner, as determined by [3H]-leucine incorporation. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 58-67 30620754-2 2019 Activation of PPARdelta by GW501516, a specific ligand of PPARdelta, significantly inhibited Ang II-stimulated protein synthesis in a concentration-dependent manner, as determined by [3H]-leucine incorporation. GW 501516 27-35 angiotensinogen Homo sapiens 93-99 30620754-3 2019 GW501516-activated PPARdelta also suppressed Ang II-induced generation of reactive oxygen species (ROS) in VSMCs. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 19-28 30620754-3 2019 GW501516-activated PPARdelta also suppressed Ang II-induced generation of reactive oxygen species (ROS) in VSMCs. GW 501516 0-8 angiotensinogen Homo sapiens 45-51 30620754-4 2019 Transfection of small interfering RNA (siRNA) against PPARdelta significantly reversed the effects of GW501516 on [3H]-leucine incorporation and ROS generation, indicating that PPARdelta is involved in these effects. GW 501516 102-110 peroxisome proliferator activated receptor delta Homo sapiens 54-63 30620754-4 2019 Transfection of small interfering RNA (siRNA) against PPARdelta significantly reversed the effects of GW501516 on [3H]-leucine incorporation and ROS generation, indicating that PPARdelta is involved in these effects. GW 501516 102-110 peroxisome proliferator activated receptor delta Homo sapiens 177-186 30620754-5 2019 By contrast, these GW501516-mediated actions were potentiated in VSMCs transfected with siRNA against NADPH oxidase (NOX) 1 or 4, suggesting that ligand-activated PPARdelta elicits these effects by modulating NOX-mediated ROS generation. GW 501516 19-27 peroxisome proliferator activated receptor delta Homo sapiens 163-172 30605833-3 2019 In this study, we hybrid FFA1 agonist AM-4668 with PPARdelta agonist GW501516, leading to the identification of orally bioavailable dual agonist 32, which revealed high selectivity over other PPARs. GW 501516 69-77 peroxisome proliferator activator receptor delta Mus musculus 51-60 30573521-3 2019 Here we investigated the impact of the peroxisome proliferator-activated receptor (PPAR) agonist GW501516 (GW), an agent known to boost FAO in other tissues, on CD8+ T-cell metabolism, function, and efficacy in a murine ACT model. GW 501516 97-105 peroxisome proliferator activated receptor alpha Rattus norvegicus 83-87 30573521-3 2019 Here we investigated the impact of the peroxisome proliferator-activated receptor (PPAR) agonist GW501516 (GW), an agent known to boost FAO in other tissues, on CD8+ T-cell metabolism, function, and efficacy in a murine ACT model. GW 501516 97-99 peroxisome proliferator activated receptor alpha Rattus norvegicus 83-87 30573521-4 2019 Via activation of both PPARalpha and PPARdelta/beta, GW treatment increased expression of carnitine palmitoyl transferase 1a, the rate-limiting enzyme of FAO, in activated CD8+ T cells. GW 501516 53-55 peroxisome proliferator activated receptor alpha Rattus norvegicus 23-32 30573521-4 2019 Via activation of both PPARalpha and PPARdelta/beta, GW treatment increased expression of carnitine palmitoyl transferase 1a, the rate-limiting enzyme of FAO, in activated CD8+ T cells. GW 501516 53-55 peroxisome proliferator activated receptor alpha Rattus norvegicus 37-51 30573521-4 2019 Via activation of both PPARalpha and PPARdelta/beta, GW treatment increased expression of carnitine palmitoyl transferase 1a, the rate-limiting enzyme of FAO, in activated CD8+ T cells. GW 501516 53-55 carnitine palmitoyltransferase 1A Rattus norvegicus 90-124 30391747-3 2019 In addition, PPARdelta agonist GW501516 enhanced pro-inflammatory gene expressions (COX-2, IL-6, IL-8 and MCP-1) in inflamed colon. GW 501516 31-39 cytochrome c oxidase II, mitochondrial Mus musculus 84-89 30391747-3 2019 In addition, PPARdelta agonist GW501516 enhanced pro-inflammatory gene expressions (COX-2, IL-6, IL-8 and MCP-1) in inflamed colon. GW 501516 31-39 interleukin 6 Mus musculus 91-95 30391747-3 2019 In addition, PPARdelta agonist GW501516 enhanced pro-inflammatory gene expressions (COX-2, IL-6, IL-8 and MCP-1) in inflamed colon. GW 501516 31-39 chemokine (C-X-C motif) ligand 15 Mus musculus 97-101 30391747-3 2019 In addition, PPARdelta agonist GW501516 enhanced pro-inflammatory gene expressions (COX-2, IL-6, IL-8 and MCP-1) in inflamed colon. GW 501516 31-39 mast cell protease 1 Mus musculus 106-111 30391747-4 2019 Further analysis showed that GW501516 increased the expressions of Glut1 and SLC1A5 in colon cancer cells as well as AOM/DSS-induced colorectal tumors. GW 501516 29-37 solute carrier family 2 (facilitated glucose transporter), member 1 Mus musculus 67-72 30391747-4 2019 Further analysis showed that GW501516 increased the expressions of Glut1 and SLC1A5 in colon cancer cells as well as AOM/DSS-induced colorectal tumors. GW 501516 29-37 solute carrier family 1 (neutral amino acid transporter), member 5 Mus musculus 77-83 30391747-5 2019 These findings revealed a new mechanism of PPARdelta agonist GW501516-mediated colitis-associated colorectal cancer. GW 501516 61-69 peroxisome proliferator activator receptor delta Mus musculus 43-52 29941059-7 2018 In Experiment 2, inhibition of PPARbeta/delta had no effect on glucose uptake and lactose synthesis but they were both increased by GW-501516 in PBMC. GW 501516 132-141 peroxisome proliferator activated receptor delta Bos taurus 31-39 29885849-11 2019 Our results show that GW501516 reduced movement impairment in PD mice; furthermore, it attenuated dopaminergic neurodegeneration in the midbrain and the depletion of dopamine in the striatum and it inhibited inflammatory reactions and NLRP3 inflammasome activation in the midbrain of PD mice. GW 501516 22-30 NLR family, pyrin domain containing 3 Mus musculus 235-240 29885849-13 2019 Collectively, our findings demonstrate for the first time that the specific PPARss/delta agonist GW501516 alleviates NLRP3 inflammasome-mediated neuroinflammation in astrocytes in the MPTP mouse model of PD. GW 501516 97-105 NLR family, pyrin domain containing 3 Mus musculus 117-122 30987865-3 2019 Treatment of mice fed a high-fat diet with the PPARbeta/delta agonist GW501516 increased the hepatic expression of Vldlr. GW 501516 70-78 peroxisome proliferator activator receptor delta Mus musculus 47-55 30987865-3 2019 Treatment of mice fed a high-fat diet with the PPARbeta/delta agonist GW501516 increased the hepatic expression of Vldlr. GW 501516 70-78 very low density lipoprotein receptor Mus musculus 115-120 30987865-4 2019 Similarly, exposure of human Huh-7 hepatocytes to GW501516 increased the expression of VLDLR and triglyceride accumulation, the latter being prevented by VLDLR knockdown. GW 501516 50-58 MIR7-3 host gene Homo sapiens 29-34 30987865-4 2019 Similarly, exposure of human Huh-7 hepatocytes to GW501516 increased the expression of VLDLR and triglyceride accumulation, the latter being prevented by VLDLR knockdown. GW 501516 50-58 very low density lipoprotein receptor Homo sapiens 87-92 30987865-4 2019 Similarly, exposure of human Huh-7 hepatocytes to GW501516 increased the expression of VLDLR and triglyceride accumulation, the latter being prevented by VLDLR knockdown. GW 501516 50-58 very low density lipoprotein receptor Homo sapiens 154-159 30204243-6 2018 Administration of the PPARdelta ligand GW501516 inhibited tumor growth in xenograft model mice bearing MDA-MB-231 cells stably expressing wild-type PPARdelta, but not those expressing dominant-negative PPARdelta, by interfering with c-Myc function through protein-protein interaction. GW 501516 39-47 peroxisome proliferator activator receptor delta Mus musculus 22-31 30204243-6 2018 Administration of the PPARdelta ligand GW501516 inhibited tumor growth in xenograft model mice bearing MDA-MB-231 cells stably expressing wild-type PPARdelta, but not those expressing dominant-negative PPARdelta, by interfering with c-Myc function through protein-protein interaction. GW 501516 39-47 peroxisome proliferator activated receptor delta Homo sapiens 148-157 30204243-6 2018 Administration of the PPARdelta ligand GW501516 inhibited tumor growth in xenograft model mice bearing MDA-MB-231 cells stably expressing wild-type PPARdelta, but not those expressing dominant-negative PPARdelta, by interfering with c-Myc function through protein-protein interaction. GW 501516 39-47 peroxisome proliferator activated receptor delta Homo sapiens 148-157 30204243-6 2018 Administration of the PPARdelta ligand GW501516 inhibited tumor growth in xenograft model mice bearing MDA-MB-231 cells stably expressing wild-type PPARdelta, but not those expressing dominant-negative PPARdelta, by interfering with c-Myc function through protein-protein interaction. GW 501516 39-47 MYC proto-oncogene, bHLH transcription factor Homo sapiens 233-238 29388693-4 2018 Activation of PPARdelta by GW501516, a specific PPARdelta agonist, inhibited glutamate release in BV-2 cells. GW 501516 27-35 peroxisome proliferator activator receptor delta Mus musculus 14-23 29388693-4 2018 Activation of PPARdelta by GW501516, a specific PPARdelta agonist, inhibited glutamate release in BV-2 cells. GW 501516 27-35 peroxisome proliferator activator receptor delta Mus musculus 48-57 29388693-8 2018 By contrast, GW501516 upregulated the expression of suppressor of cytokine signaling 1 (SOCS1), an endogenous inhibitor of JAK2. GW 501516 13-21 suppressor of cytokine signaling 1 Mus musculus 52-86 29388693-5 2018 This effect of GW501516 was significantly blocked by shRNA-mediated knockdown of PPARdelta and by treatment with GSK0660, a specific PPARdelta antagonist, indicating that PPARdelta is associated with blockade of glutamate release. GW 501516 15-23 peroxisome proliferator activator receptor delta Mus musculus 81-90 29388693-8 2018 By contrast, GW501516 upregulated the expression of suppressor of cytokine signaling 1 (SOCS1), an endogenous inhibitor of JAK2. GW 501516 13-21 suppressor of cytokine signaling 1 Mus musculus 88-93 29388693-5 2018 This effect of GW501516 was significantly blocked by shRNA-mediated knockdown of PPARdelta and by treatment with GSK0660, a specific PPARdelta antagonist, indicating that PPARdelta is associated with blockade of glutamate release. GW 501516 15-23 peroxisome proliferator activator receptor delta Mus musculus 133-142 29388693-8 2018 By contrast, GW501516 upregulated the expression of suppressor of cytokine signaling 1 (SOCS1), an endogenous inhibitor of JAK2. GW 501516 13-21 Janus kinase 2 Mus musculus 123-127 29388693-5 2018 This effect of GW501516 was significantly blocked by shRNA-mediated knockdown of PPARdelta and by treatment with GSK0660, a specific PPARdelta antagonist, indicating that PPARdelta is associated with blockade of glutamate release. GW 501516 15-23 peroxisome proliferator activator receptor delta Mus musculus 133-142 29388693-6 2018 Additionally, GW501516-activated PPARdelta suppressed generation of reactive oxygen species and expression of gp91phox, a functional subunit of NADPH oxidase 2, in BV-2 cells stimulated with LPS. GW 501516 14-22 peroxisome proliferator activator receptor delta Mus musculus 33-42 29388693-6 2018 Additionally, GW501516-activated PPARdelta suppressed generation of reactive oxygen species and expression of gp91phox, a functional subunit of NADPH oxidase 2, in BV-2 cells stimulated with LPS. GW 501516 14-22 cytochrome b-245, beta polypeptide Mus musculus 110-118 29621036-6 2018 The known PPAR-delta agonists, GW1516, L165041, and GW0742, showed potent agonist activity against human, mouse, and rat receptors (ranging from 165- to 396-fold). GW 501516 31-37 peroxisome proliferator activated receptor delta Homo sapiens 10-20 29388693-6 2018 Additionally, GW501516-activated PPARdelta suppressed generation of reactive oxygen species and expression of gp91phox, a functional subunit of NADPH oxidase 2, in BV-2 cells stimulated with LPS. GW 501516 14-22 cytochrome b-245, beta polypeptide Mus musculus 144-159 29388693-7 2018 The inhibitory effect of GW501516 on gp91phox expression and glutamate release was further potentiated in the presence of AG490, a specific inhibitor of janus kinase 2 (JAK2), leading to the inhibition of signal transducer and activator of transcription 1 (STAT1). GW 501516 25-33 cytochrome b-245, beta polypeptide Mus musculus 37-45 29388693-7 2018 The inhibitory effect of GW501516 on gp91phox expression and glutamate release was further potentiated in the presence of AG490, a specific inhibitor of janus kinase 2 (JAK2), leading to the inhibition of signal transducer and activator of transcription 1 (STAT1). GW 501516 25-33 Janus kinase 2 Mus musculus 153-167 29388693-7 2018 The inhibitory effect of GW501516 on gp91phox expression and glutamate release was further potentiated in the presence of AG490, a specific inhibitor of janus kinase 2 (JAK2), leading to the inhibition of signal transducer and activator of transcription 1 (STAT1). GW 501516 25-33 Janus kinase 2 Mus musculus 169-173 29388693-7 2018 The inhibitory effect of GW501516 on gp91phox expression and glutamate release was further potentiated in the presence of AG490, a specific inhibitor of janus kinase 2 (JAK2), leading to the inhibition of signal transducer and activator of transcription 1 (STAT1). GW 501516 25-33 signal transducer and activator of transcription 1 Mus musculus 205-255 29388693-7 2018 The inhibitory effect of GW501516 on gp91phox expression and glutamate release was further potentiated in the presence of AG490, a specific inhibitor of janus kinase 2 (JAK2), leading to the inhibition of signal transducer and activator of transcription 1 (STAT1). GW 501516 25-33 signal transducer and activator of