PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 31905247-7 2020 It was consistently indicated that digeranyl bisphosphonate, a specific inhibitor of GGPPS, and GW4064, an agonist of FXR, could also alleviate acute obstructive cholestatic liver injury in vivo. GW 4064 96-102 nuclear receptor subfamily 1, group H, member 4 Mus musculus 118-121 32662640-4 2020 M4 also significantly increased the expression of farnesoid X receptor (FXR), suppressed the purinergic ligand-gated ion channel 7 receptor (P2X7r) signaling pathway, and works as an FXR agonist, GW4064. GW 4064 196-202 nuclear receptor subfamily 1, group H, member 4 Mus musculus 183-186 32846898-5 2020 FXR agonists chenodeoxycholic acid (CDCA) and GW4064 stimulated OCT2-mediated 3H-MPP+ uptake in human renal proximal tubular cells (RPTEC/TERT1 cells) and OCT2-CHO-K1 cells. GW 4064 46-52 nuclear receptor subfamily 1 group H member 4 Homo sapiens 0-3 32846898-5 2020 FXR agonists chenodeoxycholic acid (CDCA) and GW4064 stimulated OCT2-mediated 3H-MPP+ uptake in human renal proximal tubular cells (RPTEC/TERT1 cells) and OCT2-CHO-K1 cells. GW 4064 46-52 POU class 2 homeobox 2 Homo sapiens 64-68 32846898-5 2020 FXR agonists chenodeoxycholic acid (CDCA) and GW4064 stimulated OCT2-mediated 3H-MPP+ uptake in human renal proximal tubular cells (RPTEC/TERT1 cells) and OCT2-CHO-K1 cells. GW 4064 46-52 POU class 2 homeobox 2 Homo sapiens 155-159 32258949-4 2020 Pretreatment of mice with FXR agonist 3-(2,6-dichlorophenyl)-4-(3"-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole (GW4064) attenuated liver ischemia/reperfusion injuries (IRIs) in wild-type but not FXR knockout mice. GW 4064 128-134 nuclear receptor subfamily 1, group H, member 4 Mus musculus 26-29 32565960-5 2020 Gain- and loss-of-function studies were conducted by transfecting colon cancer cells with FXR siRNA and treating them with the FXR agonist GW4064. GW 4064 139-145 nuclear receptor subfamily 1 group H member 4 Homo sapiens 127-130 32565960-9 2020 The FXR agonist GW4064 significantly inhibited the proliferation of cells but promoted the transcriptional activity of beta-catenin. GW 4064 16-22 nuclear receptor subfamily 1 group H member 4 Homo sapiens 4-7 32565960-9 2020 The FXR agonist GW4064 significantly inhibited the proliferation of cells but promoted the transcriptional activity of beta-catenin. GW 4064 16-22 catenin beta 1 Homo sapiens 119-131 32145254-4 2020 C57BL/6 mice or primary cultured mouse hepatocytes were treated with the synthetic FXR ligand GW4064 or natural ligand CDCA. GW 4064 94-100 nuclear receptor subfamily 1, group H, member 4 Mus musculus 83-86 32145254-6 2020 Real-time PCR and Western blot were applied to determine the expression of MT1 and other FXR target genes in the livers of mice and primary hepatocytes treated with GW4064 and CDCA. GW 4064 165-171 metallothionein 1 Mus musculus 75-78 32145254-6 2020 Real-time PCR and Western blot were applied to determine the expression of MT1 and other FXR target genes in the livers of mice and primary hepatocytes treated with GW4064 and CDCA. GW 4064 165-171 nuclear receptor subfamily 1, group H, member 4 Mus musculus 89-92 32145254-7 2020 Cellular and subcellular locations of MT1 in the livers of mice treated with GW4064 were examined using immunohistochemistry assay. GW 4064 77-83 metallothionein 1 Mus musculus 38-41 32145254-10 2020 RNA-seq analysis revealed that GW4064 treatment significantly induced MT1 expression in mouse liver. GW 4064 31-37 metallothionein 1 Mus musculus 70-73 32145254-11 2020 Consistently, MT1 expression in the hepatocytes of mouse livers and cultured hepatocytes was upregulated by GW4064 as well as CDCA. GW 4064 108-114 metallothionein 1 Mus musculus 14-17 31911428-12 2020 Extended stimulation of FXR by the synthetic agonist GW4064, which is suggested to induce translocation of FXR from the cytosol into the nucleus, increased the inhibitory effect of atorvastatin. GW 4064 53-59 nuclear receptor subfamily 1, group H, member 4 Mus musculus 24-27 31911428-12 2020 Extended stimulation of FXR by the synthetic agonist GW4064, which is suggested to induce translocation of FXR from the cytosol into the nucleus, increased the inhibitory effect of atorvastatin. GW 4064 53-59 nuclear receptor subfamily 1, group H, member 4 Mus musculus 107-110 32258949-7 2020 Pretreatment of KCs but not BMMs with GW4064 resulted in lower tumor necrosis factor alpha but higher interleukin-10 expressions following toll-like receptor stimulation. GW 4064 38-44 tumor necrosis factor Mus musculus 63-90 32258949-7 2020 Pretreatment of KCs but not BMMs with GW4064 resulted in lower tumor necrosis factor alpha but higher interleukin-10 expressions following toll-like receptor stimulation. GW 4064 38-44 interleukin 10 Mus musculus 102-116 32258949-8 2020 FXR-targeted gene small heterodimer partner (SHP) was critical for the regulation of KC response by GW4064. GW 4064 100-106 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-3 32258949-8 2020 FXR-targeted gene small heterodimer partner (SHP) was critical for the regulation of KC response by GW4064. GW 4064 100-106 nuclear receptor subfamily 0, group B, member 2 Mus musculus 45-48 31911244-6 2020 Mechanistically, GW4064, an FXR agonist, was carried out to verify the mechanisms of geniposide in human HepG2 and Caco2 cells. GW 4064 17-23 nuclear receptor subfamily 1 group H member 4 Homo sapiens 28-31 31779647-10 2019 As CCNG1 is a target for miR-23b-3p, the treatment of GW4064 induced the downregulation of CCNG1 through upregulating miR-23b-3p. GW 4064 54-60 microRNA 23b Homo sapiens 118-125 31836014-12 2019 The FXR agonist GW4064 significantly decreased the fasting blood glucose in mice challenged with FK506 for 3 months (P < 0.05), inhibited gluconeogenesis (P < 0.05) and significantly promoted glucose uptake (P < 0.05). GW 4064 16-22 nuclear receptor subfamily 1, group H, member 4 Mus musculus 4-7 31779647-4 2019 Their correlations were analyzed by Pearson"s test and verified by the introduction of FXR agonist, GW4064. GW 4064 100-106 nuclear receptor subfamily 1 group H member 4 Homo sapiens 87-90 31932631-4 2020 GLP-1 secretion in response to SCFAs was evaluated ex vivo in murine colonic biopsies and in colonoids of wild-type (WT) and FXR knock-out (KO) mice, in vitro in GLUTag and NCI-H716 L-cells activated with the synthetic FXR agonist GW4064 and in vivo in WT and FXR KO mice after prebiotic supplementation. GW 4064 231-237 glucagon Mus musculus 0-5 31932631-5 2020 SCFA-induced GLP-1 secretion was blunted in colonic biopsies from GW4064-treated mice and enhanced in FXR KO colonoids. GW 4064 66-72 glucagon Mus musculus 13-18 31779647-11 2019 The inhibition of miR-23b-3p obviously promoted cell viability, proliferation, and cell cycle progression but reduced apoptosis rate of MG-63 cells; however, the treatment of GW4064 could partially reverse the effects of the inhibition of miR-23b-3p on OS cells. GW 4064 175-181 microRNA 23b Homo sapiens 18-25 31779647-11 2019 The inhibition of miR-23b-3p obviously promoted cell viability, proliferation, and cell cycle progression but reduced apoptosis rate of MG-63 cells; however, the treatment of GW4064 could partially reverse the effects of the inhibition of miR-23b-3p on OS cells. GW 4064 175-181 microRNA 23b Homo sapiens 239-246 31779647-10 2019 As CCNG1 is a target for miR-23b-3p, the treatment of GW4064 induced the downregulation of CCNG1 through upregulating miR-23b-3p. GW 4064 54-60 cyclin G1 Homo sapiens 3-8 31779647-12 2019 CONCLUSIONS: Upregulated FXR by GW4064 can obviously suppress OS cell development, and the suppressive effects may rely on miR-23b-3p/CCNG1 pathway. GW 4064 32-38 nuclear receptor subfamily 1 group H member 4 Homo sapiens 25-28 31779647-10 2019 As CCNG1 is a target for miR-23b-3p, the treatment of GW4064 induced the downregulation of CCNG1 through upregulating miR-23b-3p. GW 4064 54-60 microRNA 23b Homo sapiens 25-32 31779647-10 2019 As CCNG1 is a target for miR-23b-3p, the treatment of GW4064 induced the downregulation of CCNG1 through upregulating miR-23b-3p. GW 4064 54-60 cyclin G1 Homo sapiens 91-96 31191298-4 2019 The BSEP upstream molecule farnesoid X receptor was down-regulated by small interfering RNA (siRNA) technology or guggulsterones and up-regulated by lentivirus or GW4064. GW 4064 163-169 ATP binding cassette subfamily B member 11 Rattus norvegicus 4-8 31744088-3 2019 In this study, we synthesized novel FXR agonists 1-4 possessing isoxazole and N-substituted benzimidazole moieties, and compared their effects on osteoblast differentiation with the known FXR agonists, chenodeoxycholic acid and a synthetic compound, GW4064. GW 4064 250-256 nuclear receptor subfamily 1, group H, member 4 Mus musculus 36-39 31744088-5 2019 Computer-assisted modeling suggested that the binding of the FXR agonist 3 with ligand binding domain of FXR was similar to GW4064. GW 4064 124-130 nuclear receptor subfamily 1, group H, member 4 Mus musculus 61-64 31744088-5 2019 Computer-assisted modeling suggested that the binding of the FXR agonist 3 with ligand binding domain of FXR was similar to GW4064. GW 4064 124-130 nuclear receptor subfamily 1, group H, member 4 Mus musculus 105-108 31298930-4 2019 Here, we show that agonist GW4064-mediated FXR activation inhibits the activity of the nonreceptor tyrosine kinase Src (proto-oncogene tyrosine-protein kinase), which is critical for regulation of yes-associated protein (YAP) phosphorylation and nuclear localization in renal fibrosis. GW 4064 27-33 nuclear receptor subfamily 1, group H, member 4 Mus musculus 43-46 31298930-4 2019 Here, we show that agonist GW4064-mediated FXR activation inhibits the activity of the nonreceptor tyrosine kinase Src (proto-oncogene tyrosine-protein kinase), which is critical for regulation of yes-associated protein (YAP) phosphorylation and nuclear localization in renal fibrosis. GW 4064 27-33 Rous sarcoma oncogene Mus musculus 115-118 31298930-4 2019 Here, we show that agonist GW4064-mediated FXR activation inhibits the activity of the nonreceptor tyrosine kinase Src (proto-oncogene tyrosine-protein kinase), which is critical for regulation of yes-associated protein (YAP) phosphorylation and nuclear localization in renal fibrosis. GW 4064 27-33 yes-associated protein 1 Mus musculus 197-219 31298930-4 2019 Here, we show that agonist GW4064-mediated FXR activation inhibits the activity of the nonreceptor tyrosine kinase Src (proto-oncogene tyrosine-protein kinase), which is critical for regulation of yes-associated protein (YAP) phosphorylation and nuclear localization in renal fibrosis. GW 4064 27-33 yes-associated protein 1 Mus musculus 221-224 31298930-6 2019 Moreover, GW4064 treatment in HK2 cells increased Ser127 phosphorylation, cytosolic accumulation of YAP, and interaction of the hippo core kinases (Ste20-like kinase 1, large tumor suppressor kinase 1, and salvador homolog 1). GW 4064 10-16 yes-associated protein 1 Mus musculus 100-103 31298930-6 2019 Moreover, GW4064 treatment in HK2 cells increased Ser127 phosphorylation, cytosolic accumulation of YAP, and interaction of the hippo core kinases (Ste20-like kinase 1, large tumor suppressor kinase 1, and salvador homolog 1). GW 4064 10-16 salvador family WW domain containing 1 Mus musculus 148-224 31095863-8 2019 Knockdown of CYP7A1 via small interfering RNA or activation of FXR by GW4064 blocks the effect of TMAO-induced lipogenesis in palmitic acid-treated HepG2 cells. GW 4064 70-76 nuclear receptor subfamily 1 group H member 4 Homo sapiens 63-66 30920307-0 2019 FXR agonist GW4064 improves liver and intestinal pathology and alters bile acid metabolism in rats undergoing small intestinal resection. GW 4064 12-18 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 0-3 30920307-6 2019 After intervention with the FXR agonist GW4064, both the liver histology and serum transaminase activity were improved, which demonstrated the attenuation of SBR-ALD. GW 4064 40-46 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 28-31 30920307-11 2019 This study showed that the FXR agonist GW4064 could correct BA dysmetabolism to alleviate hepatotoxicity in SBR animals. GW 4064 39-45 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 27-30 30920307-14 2019 Concomitantly, FXR activation in the presence of GW4064 decreased BA production by repressing the expression of key synthetases, including CYP7A1, CYP8B1, and CYP27A1. GW 4064 49-55 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 15-18 30920307-14 2019 Concomitantly, FXR activation in the presence of GW4064 decreased BA production by repressing the expression of key synthetases, including CYP7A1, CYP8B1, and CYP27A1. GW 4064 49-55 cytochrome P450 family 7 subfamily A member 1 Rattus norvegicus 139-145 30920307-14 2019 Concomitantly, FXR activation in the presence of GW4064 decreased BA production by repressing the expression of key synthetases, including CYP7A1, CYP8B1, and CYP27A1. GW 4064 49-55 cytochrome P450 family 8 subfamily B member 1 Rattus norvegicus 147-153 30920307-14 2019 Concomitantly, FXR activation in the presence of GW4064 decreased BA production by repressing the expression of key synthetases, including CYP7A1, CYP8B1, and CYP27A1. GW 4064 49-55 cytochrome P450, family 27, subfamily a, polypeptide 1 Rattus norvegicus 159-166 30920307-15 2019 These findings provide a clinical research direction for the prevention of liver disease in patients with SBS.NEW & NOTEWORTHY This study assessed the impact of treatment with GW4064, a farnesoid X receptor agonist, on the development of short bowel resection (SBR) associated with liver disease in a rat model of SBR. GW 4064 180-186 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 200-210 30902657-0 2019 Farnesoid X receptor agonist GW4064 indirectly inhibits HCV entry into cells via down-regulating scavenger receptor class B type I. Farnesoid X receptor (FXR) agonists play important regulatory roles in bile acid, lipid and glucose metabolism in vitro and in vivo. GW 4064 29-35 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 10-20 30902657-0 2019 Farnesoid X receptor agonist GW4064 indirectly inhibits HCV entry into cells via down-regulating scavenger receptor class B type I. Farnesoid X receptor (FXR) agonists play important regulatory roles in bile acid, lipid and glucose metabolism in vitro and in vivo. GW 4064 29-35 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 142-152 30902657-0 2019 Farnesoid X receptor agonist GW4064 indirectly inhibits HCV entry into cells via down-regulating scavenger receptor class B type I. Farnesoid X receptor (FXR) agonists play important regulatory roles in bile acid, lipid and glucose metabolism in vitro and in vivo. GW 4064 29-35 nuclear receptor subfamily 1 group H member 4 Homo sapiens 154-157 30902657-2 2019 This study investigated the effect and mechanism of FXR agonist GW4064 against HCV in vitro to explore the potential application of FXR agonists. GW 4064 64-70 nuclear receptor subfamily 1 group H member 4 Homo sapiens 52-55 30902657-4 2019 GW4064 down-regulated the expression of scavenger receptor class B type I protein via FXR and thereby indirectly inhibited HCV entry into cells, leading to interruption of HCV life cycle. GW 4064 0-6 nuclear receptor subfamily 1 group H member 4 Homo sapiens 86-89 31561852-3 2019 We evaluated pharmacological activation of FXR with the synthetic agonist GW4064 using comprehensive proteomic analysis in colorectal cancer cell lines (HCT116, SW480, and DLD1). GW 4064 74-80 nuclear receptor subfamily 1 group H member 4 Homo