transcription 1 Mus musculus 257-262 29275935-0 2018 Highly selective peroxisome proliferator-activated receptor delta (PPARdelta) modulator demonstrates improved safety profile compared to GW501516. GW 501516 137-145 peroxisome proliferator activated receptor delta Homo sapiens 67-76 30002625-0 2018 PPARbeta/delta Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma in C666-1 Cells by Promoting Apoptosis. GW 501516 23-31 peroxisome proliferator activated receptor delta Homo sapiens 0-8 30002625-5 2018 Ligand activation of PPARbeta/delta by GW501516, a specific PPARbeta/delta selective agonist, inhibited cell proliferation and colony formation strikingly, and induced a G2/M phase arrest in the EBV positive undifferentiated NPC C666-1 cells relative to the control cells. GW 501516 39-47 peroxisome proliferator activated receptor delta Homo sapiens 21-29 30002625-5 2018 Ligand activation of PPARbeta/delta by GW501516, a specific PPARbeta/delta selective agonist, inhibited cell proliferation and colony formation strikingly, and induced a G2/M phase arrest in the EBV positive undifferentiated NPC C666-1 cells relative to the control cells. GW 501516 39-47 peroxisome proliferator activated receptor delta Homo sapiens 60-68 29233935-6 2018 Finally, GW501516-activated PPARdelta improved insulin signaling and glucose intolerance in mice fed a high-fat diet through its interaction with TCPTP45. GW 501516 9-17 peroxisome proliferator activator receptor delta Mus musculus 28-37 30002625-6 2018 Moreover, GW501516 induced C666-1 cell apoptosis in a caspase and BAX dependent manner. GW 501516 10-18 BCL2 associated X, apoptosis regulator Homo sapiens 66-69 30002625-9 2018 Collectively, we showed that PPARbeta/delta expression is in reverse correlation with the degree of differentiation in the NPC cell lines, and revealed the anti-tumorigenic effects of GW501516 in NPC cells by activation of AMPKalpha. GW 501516 184-192 peroxisome proliferator activated receptor delta Homo sapiens 29-37 29275935-1 2018 Compound 1 regulates significantly fewer genes than the PPARdelta modulator, GW501516. GW 501516 77-85 peroxisome proliferator activated receptor delta Homo sapiens 56-65 29275935-3 2018 The restricted gene profile of 1 relative to GW501516 suggests that 1 may be pharmacoequivalent to GW501516 with fewer PPAR-related safety concerns. GW 501516 99-107 peroxisome proliferator activated receptor alpha Homo sapiens 119-123 29408825-7 2018 GW501516- activated PPARdelta also reduced the H2O2-induced generation of reactive oxygen species, concomitant with inhibition of VSMC migration. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 20-29 29212212-3 2017 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, led to marked inhibition in the cell migration and TSP-1 expression of breast cancer. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 29408825-4 2018 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly attenuated hydrogen peroxide (H2O2)-induced expression of TSP-1 in VSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 29408825-4 2018 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly attenuated hydrogen peroxide (H2O2)-induced expression of TSP-1 in VSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 59-68 29408825-4 2018 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly attenuated hydrogen peroxide (H2O2)-induced expression of TSP-1 in VSMCs. GW 501516 27-35 thrombospondin 1 Homo sapiens 142-147 29408825-5 2018 Small interfering RNA-mediated knockdown of PPARdelta and treatment with GSK0660, a selective PPARdelta antagonist, reversed the effect of GW501516 on H2O2-induced expression of TSP-1, suggesting that PPARdelta is associated with GW501516 activity. GW 501516 139-147 peroxisome proliferator activated receptor delta Homo sapiens 44-53 29408825-5 2018 Small interfering RNA-mediated knockdown of PPARdelta and treatment with GSK0660, a selective PPARdelta antagonist, reversed the effect of GW501516 on H2O2-induced expression of TSP-1, suggesting that PPARdelta is associated with GW501516 activity. GW 501516 139-147 peroxisome proliferator activated receptor delta Homo sapiens 94-103 29408825-5 2018 Small interfering RNA-mediated knockdown of PPARdelta and treatment with GSK0660, a selective PPARdelta antagonist, reversed the effect of GW501516 on H2O2-induced expression of TSP-1, suggesting that PPARdelta is associated with GW501516 activity. GW 501516 139-147 thrombospondin 1 Homo sapiens 178-183 29408825-5 2018 Small interfering RNA-mediated knockdown of PPARdelta and treatment with GSK0660, a selective PPARdelta antagonist, reversed the effect of GW501516 on H2O2-induced expression of TSP-1, suggesting that PPARdelta is associated with GW501516 activity. GW 501516 139-147 peroxisome proliferator activated receptor delta Homo sapiens 94-103 29408825-5 2018 Small interfering RNA-mediated knockdown of PPARdelta and treatment with GSK0660, a selective PPARdelta antagonist, reversed the effect of GW501516 on H2O2-induced expression of TSP-1, suggesting that PPARdelta is associated with GW501516 activity. GW 501516 230-238 thrombospondin 1 Homo sapiens 178-183 29212212-3 2017 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, led to marked inhibition in the cell migration and TSP-1 expression of breast cancer. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 59-68 29212212-3 2017 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, led to marked inhibition in the cell migration and TSP-1 expression of breast cancer. GW 501516 27-35 thrombospondin 1 Homo sapiens 121-126 28955982-5 2016 GW501516-activated PPARbeta/delta suppressed TNFalpha-induced Nfkb reporter activity. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 19-27 28124448-0 2017 PPARdelta Modulation by GW501516: An Unsuccessful Exercise Mimetic. GW 501516 24-32 peroxisome proliferator activated receptor delta Homo sapiens 0-9 28224611-0 2017 Response to "PPARdelta Modulation by GW501516: An Unsuccessful Exercise Mimetic". GW 501516 37-45 peroxisome proliferator activated receptor delta Homo sapiens 13-22 26661245-7 2017 In contrast, GW501516 (a selective agonist of PPARdelta) upregulated ADAM10 and increased production of sAPPalpha. GW 501516 13-21 peroxisome proliferator activator receptor delta Mus musculus 46-55 26661245-7 2017 In contrast, GW501516 (a selective agonist of PPARdelta) upregulated ADAM10 and increased production of sAPPalpha. GW 501516 13-21 a disintegrin and metallopeptidase domain 10 Mus musculus 69-75 28440451-1 2017 The aim of the present study was to investigate the protective effect of the selective peroxisome proliferator-activated receptor delta (PPARdelta) agonist GW501516 (GW) on lipopolysaccharide (LPS)-induced apoptosis in the rat cardiomyoblast cell line H9c2, and to investigate the possible underlying mechanisms. GW 501516 156-164 peroxisome proliferator-activated receptor delta Rattus norvegicus 87-135 28440451-1 2017 The aim of the present study was to investigate the protective effect of the selective peroxisome proliferator-activated receptor delta (PPARdelta) agonist GW501516 (GW) on lipopolysaccharide (LPS)-induced apoptosis in the rat cardiomyoblast cell line H9c2, and to investigate the possible underlying mechanisms. GW 501516 156-164 peroxisome proliferator-activated receptor delta Rattus norvegicus 137-146 28440451-1 2017 The aim of the present study was to investigate the protective effect of the selective peroxisome proliferator-activated receptor delta (PPARdelta) agonist GW501516 (GW) on lipopolysaccharide (LPS)-induced apoptosis in the rat cardiomyoblast cell line H9c2, and to investigate the possible underlying mechanisms. GW 501516 156-158 peroxisome proliferator-activated receptor delta Rattus norvegicus 87-135 28440451-1 2017 The aim of the present study was to investigate the protective effect of the selective peroxisome proliferator-activated receptor delta (PPARdelta) agonist GW501516 (GW) on lipopolysaccharide (LPS)-induced apoptosis in the rat cardiomyoblast cell line H9c2, and to investigate the possible underlying mechanisms. GW 501516 156-158 peroxisome proliferator-activated receptor delta Rattus norvegicus 137-146 28440451-6 2017 Pretreatment with GW also increased the bcl-2/bax ratio, and decreased CC3 protein expression as well as caspase-3 activity, in LPS-stimulated H9c2 cells. GW 501516 18-20 BCL2, apoptosis regulator Rattus norvegicus 40-45 28440451-6 2017 Pretreatment with GW also increased the bcl-2/bax ratio, and decreased CC3 protein expression as well as caspase-3 activity, in LPS-stimulated H9c2 cells. GW 501516 18-20 BCL2 associated X, apoptosis regulator Rattus norvegicus 46-49 28440451-6 2017 Pretreatment with GW also increased the bcl-2/bax ratio, and decreased CC3 protein expression as well as caspase-3 activity, in LPS-stimulated H9c2 cells. GW 501516 18-20 caspase 3 Rattus norvegicus 105-114 28440451-9 2017 ZnPP-IX, an inhibitor of HO-1, reversed the inhibitory effect of GW on LPS-induced NF-kappaB activation, leading to the attenuation of PPARdelta-mediated apoptosis resistance. GW 501516 65-67 peroxisome proliferator-activated receptor delta Rattus norvegicus 135-144 28404991-5 2017 Furthermore, absence of intestinal PPARdelta abolished the ability of PPARdelta agonist GW501516 to increase plasma levels of HDL-cholesterol. GW 501516 88-96 peroxisome proliferator activator receptor delta Mus musculus 35-44 28404991-5 2017 Furthermore, absence of intestinal PPARdelta abolished the ability of PPARdelta agonist GW501516 to increase plasma levels of HDL-cholesterol. GW 501516 88-96 peroxisome proliferator activator receptor delta Mus musculus 70-79 28166979-4 2017 In this study, oocytes and parthenotes were treated with a specific agonist of PPARdelta, GW501516. GW 501516 90-98 peroxisome proliferator activated receptor delta Homo sapiens 79-88 28955982-5 2016 GW501516-activated PPARbeta/delta suppressed TNFalpha-induced Nfkb reporter activity. GW 501516 0-8 tumor necrosis factor Homo sapiens 45-53 28955982-6 2016 RNAi knockdown of Pparb attenuated the GW501516 effect on Nfkb luciferase, while knockdown of Bcl6 enhanced TNFalpha-induced Nfkb activity. GW 501516 39-47 peroxisome proliferator activated receptor delta Homo sapiens 18-23 28955982-7 2016 PPARbeta/delta activation induced expression of several anti-inflammatory genes in a dose-dependent manner, and GW501516 inhibited Mcp1 promoter-driven luciferase in a BCL6-dependent manner. GW 501516 112-120 C-C motif chemokine ligand 2 Homo sapiens 131-135 28955982-7 2016 PPARbeta/delta activation induced expression of several anti-inflammatory genes in a dose-dependent manner, and GW501516 inhibited Mcp1 promoter-driven luciferase in a BCL6-dependent manner. GW 501516 112-120 BCL6 transcription repressor Homo sapiens 168-172 28955982-9 2016 Conditioned media from GW501516-treated pancreatic cancer cells suppressed pro-inflammatory expression in THP-1 macrophages as well as reduced invasiveness across a basement membrane. GW 501516 23-31 GLI family zinc finger 2 Homo sapiens 106-111 27638828-0 2016 Apoptotic effect of the selective PPARbeta/delta agonist GW501516 in invasive bladder cancer cells. GW 501516 57-65 peroxisome proliferator activated receptor delta Homo sapiens 34-42 27573670-3 2016 PPARdelta activated by GW501516 (2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid) significantly inhibited the migration and proliferation of vascular smooth muscle cells (VSMCs) triggered by oxidized low-density lipoprotein (oxLDL). GW 501516 23-31 peroxisome proliferator activated receptor delta Homo sapiens 0-9 27573670-4 2016 These GW501516-mediated effects were significantly reversed by PPARdelta-targeting small-interfering RNA (siRNA), indicating that PPARdelta is involved in the action of GW501516. GW 501516 6-14 peroxisome proliferator activated receptor delta Homo sapiens 63-72 27573670-4 2016 These GW501516-mediated effects were significantly reversed by PPARdelta-targeting small-interfering RNA (siRNA), indicating that PPARdelta is involved in the action of GW501516. GW 501516 6-14 peroxisome proliferator activated receptor delta Homo sapiens 130-139 27573670-4 2016 These GW501516-mediated effects were significantly reversed by PPARdelta-targeting small-interfering RNA (siRNA), indicating that PPARdelta is involved in the action of GW501516. GW 501516 169-177 peroxisome proliferator activated receptor delta Homo sapiens 63-72 27573670-4 2016 These GW501516-mediated effects were significantly reversed by PPARdelta-targeting small-interfering RNA (siRNA), indicating that PPARdelta is involved in the action of GW501516. GW 501516 169-177 peroxisome proliferator activated receptor delta Homo sapiens 130-139 27573670-5 2016 The antiproliferative effect of GW501516 was directly linked to cell cycle arrest at the G0/G1 to S phase transition, which was followed by the down-regulation of cyclin-dependent kinase 4 along with increased levels of p21 and p53. GW 501516 32-40 cyclin dependent kinase 4 Homo sapiens 163-188 27573670-5 2016 The antiproliferative effect of GW501516 was directly linked to cell cycle arrest at the G0/G1 to S phase transition, which was followed by the down-regulation of cyclin-dependent kinase 4 along with increased levels of p21 and p53. GW 501516 32-40 cyclin dependent kinase inhibitor 1A Homo sapiens 220-223 27573670-5 2016 The antiproliferative effect of GW501516 was directly linked to cell cycle arrest at the G0/G1 to S phase transition, which was followed by the down-regulation of cyclin-dependent kinase 4 along with increased levels of p21 and p53. GW 501516 32-40 tumor protein p53 Homo sapiens 228-231 27573670-6 2016 In VSMCs treated with GW501516, the expression of sirtuin 1 (SIRT1) mRNA and protein was time-dependently increased. GW 501516 22-30 sirtuin 1 Homo sapiens 50-59 27573670-6 2016 In VSMCs treated with GW501516, the expression of sirtuin 1 (SIRT1) mRNA and protein was time-dependently increased. GW 501516 22-30 sirtuin 1 Homo sapiens 61-66 27573670-7 2016 This GW501516-mediated up-regulation of SIRT1 expression was also demonstrated even in the presence of oxLDL. GW 501516 5-13 sirtuin 1 Homo sapiens 40-45 27573670-8 2016 In addition, GW501516-dependent inhibition of oxLDL-triggered migration and proliferation of VSMCs was almost completely abolished in the presence of SIRT1-targeting siRNA. GW 501516 13-21 sirtuin 1 Homo sapiens 150-155 27573670-9 2016 These effects of GW501516 on oxLDL-triggered phenotypic changes of VSMCs were also demonstrated via activation or inhibition of SIRT1 activity by resveratrol or sirtinol, respectively. GW 501516 17-25 sirtuin 1 Homo sapiens 128-133 27638828-1 2016 GW501516 is a selective and high-affinity synthetic agonist of peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta). GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 63-116 27638828-1 2016 GW501516 is a selective and high-affinity synthetic agonist of peroxisome proliferator-activated receptor beta/delta (PPARbeta/delta). GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 118-126 27638828-6 2016 Furthermore, GW501516 triggered T24 cell apoptosis in a caspase-dependent manner including both extrinsic and intrinsic apoptotic pathways through Bid cleavage. GW 501516 13-21 BH3 interacting domain death agonist Homo sapiens 147-150 26403493-2 2016 In human gingival fibroblasts (HGFs), activation of PPARdelta by GW501516, a specific ligand of PPARdelta, inhibited Pg-LPS-induced activation of MMP-2 and generation of reactive oxygen species (ROS), which was associated with reduced expression of NADPH oxidase 4 (Nox4). GW 501516 65-73 peroxisome proliferator activated receptor delta Homo sapiens 52-61 26403493-2 2016 In human gingival fibroblasts (HGFs), activation of PPARdelta by GW501516, a specific ligand of PPARdelta, inhibited Pg-LPS-induced activation of MMP-2 and generation of reactive oxygen species (ROS), which was associated with reduced expression of NADPH oxidase 4 (Nox4). GW 501516 65-73 peroxisome proliferator activated receptor delta Homo sapiens 96-105 26403493-2 2016 In human gingival fibroblasts (HGFs), activation of PPARdelta by GW501516, a specific ligand of PPARdelta, inhibited Pg-LPS-induced activation of MMP-2 and generation of reactive oxygen species (ROS), which was associated with reduced expression of NADPH oxidase 4 (Nox4). GW 501516 65-73 matrix metallopeptidase 2 Homo sapiens 146-151 26403493-2 2016 In human gingival fibroblasts (HGFs), activation of PPARdelta by GW501516, a specific ligand of PPARdelta, inhibited Pg-LPS-induced activation of MMP-2 and generation of reactive oxygen species (ROS), which was associated with reduced expression of NADPH oxidase 4 (Nox4). GW 501516 65-73 NADPH oxidase 4 Homo sapiens 249-264 26403493-2 2016 In human gingival fibroblasts (HGFs), activation of PPARdelta by GW501516, a specific ligand of PPARdelta, inhibited Pg-LPS-induced activation of MMP-2 and generation of reactive oxygen species (ROS), which was associated with reduced expression of NADPH oxidase 4 (Nox4). GW 501516 65-73 NADPH oxidase 4 Homo sapiens 266-270 26111938-6 2015 Increasing BH4 bioavailability either exogenously by BH4 supplementation or endogenously by treatment with the selective peroxisome proliferator-activated receptor--delta activator GW501516 (2 mg/kg/day, 14 days) attenuated eNOS uncoupling and decreased superoxide anion production in cerebral microvessels of Tg2576 mice (p < 0.05). GW 501516 181-189 peroxisome proliferator activator receptor delta Mus musculus 121-170 26160761-13 2016 Moreover, GW501516 suppressed the activation of ER stress markers including inositol-requiring enzyme 1alpha (IRE1alpha) and caspase-12. GW 501516 10-18 caspase 12 Rattus norvegicus 125-135 26160761-14 2016 Furthermore, GW501516 inhibited caspase-12-mediated neuronal apoptosis. GW 501516 13-21 caspase 12 Rattus norvegicus 32-42 27278004-6 2016 Results indicated that the activation of PPARdelta was correlated in a positive manner with the activity of SMS2, and the content of SM was dose dependently increased by GW501516. GW 501516 170-178 peroxisome proliferator activated receptor delta Homo sapiens 41-50 27278004-6 2016 Results indicated that the activation of PPARdelta was correlated in a positive manner with the activity of SMS2, and the content of SM was dose dependently increased by GW501516. GW 501516 170-178 sphingomyelin synthase 2 Homo sapiens 108-112 27266389-4 2016 METHODS AND RESULTS: Treatment with a highly selective PPAR-delta agonist (GW501516) induced proliferation of late EPCs and enhanced their vasculogenic potential. GW 501516 75-83 peroxisome proliferator activated receptor delta Homo sapiens 55-65 27266389-10 2016 Platelet supernatant boosted the pro-vasculogenic effects of GW501516, which was reversed by antagonist to PPAR-delta (GSK0660) or Edg (Ki16425). GW 501516 61-69 peroxisome proliferator activated receptor delta Homo sapiens 107-117 26992147-9 2016 Moreover, our results suggest a close distance between the N- and C-terminal regions of full-length PPAR-beta/delta in the presence of GW1516. GW 501516 135-141 peroxisome proliferator activated receptor delta Homo sapiens 100-109 26004782-7 2016 Several PPARdelta selective agonists had been reported in last ten years, many of them had been advanced into the late phase of clinical trials such as Endurobol (GW501516). GW 501516 163-171 peroxisome proliferator activated receptor delta Homo sapiens 8-17 26481780-5 2015 RESULTS: Activation of PPARdelta by GW501516, a specific ligand of PPARdelta, specifically upregulated the myofibroblast marker alpha-smooth muscle actin (alpha-SMA) in a time- and concentration-dependent manner. GW 501516 36-44 peroxisome proliferator activated receptor delta Homo sapiens 23-32 26481780-5 2015 RESULTS: Activation of PPARdelta by GW501516, a specific ligand of PPARdelta, specifically upregulated the myofibroblast marker alpha-smooth muscle actin (alpha-SMA) in a time- and concentration-dependent manner. GW 501516 36-44 peroxisome proliferator activated receptor delta Homo sapiens 67-76 26481780-9 2015 GW501516-activated PPARdelta also increased the migration and contractile properties of HDFs, as demonstrated by Transwell and collagen lattice contraction assays, respectively. GW 501516 0-8 peroxisome proliferator activated receptor delta Homo sapiens 19-28 25854303-2 2015 The aim of this study was to evaluate the effects of the short-term administration of GW501516 on pro-inflammatory markers in white adipose tissue (WAT) and hepatic stellate cells (HSCs), lipogenesis and insulin resistance in the liver upon high-fructose diet (HFru)-induced ACE/AT1r axis activation. GW 501516 86-94 angiotensin I converting enzyme (peptidyl-dipeptidase A) 1 Mus musculus 275-278 25854303-2 2015 The aim of this study was to evaluate the effects of the short-term administration of GW501516 on pro-inflammatory markers in white adipose tissue (WAT) and hepatic stellate cells (HSCs), lipogenesis and insulin resistance in the liver upon high-fructose diet (HFru)-induced ACE/AT1r axis activation. GW 501516 86-94 angiotensin II, type I receptor-associated protein Mus musculus 279-283 25854303-8 2015 Although GW501516 abolished the increased activation of the ACE/AT1r axis in the WAT, no differences were found in the liver. GW 501516 9-17 angiotensin I converting enzyme (peptidyl-dipeptidase A) 1 Mus musculus 60-63 25854303-8 2015 Although GW501516 abolished the increased activation of the ACE/AT1r axis in the WAT, no differences were found in the liver. GW 501516 9-17 angiotensin II, type I receptor-associated protein Mus musculus 64-68 25854303-11 2015 We conclude that GW501516 may serve as a therapeutic option for the treatment of a highly activated ACE/AT1r axis in WAT and liver. GW 501516 17-25 angiotensin I converting enzyme (peptidyl-dipeptidase A) 1 Mus musculus 100-103 25854303-11 2015 We conclude that GW501516 may serve as a therapeutic option for the treatment of a highly activated ACE/AT1r axis in WAT and liver. GW 501516 17-25 angiotensin II, type I receptor-associated protein Mus musculus 104-108 26133486-7 2015 In addition, treatment with GW501516 increased the levels of insulin-like growth factor-1 (IGF-1) and high-density lipoprotein (HDL) compared to the HFD group. GW 501516 28-36 insulin-like growth factor 1 Rattus norvegicus 61-89 26133486-7 2015 In addition, treatment with GW501516 increased the levels of insulin-like growth factor-1 (IGF-1) and high-density lipoprotein (HDL) compared to the HFD group. GW 501516 28-36 insulin-like growth factor 1 Rattus norvegicus 91-96 26133486-9 2015 RT-qPCR and immunohistochemical staining revealed that the expression levels of sterol regulatory element binding protein-1c (SREBP-1c) and glucose transporter 2 (GLUT-2) were both restored to normal control levels following treatment with GW501516. GW 501516 240-248 sterol regulatory element binding transcription factor 1 Rattus norvegicus 80-124 26133486-9 2015 RT-qPCR and immunohistochemical staining revealed that the expression levels of sterol regulatory element binding protein-1c (SREBP-1c) and glucose transporter 2 (GLUT-2) were both restored to normal control levels following treatment with GW501516. GW 501516 240-248 sterol regulatory element binding transcription factor 1 Rattus norvegicus 126-134 26133486-9 2015 RT-qPCR and immunohistochemical staining revealed that the expression levels of sterol regulatory element binding protein-1c (SREBP-1c) and glucose transporter 2 (GLUT-2) were both restored to normal control levels following treatment with GW501516. GW 501516 240-248 solute carrier family 2 member 2 Rattus norvegicus 140-161 26133486-9 2015 RT-qPCR and immunohistochemical staining revealed that the expression levels of sterol regulatory element binding protein-1c (SREBP-1c) and glucose transporter 2 (GLUT-2) were both restored to normal control levels following treatment with GW501516. GW 501516 240-248 solute carrier family 2 member 2 Rattus norvegicus 163-169 26111938-6 2015 Increasing BH4 bioavailability either exogenously by BH4 supplementation or endogenously by treatment with the selective peroxisome proliferator-activated receptor--delta activator GW501516 (2 mg/kg/day, 14 days) attenuated eNOS uncoupling and decreased superoxide anion production in cerebral microvessels of Tg2576 mice (p < 0.05). GW 501516 181-189 nitric oxide synthase 3, endothelial cell Mus musculus 224-228 25943561-0 2015 A metabolomic study of the PPARdelta agonist GW501516 for enhancing running endurance in Kunming mice. GW 501516 45-53 peroxisome proliferator activator receptor delta Mus musculus 27-36 25857370-8 2015 KEY RESULTS: PPAR-delta agonist GW501516 decreased uptake of VLDL and expression of VLDL receptor at mRNA and protein levels. GW 501516 32-40 peroxisome proliferator activated receptor delta Homo sapiens 13-23 25857370-8 2015 KEY RESULTS: PPAR-delta agonist GW501516 decreased uptake of VLDL and expression of VLDL receptor at mRNA and protein levels. GW 501516 32-40 very low density lipoprotein receptor Homo sapiens 84-97 25857370-9 2015 GW501516 inhibited the luciferase reporter activity of the 3"-UTR of VLDL receptor. GW 501516 0-8 very low density lipoprotein receptor Homo sapiens 69-82 25857370-11 2015 miR-100 was significantly increased by GW501516 in HUVECs. GW 501516 39-47 microRNA 100 Homo sapiens 0-7 25943561-3 2015 This study utilized metabolomic profiling to examine the effects of GW501516, a PPARdelta agonist, on running endurance in mice. GW 501516 68-76 peroxisome proliferator activator receptor delta Mus musculus 80-89 25943561-4 2015 While training alone increased the exhaustive running performance, GW501516 treatment enhanced running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice. GW 501516 67-75 aminoadipate-semialdehyde synthase Mus musculus 135-158 25943561-4 2015 While training alone increased the exhaustive running performance, GW501516 treatment enhanced running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice. GW 501516 67-75 aminoadipate-semialdehyde synthase Mus musculus 160-163 25331977-5 2015 METHODS: Mouse chondrocytes and knee explants were treated with a pharmacologic agonist of PPARdelta (GW501516) to evaluate changes in gene expression, histologic features, and matrix glycosaminoglycan breakdown. GW 501516 102-110 peroxisome proliferator activator receptor delta Mus musculus 91-100 25713305-14 2015 Skeletal muscle dysfunction in HF is associated with impaired PPARdelta signaling and treatment with the PPARdelta agonist GW501516 corrects oxidative capacity and FA metabolism and improves exercise capacity in mice with LV dysfunction. GW 501516 123-131 peroxisome proliferator activator receptor delta Mus musculus 105-114 25732738-4 2015 Activation of PPARdelta by GW501516, which is a specific ligand, significantly inhibited oxLDL-induced cell death and generation of reactive oxygen species in VSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 25728706-4 2015 Cultured adipocytes exposed to fructose also exhibited increased CD36 protein levels and this increase was prevented by the PPARbeta/delta activator GW501516. GW 501516 149-157 peroxisome proliferator activator receptor delta Mus musculus 124-132 25728706-5 2015 Interestingly, the levels of the nuclear factor E2-related factor 2 (Nrf2), a transcription factor reported to up-regulate