sapiens 43-46 31561852-9 2019 Co-treatment of TRAIL with GW4064 synergistically inhibited colorectal cancer cell proliferation as compared with single treatments. GW 4064 27-33 TNF superfamily member 10 Homo sapiens 16-21 30428773-0 2019 Farnesoid X Receptor Agonist GW4064 Inhibits Aromatase and ERbeta Expression in Human Endometriotic Stromal Cells. GW 4064 29-35 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 10-20 30428773-0 2019 Farnesoid X Receptor Agonist GW4064 Inhibits Aromatase and ERbeta Expression in Human Endometriotic Stromal Cells. GW 4064 29-35 estrogen receptor 2 Homo sapiens 59-65 30428773-4 2019 Here, we aimed to investigate whether FXR activation by its synthetic agonist GW4064 has a therapeutic effect on endometriosis and the underlying molecular mechanisms. GW 4064 78-84 nuclear receptor subfamily 1 group H member 4 Homo sapiens 38-41 30428773-6 2019 The GW4064 treatment led to a dose-dependent decrease in aromatase and estrogen receptor beta (ERbeta) expression and induced ERK1/2, p38, AMPK, and Stat3 activation in ESCs. GW 4064 4-10 estrogen receptor 2 Homo sapiens 71-93 30428773-6 2019 The GW4064 treatment led to a dose-dependent decrease in aromatase and estrogen receptor beta (ERbeta) expression and induced ERK1/2, p38, AMPK, and Stat3 activation in ESCs. GW 4064 4-10 estrogen receptor 2 Homo sapiens 95-101 30428773-6 2019 The GW4064 treatment led to a dose-dependent decrease in aromatase and estrogen receptor beta (ERbeta) expression and induced ERK1/2, p38, AMPK, and Stat3 activation in ESCs. GW 4064 4-10 mitogen-activated protein kinase 3 Homo sapiens 126-132 30428773-6 2019 The GW4064 treatment led to a dose-dependent decrease in aromatase and estrogen receptor beta (ERbeta) expression and induced ERK1/2, p38, AMPK, and Stat3 activation in ESCs. GW 4064 4-10 mitogen-activated protein kinase 1 Homo sapiens 134-137 30428773-6 2019 The GW4064 treatment led to a dose-dependent decrease in aromatase and estrogen receptor beta (ERbeta) expression and induced ERK1/2, p38, AMPK, and Stat3 activation in ESCs. GW 4064 4-10 signal transducer and activator of transcription 3 Homo sapiens 149-154 30428773-7 2019 In contrast, ERK1/2 inhibitor reversed the GW4064-induced reduction in aromatase expression. GW 4064 43-49 mitogen-activated protein kinase 3 Homo sapiens 13-19 30428773-8 2019 In addition, treatment with p38, AMPK, and Stat3 inhibitors or small interfering RNAs could also reverse the GW4064-induced reduction of ERbeta expression in ESCs. GW 4064 109-115 mitogen-activated protein kinase 1 Homo sapiens 28-31 30428773-8 2019 In addition, treatment with p38, AMPK, and Stat3 inhibitors or small interfering RNAs could also reverse the GW4064-induced reduction of ERbeta expression in ESCs. GW 4064 109-115 signal transducer and activator of transcription 3 Homo sapiens 43-48 30428773-8 2019 In addition, treatment with p38, AMPK, and Stat3 inhibitors or small interfering RNAs could also reverse the GW4064-induced reduction of ERbeta expression in ESCs. GW 4064 109-115 estrogen receptor 2 Homo sapiens 137-143 30428773-9 2019 The GW4064 treatment markedly increased Stat3 phosphorylation, enhancing the binding of Stat3 to the ESR2 promoter, which resulted in the downregulation of ERbeta. GW 4064 4-10 signal transducer and activator of transcription 3 Homo sapiens 40-45 30428773-9 2019 The GW4064 treatment markedly increased Stat3 phosphorylation, enhancing the binding of Stat3 to the ESR2 promoter, which resulted in the downregulation of ERbeta. GW 4064 4-10 signal transducer and activator of transcription 3 Homo sapiens 88-93 30428773-9 2019 The GW4064 treatment markedly increased Stat3 phosphorylation, enhancing the binding of Stat3 to the ESR2 promoter, which resulted in the downregulation of ERbeta. GW 4064 4-10 estrogen receptor 2 Homo sapiens 101-105 30428773-9 2019 The GW4064 treatment markedly increased Stat3 phosphorylation, enhancing the binding of Stat3 to the ESR2 promoter, which resulted in the downregulation of ERbeta. GW 4064 4-10 estrogen receptor 2 Homo sapiens 156-162 30428773-10 2019 Coimmunoprecipitation assay and chromatin immunoprecipitation analysis revealed that FXR was able to compete with cyclic AMP response element-binding (CREB) protein for binding to a common sequence on the aromatase promoter region after GW4064 treatment in ESCs. GW 4064 237-243 nuclear receptor subfamily 1 group H member 4 Homo sapiens 85-88 30428773-10 2019 Coimmunoprecipitation assay and chromatin immunoprecipitation analysis revealed that FXR was able to compete with cyclic AMP response element-binding (CREB) protein for binding to a common sequence on the aromatase promoter region after GW4064 treatment in ESCs. GW 4064 237-243 cAMP responsive element binding protein 1 Homo sapiens 151-155 30428773-11 2019 Moreover, treatment of endometriosis xenografts with GW4064 suppressed aromatase and ERbeta expression in nude mice. GW 4064 53-59 estrogen receptor 2 (beta) Mus musculus 85-91 30864232-8 2019 However, response to FXR synthetic ligands was maintained in DKO mice as treatment with GW4064 resulted in similar changes in gene expression in all strains of mice. GW 4064 88-94 nuclear receptor subfamily 1, group H, member 4 Mus musculus 21-24 31191305-3 2019 FNDC5 expression was highly induced by CDCA and GW4064 in hepatocytes, HepG2 cells, and the circulating level of Irisin increased in Rhesus macaques. GW 4064 48-54 fibronectin type III domain containing 5 Homo sapiens 0-5 30747230-5 2019 Conversely, the FXR agonist GW4064 synergistically enhanced bile acid-induced CDX2 promoter activity. GW 4064 28-34 nuclear receptor subfamily 1 group H member 4 Homo sapiens 16-19 30229432-4 2019 Furthermore, the reported agonists for the expression of DGKtheta, cAMP and GW4064, the known inhibitor for DGKtheta enzyme activity, R59949, and a potential regulator for DGKtheta enzyme expression, EGCG (the major catechin in green tea), were applied to the reporter cell line. GW 4064 76-82 diacylglycerol kinase theta Homo sapiens 108-116 30229432-4 2019 Furthermore, the reported agonists for the expression of DGKtheta, cAMP and GW4064, the known inhibitor for DGKtheta enzyme activity, R59949, and a potential regulator for DGKtheta enzyme expression, EGCG (the major catechin in green tea), were applied to the reporter cell line. GW 4064 76-82 diacylglycerol kinase theta Homo sapiens 108-116 30768114-6 2019 This regulation was associated with the alterations in the expression of target genes in the enterohepatic farnesoid X receptor-fibroblast growth factor (FXR-FGF15) axis and could be reversed using an FXR agonist, GW4064. GW 4064 214-220 nuclear receptor subfamily 1, group H, member 4 Mus musculus 154-157 30768114-6 2019 This regulation was associated with the alterations in the expression of target genes in the enterohepatic farnesoid X receptor-fibroblast growth factor (FXR-FGF15) axis and could be reversed using an FXR agonist, GW4064. GW 4064 214-220 fibroblast growth factor 15 Mus musculus 158-163 30768114-6 2019 This regulation was associated with the alterations in the expression of target genes in the enterohepatic farnesoid X receptor-fibroblast growth factor (FXR-FGF15) axis and could be reversed using an FXR agonist, GW4064. GW 4064 214-220 nuclear receptor subfamily 1, group H, member 4 Mus musculus 201-204 30747230-5 2019 Conversely, the FXR agonist GW4064 synergistically enhanced bile acid-induced CDX2 promoter activity. GW 4064 28-34 caudal type homeobox 2 Homo sapiens 78-82 30747230-9 2019 Treatment with GW4064 or Z-guggulsterone enhanced and attenuated the binding activity of p50 to the CDX2 promoter, respectively. GW 4064 15-21 nuclear factor kappa B subunit 1 Homo sapiens 89-92 30747230-9 2019 Treatment with GW4064 or Z-guggulsterone enhanced and attenuated the binding activity of p50 to the CDX2 promoter, respectively. GW 4064 15-21 caudal type homeobox 2 Homo sapiens 100-104 30996771-3 2019 In this Letter, we have elaborated on the structure of GW4064, the first nonsteroidal agonist for FXR, to identify novel isoxazoles endowed with FXR agonistic activity and improved ADME properties. GW 4064 55-61 nuclear receptor subfamily 1, group H, member 4 Mus musculus 98-101 30307769-4 2019 Treatment with the FXRalpha agonist GW4064 inhibited FXRalpha proviral effect on cccDNA similarly for wild-type and hepatitis B viral X protein (HBx)-deficient virus, whereas agonist-induced inhibition of pregenomic and precore RNA transcription and viral DNA secretion was HBx dependent. GW 4064 36-42 X protein Hepatitis B virus 145-148 30307769-4 2019 Treatment with the FXRalpha agonist GW4064 inhibited FXRalpha proviral effect on cccDNA similarly for wild-type and hepatitis B viral X protein (HBx)-deficient virus, whereas agonist-induced inhibition of pregenomic and precore RNA transcription and viral DNA secretion was HBx dependent. GW 4064 36-42 X protein Hepatitis B virus 274-277 30996771-3 2019 In this Letter, we have elaborated on the structure of GW4064, the first nonsteroidal agonist for FXR, to identify novel isoxazoles endowed with FXR agonistic activity and improved ADME properties. GW 4064 55-61 nuclear receptor subfamily 1, group H, member 4 Mus musculus 145-148 29849798-3 2018 Human gastric cell lines were treated with chenodeoxycholic acid (CDCA) or FXR agonist GW4064. GW 4064 87-93 nuclear receptor subfamily 1 group H member 4 Homo sapiens 75-78 30176263-3 2018 We showed that FXR is expressed in human CAFs isolated from four patients and treatment with the selective FXR agonist GW4064 decreased CAF migration, stress-fiber formation and contractility. GW 4064 119-125 nuclear receptor subfamily 1 group H member 4 Homo sapiens 15-18 30176263-3 2018 We showed that FXR is expressed in human CAFs isolated from four patients and treatment with the selective FXR agonist GW4064 decreased CAF migration, stress-fiber formation and contractility. GW 4064 119-125 nuclear receptor subfamily 1 group H member 4 Homo sapiens 107-110 30106441-13 2018 In the present study, activation of FXR by GW4064 increased CCNG2 expression via suppression of miR-135A1 expression, and the FXR/miR-135A1/CCNG2 axis was demonstrated to be involved in mediating cell proliferation. GW 4064 43-49 nuclear receptor subfamily 1 group H member 4 Homo sapiens 36-39 30106441-13 2018 In the present study, activation of FXR by GW4064 increased CCNG2 expression via suppression of miR-135A1 expression, and the FXR/miR-135A1/CCNG2 axis was demonstrated to be involved in mediating cell proliferation. GW 4064 43-49 cyclin G2 Homo sapiens 60-65 30106441-13 2018 In the present study, activation of FXR by GW4064 increased CCNG2 expression via suppression of miR-135A1 expression, and the FXR/miR-135A1/CCNG2 axis was demonstrated to be involved in mediating cell proliferation. GW 4064 43-49 microRNA 135a-1 Homo sapiens 96-105 30106441-13 2018 In the present study, activation of FXR by GW4064 increased CCNG2 expression via suppression of miR-135A1 expression, and the FXR/miR-135A1/CCNG2 axis was demonstrated to be involved in mediating cell proliferation. GW 4064 43-49 cyclin G2 Homo sapiens 140-145 30106441-14 2018 In conclusion, activation of FXR by GW4064 suppresses cell proliferation and causes cell cycle arrest in CRC, and the miR-135A1/CCNG2 pathway was suggested to be involved in this step. GW 4064 36-42 nuclear receptor subfamily 1 group H member 4 Homo sapiens 29-32 30139242-6 2018 We found that the FXRagonists GW4064 and INT-747 increased the protein abundance of AT2R and B2R in rat aortic VSMCs.AT2R blockade with PD123319 reversed the effects of FXR agonists on kallikrein activity, B2R, andbradykinin levels. GW 4064 30-36 angiotensin II receptor, type 2 Rattus norvegicus 84-88 30139242-6 2018 We found that the FXRagonists GW4064 and INT-747 increased the protein abundance of AT2R and B2R in rat aortic VSMCs.AT2R blockade with PD123319 reversed the effects of FXR agonists on kallikrein activity, B2R, andbradykinin levels. GW 4064 30-36 bradykinin receptor B2 Rattus norvegicus 93-96 30139242-6 2018 We found that the FXRagonists GW4064 and INT-747 increased the protein abundance of AT2R and B2R in rat aortic VSMCs.AT2R blockade with PD123319 reversed the effects of FXR agonists on kallikrein activity, B2R, andbradykinin levels. GW 4064 30-36 angiotensin II receptor, type 2 Rattus norvegicus 117-121 30139242-6 2018 We found that the FXRagonists GW4064 and INT-747 increased the protein abundance of AT2R and B2R in rat aortic VSMCs.AT2R blockade with PD123319 reversed the effects of FXR agonists on kallikrein activity, B2R, andbradykinin levels. GW 4064 30-36 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 18-21 30139242-6 2018 We found that the FXRagonists GW4064 and INT-747 increased the protein abundance of AT2R and B2R in rat aortic VSMCs.AT2R blockade with PD123319 reversed the effects of FXR agonists on kallikrein activity, B2R, andbradykinin levels. GW 4064 30-36 bradykinin receptor B2 Rattus norvegicus 206-209 29668847-5 2018 At 1 week after MI, both sham and MI mice were gavaged with 25 mg/kg/d of a synthetic FXR agonist (GW4064) or a vehicle control for 7 weeks, and cardiac performance was assessed by consecutive echocardiography studies. GW 4064 99-105 nuclear receptor subfamily 1, group H, member 4 Mus musculus 86-89 29668847-7 2018 Moreover, GW4064 treatment increased angiogenesis and mitochondrial biogenesis, reduced cardiomyocyte loss and inflammation, and ameliorated cardiac remodelling as evidenced by heart weight, lung weight, atrial natriuretic peptide/brain natriuretic peptide levels, and myocardial fibrosis at 8 weeks post-MI. GW 4064 10-16 natriuretic peptide type B Mus musculus 231-256 29668847-8 2018 At the molecular level, GW4064 significantly increased FXR mRNA expression and transcriptional activity in heart tissue. GW 4064 24-30 nuclear receptor subfamily 1, group H, member 4 Mus musculus 55-58 29377207-13 2018 Mice treated with GW4064 had increased, and FXR and SHP null mice had decreased, basal Xbp1s gene expression. GW 4064 18-24 X-box binding protein 1 Mus musculus 87-91 29958417-4 2018 FXR agonists (chenodeoxycholic acid, GW4064, and obeticholic acid):but not an antagonist (guggulsterone)&mdash;induced actin polymerization and expression of N-cadherin and phosphorylated focal adhesion kinase, although they were less effective than transforming growth factor beta (TGF-beta). GW 4064 37-43 nuclear receptor subfamily 1 group H member 4 Homo sapiens 0-3 29958417-4 2018 FXR agonists (chenodeoxycholic acid, GW4064, and obeticholic acid):but not an antagonist (guggulsterone)&mdash;induced actin polymerization and expression of N-cadherin and phosphorylated focal adhesion kinase, although they were less effective than transforming growth factor beta (TGF-beta). GW 4064 37-43 cadherin 2 Homo sapiens 162-172 30139242-7 2018 Moreover, we found that GW4064 and INT-747 decreased intracellular [Ca2+], increasedSERCA activity, downregulated IP3R1 expression, and attenuated IP3-induced Ca2+ release. GW 4064 24-30 inositol 1,4,5-trisphosphate receptor, type 1 Rattus norvegicus 114-119 29668847-10 2018 Among the four down-stream soluble molecules of FXR, plasma adiponectin was most significantly increased by GW4064. GW 4064 108-114 nuclear receptor subfamily 1, group H, member 4 Mus musculus 48-51 29668847-10 2018 Among the four down-stream soluble molecules of FXR, plasma adiponectin was most significantly increased by GW4064. GW 4064 108-114 adiponectin, C1Q and collagen domain containing Mus musculus 60-71 29668847-11 2018 In cultured adipocytes, GW4064 