Cd36 expression and to impair insulin signaling, were increased in fructose-exposed adipocytes whereas co-incubation with GW501516 abolished this increase. GW 501516 245-253 nuclear factor, erythroid derived 2, like 2 Mus musculus 69-73 25527525-6 2015 The decreased expression of Bcl-2 and the increased expression of cleaved-caspase-3 induced by Sept4_i1 could be reversed by GW501516, a PPAR-beta/delta agonist that has been reported by others to enhance Akt signaling. GW 501516 125-133 BCL2 apoptosis regulator Homo sapiens 28-33 25527525-6 2015 The decreased expression of Bcl-2 and the increased expression of cleaved-caspase-3 induced by Sept4_i1 could be reversed by GW501516, a PPAR-beta/delta agonist that has been reported by others to enhance Akt signaling. GW 501516 125-133 caspase 3 Homo sapiens 74-83 25527525-6 2015 The decreased expression of Bcl-2 and the increased expression of cleaved-caspase-3 induced by Sept4_i1 could be reversed by GW501516, a PPAR-beta/delta agonist that has been reported by others to enhance Akt signaling. GW 501516 125-133 peroxisome proliferator activated receptor delta Homo sapiens 137-146 25527525-6 2015 The decreased expression of Bcl-2 and the increased expression of cleaved-caspase-3 induced by Sept4_i1 could be reversed by GW501516, a PPAR-beta/delta agonist that has been reported by others to enhance Akt signaling. GW 501516 125-133 AKT serine/threonine kinase 1 Homo sapiens 205-208 25331977-8 2015 RESULTS: In vitro, PPARdelta activation by GW501516 resulted in increased expression of several proteases in chondrocytes, as well as aggrecan degradation and glycosaminoglycan release in knee joint explants. GW 501516 43-51 peroxisome proliferator activator receptor delta Mus musculus 19-28 25449811-0 2015 Early controlled release of peroxisome proliferator-activated receptor beta/delta agonist GW501516 improves diabetic wound healing through redox modulation of wound microenvironment. GW 501516 90-98 peroxisome proliferator activated receptor delta Homo sapiens 28-75 25449811-5 2015 The underlying mechanism involved an early GW-mediated activation of PPARbeta/delta that stimulated GPx1 and catalase expression in fibroblasts. GW 501516 43-45 peroxisome proliferator activated receptor delta Homo sapiens 69-77 25449811-5 2015 The underlying mechanism involved an early GW-mediated activation of PPARbeta/delta that stimulated GPx1 and catalase expression in fibroblasts. GW 501516 43-45 glutathione peroxidase 1 Homo sapiens 100-104 25449811-5 2015 The underlying mechanism involved an early GW-mediated activation of PPARbeta/delta that stimulated GPx1 and catalase expression in fibroblasts. GW 501516 43-45 catalase Homo sapiens 109-117 25277864-10 2015 NM23-H2 siRNA activated PPARdelta luciferase promoter activity, upregulated PPARdelta RNA and protein expression and increased GW501516-stimulated CCA growth. GW 501516 127-135 NME/NM23 nucleoside diphosphate kinase 2 Homo sapiens 0-7 25277864-11 2015 Overexpression of NM23-H2 inhibited PPARdelta luciferase promoter activity, downregulated PPARdelta expression and AKT phosphorylation and reduced GW501516-stimulated CCA growth. GW 501516 147-155 NME/NM23 nucleoside diphosphate kinase 2 Homo sapiens 18-25 25063273-4 2014 RESULTS: The PPARbeta/delta agonist GW501516 prevented lipid-induced ER stress in mouse and human myotubes and in skeletal muscle of mice fed a high-fat diet. GW 501516 36-44 peroxisome proliferator activator receptor delta Mus musculus 13-21 26604919-4 2015 Mice conditionally expressing human PPARdelta demonstrated pronounced weight loss and promoted hepatic steatosis when treated with GW501516 (PPARdelta-agonist) when compared to wild type mice. GW 501516 131-139 peroxisome proliferator activated receptor delta Homo sapiens 36-45 26604919-4 2015 Mice conditionally expressing human PPARdelta demonstrated pronounced weight loss and promoted hepatic steatosis when treated with GW501516 (PPARdelta-agonist) when compared to wild type mice. GW 501516 131-139 peroxisome proliferator activated receptor delta Homo sapiens 141-150 26604919-6 2015 This confirmed the absolute requirement for PPARdelta in the physiological actions of GW501516 and confirmed the potential utility against the human form of this receptor. GW 501516 86-94 peroxisome proliferator activated receptor delta Homo sapiens 44-53 26604919-7 2015 Surprisingly the genetic deletion of PPARalpha also abrogated the effect of GW501516 in terms of both weight loss and hepatic lipid accumulation. GW 501516 76-84 peroxisome proliferator activated receptor alpha Mus musculus 37-46 26604919-9 2015 Our results show that both PPARdelta and PPARalpha receptors are essential for GW501516-driven adipose tissue reduction and subsequently hepatic steatosis, with PPARalpha working downstream of PPARdelta. GW 501516 79-87 peroxisome proliferator activator receptor delta Mus musculus 27-36 26604919-9 2015 Our results show that both PPARdelta and PPARalpha receptors are essential for GW501516-driven adipose tissue reduction and subsequently hepatic steatosis, with PPARalpha working downstream of PPARdelta. GW 501516 79-87 peroxisome proliferator activated receptor alpha Mus musculus 41-50 26604919-9 2015 Our results show that both PPARdelta and PPARalpha receptors are essential for GW501516-driven adipose tissue reduction and subsequently hepatic steatosis, with PPARalpha working downstream of PPARdelta. GW 501516 79-87 peroxisome proliferator activated receptor alpha Mus musculus 161-170 26604919-9 2015 Our results show that both PPARdelta and PPARalpha receptors are essential for GW501516-driven adipose tissue reduction and subsequently hepatic steatosis, with PPARalpha working downstream of PPARdelta. GW 501516 79-87 peroxisome proliferator activator receptor delta Mus musculus 193-202 25520859-4 2014 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly increased the migration and invasion of highly metastatic A375SM cells, but not that of low metastatic A375P cells. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 25520859-4 2014 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly increased the migration and invasion of highly metastatic A375SM cells, but not that of low metastatic A375P cells. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 59-68 25520859-6 2014 Furthermore, a significant concentration- and time-dependent increase in the levels of Snail mRNA and protein was observed in A375SM cells (but not A375P cells) treated with GW501516. GW 501516 174-182 snail family transcriptional repressor 1 Homo sapiens 87-92 25520859-7 2014 The effects of GW501516 were almost completely abrogated by a small interfering RNA against PPARdelta, suggesting that PPARdelta mediates the effects of GW501516. GW 501516 15-23 peroxisome proliferator activated receptor delta Homo sapiens 92-101 25520859-7 2014 The effects of GW501516 were almost completely abrogated by a small interfering RNA against PPARdelta, suggesting that PPARdelta mediates the effects of GW501516. GW 501516 15-23 peroxisome proliferator activated receptor delta Homo sapiens 119-128 25520859-7 2014 The effects of GW501516 were almost completely abrogated by a small interfering RNA against PPARdelta, suggesting that PPARdelta mediates the effects of GW501516. GW 501516 153-161 peroxisome proliferator activated receptor delta Homo sapiens 92-101 25520859-7 2014 The effects of GW501516 were almost completely abrogated by a small interfering RNA against PPARdelta, suggesting that PPARdelta mediates the effects of GW501516. GW 501516 153-161 peroxisome proliferator activated receptor delta Homo sapiens 119-128 25149191-6 2014 Activation of PPARdelta by GW501516, a ligand specific for PPARdelta, markedly attenuated UVB-induced MMP-2 secretion with a concomitant increase in the level of elastin. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 25149191-6 2014 Activation of PPARdelta by GW501516, a ligand specific for PPARdelta, markedly attenuated UVB-induced MMP-2 secretion with a concomitant increase in the level of elastin. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 59-68 25149191-8 2014 Furthermore, GW501516 elicited a dose- and time-dependent increase in the expression of elastin. GW 501516 13-21 elastin Homo sapiens 88-95 25149191-6 2014 Activation of PPARdelta by GW501516, a ligand specific for PPARdelta, markedly attenuated UVB-induced MMP-2 secretion with a concomitant increase in the level of elastin. GW 501516 27-35 matrix metallopeptidase 2 Homo sapiens 102-107 25149191-9 2014 Modulation of MMP-2 secretion and elastin levels by GW501516 was associated with a reduction in reactive oxygen species (ROS) production in HDFs exposed to UVB. GW 501516 52-60 matrix metallopeptidase 2 Homo sapiens 14-19 25149191-9 2014 Modulation of MMP-2 secretion and elastin levels by GW501516 was associated with a reduction in reactive oxygen species (ROS) production in HDFs exposed to UVB. GW 501516 52-60 elastin Homo sapiens 34-41 25149191-6 2014 Activation of PPARdelta by GW501516, a ligand specific for PPARdelta, markedly attenuated UVB-induced MMP-2 secretion with a concomitant increase in the level of elastin. GW 501516 27-35 elastin Homo sapiens 162-169 25149191-10 2014 Finally, in HR-1 hairless mice, administration of GW501516 significantly reduced UVB-induced MMP-2 expression with a concomitant increase in elastin levels, and these effects were significantly reduced by the presence of GSK0660. GW 501516 50-58 matrix metallopeptidase 2 Mus musculus 93-98 24920036-6 2014 Subsequent immunoblotting experiments provided evidence for positive correlation of PPARD level and AKT and ERK signaling pathways upon GW501516 treatment. GW 501516 136-144 peroxisome proliferator activator receptor delta Mus musculus 84-89 25149191-10 2014 Finally, in HR-1 hairless mice, administration of GW501516 significantly reduced UVB-induced MMP-2 expression with a concomitant increase in elastin levels, and these effects were significantly reduced by the presence of GSK0660. GW 501516 50-58 elastin Mus musculus 141-148 24920036-6 2014 Subsequent immunoblotting experiments provided evidence for positive correlation of PPARD level and AKT and ERK signaling pathways upon GW501516 treatment. GW 501516 136-144 thymoma viral proto-oncogene 1 Mus musculus 100-103 24920036-7 2014 Furthermore, the stimulation of GW501516 increased trophoblast cell fusion gene syncytin-A (Syna), but not syncytin-B (Synb), expression, suggesting a potential role of Ppard activation in promoting cytotrophoblast differentiation. GW 501516 32-40 syncytin a Mus musculus 80-90 24920036-7 2014 Furthermore, the stimulation of GW501516 increased trophoblast cell fusion gene syncytin-A (Syna), but not syncytin-B (Synb), expression, suggesting a potential role of Ppard activation in promoting cytotrophoblast differentiation. GW 501516 32-40 syncytin a Mus musculus 92-96 24920036-7 2014 Furthermore, the stimulation of GW501516 increased trophoblast cell fusion gene syncytin-A (Syna), but not syncytin-B (Synb), expression, suggesting a potential role of Ppard activation in promoting cytotrophoblast differentiation. GW 501516 32-40 peroxisome proliferator activator receptor delta Mus musculus 169-174 24864274-8 2014 Similarly, PPARdelta-mediated attenuation of FA synthesis was partially due to AMPK activation, as GW1516 reduced lipogenesis in WT hepatocytes but not AMPKbeta1(-/-) hepatocytes. GW 501516 99-105 peroxisome proliferator activator receptor delta Mus musculus 11-20 25116592-7 2014 We first confirmed the suppression of PPARdelta both in LR and human hepatocellular carcinoma at protein level, and then demonstrated that PPARdelta agonist GW501516 reduces the proliferative potential of hepatoma cells. GW 501516 157-165 peroxisome proliferator activated receptor delta Homo sapiens 38-47 25116592-7 2014 We first confirmed the suppression of PPARdelta both in LR and human hepatocellular carcinoma at protein level, and then demonstrated that PPARdelta agonist GW501516 reduces the proliferative potential of hepatoma cells. GW 501516 157-165 peroxisome proliferator activated receptor delta Homo sapiens 139-148 25179079-0 2014 Metabolic modulators of the exercise response: doping control analysis of an agonist of the peroxisome proliferator-activated receptor delta (GW501516) and 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR). GW 501516 142-150 peroxisome proliferator activated receptor delta Homo sapiens 92-140 24482374-9 2014 Metformin and PPARdelta agonist GW1516 reversed tunicamycin (ER stress inducer)-induced ER stress, oxidative stress, and impairment of endothelium-dependent relaxation in mouse aortae as well as NO production in mouse aortic endothelial cells. GW 501516 32-38 peroxisome proliferator activator receptor delta Mus musculus 14-23 24628018-8 2014 Blood-extracted CD34(+) cells cultured with IL-5 or IL-5 + IL-3 formed Eo/B CFU, which were significantly inhibited by rosiglitazone (100 nm, P < 0 01) but not GW9578 or GW501516. GW 501516 173-181 CD34 antigen Mus musculus 16-20 24628018-8 2014 Blood-extracted CD34(+) cells cultured with IL-5 or IL-5 + IL-3 formed Eo/B CFU, which were significantly inhibited by rosiglitazone (100 nm, P < 0 01) but not GW9578 or GW501516. GW 501516 173-181 interleukin 5 Mus musculus 44-48 24628018-8 2014 Blood-extracted CD34(+) cells cultured with IL-5 or IL-5 + IL-3 formed Eo/B CFU, which were significantly inhibited by rosiglitazone (100 nm, P < 0 01) but not GW9578 or GW501516. GW 501516 173-181 interleukin 5 Mus musculus 52-56 24628018-8 2014 Blood-extracted CD34(+) cells cultured with IL-5 or IL-5 + IL-3 formed Eo/B CFU, which were significantly inhibited by rosiglitazone (100 nm, P < 0 01) but not GW9578 or GW501516. GW 501516 173-181 interleukin 3 Mus musculus 59-63 24337677-7 2014 Moreover, GW501516 was found to attenuate glucose-stimulated inflammation in cultured rat peritoneal mesothelial cells via inhibition of transforming growth factor-beta-activated kinase 1 (TAK1), and nuclear factor kappa B (NFkappaB) signaling pathway (TAK1-NFkappaB pathway), a main inflammation regulatory pathway. GW 501516 10-18 nuclear factor kappa B subunit 1 Homo sapiens 258-266 24337677-8 2014 In conclusion, inhibition of TAK1-NFkappaB pathway with GW501516 may represent a novel therapeutic approach to ameliorate peritonitis-induced peritoneal fibrosis for patients on PD. GW 501516 56-64 mitogen-activated protein kinase kinase kinase 7 Homo sapiens 29-33 24337677-8 2014 In conclusion, inhibition of TAK1-NFkappaB pathway with GW501516 may represent a novel therapeutic approach to ameliorate peritonitis-induced peritoneal fibrosis for patients on PD. GW 501516 56-64 nuclear factor kappa B subunit 1 Homo sapiens 34-42 24698256-5 2014 Co-infusion of GW501516, an activator of PPARdelta, attenuated both the incidence and the severity of Ang II-induced AAA in apoE-deficient mice. GW 501516 15-23 peroxisome proliferator activator receptor delta Mus musculus 41-50 24698256-5 2014 Co-infusion of GW501516, an activator of PPARdelta, attenuated both the incidence and the severity of Ang II-induced AAA in apoE-deficient mice. GW 501516 15-23 angiotensinogen (serpin peptidase inhibitor, clade A, member 8) Mus musculus 102-108 24698256-5 2014 Co-infusion of GW501516, an activator of PPARdelta, attenuated both the incidence and the severity of Ang II-induced AAA in apoE-deficient mice. GW 501516 15-23 apolipoprotein E Mus musculus 124-128 24698256-7 2014 The anti-inflammatory effect of GW501516 was associated with the suppression of apoptotic cell death, along with the inhibition of medial smooth muscle cell loss and focal elastin destruction, which leads to a medial dissection and aortic rupture. GW 501516 32-40 elastin Mus musculus 172-179 24698256-8 2014 These ameliorative effects of GW501516 on Ang II-induced aneurysm were correlated with increased expression of extracellular matrix (ECM) proteins, such as types I and III collagen, fibronectin, and elastin, along with the up-regulation of transforming growth factor-beta1. GW 501516 30-38 angiotensinogen (serpin peptidase inhibitor, clade A, member 8) Mus musculus 42-48 24698256-8 2014 These ameliorative effects of GW501516 on Ang II-induced aneurysm were correlated with increased expression of extracellular matrix (ECM) proteins, such as types I and III collagen, fibronectin, and elastin, along with the up-regulation of transforming growth factor-beta1. GW 501516 30-38 fibronectin 1 Mus musculus 182-193 24698256-8 2014 These ameliorative effects of GW501516 on Ang II-induced aneurysm were correlated with increased expression of extracellular matrix (ECM) proteins, such as types I and III collagen, fibronectin, and elastin, along with the up-regulation of transforming growth factor-beta1. GW 501516 30-38 elastin Mus musculus 199-206 24698256-8 2014 These ameliorative effects of GW501516 on Ang II-induced aneurysm were correlated with increased expression of extracellular matrix (ECM) proteins, such as types I and III collagen, fibronectin, and elastin, along with the up-regulation of transforming growth factor-beta1. GW 501516 30-38 transforming growth factor, beta 1 Mus musculus 240-272 24337677-0 2014 The PPARbeta/delta agonist GW501516 attenuates peritonitis in peritoneal fibrosis via inhibition of TAK1-NFkappaB pathway in rats. GW 501516 27-35 peroxisome proliferator-activated receptor delta Rattus norvegicus 4-12 24337677-0 2014 The PPARbeta/delta agonist GW501516 attenuates peritonitis in peritoneal fibrosis via inhibition of TAK1-NFkappaB pathway in rats. GW 501516 27-35 mitogen activated protein kinase kinase kinase 7 Rattus norvegicus 100-104 24337677-0 2014 The PPARbeta/delta agonist GW501516 attenuates peritonitis in peritoneal fibrosis via inhibition of TAK1-NFkappaB pathway in rats. GW 501516 27-35 nuclear factor kappa B subunit 1 Homo sapiens 105-113 24337677-6 2014 Compared to control group, exposure to PD fluids caused peritoneal fibrosis that was accompanied by increased mRNA levels of monocyte chemoattractant protein-1, tumor necrotic factor-alpha, and interleukin-6 in the uremic rats, and these effects were prevented by GW501516 treatment. GW 501516 264-272 C-C motif chemokine ligand 2 Rattus norvegicus 125-188 24337677-7 2014 Moreover, GW501516 was found to attenuate glucose-stimulated inflammation in cultured rat peritoneal mesothelial cells via inhibition of transforming growth factor-beta-activated kinase 1 (TAK1), and nuclear factor kappa B (NFkappaB) signaling pathway (TAK1-NFkappaB pathway), a main inflammation regulatory pathway. GW 501516 10-18 mitogen activated protein kinase kinase kinase 7 Rattus norvegicus 137-187 24337677-7 2014 Moreover, GW501516 was found to attenuate glucose-stimulated inflammation in cultured rat peritoneal mesothelial cells via inhibition of transforming growth factor-beta-activated kinase 1 (TAK1), and nuclear factor kappa B (NFkappaB) signaling pathway (TAK1-NFkappaB pathway), a main inflammation regulatory pathway. GW 501516 10-18 mitogen activated protein kinase kinase kinase 7 Rattus norvegicus 189-193 24337677-7 2014 Moreover, GW501516 was found to attenuate glucose-stimulated inflammation in cultured rat peritoneal mesothelial cells via inhibition of transforming growth factor-beta-activated kinase 1 (TAK1), and nuclear factor kappa B (NFkappaB) signaling pathway (TAK1-NFkappaB pathway), a main inflammation regulatory pathway. GW 501516 10-18 nuclear factor kappa B subunit 1 Homo sapiens 224-232 24337677-7 2014 Moreover, GW501516 was found to attenuate glucose-stimulated inflammation in cultured rat peritoneal mesothelial cells via inhibition of transforming growth factor-beta-activated kinase 1 (TAK1), and nuclear factor kappa B (NFkappaB) signaling pathway (TAK1-NFkappaB pathway), a main inflammation regulatory pathway. GW 501516 10-18 mitogen activated protein kinase kinase kinase 7 Rattus norvegicus 253-257 24767130-6 2014 Our results demonstrate that palmitate induced ER stress in AC16 cells, a fact which was prevented after PPARbeta/delta activation with GW501516. GW 501516 136-144 peroxisome proliferator activated receptor delta Homo sapiens 105-113 24767130-7 2014 Interestingly, the effect of GW501516 on ER stress occurred in an AMPK-independent manner. GW 501516 29-37 protein kinase AMP-activated non-catalytic subunit beta 1 Homo sapiens 66-70 24767130-8 2014 The most striking result of this study is that GW501516 treatment also upregulated the protein levels of beclin 1 and LC3II, two well-known markers of autophagy. GW 501516 47-55 beclin 1 Homo sapiens 105-113 23991827-2 2014 Only 21 genes were up-regulated and 3 genes were down-regulated after activation by the PPARdelta agonist GW501516. GW 501516 106-114 peroxisome proliferator activated receptor delta Homo sapiens 88-97 23779049-4 2014 METHOD: We first established a direct stimulatory effect of the PPARdelta agonist (GW 501516) on the HO-1 gene by demonstrating increased luciferase activity in COS-7 cells transfected with a luciferase-HO-1 promoter construct. GW 501516 83-92 peroxisome proliferator-activated receptor delta Rattus norvegicus 64-73 23779049-4 2014 METHOD: We first established a direct stimulatory effect of the PPARdelta agonist (GW 501516) on the HO-1 gene by demonstrating increased luciferase activity in COS-7 cells transfected with a luciferase-HO-1 promoter construct. GW 501516 83-92 heme oxygenase 1 Rattus norvegicus 101-105 23779049-4 2014 METHOD: We first established a direct stimulatory effect of the PPARdelta agonist (GW 501516) on the HO-1 gene by demonstrating increased luciferase activity in COS-7 cells transfected with a luciferase-HO-1 promoter construct. GW 501516 83-92 heme oxygenase 1 Rattus norvegicus 203-207 24287635-3 2014 Exposure of U937 cells to the PPARdelta agonist GW501516 resulted in a marked increase in mRNA expression of the PPARdelta target gene Angptl4 which was quantified by qRT-PCR analysis. GW 501516 48-56 peroxisome proliferator activated receptor delta Homo sapiens 30-39 24269940-10 2014 GW enhanced glucose-stimulated insulin secretion (GSIS) impaired by PA through stimulation of GLP-1R expression in beta cells. GW 501516 0-2 glucagon-like peptide 1 receptor Rattus norvegicus 94-100 24287635-3 2014 Exposure of U937 cells to the PPARdelta agonist GW501516 resulted in a marked increase in mRNA expression of the PPARdelta target gene Angptl4 which was quantified by qRT-PCR analysis. GW 501516 48-56 peroxisome proliferator activated receptor delta Homo sapiens 113-122 24287635-3 2014 Exposure of U937 cells to the PPARdelta agonist GW501516 resulted in a marked increase in mRNA expression of the PPARdelta target gene Angptl4 which was quantified by qRT-PCR analysis. GW 501516 48-56 angiopoietin like 4 Homo sapiens 135-142 24287635-4 2014 Exposure of HepG2 cells transiently transfected with a PPARdelta expression plasmid and a PPAR-response element-driven luciferase reporter plasmid to PPARdelta agonists GW501516, GW610742 and L-165041 resulted in clear dose-response curves. GW 501516 169-177 peroxisome proliferator activated receptor delta Homo sapiens 150-159 24158519-0 2014 Peroxisome proliferator-activated receptor delta agonist GW1516 attenuates diet-induced aortic inflammation, insulin resistance, and atherosclerosis in low-density lipoprotein receptor knockout mice. GW 501516 57-63 low density lipoprotein receptor Mus musculus 152-184 24158519-8 2014 In aortae, GW1516 increased the expression of the PPARdelta-specific gene Adfp but not PPARalpha- or gamma-specific genes. GW 501516 11-17 peroxisome proliferator activator receptor delta Mus musculus 50-59 24158519-0 2014 Peroxisome proliferator-activated receptor delta agonist GW1516 attenuates diet-induced aortic inflammation, insulin resistance, and atherosclerosis in low-density lipoprotein receptor knockout mice. GW 501516 57-63 peroxisome proliferator activator receptor delta Mus musculus 0-48 24158519-8 2014 In aortae, GW1516 increased the expression of the PPARdelta-specific gene Adfp but not PPARalpha- or gamma-specific genes. GW 501516 11-17 perilipin 2 Mus musculus 74-78 24158519-9 2014 GW1516 intervention decreased the expression of aortic proinflammatory M1 cytokines, increased the expression of the anti-inflammatory M2 cytokine Arg1, and attenuated the iNos/Arg1 ratio. GW 501516 0-6 arginase, liver Mus musculus 147-151 24158519-9 2014 GW1516 intervention decreased the expression of aortic proinflammatory M1 cytokines, increased the expression of the anti-inflammatory M2 cytokine Arg1, and attenuated the iNos/Arg1 ratio. GW 501516 0-6 nitric oxide synthase 2, inducible Mus musculus 172-176 24158519-9 2014 GW1516 intervention decreased the expression of aortic proinflammatory M1 cytokines, increased the expression of the anti-inflammatory M2 cytokine Arg1, and attenuated the iNos/Arg1 ratio. GW 501516 0-6 arginase, liver Mus musculus 177-181 21920965-7 2013 In a mouse hindlimb ischaemia model, systemic treatment of GW501516 or local transplantation of GW501516-treated EPCs induced IGF-1R phosphorylation in ECs and skeletal muscle in the ischaemic limbs, leading to augmented angiogenesis and skeletal muscle regeneration. GW 501516 59-67 insulin-like growth factor I receptor Mus musculus 126-132 24890166-17 2014 In vitro, GW501516 and over-expression of PPARbeta/delta attenuated gene expression of TNF-alpha, IL-1beta and IL-6 in alveolar macrophages. GW 501516 10-18 tumor necrosis factor Rattus norvegicus 87-96 24890166-17 2014 In vitro, GW501516 and over-expression of PPARbeta/delta attenuated gene expression of TNF-alpha, IL-1beta and IL-6 in alveolar macrophages. GW 501516 10-18 interleukin 1 beta Rattus norvegicus 98-106 24890166-17 2014 In vitro, GW501516 and over-expression of PPARbeta/delta attenuated gene expression of TNF-alpha, IL-1beta and IL-6 in alveolar macrophages. GW 501516 10-18 interleukin 6 Rattus norvegicus 111-115 25116733-2 2014 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, attenuated Ang II-induced activation of MMP-2 in a concentration-dependent manner. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 25116733-2 2014 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, attenuated Ang II-induced activation of MMP-2 in a concentration-dependent manner. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 59-68 25116733-2 2014 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, attenuated Ang II-induced activation of MMP-2 in a concentration-dependent manner. GW 501516 27-35 matrix metallopeptidase 2 Homo sapiens 110-115 25116733-4 2014 A marked increase in the mRNA levels of tissue inhibitor of metalloproteinase (TIMP)-2 and -3, endogenous antagonists of MMPs, was also observed in GW501516-treated VSMCs. GW 501516 148-156 TIMP metallopeptidase inhibitor 2 Homo sapiens 40-93 25116733-4 2014 A marked increase in the mRNA levels of tissue inhibitor of metalloproteinase (TIMP)-2 and -3, endogenous antagonists of MMPs, was also observed in GW501516-treated VSMCs. GW 501516 148-156 matrix metallopeptidase 2 Homo sapiens 121-125 25116733-5 2014 These effects were markedly reduced in the presence of siRNAs against PPARdelta, indicating that the effects of GW501516 are PPARdelta dependent. GW 501516 112-120 peroxisome proliferator activated receptor delta Homo sapiens 70-79 25116733-5 2014 These effects were markedly reduced in the presence of siRNAs against PPARdelta, indicating that the effects of GW501516 are PPARdelta dependent. GW 501516 112-120 peroxisome proliferator activated receptor delta Homo sapiens 125-134 25116733-6 2014 Among the protein kinases inhibited by GW501516, suppression of phosphatidylinositol 3-kinase/Akt signaling was shown to have the greatest effect on activation of MMP-2 in VSMCs treated with Ang II. GW 501516 39-47 AKT serine/threonine kinase 1 Homo sapiens 94-97 25116733-6 2014 Among the protein kinases inhibited by GW501516, suppression of phosphatidylinositol 3-kinase/Akt signaling was shown to have the greatest effect on activation of MMP-2 in VSMCs treated with Ang II. GW 501516 39-47 matrix metallopeptidase 2 Homo sapiens 163-168 25116733-7 2014 Concomitantly, GW501516-mediated inhibition of MMP-2 activation in VSMCs treated with Ang II was associated with the suppression of cell migration to levels approaching those in cells not exposed to Ang II. GW 501516 15-23 matrix metallopeptidase 2 Homo sapiens 47-52 23943160-4 2013 We found that when activated with the highly selective PPARbeta/delta agonists, GW0742 and GW501516, PPARbeta/delta inhibited the proliferation and markedly induced the apoptosis of three endometrial cancer cell lines. GW 501516 91-99 peroxisome proliferator activated receptor delta Homo sapiens 55-63 23943160-4 2013 We found that when activated with the highly selective PPARbeta/delta agonists, GW0742 and GW501516, PPARbeta/delta inhibited the proliferation and markedly induced the apoptosis of three endometrial cancer cell lines. GW 501516 91-99 peroxisome proliferator activated receptor delta Homo sapiens 101-109 23639976-2 2013 In human dermal fibroblasts (HDFs), activation of PPARdelta by its specific ligand GW501516 markedly attenuated UVB-induced secretion of matrix metalloproteinase (MMP)-1, concomitant with decreased generation of reactive oxygen species. GW 501516 83-91 peroxisome proliferator activated receptor delta Homo sapiens 50-59 23639976-2 2013 In human dermal fibroblasts (HDFs), activation of PPARdelta by its specific ligand GW501516 markedly attenuated UVB-induced secretion of matrix metalloproteinase (MMP)-1, concomitant with decreased generation of reactive oxygen species. GW 501516 83-91 matrix metallopeptidase 1 Homo sapiens 137-169 23639976-5 2013 PPARdelta-mediated messenger RNA stabilization of mitogen-activated protein kinase phosphatase (MKP)-7 was responsible for the GW501516-mediated inhibition of JNK signaling. GW 501516 127-135 peroxisome proliferator activated receptor delta Homo sapiens 0-9 23639976-5 2013 PPARdelta-mediated messenger RNA stabilization of mitogen-activated protein kinase phosphatase (MKP)-7 was responsible for the GW501516-mediated inhibition of JNK signaling. GW 501516 127-135 dual specificity phosphatase 16 Homo sapiens 96-102 23639976-5 2013 PPARdelta-mediated messenger RNA stabilization of mitogen-activated protein kinase phosphatase (MKP)-7 was responsible for the GW501516-mediated inhibition of JNK signaling. GW 501516 127-135 mitogen-activated protein kinase 8 Homo sapiens 159-162 23639976-7 2013 Finally, in HR-1 hairless mice exposed to UVB, administration of GW501516 significantly reduced wrinkle formation and skin thickness, downregulated MMP-1 and JNK phosphorylation, and restored the levels of MKP-7, types I and III collagen. GW 501516 65-73 matrix metallopeptidase 13 Mus musculus 148-153 23639976-7 2013 Finally, in HR-1 hairless mice exposed to UVB, administration of GW501516 significantly reduced wrinkle formation and skin thickness, downregulated MMP-1 and JNK phosphorylation, and restored the levels of MKP-7, types I and III collagen. GW 501516 65-73 mitogen-activated protein kinase 8 Mus musculus 158-161 23639976-7 2013 Finally, in HR-1 hairless mice exposed to UVB, administration of GW501516 significantly reduced wrinkle formation and skin thickness, downregulated MMP-1 and JNK phosphorylation, and restored the levels of MKP-7, types I and III collagen. GW 501516 65-73 dual specificity phosphatase 16 Mus musculus 206-211 23811944-4 2013 Multiparous mice presented with mammary carcinomas after a latency of 12 months, and administration of the PPARdelta ligand GW501516 reduced tumor latency to 5 months. GW 501516 124-132 peroxisome proliferator activator receptor delta Mus musculus 107-116 23811944-5 2013 Histopathologic changes occurred concurrently with an increase in an inflammatory, invasive, metabolic, and proliferative gene signature, including expression of the trophoblast gene, Plac1, beginning 1 week after GW501516 treatment, and remained elevated throughout tumorigenesis. GW 501516 214-222 placental specific protein 1 Mus musculus 184-189 21920965-3 2013 METHODS AND RESULTS: Treatment of EPCs with GW501516, a PPAR-delta agonist, induced specifically matrix metallo-proteinase (MMP)-9 by direct transcriptional activation. GW 501516 44-52 peroxisome proliferator activator receptor delta Mus musculus 56-66 21920965-3 2013 METHODS AND RESULTS: Treatment of EPCs with GW501516, a PPAR-delta agonist, induced specifically matrix metallo-proteinase (MMP)-9 by direct transcriptional activation. GW 501516 44-52 matrix metallopeptidase 9 Mus musculus 97-130 21920965-5 2013 Treatment of conditioned medium from GW501516-stimulated EPCs enhanced the number and functions of human umbilical vein ECs and C2C12 myoblasts via MMP-9-mediated IGF-1R activation. GW 501516 37-45 matrix metallopeptidase 9 Homo sapiens 148-153 21920965-5 2013 Treatment of conditioned medium from GW501516-stimulated EPCs enhanced the number and functions of human umbilical vein ECs and C2C12 myoblasts via MMP-9-mediated IGF-1R activation. GW 501516 37-45 insulin like growth factor 1 receptor Homo sapiens 163-169 21920965-6 2013 Systemic administration of GW501516 in mice increased MMP-9 expression in EPCs, and augmented IGFBP-3 degradation in serum. GW 501516 27-35 matrix metallopeptidase 9 Mus musculus 54-59 21920965-6 2013 Systemic administration of GW501516 in mice increased MMP-9 expression in EPCs, and augmented IGFBP-3 degradation in serum. GW 501516 27-35 insulin-like growth factor binding protein 3 Mus musculus 94-101 21920965-7 2013 In a mouse hindlimb ischaemia model, systemic treatment of GW501516 or local transplantation of GW501516-treated EPCs induced IGF-1R phosphorylation in ECs and skeletal muscle in the ischaemic limbs, leading to augmented angiogenesis and skeletal muscle regeneration. GW 501516 96-104 insulin-like growth factor I receptor Mus musculus 126-132 23849213-9 2013 GW501516 treatment also increased Lipin1 protein levels in the nucleus, led to the amplification of the PGC-1alpha-PPARalpha pathway and increased PPARalpha DNA-binding activity, as well as the expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 lipin 1 Mus musculus 34-40 23611928-1 2013 OBJECTIVES: This study aimed to measure the effects of peroxisome proliferator-activated receptor-delta (PPARdelta) agonist GW501516 (GW) and zinc sulfate (ZS) on ovariectomized rats" vaginal histomorphology and collagen expression. GW 501516 124-132 peroxisome proliferator-activated receptor delta Rattus norvegicus 55-103 23611928-1 2013 OBJECTIVES: This study aimed to measure the effects of peroxisome proliferator-activated receptor-delta (PPARdelta) agonist GW501516 (GW) and zinc sulfate (ZS) on ovariectomized rats" vaginal histomorphology and collagen expression. GW 501516 124-132 peroxisome proliferator-activated receptor delta Rattus norvegicus 105-114 23611928-1 2013 OBJECTIVES: This study aimed to measure the effects of peroxisome proliferator-activated receptor-delta (PPARdelta) agonist GW501516 (GW) and zinc sulfate (ZS) on ovariectomized rats" vaginal histomorphology and collagen expression. GW 501516 124-126 peroxisome proliferator-activated receptor delta Rattus norvegicus 55-103 23611928-1 2013 OBJECTIVES: This study aimed to measure the effects of peroxisome proliferator-activated receptor-delta (PPARdelta) agonist GW501516 (GW) and zinc sulfate (ZS) on ovariectomized rats" vaginal histomorphology and collagen expression. GW 501516 124-126 peroxisome proliferator-activated receptor delta Rattus norvegicus 105-114 23525285-6 2013 Furthermore, treatment with the PPARdelta agonist, GW501516, induced the expression of PPARdelta target genes in the pro-inflammatory M1 macrophages while no change was observed in the anti-inflammatory M2 macrophages. GW 501516 51-59 peroxisome proliferator activated receptor delta Homo sapiens 32-41 23525285-6 2013 Furthermore, treatment with the PPARdelta agonist, GW501516, induced the expression of PPARdelta target genes in the pro-inflammatory M1 macrophages while no change was observed in the anti-inflammatory M2 macrophages. GW 501516 51-59 peroxisome proliferator activated receptor delta Homo sapiens 87-96 23849213-9 2013 GW501516 treatment also increased Lipin1 protein levels in the nucleus, led to the amplification of the PGC-1alpha-PPARalpha pathway and increased PPARalpha DNA-binding activity, as well as the expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 104-114 23849213-9 2013 GW501516 treatment also increased Lipin1 protein levels in the nucleus, led to the amplification of the PGC-1alpha-PPARalpha pathway and increased PPARalpha DNA-binding activity, as well as the expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 115-124 23849213-9 2013 GW501516 treatment also increased Lipin1 protein levels in the nucleus, led to the amplification of the PGC-1alpha-PPARalpha pathway and increased PPARalpha DNA-binding activity, as well as the expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 147-156 23849213-9 2013 GW501516 treatment also increased Lipin1 protein levels in the nucleus, led to the amplification of the PGC-1alpha-PPARalpha pathway and increased PPARalpha DNA-binding activity, as well as the expression of PPARalpha-target genes involved in fatty acid oxidation. GW 501516 0-8 peroxisome proliferator activated receptor alpha Mus musculus 147-156 23849213-11 2013 Finally, GW501516 increased the hepatic levels of the PPARalpha endogenous ligand 16:0/18:1-PC and the expression of the VLDL receptor. GW 501516 9-17 peroxisome proliferator activated receptor alpha Mus musculus 54-63 23849213-11 2013 Finally, GW501516 increased the hepatic levels of the PPARalpha endogenous ligand 16:0/18:1-PC and the expression of the VLDL receptor. GW 501516 9-17 very low density lipoprotein receptor Mus musculus 121-134 23849213-12 2013 CONCLUSION: These data indicate that the hypotriglyceridemic effect of GW501516 in mice subjected to HFD-fed mice is accompanied by an increase in phospho-AMPK levels and the amplification of the PGC-1alpha-Lipin1-PPARalpha pathway. GW 501516 71-79 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 196-206 23849213-12 2013 CONCLUSION: These data indicate that the hypotriglyceridemic effect of GW501516 in mice subjected to HFD-fed mice is accompanied by an increase in phospho-AMPK levels and the amplification of the PGC-1alpha-Lipin1-PPARalpha pathway. GW 501516 71-79 lipin 1 Mus musculus 207-213 23849213-12 2013 CONCLUSION: These data indicate that the hypotriglyceridemic effect of GW501516 in mice subjected to HFD-fed mice is accompanied by an increase in phospho-AMPK levels and the amplification of the PGC-1alpha-Lipin1-PPARalpha pathway. GW 501516 71-79 peroxisome proliferator activated receptor alpha Mus musculus 214-223 22933110-8 2012 PPARdelta agonist GW1516 restored EDRs in mouse aortae under high-glucose conditions or in db/db mouse aortae ex vivo. GW 501516 18-24 peroxisome proliferator activator receptor delta Mus musculus 0-9 23100242-0 2013 Synthesis, mass spectrometric characterization, and analysis of the PPARdelta agonist GW1516 and its major human metabolites: targets in sports drug testing. GW 501516 86-92 peroxisome proliferator activated receptor delta Homo sapiens 68-77 23100242-2 2013 A new drug candidate belonging to the family of the peroxisome proliferator-activated receptor-delta agonists termed GW1516 (also referred to as GW501516) has been prohibited by the World Anti-Doping Agency in 2009 due to its potential to artificially increase endurance. GW 501516 117-123 peroxisome proliferator activated receptor delta Homo sapiens 52-100 23100242-2 2013 A new drug candidate belonging to the family of the peroxisome proliferator-activated receptor-delta agonists termed GW1516 (also referred to as GW501516) has been prohibited by the World Anti-Doping Agency in 2009 due to its potential to artificially increase endurance. GW 501516 145-153 peroxisome proliferator activated receptor delta Homo sapiens 52-100 23737761-6 2013 Through the use of short hairpin RNA inhibitors of PPARbeta/delta, BCL-6, and MMP-9, it was evident that PPARbeta/delta was responsible for the ligand-dependent effects whereas BCL-6 dissociation upon GW501516 treatment was ultimately responsible for decreasing MMP-9 expression and hence invasion activity. GW 501516 201-209 peroxisome proliferator activated receptor delta Homo sapiens 51-59 23737761-6 2013 Through the use of short hairpin RNA inhibitors of PPARbeta/delta, BCL-6, and MMP-9, it was evident that PPARbeta/delta was responsible for the ligand-dependent effects whereas BCL-6 dissociation upon GW501516 treatment was ultimately responsible for decreasing MMP-9 expression and hence invasion activity. GW 501516 201-209 matrix metallopeptidase 9 Homo sapiens 78-83 23737761-6 2013 Through the use of short hairpin RNA inhibitors of PPARbeta/delta, BCL-6, and MMP-9, it was evident that PPARbeta/delta was responsible for the ligand-dependent effects whereas BCL-6 dissociation upon GW501516 treatment was ultimately responsible