increased mRNA levels and protein expression of adiponectin. GW 4064 24-30 adiponectin, C1Q and collagen domain containing Mus musculus 79-90 29668847-12 2018 Conditioned medium of GW4064-treated adipocytes activated AMPK-PGC-1alpha signalling and reduced hypoxia-induced cardiomyocyte apoptosis, all of which were attenuated by an adiponectin neutralizing anti-body. GW 4064 22-28 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 63-73 29668847-12 2018 Conditioned medium of GW4064-treated adipocytes activated AMPK-PGC-1alpha signalling and reduced hypoxia-induced cardiomyocyte apoptosis, all of which were attenuated by an adiponectin neutralizing anti-body. GW 4064 22-28 adiponectin, C1Q and collagen domain containing Mus musculus 173-184 29668847-13 2018 More importantly, when knocking-out adiponectin in mice, the cardioprotective effects of GW4064 were attenuated. GW 4064 89-95 adiponectin, C1Q and collagen domain containing Mus musculus 36-47 29377207-7 2018 XBP1 pathway activation increased in Huh7-Ntcp and HepG2 cells treated with bile acids, 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA) or GW4064. GW 4064 136-142 X-box binding protein 1 Homo sapiens 0-4 29377207-7 2018 XBP1 pathway activation increased in Huh7-Ntcp and HepG2 cells treated with bile acids, 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA) or GW4064. GW 4064 136-142 MIR7-3 host gene Homo sapiens 37-41 29377207-7 2018 XBP1 pathway activation increased in Huh7-Ntcp and HepG2 cells treated with bile acids, 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA) or GW4064. GW 4064 136-142 solute carrier family 10 member 1 Homo sapiens 42-46 29235094-3 2018 In the cellular experiments, FXR expression was up-regulated by either lentiviral transduction or GW4064 treatment and down-regulated by either siRNA technology or treatment with guggulsterones. GW 4064 98-104 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 29-32 29351391-8 2018 DCA also induced nuclear accumulation of the farnesoid X receptor (FXR), whereas an FXR agonist, GW4064 (10 microM), inhibited wound closure. GW 4064 97-103 nuclear receptor subfamily 1 group H member 4 Homo sapiens 84-87 29351391-9 2018 Both DCA and GW4064 attenuated the expression of CFTR Cl- channels, whereas inhibition of CFTR activity with either CFTR-inh-172 (10 microM) or GlyH-101 (25 microM) also prevented wound healing. GW 4064 13-19 CF transmembrane conductance regulator Homo sapiens 49-53 29328388-8 2018 These results indicated that in WT mice, administration of GW4064 ameliorated LPS-mediated liver injury by upregulation of FXR expression, which was in part mediated by the TLR4/p38 MAPK pathway. GW 4064 59-65 nuclear receptor subfamily 1, group H, member 4 Mus musculus 123-126 29328388-8 2018 These results indicated that in WT mice, administration of GW4064 ameliorated LPS-mediated liver injury by upregulation of FXR expression, which was in part mediated by the TLR4/p38 MAPK pathway. GW 4064 59-65 toll-like receptor 4 Mus musculus 173-177 29328388-0 2018 GW4064 attenuates lipopolysaccharide-induced hepatic inflammation and apoptosis through inhibition of the Toll-like receptor 4-mediated p38 mitogen-activated protein kinase signaling pathway in mice. GW 4064 0-6 toll-like receptor 4 Mus musculus 106-126 29328388-8 2018 These results indicated that in WT mice, administration of GW4064 ameliorated LPS-mediated liver injury by upregulation of FXR expression, which was in part mediated by the TLR4/p38 MAPK pathway. GW 4064 59-65 mitogen-activated protein kinase 14 Mus musculus 178-181 29328388-0 2018 GW4064 attenuates lipopolysaccharide-induced hepatic inflammation and apoptosis through inhibition of the Toll-like receptor 4-mediated p38 mitogen-activated protein kinase signaling pathway in mice. GW 4064 0-6 mitogen-activated protein kinase 14 Mus musculus 136-139 29328388-3 2018 The present study investigated the capacity of the FXR agonist GW4064 to protect the livers of mice from lipopolysaccharide (LPS)-induced inflammation and apoptosis. GW 4064 63-69 nuclear receptor subfamily 1, group H, member 4 Mus musculus 51-54 29328388-6 2018 Activation of FXR by GW4064 alleviated hepatic inflammation in the LPS-induced murine liver injury model as reflected by reduced serum levels of aspartate aminotransferase and pro-inflammatory cytokine mRNA expression, including tumor necrosis factor-alpha, as well as interleukin-6 and -1beta in WT mice. GW 4064 21-27 nuclear receptor subfamily 1, group H, member 4 Mus musculus 14-17 28912067-3 2017 Treatment with specific FXR agonists (i.e., GW4064 and CDCA) significantly decreased both mRNA and protein levels of SULT1E1 in HepG2 cells. GW 4064 44-50 nuclear receptor subfamily 1, group H, member 4 Mus musculus 24-27 29328388-6 2018 Activation of FXR by GW4064 alleviated hepatic inflammation in the LPS-induced murine liver injury model as reflected by reduced serum levels of aspartate aminotransferase and pro-inflammatory cytokine mRNA expression, including tumor necrosis factor-alpha, as well as interleukin-6 and -1beta in WT mice. GW 4064 21-27 tumor necrosis factor Mus musculus 229-256 29328388-6 2018 Activation of FXR by GW4064 alleviated hepatic inflammation in the LPS-induced murine liver injury model as reflected by reduced serum levels of aspartate aminotransferase and pro-inflammatory cytokine mRNA expression, including tumor necrosis factor-alpha, as well as interleukin-6 and -1beta in WT mice. GW 4064 21-27 interleukin 6 Mus musculus 269-293 28912067-3 2017 Treatment with specific FXR agonists (i.e., GW4064 and CDCA) significantly decreased both mRNA and protein levels of SULT1E1 in HepG2 cells. GW 4064 44-50 sulfotransferase family 1E, member 1 Mus musculus 117-124 28267333-3 2017 GW4064 and chenodeoxycholic acid (two specific FXR agonists) treatment of HepG2 cells led to a significant increase in the mRNA level of UGT2B10. GW 4064 0-6 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 137-144 28267333-3 2017 GW4064 and chenodeoxycholic acid (two specific FXR agonists) treatment of HepG2 cells led to a significant increase in the mRNA level of UGT2B10. GW 4064 0-6 nuclear receptor subfamily 1 group H member 4 Homo sapiens 47-50 28787755-0 2017 A rapid administration of GW4064 inhibits the NLRP3 inflammasome activation independent of farnesoid X receptor agonism. GW 4064 26-32 NLR family pyrin domain containing 3 Homo sapiens 46-51 28787755-1 2017 GW4064 is a small molecule known to be an agonist of the nuclear farnesoid X receptor (FXR). GW 4064 0-6 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 75-85 28787755-1 2017 GW4064 is a small molecule known to be an agonist of the nuclear farnesoid X receptor (FXR). GW 4064 0-6 nuclear receptor subfamily 1 group H member 4 Homo sapiens 87-90 28787755-2 2017 We found that GW4064 inhibits the NLR family CARD domain containing 3 (NLRP3) inflammasome activation in an FXR-independent manner as evidenced by its similar inhibitory effect on NLRP3 inflammasome activation in FXR-deficient macrophages. GW 4064 14-20 NLR family pyrin domain containing 3 Homo sapiens 71-76 28787755-2 2017 We found that GW4064 inhibits the NLR family CARD domain containing 3 (NLRP3) inflammasome activation in an FXR-independent manner as evidenced by its similar inhibitory effect on NLRP3 inflammasome activation in FXR-deficient macrophages. GW 4064 14-20 nuclear receptor subfamily 1 group H member 4 Homo sapiens 108-111 28787755-2 2017 We found that GW4064 inhibits the NLR family CARD domain containing 3 (NLRP3) inflammasome activation in an FXR-independent manner as evidenced by its similar inhibitory effect on NLRP3 inflammasome activation in FXR-deficient macrophages. GW 4064 14-20 NLR family pyrin domain containing 3 Homo sapiens 180-185 28787755-2 2017 We found that GW4064 inhibits the NLR family CARD domain containing 3 (NLRP3) inflammasome activation in an FXR-independent manner as evidenced by its similar inhibitory effect on NLRP3 inflammasome activation in FXR-deficient macrophages. GW 4064 14-20 nuclear receptor subfamily 1 group H member 4 Homo sapiens 213-216 28787755-3 2017 Interestingly, GW4064 decreases the nigericin-induced oligomerization and ubiquitination of ASC which is critical for the NLRP3 inflammasome activation. GW 4064 15-21 PYD and CARD domain containing Homo sapiens 92-95 28787755-3 2017 Interestingly, GW4064 decreases the nigericin-induced oligomerization and ubiquitination of ASC which is critical for the NLRP3 inflammasome activation. GW 4064 15-21 NLR family pyrin domain containing 3 Homo sapiens 122-127 28787755-4 2017 In vivo results indicate that GW4064 could partially rescue the symptoms of NLRP3-dependent inflammatory disease models. GW 4064 30-36 NLR family pyrin domain containing 3 Homo sapiens 76-81 28787755-5 2017 These results not only necessitate cautious interpretation of the biological function of GW4064 as an FXR agonist, but also provide a potential therapeutic approach using GW4064 in the treatment of NLRP3-related diseases. GW 4064 89-95 nuclear receptor subfamily 1 group H member 4 Homo sapiens 102-105 28787755-5 2017 These results not only necessitate cautious interpretation of the biological function of GW4064 as an FXR agonist, but also provide a potential therapeutic approach using GW4064 in the treatment of NLRP3-related diseases. GW 4064 171-177 NLR family pyrin domain containing 3 Homo sapiens 198-203 28086800-10 2017 Expectedly, GW4064 induced phosphorylation of Akt, expression of the anti-apoptotic molecules (Bcl-xL and Bcl-2), and reduced harmful hepatic molecules (Fas ligand and Fas). GW 4064 12-18 BCL2-like 1 Mus musculus 95-101 28086800-6 2017 RESULTS: An FXR-specific agonist, GW4064, induced expressions of the p62/SQSTM1 gene and protein in AML12 mouse liver cells. GW 4064 34-40 nuclear receptor subfamily 1, group H, member 4 Mus musculus 12-15 28647362-0 2017 Farnesoid X receptor agonist GW4064 ameliorates lipopolysaccharide-induced ileocolitis through TLR4/MyD88 pathway related mitochondrial dysfunction in mice. GW 4064 29-35 toll-like receptor 4 Mus musculus 95-99 28647362-0 2017 Farnesoid X receptor agonist GW4064 ameliorates lipopolysaccharide-induced ileocolitis through TLR4/MyD88 pathway related mitochondrial dysfunction in mice. GW 4064 29-35 myeloid differentiation primary response gene 88 Mus musculus 100-105 28647362-3 2017 Here we show the mechanisms of FXR agonist, GW4064, inhibits mucosal injury in ileum caused by lipopolysaccharides (LPS). GW 4064 44-50 nuclear receptor subfamily 1, group H, member 4 Mus musculus 31-34 28647362-6 2017 Interesting, GW4064 suppresses NACHT, LRR and PYD domains-containing protein 3 (NALP3) inflammasome mediates tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-6 and IL-1beta, as well as mitochondrial respiratory complexes mRNA expression in WT and FXR KO mice treated with LPS. GW 4064 13-19 NLR family, pyrin domain containing 3 Mus musculus 31-78 28647362-6 2017 Interesting, GW4064 suppresses NACHT, LRR and PYD domains-containing protein 3 (NALP3) inflammasome mediates tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-6 and IL-1beta, as well as mitochondrial respiratory complexes mRNA expression in WT and FXR KO mice treated with LPS. GW 4064 13-19 NLR family, pyrin domain containing 3 Mus musculus 80-85 28647362-6 2017 Interesting, GW4064 suppresses NACHT, LRR and PYD domains-containing protein 3 (NALP3) inflammasome mediates tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-6 and IL-1beta, as well as mitochondrial respiratory complexes mRNA expression in WT and FXR KO mice treated with LPS. GW 4064 13-19 tumor necrosis factor Mus musculus 109-136 28647362-6 2017 Interesting, GW4064 suppresses NACHT, LRR and PYD domains-containing protein 3 (NALP3) inflammasome mediates tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-6 and IL-1beta, as well as mitochondrial respiratory complexes mRNA expression in WT and FXR KO mice treated with LPS. GW 4064 13-19 tumor necrosis factor Mus musculus 138-147 28647362-6 2017 Interesting, GW4064 suppresses NACHT, LRR and PYD domains-containing protein 3 (NALP3) inflammasome mediates tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-6 and IL-1beta, as well as mitochondrial respiratory complexes mRNA expression in WT and FXR KO mice treated with LPS. GW 4064 13-19 interleukin 6 Mus musculus 150-168 28647362-6 2017 Interesting, GW4064 suppresses NACHT, LRR and PYD domains-containing protein 3 (NALP3) inflammasome mediates tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-6 and IL-1beta, as well as mitochondrial respiratory complexes mRNA expression in WT and FXR KO mice treated with LPS. GW 4064 13-19 interleukin 1 beta Mus musculus 173-181 28647362-6 2017 Interesting, GW4064 suppresses NACHT, LRR and PYD domains-containing protein 3 (NALP3) inflammasome mediates tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-6 and IL-1beta, as well as mitochondrial respiratory complexes mRNA expression in WT and FXR KO mice treated with LPS. GW 4064 13-19 nuclear receptor subfamily 1, group H, member 4 Mus musculus 256-259 28351411-16 2017 CONCLUSIONS: Our data suggest that FXR is dispensable for oligodendroglial differentiation and that FXR agonists, such as GW4064, represent a potential therapeutic approach for MS which specifically targets peripheral immune cells including macrophages but not brain-resident cells, such as oligodendrocytes, astrocytes or microglia. GW 4064 122-128 nuclear receptor subfamily 1, group H, member 4 Mus musculus 100-103 26646674-4 2017 METHODS: This study investigated the effect of LQ, metformin [an activator of activated AMP-activated protein kinase (AMPK)] and GW4064 [a ligand of farnesoid X receptor (FXR)] on mitochondrial dysfunction and oxidative stress induced by serum deprivation as well as its molecular mechanism, as assessed by immunoblot and flow cytometer assays. GW 4064 129-135 nuclear receptor subfamily 1 group H member 4 Homo sapiens 149-169 26646674-4 2017 METHODS: This study investigated the effect of LQ, metformin [an activator of activated AMP-activated protein kinase (AMPK)] and GW4064 [a ligand of farnesoid X receptor (FXR)] on mitochondrial dysfunction and oxidative stress induced by serum deprivation as well as its molecular mechanism, as assessed by immunoblot and flow cytometer assays. GW 4064 129-135 nuclear receptor subfamily 1 group H member 4 Homo sapiens 171-174 26646674-9 2017 LQ also induced protein and mRNA expression of both FXR as well as small heterodimer partner, which is important since treatment with FXR ligand GW4064 protected hepatocytes against cell death and mitochondrial damage induced by serum deprivation. GW 4064 145-151 nuclear receptor subfamily 1 group H member 4 Homo sapiens 52-55 26646674-9 2017 LQ also induced protein and mRNA expression of both FXR as well as small heterodimer partner, which is important since treatment with FXR ligand GW4064 protected hepatocytes against cell death and mitochondrial damage induced by serum deprivation. GW 4064 145-151 nuclear receptor subfamily 1 group H member 4 Homo sapiens 134-137 28086800-6 2017 RESULTS: An FXR-specific agonist, GW4064, induced expressions of the p62/SQSTM1 gene and protein in AML12 mouse liver cells. GW 4064 34-40 sequestosome 1 Mus musculus 69-72 28086800-6 2017 RESULTS: An FXR-specific agonist, GW4064, induced expressions of the p62/SQSTM1 gene and protein in AML12 mouse liver cells. GW 4064 34-40 sequestosome 1 Mus musculus 73-79 28086800-7 2017 Because we previously reported p62/SQSTM1 as a key molecule for antioxidation and cell survival in hepatocytes, we next examined the activation of nuclear factor erythroid 2-related factor-2 (Nrf2) and induction of the antioxidant molecules by GW4064. GW 4064 244-250 sequestosome 1 Mus musculus 31-34 28086800-10 2017 Expectedly, GW4064 induced phosphorylation of Akt, expression of the anti-apoptotic molecules (Bcl-xL and Bcl-2), and reduced harmful hepatic molecules (Fas ligand and Fas). GW 4064 12-18 B cell leukemia/lymphoma 2 Mus musculus 106-111 28086800-8 2017 GW4064 activated Nrf2 and subsequently induced antioxidant molecules (Nrf2, catalase, HO-1, and thioredoxin). GW 4064 0-6 nuclear factor, erythroid derived 2, like 2 Mus musculus 17-21 28086800-8 2017 GW4064 activated Nrf2 and subsequently induced antioxidant molecules (Nrf2, catalase, HO-1, and thioredoxin). GW 4064 0-6 nuclear factor, erythroid derived 2, like 2 Mus musculus 70-74 28086800-8 2017 GW4064 activated Nrf2 and subsequently induced antioxidant molecules (Nrf2, catalase, HO-1, and thioredoxin). GW 4064 0-6 catalase Mus musculus 76-84 28086800-8 2017 GW4064 activated Nrf2 and subsequently induced antioxidant molecules (Nrf2, catalase, HO-1, and thioredoxin). GW 4064 0-6 heme oxygenase 1 Mus musculus 86-90 28086800-8 2017 GW4064 activated Nrf2 and subsequently induced antioxidant molecules (Nrf2, catalase, HO-1, and thioredoxin). GW 4064 0-6 thioredoxin 1 Mus musculus 96-107 28086800-10 2017 Expectedly, GW4064 induced phosphorylation of Akt, expression of the anti-apoptotic molecules (Bcl-xL and Bcl-2), and reduced harmful hepatic molecules (Fas ligand and Fas). GW 4064 12-18 thymoma viral proto-oncogene 1 Mus musculus 46-49 28086800-11 2017 GW4064 promoted hepatocyte survival, which was cancelled by p62/SQSTM1 siRNA. GW 4064 0-6 sequestosome 1 Mus musculus 60-63 28086800-11 2017 GW4064 promoted hepatocyte survival, which was cancelled by p62/SQSTM1 siRNA. GW 4064 0-6 sequestosome 1 Mus musculus 64-70 28086800-13 2017 Furthermore, GW4064 induced the expression of small heterodimer partners (SHP) and suppressed liver X receptor (LXR)-induced steatosis in hepatocytes, expecting the in vivo protective effect of FXR on liver injury especially with steatosis. GW 4064 13-19 nuclear receptor subfamily 0, group B, member 2 Mus musculus 74-77 28086800-13 2017 Furthermore, GW4064 induced the expression of small heterodimer partners (SHP) and suppressed liver X receptor (LXR)-induced steatosis in hepatocytes, expecting the in vivo protective effect of FXR on liver injury especially with steatosis. GW 4064 13-19 nuclear receptor subfamily 1, group H, member 3 Mus musculus 94-110 28086800-13 2017 Furthermore, GW4064 induced the expression of small heterodimer partners (SHP) and suppressed liver X receptor (LXR)-induced steatosis in hepatocytes, expecting the in vivo protective effect of FXR on liver injury especially with steatosis. GW 4064 13-19 nuclear receptor subfamily 1, group H, member 3 Mus musculus 112-115 28086800-13 2017 Furthermore, GW4064 induced the expression of small heterodimer partners (SHP) and suppressed liver X receptor (LXR)-induced steatosis in hepatocytes, expecting the in vivo protective effect of FXR on liver injury especially with steatosis. GW 4064 13-19 nuclear receptor subfamily 1, group H, member 4 Mus musculus 194-197 28086800-14 2017 In the hepatectomy model of db/db mice with fatty liver, pre-treatment by GW4064 significantly reduced post-PH liver injury (serum levels of LDH, AST & ALT and histological study) and improved steatosis. GW 4064 74-80 transmembrane protease, serine 11d Mus musculus 146-149 28086800-14 2017 In the hepatectomy model of db/db mice with fatty liver, pre-treatment by GW4064 significantly reduced post-PH liver injury (serum levels of LDH, AST & ALT and histological study) and improved steatosis. GW 4064 74-80 glutamic pyruvic transaminase, soluble Mus musculus 156-159 28086800-15 2017 The key molecules, p62/SQSTM1, Nrf2 and SHP were upregulated in fatty liver tissue by GW4064 treatment. GW 4064 86-92 sequestosome 1 Mus musculus 19-22 28086800-15 2017 The key molecules, p62/SQSTM1, Nrf2 and SHP were upregulated in fatty liver tissue by GW4064 treatment. GW 4064 86-92 sequestosome 1 Mus musculus 23-29 28086800-15 2017 The key molecules, p62/SQSTM1, Nrf2 and SHP were upregulated in fatty liver tissue by GW4064 treatment. GW 4064 86-92 nuclear factor, erythroid derived 2, like 2 Mus musculus 31-35 28086800-15 2017 The key molecules, p62/SQSTM1, Nrf2 and SHP were upregulated in fatty liver tissue by GW4064 treatment. GW 4064 86-92 nuclear receptor subfamily 0, group B, member 2 Mus musculus 40-43 27758768-3 2016 In this study, we show that FXR is present in human platelets and FXR ligands, GW4064 and 6alpha-ethyl-chenodeoxycholic acid, modulate platelet activation nongenomically. GW 4064 79-85 nuclear receptor subfamily 1 group H member 4 Homo sapiens 28-31 29283075-4 2017 RESULTS: In human hepatocytes, treatment with the FXR agonists GW4064 (1.0 microM) and WAY362450 (0.1 microM) did not significantly induce the mRNA expression of BACS and BAT genes. GW 4064 63-69 nuclear receptor subfamily 1 group H member 4 Homo sapiens 50-53 29283075-6 2017 Interestingly, a follow up study conducted in rat hepatocytes indicated that GW4064 induced the BACS gene while WAY362450 induced the BAT gene, confirming literature results that these genes can be induced in rat. GW 4064 77-83 solute carrier family 27 member 5 Rattus norvegicus 96-100 27758768-3 2016 In this study, we show that FXR is present in human platelets and FXR ligands, GW4064 and 6alpha-ethyl-chenodeoxycholic acid, modulate platelet activation nongenomically. GW 4064 79-85 nuclear receptor subfamily 1 group H member 4 Homo sapiens 66-69 27758768-9 2016 The atheroprotective effects of GW4064, with its novel antiplatelet effects, indicate FXR as a potential target for the prevention of atherothrombotic disease. GW 4064 32-38 nuclear receptor subfamily 1 group H member 4 Homo sapiens 86-89 27471003-4 2016 Activation of FXR by chenodeoxycholic acid (CDCA) or GW4064 significantly decreased PLA2G12B expression in HepG2 cells. GW 4064 53-59 nuclear receptor subfamily 1 group H member 4 Homo sapiens 14-17 27471003-4 2016 Activation of FXR by chenodeoxycholic acid (CDCA) or GW4064 significantly decreased PLA2G12B expression in HepG2 cells. GW 4064 53-59 phospholipase A2 group XIIB Homo sapiens 84-92 27251172-4 2016 In HepaRG cells, FXR agonists (6-ethyl chenodeoxycholic acid and GW4064), but no antagonist, and an FXR-unrelated bile salt inhibited viral mRNA, DNA, and protein production (IC50, 0.1-0.5 muM) and reduced covalently closed circular DNA pool size. GW 4064 65-71 nuclear receptor subfamily 1 group H member 4 Homo sapiens 17-20 28066584-9 2016 FXR agonist GW4064 remarkably enhanced and FXR antagonist Z-Guggulsterone significantly inhibited EMT changes in TGF-beta1-treated HBE cells. GW 4064 12-18 nuclear receptor subfamily 1 group H member 4 Homo sapiens 0-3 28066584-10 2016 Both chenodeoxycholic acid (CDCA) and GW4064 increased COX-2 expression in HBE cells, whereas Z-Guggulsterone dramatically restrained CDCA-induced COX-2 expression. GW 4064 38-44 prostaglandin-endoperoxide synthase 2 Homo sapiens 55-60 27609522-0 2016 Restoration of enterohepatic bile acid pathways in pregnant mice following short term activation of Fxr by GW4064. GW 4064 107-113 nuclear receptor subfamily 1, group H, member 4 Mus musculus 100-103 27609522-5 2016 The objective of this study was to determine whether short-term treatment of pregnant mice with GW4064 (a potent FXR agonist) restores Fxr signaling to the level observed in virgin mice. GW 4064 96-102 nuclear receptor subfamily 1, group H, member 4 Mus musculus 113-116 27609522-5 2016 The objective of this study was to determine whether short-term treatment of pregnant mice with GW4064 (a potent FXR agonist) restores Fxr signaling to the level observed in virgin mice. GW 4064 96-102 nuclear receptor subfamily 1, group H, member 4 Mus musculus 135-138 27609522-7 2016 Treatment of pregnant mice with GW4064 induced ileal Fgf15, Shp and Ostalpha/beta mRNAs, and restored hepatic Shp, Bal, Ntcp, and Bsep back to vehicle-treated virgin levels. GW 4064 32-38 fibroblast growth factor 15 Mus musculus 53-58 27609522-7 2016 Treatment of pregnant mice with GW4064 induced ileal Fgf15, Shp and Ostalpha/beta mRNAs, and restored hepatic Shp, Bal, Ntcp, and Bsep back to vehicle-treated virgin levels. GW 4064 32-38 nuclear receptor subfamily 0, group B, member 2 Mus musculus 60-63 27609522-7 2016 Treatment of pregnant mice with GW4064 induced ileal Fgf15, Shp and Ostalpha/beta mRNAs, and restored hepatic Shp, Bal, Ntcp, and Bsep back to vehicle-treated virgin levels. GW 4064 32-38 nuclear receptor subfamily 0, group B, member 2 Mus musculus 110-113 27609522-7 2016 Treatment of pregnant mice with GW4064 induced ileal Fgf15, Shp and Ostalpha/beta mRNAs, and restored hepatic Shp, Bal, Ntcp, and Bsep back to vehicle-treated virgin levels. GW 4064 32-38 poly (ADP-ribose) polymerase family, member 9 Mus musculus 115-118 27609522-7 2016 Treatment of pregnant mice with GW4064 induced ileal Fgf15, Shp and Ostalpha/beta mRNAs, and restored hepatic Shp, Bal, Ntcp, and Bsep back to vehicle-treated virgin levels. GW 4064 32-38 solute carrier family 10 (sodium/bile acid cotransporter family), member 1 Mus musculus 120-124 27609522-7 2016 Treatment of pregnant mice with GW4064 induced ileal Fgf15, Shp and Ostalpha/beta mRNAs, and restored hepatic Shp, Bal, Ntcp, and Bsep back to vehicle-treated virgin levels. GW 4064 32-38 ATP-binding cassette, sub-family B (MDR/TAP), member 11 Mus musculus 130-134 27609522-8 2016 Pregnant mice exhibited 2.5-fold increase in Cyp7a1 mRNA compared to virgin controls, which was reduced by GW4064. GW 4064 107-113 cytochrome P450, family 7, subfamily a, polypeptide 1 Mus musculus 45-51 27609522-9 2016 Similarly treatment of mouse primary hepatocytes with plasma isolated from pregnant mice induced Cyp7a1 mRNA by nearly 3-fold as compared to virgin plasma, which could be attenuated by co-treatment with either GW4064 or recombinant FGF19 protein. GW 4064 210-216 cytochrome P450, family 7, subfamily a, polypeptide 1 Mus musculus 97-103 27127878-3 2016 In the present study, we for the first time tested the effect of farnesoid X receptor (FXR) agonists GW4064 and CDCA (chenodeoxycholic acid) in combination with cisplatin (CDDP) on increasing the chemosensitivity in BTC. GW 4064 101-107 nuclear receptor subfamily 1 group H member 4 Homo sapiens 87-90 27127878-6 2016 Moreover, the experiments on tumor-bearing mice showed that GW4064/CDDP co-treatment inhibited the tumor growth in vivo by up-regulating SHP expression and down-regulating STAT3 phosphorylation. GW 4064 60-66 nuclear receptor subfamily 0, group B, member 2 Mus musculus 137-140 27127878-6 2016 Moreover, the experiments on tumor-bearing mice showed that GW4064/CDDP co-treatment inhibited the tumor growth in vivo by up-regulating SHP expression and down-regulating STAT3 phosphorylation. GW 4064 60-66 signal transducer and activator of transcription 3 Mus musculus 172-177 26950211-12 2016 GCDCA-, CDCA- and GW4064- preconditioning enhanced ABCB11 mRNA levels, but in contrast to the bile acids, GW4064 did not significantly reduce GCDCA-induced caspase-3/7 activity. GW 4064 18-24 ATP binding cassette subfamily B member 11 Homo sapiens 51-57 26899873-4 2016 Herein, we demonstrated, for the first time, that the synthetic FXR agonist GW4064, inhibiting leptin signaling, affects the tumor-promoting activities of CAFs in breast malignancy. GW 4064 76-82 nuclear receptor subfamily 1 group H member 4 Homo sapiens 64-67 26710942-7 2016 It was found that the FXR agonists GW4064 and INT-747, in a dose-dependent manner, increased the protein abundance of AT2 R, B2 R and SHP-1 and decreased that of AT1 R. GW 4064 35-41 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 22-25 26710942-7 2016 It was found that the FXR agonists GW4064 and INT-747, in a dose-dependent manner, increased the protein abundance of AT2 R, B2 R and SHP-1 and decreased that of AT1 R. GW 4064 35-41 angiotensin II receptor, type 2 Rattus norvegicus 118-123 26710942-7 2016 It was found that the FXR agonists GW4064 and INT-747, in a dose-dependent manner, increased the protein abundance of AT2 R, B2 R and SHP-1 and decreased that of AT1 R. GW 4064 35-41 bradykinin receptor B2 Rattus norvegicus 125-129 26710942-7 2016 It was found that the FXR agonists GW4064 and INT-747, in a dose-dependent manner, increased the protein abundance of AT2 R, B2 R and SHP-1 and decreased that of AT1 R. GW 4064 35-41 angiotensin II receptor, type 1a Rattus norvegicus 162-167 26899873-8 2016 Interestingly, GW4064-treated tumors exhibited decreased levels of leptin-regulated proteins along with a strong staining intensity for SOCS3. GW 4064 15-21 suppressor of cytokine signaling 3 Homo sapiens 136-141 26545738-4 2016 We show that activation of the nuclear receptor FXR, either by its endogenous ligand CDCA or the synthetic GW4064, leads to cell death in four breast cancer cell lines with distinct phenotypes: MCF-10A (normal), MCF-7 (receptor positive), MDA-MB-231 and MDA-MB-468 (triple negative). GW 4064 107-113 nuclear receptor subfamily 1 group H member 4 Homo sapiens 48-51 26450152-4 2016 In this study, we reported that FXR agonist GW4064 reduced high glucose induced human mesangial cells (HMCs) inflammation, fibrosis and proliferation by downregulating visfatin expression, which can be blunted by exogenous visfatin treatment. GW 4064 44-50 nuclear receptor subfamily 1 group H member 4 Homo sapiens 32-35 26450152-4 2016 In this study, we reported that FXR agonist GW4064 reduced high glucose induced human mesangial cells (HMCs) inflammation, fibrosis and proliferation by downregulating visfatin expression, which can be blunted by exogenous visfatin treatment. GW 4064 44-50 nicotinamide phosphoribosyltransferase Homo sapiens 168-176 26450152-4 2016 In this study, we reported that FXR agonist GW4064 reduced high glucose induced human mesangial cells (HMCs) inflammation, fibrosis and proliferation by downregulating visfatin expression, which can be blunted by exogenous visfatin treatment. GW 4064 44-50 nicotinamide phosphoribosyltransferase Homo sapiens 223-231 26450152-6 2016 In vivo study also showed that GW4064 ameliorated the progression of DN in db/db mice with a decreased visfatin expression. GW 4064 31-37 nicotinamide phosphoribosyltransferase Mus musculus 103-111 26697325-1 2015 To assess the effect of farnesoid X receptor (FXR), a bile acid nuclear receptor, on renal proximal tubular cells, primary cultured mouse kidney proximal tubular cells were treated with GW4064 (a FXR agonist) or DMSO (as controls) overnight. GW 4064 186-192 nuclear receptor subfamily 1, group H, member 4 Mus musculus 196-199 26670557-4 2015 The high-affinity FXR agonist GW4064 blocks Gly-MCA action in the gut, and intestine-specific Fxr-null mice are unresponsive to the beneficial effects of Gly-MCA. GW 4064 30-36 nuclear receptor subfamily 1, group H, member 4 Mus musculus 18-21 26324224-4 2015 The treatment of FXR agonist GW4064/antagonist guggulsterone (Gug.) GW 4064 29-35 nuclear receptor subfamily 1 group H member 4 Homo sapiens 17-20 26416445-8 2015 The in vivo study in nude mice showed that treatment with FXR ligand GW4064 could decelerate the growth of HCC xenografts, up-regulate SOCS3 and p21 expression and inhibit STAT3 phosphorylation in the xenografts. GW 4064 69-75 signal transducer and activator of transcription 3 Mus musculus 172-177 26321738-6 2015 In addition, the