for decreasing MMP-9 expression and hence invasion activity. GW 501516 201-209 BCL6 transcription repressor Homo sapiens 177-182 23000914-4 2012 Activation of PPARdelta by the specific ligand GW501516 significantly inhibited Ang II-induced premature senescence and generation of reactive oxygen species (ROS) in HCAECs. GW 501516 47-55 peroxisome proliferator activated receptor delta Homo sapiens 14-23 23000914-5 2012 A marked concentration- and time-dependent increase in the mRNA levels of SIRT1 was observed in GW501516-treated HCAECs. GW 501516 96-104 sirtuin 1 Homo sapiens 74-79 23000914-6 2012 The effects of GW501516 were almost completely abolished in the presence of small interfering (si) RNA against PPARdelta, indicating that PPARdelta mediates the effects of GW501516. GW 501516 15-23 peroxisome proliferator activated receptor delta Homo sapiens 111-120 23000914-6 2012 The effects of GW501516 were almost completely abolished in the presence of small interfering (si) RNA against PPARdelta, indicating that PPARdelta mediates the effects of GW501516. GW 501516 15-23 peroxisome proliferator activated receptor delta Homo sapiens 138-147 23000914-6 2012 The effects of GW501516 were almost completely abolished in the presence of small interfering (si) RNA against PPARdelta, indicating that PPARdelta mediates the effects of GW501516. GW 501516 172-180 peroxisome proliferator activated receptor delta Homo sapiens 111-120 23000914-6 2012 The effects of GW501516 were almost completely abolished in the presence of small interfering (si) RNA against PPARdelta, indicating that PPARdelta mediates the effects of GW501516. GW 501516 172-180 peroxisome proliferator activated receptor delta Homo sapiens 138-147 23607100-0 2013 PPARdelta agonist GW501516 inhibits PDGF-stimulated pulmonary arterial smooth muscle cell function related to pathological vascular remodeling. GW 501516 18-26 peroxisome proliferator activated receptor delta Homo sapiens 0-9 23607100-7 2013 Activation of PPAR delta by GW501516, a specific PPAR delta ligand, significantly inhibited PDGF-induced proliferation in HPASMCs. GW 501516 28-36 peroxisome proliferator activated receptor delta Homo sapiens 14-24 23607100-7 2013 Activation of PPAR delta by GW501516, a specific PPAR delta ligand, significantly inhibited PDGF-induced proliferation in HPASMCs. GW 501516 28-36 peroxisome proliferator activated receptor delta Homo sapiens 49-59 23607100-8 2013 The inhibitory effect of GW501516 on HPASMCs was associated with decreased expression of cyclin D1, cyclin D3, CDK2, and CDK4 as well as increased expression of the cell cycle inhibitory genes G0S2 and P27(kip1). GW 501516 25-33 cyclin D1 Homo sapiens 89-98 23607100-8 2013 The inhibitory effect of GW501516 on HPASMCs was associated with decreased expression of cyclin D1, cyclin D3, CDK2, and CDK4 as well as increased expression of the cell cycle inhibitory genes G0S2 and P27(kip1). GW 501516 25-33 cyclin D3 Homo sapiens 100-109 23607100-8 2013 The inhibitory effect of GW501516 on HPASMCs was associated with decreased expression of cyclin D1, cyclin D3, CDK2, and CDK4 as well as increased expression of the cell cycle inhibitory genes G0S2 and P27(kip1). GW 501516 25-33 cyclin dependent kinase 2 Homo sapiens 111-115 23607100-8 2013 The inhibitory effect of GW501516 on HPASMCs was associated with decreased expression of cyclin D1, cyclin D3, CDK2, and CDK4 as well as increased expression of the cell cycle inhibitory genes G0S2 and P27(kip1). GW 501516 25-33 cyclin dependent kinase 4 Homo sapiens 121-125 23607100-8 2013 The inhibitory effect of GW501516 on HPASMCs was associated with decreased expression of cyclin D1, cyclin D3, CDK2, and CDK4 as well as increased expression of the cell cycle inhibitory genes G0S2 and P27(kip1). GW 501516 25-33 cyclin dependent kinase inhibitor 1B Homo sapiens 202-210 23607100-10 2013 GW501516 also significantly attenuated TNF-mediated expression of MCP-1. GW 501516 0-8 tumor necrosis factor Homo sapiens 39-42 23607100-10 2013 GW501516 also significantly attenuated TNF-mediated expression of MCP-1. GW 501516 0-8 C-C motif chemokine ligand 2 Homo sapiens 66-71 22933110-9 2012 After oral treatment with GW1516, EDRs in aortae and FMDs in mesenteric resistance arteries were improved in obese mice in a PPARdelta-specific manner. GW 501516 26-32 peroxisome proliferator activator receptor delta Mus musculus 125-134 22933110-10 2012 The effects of GW1516 on endothelial function were mediated through phosphatidylinositol 3-kinase (PI3K) and Akt with a subsequent increase of endothelial nitric oxide synthase (eNOS) activity and NO production. GW 501516 15-21 phosphoinositide-3-kinase regulatory subunit 1 Mus musculus 68-97 22933110-10 2012 The effects of GW1516 on endothelial function were mediated through phosphatidylinositol 3-kinase (PI3K) and Akt with a subsequent increase of endothelial nitric oxide synthase (eNOS) activity and NO production. GW 501516 15-21 thymoma viral proto-oncogene 1 Mus musculus 109-112 22933110-10 2012 The effects of GW1516 on endothelial function were mediated through phosphatidylinositol 3-kinase (PI3K) and Akt with a subsequent increase of endothelial nitric oxide synthase (eNOS) activity and NO production. GW 501516 15-21 nitric oxide synthase 3, endothelial cell Mus musculus 143-176 22933110-10 2012 The effects of GW1516 on endothelial function were mediated through phosphatidylinositol 3-kinase (PI3K) and Akt with a subsequent increase of endothelial nitric oxide synthase (eNOS) activity and NO production. GW 501516 15-21 nitric oxide synthase 3, endothelial cell Mus musculus 178-182 22982594-0 2012 PPARdelta agonist GW501516 prevents uncoupling of endothelial nitric oxide synthase in cerebral microvessels of hph-1 mice. GW 501516 18-26 peroxisome proliferator activator receptor delta Mus musculus 0-9 22576330-7 2012 Tropoelastin production was significantly increased by 20 muM ZS and by 10 nM GW. GW 501516 78-80 elastin Homo sapiens 0-12 22576330-8 2012 Cell culture surface deposited elastin production was significantly increased by 20 muM ZS and by the combination of 20 muM ZS with 10 nM GW, and collagen production was significantly increased by 10 nM GW and by the combination of 20 muM ZS with 10 nM GW. GW 501516 138-140 elastin Homo sapiens 31-38 22576330-8 2012 Cell culture surface deposited elastin production was significantly increased by 20 muM ZS and by the combination of 20 muM ZS with 10 nM GW, and collagen production was significantly increased by 10 nM GW and by the combination of 20 muM ZS with 10 nM GW. GW 501516 203-205 elastin Homo sapiens 31-38 22576330-8 2012 Cell culture surface deposited elastin production was significantly increased by 20 muM ZS and by the combination of 20 muM ZS with 10 nM GW, and collagen production was significantly increased by 10 nM GW and by the combination of 20 muM ZS with 10 nM GW. GW 501516 203-205 elastin Homo sapiens 31-38 22886847-10 2012 Treatment with PPARdelta ligand GW501516 (2 mg/kg/day) for 14 days significantly increased BH(4) bioavailability and improved endothelium-dependent relaxations in Tg2576 mice aortas. GW 501516 32-40 peroxisome proliferator activator receptor delta Mus musculus 15-24 22886847-11 2012 GW501516 also normalized protein expression of gp91(phox) and SODs, thereby reducing production of superoxide anion in the aortas. GW 501516 0-8 paired Ig-like receptor B Mus musculus 47-51 22982594-3 2012 In the present study, the effects of PPARdelta agonist GW501516 on uncoupling of endothelial nitric oxide synthase (eNOS) were determined in cerebral microvessels of BH4-deficient hph-1 mice. GW 501516 55-63 nitric oxide synthase 3, endothelial cell Mus musculus 81-114 22982594-4 2012 Wild-type (B6CBA) and hph-1 mice were orally gavaged with a selective PPARdelta activator, GW501516 (2 mg/kg/day) for 14 days, and thereafter, cerebral microvessels were isolated and studied. GW 501516 91-99 peroxisome proliferator activator receptor delta Mus musculus 70-79 22982594-0 2012 PPARdelta agonist GW501516 prevents uncoupling of endothelial nitric oxide synthase in cerebral microvessels of hph-1 mice. GW 501516 18-26 nitric oxide synthase 3, endothelial cell Mus musculus 50-83 22982594-5 2012 Treatment of hph-1 mice with GW501516 significantly reduced oxidation of BH4 and increased the ratio of BH4 to 7,8-BH2 (P<0.05, n=6-9). GW 501516 29-37 hyperphenylalaninemia 1 Mus musculus 13-18 22982594-6 2012 Attenuation of L-NAME-inhibitable superoxide anion levels by GW501516 demonstrated that activation of PPARdelta might prevent uncoupling of endothelial nitric oxide synthase (eNOS, P<0.05, n=6-9). GW 501516 61-69 peroxisome proliferator activator receptor delta Mus musculus 102-111 22982594-0 2012 PPARdelta agonist GW501516 prevents uncoupling of endothelial nitric oxide synthase in cerebral microvessels of hph-1 mice. GW 501516 18-26 hyperphenylalaninemia 1 Mus musculus 112-117 22814748-0 2012 Lipid effects of peroxisome proliferator-activated receptor-delta agonist GW501516 in subjects with low high-density lipoprotein cholesterol: characteristics of metabolic syndrome. GW 501516 74-82 peroxisome proliferator activated receptor delta Homo sapiens 17-65 23046570-0 2012 GW501516-activated PPARbeta/delta promotes liver fibrosis via p38-JNK MAPK-induced hepatic stellate cell proliferation. GW 501516 0-8 peroxisome proliferator activator receptor delta Mus musculus 19-27 23046570-0 2012 GW501516-activated PPARbeta/delta promotes liver fibrosis via p38-JNK MAPK-induced hepatic stellate cell proliferation. GW 501516 0-8 mitogen-activated protein kinase 14 Mus musculus 62-65 23046570-0 2012 GW501516-activated PPARbeta/delta promotes liver fibrosis via p38-JNK MAPK-induced hepatic stellate cell proliferation. GW 501516 0-8 mitogen-activated protein kinase 8 Mus musculus 66-69 23046570-3 2012 This study investigated whether activation of PPARbeta/delta with the ligand GW501516 influenced the fibrotic response to injury from chronic carbon tetrachloride (CCl4) treatment in mice. GW 501516 77-85 peroxisome proliferator activator receptor delta Mus musculus 46-54 23046570-7 2012 Compared to the other experimental groups, CCl4/GW501516-treated wild type mice exhibited increased expression of various profibrotic and pro-inflammatory genes, such as those involved in extracellular matrix deposition and macrophage recruitment. GW 501516 48-56 chemokine (C-C motif) ligand 4 Mus musculus 43-47 23046570-9 2012 GW501516 stimulated HSC proliferation that caused enhanced fibrotic and inflammatory responses, by increasing the phosphorylation of p38 and c-Jun N-terminal kinases through the phosphoinositide-3 kinase/protein kinase-C alpha/beta mixed lineage kinase-3 pathway. GW 501516 0-8 mitogen-activated protein kinase 14 Mus musculus 133-136 23046570-9 2012 GW501516 stimulated HSC proliferation that caused enhanced fibrotic and inflammatory responses, by increasing the phosphorylation of p38 and c-Jun N-terminal kinases through the phosphoinositide-3 kinase/protein kinase-C alpha/beta mixed lineage kinase-3 pathway. GW 501516 0-8 jun proto-oncogene Mus musculus 141-146 23046570-10 2012 CONCLUSIONS: This study clarified the mechanism underlying GW501516-dependent promotion of hepatic repair by stimulating proliferation of HSCs via the p38 and JNK MAPK pathways. GW 501516 59-67 mitogen-activated protein kinase 14 Mus musculus 151-154 23046570-10 2012 CONCLUSIONS: This study clarified the mechanism underlying GW501516-dependent promotion of hepatic repair by stimulating proliferation of HSCs via the p38 and JNK MAPK pathways. GW 501516 59-67 mitogen-activated protein kinase 8 Mus musculus 159-162 22977012-0 2012 Detection of PPARdelta agonists GW1516 and GW0742 and their metabolites in human urine. GW 501516 32-38 peroxisome proliferator activated receptor delta Homo sapiens 13-22 22683888-7 2012 Interestingly, the PPARbeta/delta ligand GW501516 prevented the expression of inflammatory markers and the reduction in the expression of PPARbeta/delta-target genes in adipocytes stimulated with TNF-alpha. GW 501516 41-49 peroxisome proliferator activated receptor delta Homo sapiens 19-27 22683888-7 2012 Interestingly, the PPARbeta/delta ligand GW501516 prevented the expression of inflammatory markers and the reduction in the expression of PPARbeta/delta-target genes in adipocytes stimulated with TNF-alpha. GW 501516 41-49 peroxisome proliferator activated receptor delta Homo sapiens 138-146 22683888-7 2012 Interestingly, the PPARbeta/delta ligand GW501516 prevented the expression of inflammatory markers and the reduction in the expression of PPARbeta/delta-target genes in adipocytes stimulated with TNF-alpha. GW 501516 41-49 tumor necrosis factor Homo sapiens 196-205 23078396-5 2012 This study reveals an inhibitory effect of two commonly used PPARdelta agonists, GW501516 and L-165,041, on the protein expression and enzyme activity of cathepsin B in human endothelial cells. GW 501516 81-89 peroxisome proliferator activated receptor delta Homo sapiens 61-70 23078396-5 2012 This study reveals an inhibitory effect of two commonly used PPARdelta agonists, GW501516 and L-165,041, on the protein expression and enzyme activity of cathepsin B in human endothelial cells. GW 501516 81-89 cathepsin B Homo sapiens 154-165 22814748-8 2012 CONCLUSIONS: GW501516 produced significant changes in HDL cholesterol, LDL cholesterol, apoA1, and apoB. GW 501516 13-21 apolipoprotein A1 Homo sapiens 88-93 22814748-8 2012 CONCLUSIONS: GW501516 produced significant changes in HDL cholesterol, LDL cholesterol, apoA1, and apoB. GW 501516 13-21 apolipoprotein B Homo sapiens 99-103 22473775-3 2012 Activation of PPARdelta by