protective effect of the selective FXR agonist GW4064 on triptolide-induced hepatotoxicity was explored in BALB/c mice. GW 4064 64-70 nuclear receptor subfamily 1, group H, member 4 Mus musculus 52-55 26321738-12 2015 In BALB/c mice, treatment with the FXR agonist GW4064 attenuated triptolide-induced liver dysfunction, structural damage, glutathione depletion and lipid peroxidation. GW 4064 47-53 nuclear receptor subfamily 1, group H, member 4 Mus musculus 35-38 26505219-3 2016 Activation of FXR by a synthetic agonist, GW4064, in mice increased occupancy of FXR and its DNA-binding partner, retinoid X receptor-alpha, at FGF15-signaling component genes, particularly betaKL, and induced expression of these genes. GW 4064 42-48 nuclear receptor subfamily 1, group H, member 4 Mus musculus 14-17 26505219-3 2016 Activation of FXR by a synthetic agonist, GW4064, in mice increased occupancy of FXR and its DNA-binding partner, retinoid X receptor-alpha, at FGF15-signaling component genes, particularly betaKL, and induced expression of these genes. GW 4064 42-48 nuclear receptor subfamily 1, group H, member 4 Mus musculus 81-84 26505219-3 2016 Activation of FXR by a synthetic agonist, GW4064, in mice increased occupancy of FXR and its DNA-binding partner, retinoid X receptor-alpha, at FGF15-signaling component genes, particularly betaKL, and induced expression of these genes. GW 4064 42-48 retinoid X receptor alpha Mus musculus 114-139 26505219-3 2016 Activation of FXR by a synthetic agonist, GW4064, in mice increased occupancy of FXR and its DNA-binding partner, retinoid X receptor-alpha, at FGF15-signaling component genes, particularly betaKL, and induced expression of these genes. GW 4064 42-48 fibroblast growth factor 15 Mus musculus 144-149 26505219-3 2016 Activation of FXR by a synthetic agonist, GW4064, in mice increased occupancy of FXR and its DNA-binding partner, retinoid X receptor-alpha, at FGF15-signaling component genes, particularly betaKL, and induced expression of these genes. GW 4064 42-48 klotho beta Mus musculus 190-196 26505219-7 2016 In mice, transient inductions of intestinal Fgf15 and hepatic betaKL were temporally correlated after GW4064 treatment, and pretreatment of hepatocytes with GW4064 before FGF19 treatment enhanced FGF19 signaling, which was abolished by transcriptional inhibition or betaKL down-regulation. GW 4064 157-163 fibroblast growth factor 15 Mus musculus 44-49 26505219-7 2016 In mice, transient inductions of intestinal Fgf15 and hepatic betaKL were temporally correlated after GW4064 treatment, and pretreatment of hepatocytes with GW4064 before FGF19 treatment enhanced FGF19 signaling, which was abolished by transcriptional inhibition or betaKL down-regulation. GW 4064 157-163 klotho beta Mus musculus 62-68 26505219-7 2016 In mice, transient inductions of intestinal Fgf15 and hepatic betaKL were temporally correlated after GW4064 treatment, and pretreatment of hepatocytes with GW4064 before FGF19 treatment enhanced FGF19 signaling, which was abolished by transcriptional inhibition or betaKL down-regulation. GW 4064 157-163 fibroblast growth factor 15 Mus musculus 196-201 26505219-7 2016 In mice, transient inductions of intestinal Fgf15 and hepatic betaKL were temporally correlated after GW4064 treatment, and pretreatment of hepatocytes with GW4064 before FGF19 treatment enhanced FGF19 signaling, which was abolished by transcriptional inhibition or betaKL down-regulation. GW 4064 157-163 klotho beta Mus musculus 266-272 26583035-6 2015 Human kidney 2 (HK2) cells were exposed to high glucose with or without the FXR agonist GW4064 or when FXR mRNA was silenced. GW 4064 88-94 nuclear receptor subfamily 1 group H member 4 Homo sapiens 76-79 26583035-8 2015 HK2 cells exposed to high glucose had reduced FXR expression and increased MCP-1, TGF-beta1, fibronectin and collagen IV expression, which was reversed in the presence of GW4064. GW 4064 171-177 hexokinase 2 Homo sapiens 0-3 26583035-8 2015 HK2 cells exposed to high glucose had reduced FXR expression and increased MCP-1, TGF-beta1, fibronectin and collagen IV expression, which was reversed in the presence of GW4064. GW 4064 171-177 nuclear receptor subfamily 1 group H member 4 Homo sapiens 46-49 26583035-8 2015 HK2 cells exposed to high glucose had reduced FXR expression and increased MCP-1, TGF-beta1, fibronectin and collagen IV expression, which was reversed in the presence of GW4064. GW 4064 171-177 C-C motif chemokine ligand 2 Homo sapiens 75-80 26583035-8 2015 HK2 cells exposed to high glucose had reduced FXR expression and increased MCP-1, TGF-beta1, fibronectin and collagen IV expression, which was reversed in the presence of GW4064. GW 4064 171-177 transforming growth factor beta 1 Homo sapiens 82-91 26583035-8 2015 HK2 cells exposed to high glucose had reduced FXR expression and increased MCP-1, TGF-beta1, fibronectin and collagen IV expression, which was reversed in the presence of GW4064. GW 4064 171-177 fibronectin 1 Homo sapiens 93-104 26416445-4 2015 In the present study, we found that activation of FXR by its specific agonist GW4064 in HCC cells inhibited cell growth, induced cell cycle arrest at G1 phase, elevated p21 expression and repressed STAT3 activity. GW 4064 78-84 nuclear receptor subfamily 1, group H, member 4 Mus musculus 50-53 26416445-4 2015 In the present study, we found that activation of FXR by its specific agonist GW4064 in HCC cells inhibited cell growth, induced cell cycle arrest at G1 phase, elevated p21 expression and repressed STAT3 activity. GW 4064 78-84 transcription elongation factor A (SII)-like 1 Mus musculus 169-172 26416445-4 2015 In the present study, we found that activation of FXR by its specific agonist GW4064 in HCC cells inhibited cell growth, induced cell cycle arrest at G1 phase, elevated p21 expression and repressed STAT3 activity. GW 4064 78-84 signal transducer and activator of transcription 3 Mus musculus 198-203 26416445-8 2015 The in vivo study in nude mice showed that treatment with FXR ligand GW4064 could decelerate the growth of HCC xenografts, up-regulate SOCS3 and p21 expression and inhibit STAT3 phosphorylation in the xenografts. GW 4064 69-75 nuclear receptor subfamily 1, group H, member 4 Mus musculus 58-61 26416445-8 2015 The in vivo study in nude mice showed that treatment with FXR ligand GW4064 could decelerate the growth of HCC xenografts, up-regulate SOCS3 and p21 expression and inhibit STAT3 phosphorylation in the xenografts. GW 4064 69-75 suppressor of cytokine signaling 3 Mus musculus 135-140 26416445-8 2015 The in vivo study in nude mice showed that treatment with FXR ligand GW4064 could decelerate the growth of HCC xenografts, up-regulate SOCS3 and p21 expression and inhibit STAT3 phosphorylation in the xenografts. GW 4064 69-75 transcription elongation factor A (SII)-like 1 Mus musculus 145-148 26321738-13 2015 Moreover, the livers of GW4064-treated mice showed increased expression of FXR and several related target genes involved in phase II and phase III xenobiotic metabolism. GW 4064 24-30 nuclear receptor subfamily 1, group H, member 4 Mus musculus 75-78 26098428-5 2015 Distinctly from CDCA, MG132 prevented SHP and an exogenous FXR agonist, GW4064 from reducing HIF-1alpha protein. GW 4064 72-78 nuclear receptor subfamily 1 group H member 4 Homo sapiens 59-62 25934227-0 2015 Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties. GW 4064 17-23 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 65-75 25934227-3 2015 Evaluation of the co-crystal structures of the widely used FXR agonist GW4064 and related compounds in complex with the FXR ligand binding domain indicated that their disubstituted isoxazole moiety is especially relevant for FXR activation. GW 4064 71-77 nuclear receptor subfamily 1 group H member 4 Homo sapiens 59-62 25934227-3 2015 Evaluation of the co-crystal structures of the widely used FXR agonist GW4064 and related compounds in complex with the FXR ligand binding domain indicated that their disubstituted isoxazole moiety is especially relevant for FXR activation. GW 4064 71-77 nuclear receptor subfamily 1 group H member 4 Homo sapiens 120-123 25934227-3 2015 Evaluation of the co-crystal structures of the widely used FXR agonist GW4064 and related compounds in complex with the FXR ligand binding domain indicated that their disubstituted isoxazole moiety is especially relevant for FXR activation. GW 4064 71-77 nuclear receptor subfamily 1 group H member 4 Homo sapiens 120-123 25926433-6 2015 The objective of this study is to investigate whether an agonist of FXR, 3-(2,6-dichlorophenyl)-4-(3"-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole (GW4064), alters CYP2D6 expression and activity. GW 4064 163-169 nuclear receptor subfamily 1, group H, member 4 Mus musculus 68-71 25926433-7 2015 In CYP2D6-humanized transgenic mice, GW4064 decreased hepatic CYP2D6 expression and activity (by 2-fold) while increasing SHP expression (by 2-fold) and SHP recruitment to the CYP2D6 promoter. GW 4064 37-43 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 3-9 25926433-7 2015 In CYP2D6-humanized transgenic mice, GW4064 decreased hepatic CYP2D6 expression and activity (by 2-fold) while increasing SHP expression (by 2-fold) and SHP recruitment to the CYP2D6 promoter. GW 4064 37-43 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 62-68 25926433-7 2015 In CYP2D6-humanized transgenic mice, GW4064 decreased hepatic CYP2D6 expression and activity (by 2-fold) while increasing SHP expression (by 2-fold) and SHP recruitment to the CYP2D6 promoter. GW 4064 37-43 nuclear receptor subfamily 0, group B, member 2 Mus musculus 122-125 25926433-7 2015 In CYP2D6-humanized transgenic mice, GW4064 decreased hepatic CYP2D6 expression and activity (by 2-fold) while increasing SHP expression (by 2-fold) and SHP recruitment to the CYP2D6 promoter. GW 4064 37-43 nuclear receptor subfamily 0, group B, member 2 Mus musculus 153-156 25926433-7 2015 In CYP2D6-humanized transgenic mice, GW4064 decreased hepatic CYP2D6 expression and activity (by 2-fold) while increasing SHP expression (by 2-fold) and SHP recruitment to the CYP2D6 promoter. GW 4064 37-43 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 62-68 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 21-27 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 21-27 nuclear receptor subfamily 0, group B, member 2 Mus musculus 45-48 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 21-27 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 54-60 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 21-27 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 54-60 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 125-131 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 125-131 nuclear receptor subfamily 0, group B, member 2 Mus musculus 45-48 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 125-131 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 54-60 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 125-131 nuclear receptor subfamily 0, group B, member 2 Mus musculus 97-100 25926433-8 2015 CYP2D6 repression by GW4064 was abrogated in Shp(-/-);CYP2D6 mice, indicating a critical role of SHP in CYP2D6 regulation by GW4064. GW 4064 125-131 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 54-60 25926433-9 2015 Also, GW4064 decreased CYP2D6 expression (by 2-fold) in primary human hepatocytes, suggesting that the results obtained in CYP2D6-humanized transgenic mice can be translated to humans. GW 4064 6-12 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 23-29 25926433-9 2015 Also, GW4064 decreased CYP2D6 expression (by 2-fold) in primary human hepatocytes, suggesting that the results obtained in CYP2D6-humanized transgenic mice can be translated to humans. GW 4064 6-12 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 123-129 25926433-10 2015 This proof of concept study provides evidence for CYP2D6 regulation by an inducer of SHP expression, namely, the FXR agonist GW4064. GW 4064 125-131 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 50-56 25926433-10 2015 This proof of concept study provides evidence for CYP2D6 regulation by an inducer of SHP expression, namely, the FXR agonist GW4064. GW 4064 125-131 nuclear receptor subfamily 0, group B, member 2 Mus musculus 85-88 25926433-10 2015 This proof of concept study provides evidence for CYP2D6 regulation by an inducer of SHP expression, namely, the FXR agonist GW4064. GW 4064 125-131 nuclear receptor subfamily 1, group H, member 4 Mus musculus 113-116 26098428-5 2015 Distinctly from CDCA, MG132 prevented SHP and an exogenous FXR agonist, GW4064 from reducing HIF-1alpha protein. GW 4064 72-78 hypoxia inducible factor 1 subunit alpha Homo sapiens 93-103 25725071-7 2015 Interestingly, GW4064 did not repress expression of CYP2B6, another target gene of PXR and CAR; GW4064 enhanced CYP2B6 promoter activity. GW 4064 96-102 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 112-118 25725071-0 2015 GW4064, an agonist of farnesoid X receptor, represses CYP3A4 expression in human hepatocytes by inducing small heterodimer partner expression. GW 4064 0-6 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 32-42 25725071-8 2015 In conclusion, GW4064 represses CYP3A4 expression in human hepatocytes, potentially through upregulation of SHP expression and subsequent repression of CYP3A4 promoter activity. GW 4064 15-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 25725071-0 2015 GW4064, an agonist of farnesoid X receptor, represses CYP3A4 expression in human hepatocytes by inducing small heterodimer partner expression. GW 4064 0-6 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-60 25725071-8 2015 In conclusion, GW4064 represses CYP3A4 expression in human hepatocytes, potentially through upregulation of SHP expression and subsequent repression of CYP3A4 promoter activity. GW 4064 15-21 nuclear receptor subfamily 0 group B member 2 Homo sapiens 108-111 25725071-5 2015 In human hepatocytes, treatment of GW4064 (1 muM) for 48 hours resulted in a 75% decrease in CYP3A4 mRNA expression and a 25% decrease in CYP3A4 activity, accompanied by ~3-fold increase in SHP mRNA expression. GW 4064 35-41 latexin Homo sapiens 45-48 25725071-5 2015 In human hepatocytes, treatment of GW4064 (1 muM) for 48 hours resulted in a 75% decrease in CYP3A4 mRNA expression and a 25% decrease in CYP3A4 activity, accompanied by ~3-fold increase in SHP mRNA expression. GW 4064 35-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 25725071-5 2015 In human hepatocytes, treatment of GW4064 (1 muM) for 48 hours resulted in a 75% decrease in CYP3A4 mRNA expression and a 25% decrease in CYP3A4 activity, accompanied by ~3-fold increase in SHP mRNA expression. GW 4064 35-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 25725071-8 2015 In conclusion, GW4064 represses CYP3A4 expression in human hepatocytes, potentially through upregulation of SHP expression and subsequent repression of CYP3A4 promoter activity. GW 4064 15-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 152-158 25725071-5 2015 In human hepatocytes, treatment of GW4064 (1 muM) for 48 hours resulted in a 75% decrease in CYP3A4 mRNA expression and a 25% decrease in CYP3A4 activity, accompanied by ~3-fold increase in SHP mRNA expression. GW 4064 35-41 nuclear receptor subfamily 0 group B member 2 Homo sapiens 190-193 25496033-8 2015 FXR knockdown abolished the inhibition of 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-Benzoic acid (GW4064) on JNK phosphorylation and ROS production induced by H2O2in HepG2 