GW501516, a specific ligand, significantly inhibited glutamate-induced cell death and reactive oxygen species (ROS) production in HT22 cells. GW 501516 27-35 peroxisome proliferator activator receptor delta Mus musculus 14-23 22820186-5 2012 The PPARdelta agonist GW501516 had no effect on LPL mRNA, but increased ANGPTL4 mRNA and caused a marked reduction of the heparin-releasable LPL activity concomitantly with accumulation of inactive, monomeric LPL in the medium. GW 501516 22-30 peroxisome proliferator activated receptor delta Homo sapiens 4-13 22820186-5 2012 The PPARdelta agonist GW501516 had no effect on LPL mRNA, but increased ANGPTL4 mRNA and caused a marked reduction of the heparin-releasable LPL activity concomitantly with accumulation of inactive, monomeric LPL in the medium. GW 501516 22-30 angiopoietin like 4 Homo sapiens 72-79 22820186-5 2012 The PPARdelta agonist GW501516 had no effect on LPL mRNA, but increased ANGPTL4 mRNA and caused a marked reduction of the heparin-releasable LPL activity concomitantly with accumulation of inactive, monomeric LPL in the medium. GW 501516 22-30 lipoprotein lipase Homo sapiens 141-144 22820186-5 2012 The PPARdelta agonist GW501516 had no effect on LPL mRNA, but increased ANGPTL4 mRNA and caused a marked reduction of the heparin-releasable LPL activity concomitantly with accumulation of inactive, monomeric LPL in the medium. GW 501516 22-30 lipoprotein lipase Homo sapiens 141-144 22820186-7 2012 GW501516 caused an increase in the amount of ANGPTL4 oligomers on the cell surface that paralleled the decrease in LPL activity. GW 501516 0-8 angiopoietin like 4 Homo sapiens 45-52 22820186-7 2012 GW501516 caused an increase in the amount of ANGPTL4 oligomers on the cell surface that paralleled the decrease in LPL activity. GW 501516 0-8 lipoprotein lipase Homo sapiens 115-118 22820186-8 2012 Actinomycin D blocked the effects of GW501516 on ANGPTL4 oligomer formation and prevented the inactivation of LPL. GW 501516 37-45 angiopoietin like 4 Homo sapiens 49-56 22473775-4 2012 The siRNA-mediated knockdown of PPARdelta abrogated the effects of GW501516 in neuronal toxicity and ROS production induced by glutamate. GW 501516 67-75 peroxisome proliferator activator receptor delta Mus musculus 32-41 22234939-8 2012 We confirmed whether these antiangiogenic effects of L-165041 were PPARdelta-dependent using GW501516 and PPARdelta siRNA. GW 501516 93-101 peroxisome proliferator activated receptor delta Homo sapiens 67-76 22586590-7 2012 Treatment with ruboxistaurin (a PKCbeta inhibitor) or with GW501516 (a peroxisome proliferator-activated receptor delta activator) reduced atrogin-1 expression and restored BK channel-mediated coronary vasodilation in diabetic mice. GW 501516 59-67 F-box protein 32 Homo sapiens 139-148 22519881-3 2012 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly reduced Ang II-induced ROS generation in VSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 22519881-3 2012 Activation of PPARdelta by GW501516, a specific ligand for PPARdelta, significantly reduced Ang II-induced ROS generation in VSMCs. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 59-68 22519881-6 2012 Accordingly, ablation of Akt with siRNA further enhanced the inhibitory effects of GW501516 in Ang II-induced superoxide production. GW 501516 83-91 AKT serine/threonine kinase 1 Homo sapiens 25-28 22466807-6 2012 The expression of MafA, glucose transportor-2 (GLUT2), and insulin was found to be up-regulated in cells treated with GW501516. GW 501516 118-126 MAF bZIP transcription factor A Rattus norvegicus 18-22 22466807-6 2012 The expression of MafA, glucose transportor-2 (GLUT2), and insulin was found to be up-regulated in cells treated with GW501516. GW 501516 118-126 solute carrier family 2 member 2 Rattus norvegicus 24-45 22466807-6 2012 The expression of MafA, glucose transportor-2 (GLUT2), and insulin was found to be up-regulated in cells treated with GW501516. GW 501516 118-126 solute carrier family 2 member 2 Rattus norvegicus 47-52 22179221-0 2012 The peroxisome proliferator-activated receptor (PPAR) beta/delta agonist GW501516 inhibits IL-6-induced signal transducer and activator of transcription 3 (STAT3) activation and insulin resistance in human liver cells. GW 501516 73-81 peroxisome proliferator activated receptor delta Homo sapiens 4-58 22335598-4 2012 Activation of PPARdelta by GW501516, a specific ligand of PPARdelta, significantly attenuated UVB-mediated generation of ROS (reactive oxygen species) and suppressed senescence of human keratinocytes. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 14-23 22335598-4 2012 Activation of PPARdelta by GW501516, a specific ligand of PPARdelta, significantly attenuated UVB-mediated generation of ROS (reactive oxygen species) and suppressed senescence of human keratinocytes. GW 501516 27-35 peroxisome proliferator activated receptor delta Homo sapiens 58-67 22179221-6 2012 Moreover, GW501516 prevented IL-6-dependent induction of extracellular-related kinase 1/2 (ERK1/2), a serine-threonine protein kinase involved in serine STAT3 phosphorylation; the livers of Pparbeta/delta-null mice showed increased Tyr705- and Ser727-STAT3 as well as phospho-ERK1/2 levels. GW 501516 10-18 signal transducer and activator of transcription 3 Mus musculus 153-158 22179221-6 2012 Moreover, GW501516 prevented IL-6-dependent induction of extracellular-related kinase 1/2 (ERK1/2), a serine-threonine protein kinase involved in serine STAT3 phosphorylation; the livers of Pparbeta/delta-null mice showed increased Tyr705- and Ser727-STAT3 as well as phospho-ERK1/2 levels. GW 501516 10-18 peroxisome proliferator activator receptor delta Mus musculus 190-198 22179221-6 2012 Moreover, GW501516 prevented IL-6-dependent induction of extracellular-related kinase 1/2 (ERK1/2), a serine-threonine protein kinase involved in serine STAT3 phosphorylation; the livers of Pparbeta/delta-null mice showed increased Tyr705- and Ser727-STAT3 as well as phospho-ERK1/2 levels. GW 501516 10-18 signal transducer and activator of transcription 3 Mus musculus 251-256 22179221-0 2012 The peroxisome proliferator-activated receptor (PPAR) beta/delta agonist GW501516 inhibits IL-6-induced signal transducer and activator of transcription 3 (STAT3) activation and insulin resistance in human liver cells. GW 501516 73-81 interleukin 6 Homo sapiens 91-95 22179221-6 2012 Moreover, GW501516 prevented IL-6-dependent induction of extracellular-related kinase 1/2 (ERK1/2), a serine-threonine protein kinase involved in serine STAT3 phosphorylation; the livers of Pparbeta/delta-null mice showed increased Tyr705- and Ser727-STAT3 as well as phospho-ERK1/2 levels. GW 501516 10-18 mitogen-activated protein kinase 3 Mus musculus 276-282 22179221-8 2012 In agreement with the recovery in phospho-AMPK levels observed following GW501516 treatment, this drug increased the AMP/ATP ratio and decreased the ATP/ADP ratio. GW 501516 73-81 protein kinase AMP-activated non-catalytic subunit beta 1 Homo sapiens 42-46 22179221-9 2012 CONCLUSIONS/INTERPRETATION: Overall, our findings show that the PPARbeta/delta activator GW501516 prevents IL-6-induced STAT3 activation by inhibiting ERK1/2 phosphorylation and preventing the reduction in phospho-AMPK levels. GW 501516 89-97 peroxisome proliferator activated receptor delta Homo sapiens 64-72 22179221-0 2012 The peroxisome proliferator-activated receptor (PPAR) beta/delta agonist GW501516 inhibits IL-6-induced signal transducer and activator of transcription 3 (STAT3) activation and insulin resistance in human liver cells. GW 501516 73-81 signal transducer and activator of transcription 3 Homo sapiens 104-154 22179221-9 2012 CONCLUSIONS/INTERPRETATION: Overall, our findings show that the PPARbeta/delta activator GW501516 prevents IL-6-induced STAT3 activation by inhibiting ERK1/2 phosphorylation and preventing the reduction in phospho-AMPK levels. GW 501516 89-97 interleukin 6 Homo sapiens 107-111 22179221-9 2012 CONCLUSIONS/INTERPRETATION: Overall, our findings show that the PPARbeta/delta activator GW501516 prevents IL-6-induced STAT3 activation by inhibiting ERK1/2 phosphorylation and preventing the reduction in phospho-AMPK levels. GW 501516 89-97 signal transducer and activator of transcription 3 Homo sapiens 120-125 22179221-0 2012 The peroxisome proliferator-activated receptor (PPAR) beta/delta agonist GW501516 inhibits IL-6-induced signal transducer and activator of transcription 3 (STAT3) activation and insulin resistance in human liver cells. GW 501516 73-81 signal transducer and activator of transcription 3 Homo sapiens 156-161 22179221-9 2012 CONCLUSIONS/INTERPRETATION: Overall, our findings show that the PPARbeta/delta activator GW501516 prevents IL-6-induced STAT3 activation by inhibiting ERK1/2 phosphorylation and preventing the reduction in phospho-AMPK levels. GW 501516 89-97 mitogen-activated protein kinase 3 Homo sapiens 151-157 22179221-0 2012 The peroxisome proliferator-activated receptor (PPAR) beta/delta agonist GW501516 inhibits IL-6-induced signal transducer and activator of transcription 3 (STAT3) activation and insulin resistance in human liver cells. GW 501516 73-81 insulin Homo sapiens 178-185 22179221-9 2012 CONCLUSIONS/INTERPRETATION: Overall, our findings show that the PPARbeta/delta activator GW501516 prevents IL-6-induced STAT3 activation by inhibiting ERK1/2 phosphorylation and preventing the reduction in phospho-AMPK levels. GW 501516 89-97 protein kinase AMP-activated non-catalytic subunit beta 1 Homo sapiens 214-218 22179221-10 2012 These effects of GW501516 may contribute to the prevention of cytokine-induced insulin resistance in hepatic cells. GW 501516 17-25 insulin Homo sapiens 79-86 22179221-2 2012 Here we examined whether the peroxisome proliferator-activated receptor (PPAR)beta/delta agonist GW501516 prevented activation of the IL-6-STAT3-suppressor of cytokine signalling 3 (SOCS3) pathway and insulin resistance in human hepatic HepG2 cells. GW 501516 97-105 peroxisome proliferator activated receptor alpha Homo sapiens 29-71 22179221-2 2012 Here we examined whether the peroxisome proliferator-activated receptor (PPAR)beta/delta agonist GW501516 prevented activation of the IL-6-STAT3-suppressor of cytokine signalling 3 (SOCS3) pathway and insulin resistance in human hepatic HepG2 cells. GW 501516 97-105 peroxisome proliferator activated receptor alpha Homo sapiens 73-77 22179221-2 2012 Here we examined whether the peroxisome proliferator-activated receptor (PPAR)beta/delta agonist GW501516 prevented activation of the IL-6-STAT3-suppressor of cytokine signalling 3 (SOCS3) pathway and insulin resistance in human hepatic HepG2 cells. GW 501516 97-105 suppressor of cytokine signaling 3 Homo sapiens 134-180 22179221-2 2012 Here we examined whether the peroxisome proliferator-activated receptor (PPAR)beta/delta agonist GW501516 prevented activation of the IL-6-STAT3-suppressor of cytokine signalling 3 (SOCS3) pathway and insulin resistance in human hepatic HepG2 cells. GW 501516 97-105 suppressor of cytokine signaling 3 Homo sapiens 182-187 22179221-2 2012 Here we examined whether the peroxisome proliferator-activated receptor (PPAR)beta/delta agonist GW501516 prevented activation of the IL-6-STAT3-suppressor of cytokine signalling 3 (SOCS3) pathway and insulin resistance in human hepatic HepG2 cells. GW 501516 97-105 insulin Homo sapiens 201-208 22179221-4 2012 RESULTS: GW501516 prevented IL-6-dependent reduction in insulin-stimulated v-akt murine thymoma viral oncogene homologue 1 (AKT) phosphorylation and in IRS-1 and IRS-2 protein levels. GW 501516 9-17 interleukin 6 Mus musculus 28-32 22179221-4 2012 RESULTS: GW501516 prevented IL-6-dependent reduction in insulin-stimulated v-akt murine thymoma viral oncogene homologue 1 (AKT) phosphorylation and in IRS-1 and IRS-2 protein levels. GW 501516 9-17 insulin Homo sapiens 56-63 22179221-4 2012 RESULTS: GW501516 prevented IL-6-dependent reduction in insulin-stimulated v-akt murine thymoma viral oncogene homologue 1 (AKT) phosphorylation and in IRS-1 and IRS-2 protein levels. GW 501516 9-17 thymoma viral proto-oncogene 1 Mus musculus 77-80 22179221-4 2012 RESULTS: GW501516 prevented IL-6-dependent reduction in insulin-stimulated v-akt murine thymoma viral oncogene homologue 1 (AKT) phosphorylation and in IRS-1 and IRS-2 protein levels. GW 501516 9-17 thymoma viral proto-oncogene 1 Mus musculus 124-127 22179221-4 2012 RESULTS: GW501516 prevented IL-6-dependent reduction in insulin-stimulated v-akt murine thymoma viral oncogene homologue 1 (AKT) phosphorylation and in IRS-1 and IRS-2 protein levels. GW 501516 9-17 insulin receptor substrate 1 Mus musculus 152-157 22179221-4 2012 RESULTS: GW501516 prevented IL-6-dependent reduction in insulin-stimulated v-akt murine thymoma viral oncogene homologue 1 (AKT) phosphorylation and in IRS-1 and IRS-2 protein levels. GW 501516 9-17 insulin receptor substrate 2 Mus musculus 162-167 22179221-6 2012 Moreover, GW501516 prevented IL-6-dependent induction of extracellular-related kinase 1/2 (ERK1/2), a serine-threonine protein kinase involved in serine STAT3 phosphorylation; the livers of Pparbeta/delta-null mice showed increased Tyr705- and Ser727-STAT3 as well as phospho-ERK1/2 levels. GW 501516 10-18 interleukin 6 Mus musculus 29-33 22179221-6 2012 Moreover, GW501516 prevented IL-6-dependent induction of extracellular-related kinase 1/2 (ERK1/2), a serine-threonine protein kinase involved in serine STAT3 phosphorylation; the livers of Pparbeta/delta-null mice showed increased Tyr705- and Ser727-STAT3 as well as phospho-ERK1/2 levels. GW 501516 10-18 mitogen-activated protein kinase 3 Mus musculus 91-97