cells. GW 4064 153-159 nuclear receptor subfamily 1 group H member 4 Homo sapiens 0-3 25593129-3 2015 Consistent with this observation, treatment of mice with FXR-specific agonists (GSK2324 or GW4064) rapidly increased hepatic levels of Srebp-2 mRNA, precursor sterol response element binding protein 2 (pSREBP-2) protein, and miR-33. GW 4064 91-97 nuclear receptor subfamily 1, group H, member 4 Mus musculus 57-60 25593129-3 2015 Consistent with this observation, treatment of mice with FXR-specific agonists (GSK2324 or GW4064) rapidly increased hepatic levels of Srebp-2 mRNA, precursor sterol response element binding protein 2 (pSREBP-2) protein, and miR-33. GW 4064 91-97 sterol regulatory element binding factor 2 Mus musculus 135-142 25593129-3 2015 Consistent with this observation, treatment of mice with FXR-specific agonists (GSK2324 or GW4064) rapidly increased hepatic levels of Srebp-2 mRNA, precursor sterol response element binding protein 2 (pSREBP-2) protein, and miR-33. GW 4064 91-97 microRNA 33 Mus musculus 225-231 25987835-4 2015 In addition, we investigated the effects of farnesoid X receptor agonist GW4064 on hepatic ApoM expression in vitro. GW 4064 73-79 apolipoprotein M Homo sapiens 91-95 25987835-5 2015 In HepG2 cell cultures, both mRNA and protein levels of ApoM and LRH-1 were decreased in a time-dependent manner in the presence of 1 muM GW4064, and the inhibition effect was gradually attenuated after 24 hours. GW 4064 138-144 apolipoprotein M Homo sapiens 56-60 25987835-5 2015 In HepG2 cell cultures, both mRNA and protein levels of ApoM and LRH-1 were decreased in a time-dependent manner in the presence of 1 muM GW4064, and the inhibition effect was gradually attenuated after 24 hours. GW 4064 138-144 nuclear receptor subfamily 5 group A member 2 Homo sapiens 65-70 25496033-11 2015 SOD3 knockdown abolished the inhibition of GW4064 on JNK phosphorylation induced by H2O2in HepG2 cells. GW 4064 43-49 superoxide dismutase 3 Homo sapiens 0-4 25496033-11 2015 SOD3 knockdown abolished the inhibition of GW4064 on JNK phosphorylation induced by H2O2in HepG2 cells. GW 4064 43-49 mitogen-activated protein kinase 8 Homo sapiens 53-56 24335393-6 2014 SULT1C2 protein content was strongly increased by 1,25(OH)2D3 treatment and moderately increased by GW3965, GW4064, and rifampicin. GW 4064 108-114 sulfotransferase family 1C member 4 Homo sapiens 0-7 25499883-0 2015 Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists. GW 4064 32-38 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 52-62 25499883-2 2015 Previous work has described GW4064 as an FXR agonist with an interesting activity profile. GW 4064 28-34 nuclear receptor subfamily 1 group H member 4 Homo sapiens 41-44 25400456-0 2014 GW4064, a farnesoid X receptor agonist, upregulates adipokine expression in preadipocytes and HepG2 cells. GW 4064 0-6 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 20-30 25400456-3 2014 Moreover, mRNA expression of AdipoR2 and OB-Rb was also examined using fluorescent real-time PCR at 0, 12, 24, and 48 h in HepG2 cells treated with GW4064. GW 4064 148-154 adiponectin receptor 2 Homo sapiens 29-36 25339829-0 2014 FXR agonist GW4064 alleviates endotoxin-induced hepatic inflammation by repressing macrophage activation. GW 4064 12-18 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-3 25339829-1 2014 AIM: To examine the effect of farnesoid X receptor (FXR) activation by GW4064 on endotoxin-induced hepatic inflammation in nonalcoholic fatty liver disease (NAFLD) and the underlying mechanism. GW 4064 71-77 nuclear receptor subfamily 1, group H, member 4 Mus musculus 52-55 25339829-7 2014 Activation of FXR by GW4064 alleviated hepatic inflammation induced by endotoxin in a murine NAFLD model fed an HF diet as reflected by reduced serum levels of aspartate aminotransferase and alanine aminotransferase. GW 4064 21-27 nuclear receptor subfamily 1, group H, member 4 Mus musculus 14-17 23916961-6 2014 Antidiarrhoeal efficacy of GW4064 was assessed using two in vivo mouse models: the ovalbumin-induced diarrhoea model and cholera toxin (CTX)-induced intestinal fluid accumulation. GW 4064 27-33 serine (or cysteine) peptidase inhibitor, clade B, member 1, pseudogene Mus musculus 83-92 23916961-7 2014 RESULTS: GW4064 (5 mumol/L; 24 h), a specific FXR agonist, induced nuclear translocation of the receptor in T84 cells and attenuated Cl(-) secretory responses to both Ca(2+) and cAMP-dependent agonists. GW 4064 9-15 nuclear receptor subfamily 1 group H member 4 Homo sapiens 46-49 23916961-8 2014 GW4064 also prevented agonist-induced inhibition of NHE3 in Caco-2 cells. GW 4064 0-6 solute carrier family 9 member A3 Homo sapiens 52-56 23916961-9 2014 In mice, intraperitoneal administration of GW4064 (50 mg/mL) also inhibited Ca(2+) and cAMP-dependent secretory responses across ex vivo colonic tissues and prevented ovalbumin-induced diarrhoea and CTX-induced intestinal fluid accumulation in vivo. GW 4064 43-49 serine (or cysteine) peptidase inhibitor, clade B, member 1, pseudogene Mus musculus 167-176 24597548-0 2014 Synthetic FXR agonist GW4064 is a modulator of multiple G protein-coupled receptors. GW 4064 22-28 nuclear receptor subfamily 1 group H member 4 Homo sapiens 10-13 24597548-1 2014 The synthetic nuclear bile acid receptor (farnesoid X receptor [FXR]) agonist GW4064 is extensively used as a specific pharmacological tool to illustrate FXR functions. GW 4064 78-84 nuclear receptor subfamily 1 group H member 4 Homo sapiens 64-67 24597548-1 2014 The synthetic nuclear bile acid receptor (farnesoid X receptor [FXR]) agonist GW4064 is extensively used as a specific pharmacological tool to illustrate FXR functions. GW 4064 78-84 nuclear receptor subfamily 1 group H member 4 Homo sapiens 154-157 24597548-2 2014 We noticed that GW4064 activated empty luciferase reporters in FXR-deficient HEK-293T cells. GW 4064 16-22 nuclear receptor subfamily 1 group H member 4 Homo sapiens 63-66 24597548-9 2014 We also found that MCF-7 breast cancer cells, reported to undergo GW4064-induced apoptosis in an FXR-dependent manner, did not express FXR, and the GW4064-mediated apoptosis, also apparent in HEK-293T cells, could be blocked by selective histamine receptor regulators. GW 4064 66-72 nuclear receptor subfamily 1 group H member 4 Homo sapiens 97-100 26574146-7 2015 GW4064, a farnesoid X receptor agonist, decreases hepatic CYP2D6 expression and activity while increasing small heterodimer partner expression and its recruitment to the CYP2D6 promoter. GW 4064 0-6 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 58-64 26574146-7 2015 GW4064, a farnesoid X receptor agonist, decreases hepatic CYP2D6 expression and activity while increasing small heterodimer partner expression and its recruitment to the CYP2D6 promoter. GW 4064 0-6 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 170-176 25466848-6 2015 RESULTS: 13 nuclear hormone receptor ligands were assayed, being GW4064 (FXR ligand) the most potent activator. GW 4064 65-71 nuclear receptor subfamily 1 group H member 4 Homo sapiens 73-76 25419825-8 2014 Furthermore, we found that administration of TNF-alpha, the bile acid, chenodeoxycholic acid, and FXR nuclear receptor activation (GW4064) induced apoptosis and impaired SP-B and SP-C production in alveolar epithelial cells in vitro. GW 4064 131-137 tumor necrosis factor Homo sapiens 45-54 25419825-8 2014 Furthermore, we found that administration of TNF-alpha, the bile acid, chenodeoxycholic acid, and FXR nuclear receptor activation (GW4064) induced apoptosis and impaired SP-B and SP-C production in alveolar epithelial cells in vitro. GW 4064 131-137 surfactant protein B Homo sapiens 170-174 25419825-8 2014 Furthermore, we found that administration of TNF-alpha, the bile acid, chenodeoxycholic acid, and FXR nuclear receptor activation (GW4064) induced apoptosis and impaired SP-B and SP-C production in alveolar epithelial cells in vitro. GW 4064 131-137 surfactant protein C Homo sapiens 179-183 25010412-8 2014 In addition, cell-permeable bile acids reduced HDL endocytosis by farnesoid X receptor (FXR) activation: chenodeoxycholate and the non-steroidal FXR agonist GW4064 reduced HDL endocytosis, whereas selective CE uptake was unaltered. GW 4064 157-163 nuclear receptor subfamily 1 group H member 4 Homo sapiens 88-91 25010412-8 2014 In addition, cell-permeable bile acids reduced HDL endocytosis by farnesoid X receptor (FXR) activation: chenodeoxycholate and the non-steroidal FXR agonist GW4064 reduced HDL endocytosis, whereas selective CE uptake was unaltered. GW 4064 157-163 nuclear receptor subfamily 1 group H member 4 Homo sapiens 145-148 24597548-10 2014 Taken together, our results demonstrate identification of histamine receptors as alternate targets for GW4064, which not only necessitates cautious interpretation of the biological functions attributed to FXR using GW4064 as a pharmacological tool but also provides a basis for the rational designing of new pharmacophores for histamine receptor modulation. GW 4064 103-109 nuclear receptor subfamily 1 group H member 4 Homo sapiens 205-208 24335393-8 2014 Treatment with GW3965, GW4064, or 1,25(OH)2D3 increased reporter activity ~2-, 5-, and 5.5-fold, respectively, from a construct containing mostly intron 1 of the SULT1C2 gene. GW 4064 23-29 sulfotransferase family 1C member 4 Homo sapiens 162-169 23928191-6 2013 When FXR was expressed in liver and intestinal cells the magnitude of the response to GW4064 and bile acids differs among FXR isoforms. GW 4064 86-92 nuclear receptor subfamily 1 group H member 4 Homo sapiens 5-8 24321096-4 2014 In reporter assays, active SREBP-2 overexpression suppressed GW4064/FXR-mediated increase in reporter activities in regions containing the IR-1 motif (+848 to +5200) in the FGF19 gene. GW 4064 61-67 sterol regulatory element binding transcription factor 2 Homo sapiens 27-34 24321096-4 2014 In reporter assays, active SREBP-2 overexpression suppressed GW4064/FXR-mediated increase in reporter activities in regions containing the IR-1 motif (+848 to +5200) in the FGF19 gene. GW 4064 61-67 nuclear receptor subfamily 1 group H member 4 Homo sapiens 68-71 24321096-4 2014 In reporter assays, active SREBP-2 overexpression suppressed GW4064/FXR-mediated increase in reporter activities in regions containing the IR-1 motif (+848 to +5200) in the FGF19 gene. GW 4064 61-67 fibroblast growth factor 19 Homo sapiens 173-178 24463129-4 2014 RESULTS: The mRNA expressions of FXR, PPARgamma2, adiponectin, and AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells treated with GW4064 was significantly increased compared with the control group (all P<0.05). GW 4064 139-145 adiponectin, C1Q and collagen domain containing Homo sapiens 50-61 24463129-4 2014 RESULTS: The mRNA expressions of FXR, PPARgamma2, adiponectin, and AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells treated with GW4064 was significantly increased compared with the control group (all P<0.05). GW 4064 139-145 adiponectin receptor 2 Homo sapiens 67-74 24463129-4 2014 RESULTS: The mRNA expressions of FXR, PPARgamma2, adiponectin, and AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells treated with GW4064 was significantly increased compared with the control group (all P<0.05). GW 4064 139-145 adiponectin receptor 2 Homo sapiens 103-110 24463129-5 2014 The protein level of adiponectin was also significantly increased after GW4064 treatment. GW 4064 72-78 adiponectin, C1Q and collagen domain containing Homo sapiens 21-32 24463129-7 2014 CONCLUSION: GW4064 can up-regulate the expressions of FXR, PPARgamma2, adiponectin, AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells. GW 4064 12-18 nuclear receptor subfamily 1 group H member 4 Homo sapiens 54-57 24463129-7 2014 CONCLUSION: GW4064 can up-regulate the expressions of FXR, PPARgamma2, adiponectin, AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells. GW 4064 12-18 adiponectin, C1Q and collagen domain containing Homo sapiens 71-82 24463129-7 2014 CONCLUSION: GW4064 can up-regulate the expressions of FXR, PPARgamma2, adiponectin, AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells. GW 4064 12-18 adiponectin receptor 2 Homo sapiens 84-91 24463129-7 2014 CONCLUSION: GW4064 can up-regulate the expressions of FXR, PPARgamma2, adiponectin, AdipoR2 in 3T3-L1 preadipocytes and AdipoR2 in HepG2 cells. GW 4064 12-18 adiponectin receptor 2 Homo sapiens 120-127 24297698-5 2014 Here, we showed that, in hepatocarcinoma-derived Huh-7 cells, combined activation of FXRalpha by GW4064 and SIRT1 by activator 3 increased HBV core promoter-controlled luciferase expression by 25-fold, compared with a 10-fold increase with GW4064 alone. GW 4064 240-246 sirtuin 1 Homo sapiens 108-113 24115725-4 2014 Among the selected compounds, the stilbene carboxylic acid GW4064 was identified as an effective antagonist of EphA2, being able to block EphA2 activation in prostate carcinoma cells, in the micromolar range. GW 4064 59-65 EPH receptor A2 Homo sapiens 111-116 24115725-4 2014 Among the selected compounds, the stilbene carboxylic acid GW4064 was identified as an effective antagonist of EphA2, being able to block EphA2 activation in prostate carcinoma cells, in the micromolar range. GW 4064 59-65 EPH receptor A2 Homo sapiens 138-143 25388536-3 2014 The quest for synthetic non-steroidal FXR agonists with general drug likeliness and improved pharmacokinetic and - dynamic properties has started more than a decade ago: The first non-steroidal and selective FXR agonist with decent submicromolar potency, GW4064, was patented in 1998 and published in 2000. GW 4064 255-261 nuclear receptor subfamily 1 group H member 4 Homo sapiens 38-41 25388536-3 2014 The quest for synthetic non-steroidal FXR agonists with general drug likeliness and improved pharmacokinetic and - dynamic properties has started more than a decade ago: The first non-steroidal and selective FXR agonist with decent submicromolar potency, GW4064, was patented in 1998 and published in 2000. GW 4064 255-261 nuclear receptor subfamily 1 group H member 4 Homo sapiens 208-211 25388536-4 2014 Since then, many pharmaceutical companies have taken GW4064 as a structural template for their efforts in identifying novel patentable FXR agonists with the GW-derived trisubstituted isoxazole general structure. GW 4064 53-59 nuclear receptor subfamily 1 group H member 4 Homo sapiens 135-138 24463129-1 2014 OBJECTIVE: To investigate the effects of GW4064, a farnesoid X receptor (FXR) agonist, on adiponectin and its receptors during the differentiation of 3T3-L1 preadipocytes and on adiponectin receptors in HepG2 cells. GW 4064 41-47 adiponectin, C1Q and collagen domain containing Homo sapiens 90-101 24211198-6 2013 The FXR agonist Chenodeoxycholic acid (CDCA) and GW4064 both can activate the expression of apoF in liver cell lines and in C57/BL6 mouse liver. GW 4064 49-55 apolipoprotein F Mus musculus 92-96 23680185-6 2013 In human hepatocytes, the activation of FXR with the agonist GW4064 resulted in a significant protection against cisplatin-induced toxicity. GW 4064 61-67 nuclear receptor subfamily 1 group H member 4 Homo sapiens 40-43 23680185-7 2013 In human hepatoma Alexander cells, with negligible endogenous expression of FXR, GW4064 also protected against cisplatin-induced toxicity, but only if they were previously transfected with FXR/RXR. GW 4064 81-87 nuclear receptor subfamily 1 group H member 4 Homo sapiens 189-192 23680185-7 2013 In human hepatoma Alexander cells, with negligible endogenous expression of FXR, GW4064 also protected against cisplatin-induced toxicity, but only if they were previously transfected with FXR/RXR. GW 4064 81-87 retinoid X receptor alpha Homo sapiens 193-196 23680185-9 2013 In both models, cisplatin, even in the absence of FXR agonists, such as bile acids and GW4064, was able to up-regulate FXR targets genes, which was due to FXR-mediated trans-activation of response elements in the promoter region. GW 4064 87-93 nuclear receptor subfamily 1 group H member 4 Homo sapiens 119-122 23680185-9 2013 In both models, cisplatin, even in the absence of FXR agonists, such as bile acids and GW4064, was able to up-regulate FXR targets genes, which was due to FXR-mediated trans-activation of response elements in the promoter region. GW 4064 87-93 nuclear receptor subfamily 1 group H member 4 Homo sapiens 119-122 23928191-6 2013 When FXR was expressed in liver and intestinal cells the magnitude of the response to GW4064 and bile acids differs among FXR isoforms. GW 4064 86-92 nuclear receptor subfamily 1 group H member 4 Homo sapiens 122-125 23609136-10 2013 In vitro, activation of FXR by bile acids (chenodeoxycholic acid [CDCA] or 6-ECDCA) or FXR agonists (GW4064 or Fexaramine) significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and beta-catenin signaling. GW 4064 101-107 nuclear receptor subfamily 1, group H, member 4 Mus musculus 24-27 23609136-10 2013 In vitro, activation of FXR by bile acids (chenodeoxycholic acid [CDCA] or 6-ECDCA) or FXR agonists (GW4064 or Fexaramine) significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and beta-catenin signaling. GW 4064 101-107 nuclear receptor subfamily 1, group H, member 4 Mus musculus 87-90 23609136-10 2013 In vitro, activation of FXR by bile acids (chenodeoxycholic acid [CDCA] or 6-ECDCA) or FXR agonists (GW4064 or Fexaramine) significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and beta-catenin signaling. GW 4064 101-107 runt related transcription factor 2 Mus musculus 203-208 23609136-10 2013 In vitro, activation of FXR by bile acids (chenodeoxycholic acid [CDCA] or 6-ECDCA) or FXR agonists (GW4064 or Fexaramine) significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and beta-catenin signaling. GW 4064 101-107 mitogen-activated protein kinase 1 Mus musculus 222-259 23609136-10 2013 In vitro, activation of FXR by bile acids (chenodeoxycholic acid [CDCA] or 6-ECDCA) or FXR agonists (GW4064 or Fexaramine) significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and beta-catenin signaling. GW 4064 101-107 mitogen-activated protein kinase 1 Mus musculus 261-264 23609136-10 2013 In vitro, activation of FXR by bile acids (chenodeoxycholic acid [CDCA] or 6-ECDCA) or FXR agonists (GW4064 or Fexaramine) significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and beta-catenin signaling. GW 4064 101-107 catenin (cadherin associated protein), beta 1 Mus musculus 270-282 23507574-3 2013 Moreover, we report that chemerin expression and secretion are induced in HepG2 cells and primary hepatocytes from wild-type mice, but not farnesoid X receptor (FXR)-/- mice, in response to the synthetic FXR ligand GW4064. GW 4064 215-221 retinoic acid receptor responder 2 Homo sapiens 25-33 23767959-2 2013 We have found that chenodeoxycholic acid and the synthetic FXR (farnesoid X receptor) ligand GW4064 induce the mRNA and protein expression of DGKtheta in the HepG2 cell line and in primary human hepatocytes. GW 4064 93-99 nuclear receptor subfamily 1 group H member 4 Homo sapiens 59-62 23767959-2 2013 We have found that chenodeoxycholic acid and the synthetic FXR (farnesoid X receptor) ligand GW4064 induce the mRNA and protein expression of DGKtheta in the HepG2 cell line and in primary human hepatocytes. GW 4064 93-99 nuclear receptor subfamily 1 group H member 4 Homo sapiens 64-84 23767959-7 2013 We also found that GW4064 and PA promote the phosphorylation of mTOR, Akt and FoxO1 (forkhead box O1), and that silencing DGKtheta expression significantly abrogated the ability of GW4046 to promote the phosphorylation of these PA-regulated targets. GW 4064 19-25 mechanistic target of rapamycin kinase Homo sapiens 64-68 23767959-7 2013 We also found that GW4064 and PA promote the phosphorylation of mTOR, Akt and FoxO1 (forkhead box O1), and that silencing DGKtheta expression significantly abrogated the ability of GW4046 to promote the phosphorylation of these PA-regulated targets. GW 4064 19-25 AKT serine/threonine kinase 1 Homo sapiens 70-73 23767959-7 2013 We also found that GW4064 and PA promote the phosphorylation of mTOR, Akt and FoxO1 (forkhead box O1), and that silencing DGKtheta expression significantly abrogated the ability of GW4046 to promote the phosphorylation of these PA-regulated targets. GW 4064 19-25 forkhead box O1 Homo sapiens 78-83 23767959-7 2013 We also found that GW4064 and PA promote the phosphorylation of mTOR, Akt and FoxO1 (forkhead box O1), and that silencing DGKtheta expression significantly abrogated the ability of GW4046 to promote the phosphorylation of these PA-regulated targets. GW 4064 19-25 forkhead box O1 Homo sapiens 85-100 23772048-3 2013 In human hepatocytes, both the endogenous FXR ligand chenodeoxycholic acid and synthetic FXR-specific agonist GW4064 increased ADH1 mRNA, protein, and activity. GW 4064 110-116 nuclear receptor subfamily 1 group H member 4 Homo sapiens 89-92 23772048-3 2013 In human hepatocytes, both the endogenous FXR ligand chenodeoxycholic acid and synthetic FXR-specific agonist GW4064 increased ADH1 mRNA, protein, and activity. GW 4064 110-116 alcohol dehydrogenase 1A (class I), alpha polypeptide Homo sapiens 127-131 23674610-7 2013 PAPSS1/2 knockdown significantly activated farnesoid X receptor (FXR), retinoid-related orphan receptor, and pregnane X receptor responsive reporters, and treatment with the FXR agonist GW4064 [3-(2,6-dichlorophenyl)-4-(3"-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole] increased Sult2a1 promoter activity when the IR0 was intact. GW 4064 186-192 3'-phosphoadenosine 5'-phosphosulfate synthase 1 Mus musculus 0-6 23688559-4 2013 Here we describe the use of the X-ray crystal structure of FXR complexed with the potent small molecule agonist GW4064 to design and synthesize a novel fluorescent, high-affinity probe (DY246) for time resolved fluorescence resonance energy transfer (TR-FRET) assays. GW 4064 112-118 nuclear receptor subfamily 1 group H member 4 Homo sapiens 59-62 23124354-4 2013 Here, we demonstrated that treatment with GW4064, a specific FXR agonist, markedly reduced Leydig tumor growth in vivo by inhibiting proliferation and inducing apoptosis. GW 4064 42-48 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 61-64 23674610-7 2013 PAPSS1/2 knockdown significantly activated farnesoid X receptor (FXR), retinoid-related orphan receptor, and pregnane X receptor responsive reporters, and treatment with the FXR agonist GW4064 [3-(2,6-dichlorophenyl)-4-(3"-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole] increased Sult2a1 promoter activity when the IR0 was intact. GW 4064 186-192 nuclear receptor subfamily 1, group H, member 4 Mus musculus 174-177 23674610-7 2013 PAPSS1/2 knockdown significantly activated farnesoid X receptor (FXR), retinoid-related orphan receptor, and pregnane X receptor responsive reporters, and treatment with the FXR agonist GW4064 [3-(2,6-dichlorophenyl)-4-(3"-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole] increased Sult2a1 promoter activity when the IR0 was intact. GW 4064 186-192 sulfotransferase family 2A, dehydroepiandrosterone (DHEA)-preferring, member 1 Mus musculus 294-301 23507574-4 2013 Hepatic chemerin expression is decreased in FXR-/- mice but up-regulated by GW4064 administration in wild-type mice. GW 4064 76-82 retinoic acid receptor responder (tazarotene induced) 2 Mus musculus 8-16 21924881-5 2013 METHODS AND RESULTS: FXR is expressed in neonatal cardiomyocytes and the treatment with FXR agonists, chenodeoxycholic acid (CDCA), and GW4064, increased the mRNA expression of FXR and its canonical target gene, the small heterodimer partner (SHP), as well as proliferator-activated receptor alpha PPARalpha, acyl-CoA oxidase (AOX) and pyruvate dehydrogenase kinase (PDK-4). GW 4064 136-142 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 21-24 23541942-1 2013 Here we report that bile acid chenodeoxycholic acid (CDCA) and synthetic farnesoid X receptor (FXR) agonist GW4064 robustly induced tumor suppressor N-Myc downstream regulated gene 2 (NDRG2) expression in human hepatoma cells and primary hepatocytes. GW 4064 108-114 nuclear receptor subfamily 1 group H member 4 Homo sapiens 95-98 23541942-1 2013 Here we report that bile acid chenodeoxycholic acid (CDCA) and synthetic farnesoid X receptor (FXR) agonist GW4064 robustly induced tumor suppressor N-Myc downstream regulated gene 2 (NDRG2) expression in human hepatoma cells and primary hepatocytes. GW 4064 108-114 NDRG family member 2 Homo sapiens 149-182 23541942-1 2013 Here we report that bile acid chenodeoxycholic acid (CDCA) and synthetic farnesoid X receptor (FXR) agonist GW4064 robustly induced tumor suppressor N-Myc downstream regulated gene 2 (NDRG2) expression in human hepatoma cells and primary hepatocytes. GW 4064 108-114 NDRG family member 2 Homo sapiens 184-189 23541942-4 2013 Moreover, mice given GW4064 exhibit an increase of Ndrg2 expression in liver and kidney, where both NDRG2 and FXR are enriched. GW 4064 21-27 N-myc downstream regulated gene 2 Mus musculus 51-56 23541942-4 2013 Moreover, mice given GW4064 exhibit an increase of Ndrg2 expression in liver and kidney, where both NDRG2 and FXR are enriched. GW 4064 21-27 N-myc downstream regulated gene 2 Mus musculus 100-105 23541942-4 2013 Moreover, mice given GW4064 exhibit an increase of Ndrg2 expression in liver and kidney, where both NDRG2 and FXR are enriched. GW 4064 21-27 nuclear receptor subfamily 1, group H, member 4 Mus musculus 110-113 23313557-6 2013 In HepG2 cells, GCs induced a decreased expression of FXR and SHP, and inhibited the regulatory effect of GW4064 on FXR-target genes. GW 4064 106-112 nuclear receptor subfamily 1 group H member 4 Homo sapiens 116-119 23313557-7 2013 In Alexander cells, only when they were transfected with FXR+RXR, GW4064 caused up-regulation of SHP and OSTbeta, and a down-regulation of CYP27A1. GW 4064 66-72 nuclear receptor subfamily 1 group H member 4 Homo sapiens 57-60 23313557-7 2013 In Alexander cells, only when they were transfected with FXR+RXR, GW4064 caused up-regulation of SHP and OSTbeta, and a down-regulation of CYP27A1. GW 4064 66-72 retinoid X receptor alpha Homo sapiens 61-64 23313557-7 2013 In Alexander cells, only when they were transfected with FXR+RXR, GW4064 caused up-regulation of SHP and OSTbeta, and a down-regulation of CYP27A1. GW 4064 66-72 nuclear receptor subfamily 0 group B member 2 Homo sapiens 97-100 23313557-7 2013 In Alexander cells, only when they were transfected with FXR+RXR, GW4064 caused up-regulation of SHP and OSTbeta, and a down-regulation of CYP27A1. GW 4064 66-72 solute carrier family 51 subunit beta Homo sapiens 105-112 23313557-7 2013 In Alexander cells, only when they were transfected with FXR+RXR, GW4064 caused up-regulation of SHP and OSTbeta, and a down-regulation of CYP27A1. GW 4064 66-72 cytochrome P450 family 27 subfamily A member 1 Homo sapiens 139-146 23313557-10 2013 Moreover, GCs have a synergistic effect on GW4064-induced FXR activation, whereas chenodeoxycholate and GW4064 have an additive effect. GW 4064 43-49 nuclear receptor subfamily 1 group H member 4 Homo sapiens 58-61 23371517-0 2013 Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and insulin resistance. GW 4064 22-28 nuclear receptor subfamily 1, group H, member 4 Mus musculus 10-13 23371517-7 2013 RESULTS: Activation of FXR by GW4064 suppressed weight gain in C57BL/6 mice fed with either HFD or high-fat and high-cholesterol diet. GW 4064 30-36 nuclear receptor subfamily 1, group H, member 4 Mus musculus 23-26 23371517-11 2013 In addition, activation of FXR by GW4064 avoided diet-induced hyperinsulinemia and hyperglycemia through decreasing the transcript levels of phosphoenolpyruvate carboxykinase (Pepck) and glucose-6-phosphatase (G6pase), two key enzymes in gluconeogenesis. GW 4064 34-40 nuclear receptor subfamily 1, group H, member 4 Mus musculus 27-30 23371517-11 2013 In addition, activation of FXR by GW4064 avoided diet-induced hyperinsulinemia and hyperglycemia through decreasing the transcript levels of phosphoenolpyruvate carboxykinase (Pepck) and glucose-6-phosphatase (G6pase), two key enzymes in gluconeogenesis. GW 4064 34-40 phosphoenolpyruvate carboxykinase 1, cytosolic Mus musculus 141-174 23371517-11 2013 In addition, activation of FXR by GW4064 avoided diet-induced hyperinsulinemia and hyperglycemia through decreasing the transcript levels of phosphoenolpyruvate carboxykinase (Pepck) and glucose-6-phosphatase (G6pase), two key enzymes in gluconeogenesis. GW 4064 34-40 phosphoenolpyruvate carboxykinase 1, cytosolic Mus musculus 176-181 23371517-11 2013 In addition, activation of FXR by GW4064 avoided diet-induced hyperinsulinemia and hyperglycemia through decreasing the transcript levels of phosphoenolpyruvate carboxykinase (Pepck) and glucose-6-phosphatase (G6pase), two key enzymes in gluconeogenesis. GW 4064 34-40 glucose-6-phosphatase, catalytic Mus musculus 187-208 23371517-11 2013 In addition, activation of FXR by GW4064 avoided diet-induced hyperinsulinemia and hyperglycemia through decreasing the transcript levels of phosphoenolpyruvate carboxykinase (Pepck) and glucose-6-phosphatase (G6pase), two key enzymes in gluconeogenesis. GW 4064 34-40 glucose-6-phosphatase, catalytic Mus musculus 210-216 21924881-5 2013 METHODS AND RESULTS: FXR is expressed in neonatal cardiomyocytes and the treatment with FXR agonists, chenodeoxycholic acid (CDCA), and GW4064, increased the mRNA expression of FXR and its canonical target gene, the small heterodimer partner (SHP), as well as proliferator-activated receptor alpha PPARalpha, acyl-CoA oxidase (AOX) and pyruvate dehydrogenase kinase (PDK-4). GW 4064 136-142 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 88-91 21924881-5 2013 METHODS AND RESULTS: FXR is expressed in neonatal cardiomyocytes and the treatment with FXR agonists, chenodeoxycholic acid (CDCA), and GW4064, increased the mRNA expression of FXR and its canonical target gene, the small heterodimer partner (SHP), as well as proliferator-activated receptor alpha PPARalpha, acyl-CoA oxidase (AOX) and pyruvate dehydrogenase kinase (PDK-4). GW 4064 136-142 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 88-91 21924881-5 2013 METHODS AND RESULTS: FXR is expressed in neonatal cardiomyocytes and the treatment with FXR agonists, chenodeoxycholic acid (CDCA), and GW4064, increased the mRNA expression of FXR and its canonical target gene, the small heterodimer partner (SHP), as well as proliferator-activated receptor alpha PPARalpha, acyl-CoA oxidase (AOX) and pyruvate dehydrogenase kinase (PDK-4). GW 4064 136-142 nuclear receptor subfamily 0, group B, member 2 Rattus norvegicus 243-246 21924881-5 2013 METHODS AND RESULTS: FXR is expressed in neonatal cardiomyocytes and the treatment with FXR agonists, chenodeoxycholic acid (CDCA), and GW4064, increased the mRNA expression of FXR and its canonical target gene, the small heterodimer partner (SHP), as well as proliferator-activated receptor alpha PPARalpha, acyl-CoA oxidase (AOX) and pyruvate dehydrogenase kinase (PDK-4). GW 4064 136-142 peroxisome proliferator activated receptor alpha Rattus norvegicus 298-307 21924881-5 2013 METHODS AND RESULTS: FXR is expressed in neonatal cardiomyocytes and the treatment with FXR agonists, chenodeoxycholic acid (CDCA), and GW4064, increased the mRNA expression of FXR and its canonical target gene, the small heterodimer partner (SHP), as well as proliferator-activated receptor alpha PPARalpha, acyl-CoA oxidase (AOX) and pyruvate dehydrogenase kinase (PDK-4). GW 4064 136-142 acyl-CoA oxidase 1 Rattus norvegicus 309-325 21924881-5 2013 METHODS AND RESULTS: FXR is expressed in neonatal cardiomyocytes and the treatment with FXR agonists, chenodeoxycholic acid (CDCA), and GW4064, increased the mRNA expression of FXR and its canonical target gene, the small heterodimer partner (SHP), as well as proliferator-activated receptor alpha PPARalpha, acyl-CoA oxidase (AOX) and pyruvate dehydrogenase kinase (PDK-4). GW 4064 136-142 acyl-CoA oxidase 1 Rattus norvegicus 327-330 21924881-5 2013 METHODS AND RESULTS: FXR is expressed in neonatal cardiomyocytes and the treatment with FXR agonists, chenodeoxycholic acid (CDCA), and GW4064, increased the mRNA expression of FXR and its canonical target gene, the small heterodimer partner (SHP), as well as proliferator-activated receptor alpha PPARalpha, acyl-CoA oxidase (AOX) and pyruvate dehydrogenase kinase (PDK-4). GW 4064 136-142 pyruvate dehydrogenase kinase 4 Rattus norvegicus 367-372 22817871-4 2012 In the present study, we for the first time identified that in human hepatoma cell line HepG2 the activation of FXR by the natural agonist chenodeoxycholic acid (CDCA) and the synthetic specific agonist GW4064 upregulated CISH at both transcriptional and translational levels, and inhibited interleukin (IL)6-induced STAT5 activation. GW 4064 203-209 nuclear receptor subfamily 1 group H member 4 Homo sapiens 112-115 23878601-4 2013 Interestingly, activation of the farnesoid X receptor (FXR) through the bile acid ursodeoxycholic acid (UDCA) or synthetic FXR agonists, such as GW4064, can increase DDAH1 expression. GW 4064 145-151 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 43-53 23878601-4 2013 Interestingly, activation of the farnesoid X receptor (FXR) through the bile acid ursodeoxycholic acid (UDCA) or synthetic FXR agonists, such as GW4064, can increase DDAH1 expression. GW 4064 145-151 nuclear receptor subfamily 1 group H member 4 Homo sapiens 55-58 23878601-4 2013 Interestingly, activation of the farnesoid X receptor (FXR) through the bile acid ursodeoxycholic acid (UDCA) or synthetic FXR agonists, such as GW4064, can increase DDAH1 expression. GW 4064 145-151 nuclear receptor subfamily 1 group H member 4 Homo sapiens 123-126 23878601-4 2013 Interestingly, activation of the farnesoid X receptor (FXR) through the bile acid ursodeoxycholic acid (UDCA) or synthetic FXR agonists, such as GW4064, can increase DDAH1 expression. GW 4064 145-151 dimethylarginine dimethylaminohydrolase 1 Homo sapiens 166-171 23101941-0 2012 Unbinding pathways of GW4064 from human farnesoid X receptor as revealed by molecular dynamics simulations. GW 4064 22-28 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 50-60 23101941-2 2012 GW4064 is a potent and selective FXR agonist and has become a tool compound to probe the physiological functions of FXR. GW 4064 0-6 nuclear receptor subfamily 1 group H member 4 Homo sapiens 33-36 23101941-2 2012 GW4064 is a potent and selective FXR agonist and has become a tool compound to probe the physiological functions of FXR. GW 4064 0-6 nuclear receptor subfamily 1 group H member 4 Homo sapiens 116-119 23101941-3 2012 Until now, the mechanism of GW4064 entering and leaving the FXR pocket is still poorly understood. GW 4064 28-34 nuclear receptor subfamily 1 group H member 4 Homo sapiens 60-63 23101941-4 2012 Here, we report a computational study of GW4064 unbinding pathways from FXR by using several molecular dynamics (MD) simulation techniques. GW 4064 41-47 nuclear receptor subfamily 1 group H member 4 Homo sapiens 72-75 23101941-5 2012 Based on the crystal structure of FXR in complex with GW4064, conventional MD was first used to refine the binding and check the stability of GW4064 in the FXR pocket. GW 4064 54-60 nuclear receptor subfamily 1 group H member 4 Homo sapiens 34-37 23101941-5 2012 Based on the crystal structure of FXR in complex with GW4064, conventional MD was first used to refine the binding and check the stability of GW4064 in the FXR pocket. GW 4064 54-60 nuclear receptor subfamily 1 group H member 4 Homo sapiens 156-159 23101941-5 2012 Based on the crystal structure of FXR in complex with GW4064, conventional MD was first used to refine the binding and check the stability of GW4064 in the FXR pocket. GW 4064 142-148 nuclear receptor subfamily 1 group H member 4 Homo sapiens 34-37 23101941-5 2012 Based on the crystal structure of FXR in complex with GW4064, conventional MD was first used to refine the binding and check the stability of GW4064 in the FXR pocket. GW 4064 142-148 nuclear receptor subfamily 1 group H member 4 Homo sapiens 156-159 23101941-6 2012 Random acceleration MD simulations were then performed to explore the possible unbinding pathways of GW4064 from FXR. GW 4064 101-107 nuclear receptor subfamily 1 group H member 4 Homo sapiens 113-116 22817871-4 2012 In the present study, we for the first time identified that in human hepatoma cell line HepG2 the activation of FXR by the natural agonist chenodeoxycholic acid (CDCA) and the synthetic specific agonist GW4064 upregulated CISH at both transcriptional and translational levels, and inhibited interleukin (IL)6-induced STAT5 activation. GW 4064 203-209 cytokine inducible SH2 containing protein Homo sapiens 222-226 22817871-4 2012 In the present study, we for the first time identified that in human hepatoma cell line HepG2 the activation of FXR by the natural agonist chenodeoxycholic acid (CDCA) and the synthetic specific agonist GW4064 upregulated CISH at both transcriptional and translational levels, and inhibited interleukin (IL)6-induced STAT5 activation. GW 4064 203-209 signal transducer and activator of transcription 5A Homo sapiens 317-322 22643070-0 2012 FXR agonist GW4064 increases plasma glucocorticoid levels in C57BL/6 mice. GW 4064 12-18 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-3 22579649-0 2012 Synergistic growth inhibition of human hepatocellular carcinoma cells by acyclic retinoid and GW4064, a farnesoid X receptor ligand. GW 4064 94-100 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 114-124 22579649-3 2012 In the present study, we examined the effects of acyclic retinoid (ACR), a synthetic retinoid targeting RXRalpha, plus GW4064, a ligand for FXR, on the growth of human HCC cells. GW 4064 119-125 nuclear receptor subfamily 1 group H member 4 Homo sapiens 140-143 22579649-4 2012 We found that ACR and GW4064 preferentially inhibited the growth of HLE, HLF, and Huh7 human HCC cells in comparison with Hc normal hepatocytes. GW 4064 22-28 MIR7-3 host gene Homo sapiens 82-86 22579649-9 2012 Our results suggest that ACR and GW4064 cooperatively inhibit RXRalpha phosphorylation, modulate the expression of FXR-regulated genes, thus resulting in the induction of apoptosis and the inhibition of growth in HCC cells. GW 4064 33-39 retinoid X receptor alpha Homo sapiens 62-70 22579649-9 2012 Our results suggest that ACR and GW4064 cooperatively inhibit RXRalpha phosphorylation, modulate the expression of FXR-regulated genes, thus resulting in the induction of apoptosis and the inhibition of growth in HCC cells. GW 4064 33-39 nuclear receptor subfamily 1 group H member 4 Homo sapiens 115-118 22643070-2 2012 FXR agonist GW4064 increased fasting plasma corticosterone levels (+45%; P<0.01) in C57BL/6 mice, indicative of enhanced adrenal steroidogenesis. GW 4064 12-18 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-3 22643070-4 2012 Scavenger receptor BI (SR-BI) mRNA and protein expression, respectively, increased 1.9-fold (P<0.01) and 1.5-fold, which suggests a stimulated lipoprotein-associated cholesterol uptake into the adrenals upon GW4064 treatment. GW 4064 211-217 scavenger receptor class B, member 1 Mus musculus 0-21 22643070-4 2012 Scavenger receptor BI (SR-BI) mRNA and protein expression, respectively, increased 1.9-fold (P<0.01) and 1.5-fold, which suggests a stimulated lipoprotein-associated cholesterol uptake into the adrenals upon GW4064 treatment. GW 4064 211-217 scavenger receptor class B, member 1 Mus musculus 23-28 22643070-6 2012 In conclusion, we have shown that the FXR agonist GW4064 stimulates plasma corticosterone levels in C57BL/6 mice. GW 4064 50-56 nuclear receptor subfamily 1, group H, member 4 Mus musculus 38-41 22561792-8 2012 Lithocholic acid (LCA) (10 muM), chenodeoxycholic acid (CDCA) (10 muM), or GW4064 (0.1 muM) treatment increased reporter activity in a construct including the three motifs under FXR-expressing conditions whereas LCA and not CDCA or GW4064 treatment increased the reporter activity under pregnane X receptor (PXR)-expressing conditions. GW 4064 75-81 nuclear receptor subfamily 1 group H member 4 Homo sapiens 178-181 22561792-8 2012 Lithocholic acid (LCA) (10 muM), chenodeoxycholic acid (CDCA) (10 muM), or GW4064 (0.1 muM) treatment increased reporter activity in a construct including the three motifs under FXR-expressing conditions whereas LCA and not CDCA or GW4064 treatment increased the reporter activity under pregnane X receptor (PXR)-expressing conditions. GW 4064 75-81 nuclear receptor subfamily 1 group I member 2 Homo sapiens 287-306 22561792-8 2012 Lithocholic acid (LCA) (10 muM), chenodeoxycholic acid (CDCA) (10 muM), or GW4064 (0.1 muM) treatment increased reporter activity in a construct including the three motifs under FXR-expressing conditions whereas LCA and not CDCA or GW4064 treatment increased the reporter activity under pregnane X receptor (PXR)-expressing conditions. GW 4064 75-81 nuclear receptor subfamily 1 group I member 2 Homo sapiens 308-311 22583617-0 2012 E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity. GW 4064 75-81 ATP binding cassette subfamily B member 11 Homo sapiens 14-35 22800197-11 2012 In LS174T/R cells, GW4064 induced the expression of FGF19, SHP, OSTalpha/beta, but not MRP2 and BCRP, although the sensitivity of these cells to cisplatin was further reduced. GW 4064 19-25 fibroblast growth factor 19 Homo sapiens 52-57 22800197-11 2012 In LS174T/R cells, GW4064 induced the expression of FGF19, SHP, OSTalpha/beta, but not MRP2 and BCRP, although the sensitivity of these cells to cisplatin was further reduced. GW 4064 19-25 nuclear receptor subfamily 0 group B member 2 Homo sapiens 59-62 22800197-11 2012 In LS174T/R cells, GW4064 induced the expression of FGF19, SHP, OSTalpha/beta, but not MRP2 and BCRP, although the sensitivity of these cells to cisplatin was further reduced. GW 4064 19-25 solute carrier family 51 subunit alpha Homo sapiens 64-77 22800197-12 2012 In LS174T cells, GW4064-induced chemoresistance was seen only after being transfected with FXR+RXR, when BCRP, but not MRP2, was up-regulated. GW 4064 17-23 nuclear receptor subfamily 1 group H member 4 Homo sapiens 91-94 22800197-12 2012 In LS174T cells, GW4064-induced chemoresistance was seen only after being transfected with FXR+RXR, when BCRP, but not MRP2, was up-regulated. GW 4064 17-23 retinoid X receptor alpha Homo sapiens 95-98 22800197-12 2012 In LS174T cells, GW4064-induced chemoresistance was seen only after being transfected with FXR+RXR, when BCRP, but not MRP2, was up-regulated. GW 4064 17-23 BCR pseudogene 1 Homo sapiens 105-109 22800197-12 2012 In LS174T cells, GW4064-induced chemoresistance was seen only after being transfected with FXR+RXR, when BCRP, but not MRP2, was up-regulated. GW 4064 17-23 ATP binding cassette subfamily C member 2 Homo sapiens 119-123 22732083-9 2012 While a synthetic ligand for farnesoid X receptor (FXR), GW4064, did not increase the transcriptional activation in HrRXR- or HrRXR/HrFXR-transfected HEK-293 cells, the ligand showed weak but significant activity for a single amino acid mutant of HrRXR ((Phe)231(Cys)) and HrFXR cotransfected cells. GW 4064 57-63 nuclear receptor subfamily 1 group H member 4 Homo sapiens 51-54 22661717-3 2012 In addition, we discovered that natural (i.e. bile acids) and synthetic (i.e. GW4064) activators of the farnesoid X receptor (FXR) increased FGF21 gene expression and secretion. GW 4064 78-84 nuclear receptor subfamily 1, group H, member 4 Mus musculus 104-124 22661717-3 2012 In addition, we discovered that natural (i.e. bile acids) and synthetic (i.e. GW4064) activators of the farnesoid X receptor (FXR) increased FGF21 gene expression and secretion. GW 4064 78-84 nuclear receptor subfamily 1, group H, member 4 Mus musculus 126-129 22661717-3 2012 In addition, we discovered that natural (i.e. bile acids) and synthetic (i.e. GW4064) activators of the farnesoid X receptor (FXR) increased FGF21 gene expression and secretion. GW 4064 78-84 fibroblast growth factor 21 Mus musculus 141-146 22278336-4 2012 A total of 15,263 and 5,272 FXR binding sites were identified in livers of healthy and obese mice, respectively, after a short 1-hour treatment with the synthetic FXR agonist, GW4064. GW 4064 176-182 nuclear receptor subfamily 1, group H, member 4 Mus musculus 28-31 22278336-4 2012 A total of 15,263 and 5,272 FXR binding sites were identified in livers of healthy and obese mice, respectively, after a short 1-hour treatment with the synthetic FXR agonist, GW4064. GW 4064 176-182 nuclear receptor subfamily 1, group H, member 4 Mus musculus 163-166 22583617-3 2012 We previously found that compounds based on GW4064, a representative farnesoid X receptor (FXR) agonist, enhanced E297G BSEP transport activity. GW 4064 44-50 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 79-89 22583617-3 2012 We previously found that compounds based on GW4064, a representative farnesoid X receptor (FXR) agonist, enhanced E297G BSEP transport activity. GW 4064 44-50 nuclear receptor subfamily 1 group H member 4 Homo sapiens 91-94 22583617-3 2012 We previously found that compounds based on GW4064, a representative farnesoid X receptor (FXR) agonist, enhanced E297G BSEP transport activity. GW 4064 44-50 ATP binding cassette subfamily B member 11 Homo sapiens 120-124 22583617-4 2012 Here, we conducted a structure-activity relationship analysis of GW4064 derivatives aimed at separating E297G BSEP-function-promoting activity and FXR-agonistic activity. GW 4064 65-71 ATP binding cassette subfamily B member 11 Homo sapiens 110-114 22583617-4 2012 Here, we conducted a structure-activity relationship analysis of GW4064 derivatives aimed at separating E297G BSEP-function-promoting activity and FXR-agonistic activity. GW 4064 65-71 nuclear receptor subfamily 1 group H member 4 Homo sapiens 147-150 22560881-6 2012 Moreover we observed both natural ligand CDCA and synthetic ligand GW4064 could upregulate SOCS 3 expression by enhancing the promoter activity in hepatocytes. GW 4064 67-73 suppressor of cytokine signaling 3 Homo sapiens 91-97 22583617-0 2012 E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity. GW 4064 75-81 ATP binding cassette subfamily B member 11 Homo sapiens 37-41 22583617-5 2012 Among newly synthesized reversed-amide derivatives of previously reported GW4064 analogs 2a-2f, we identified 7c as a selective BSEP function enhancer. GW 4064 74-80 ATP binding cassette subfamily B member 11 Homo sapiens 128-132 23119029-5 2012 In contrast, FXR overexpression and activation with GW4064 attenuated cell proliferation by down-regulating EGFR (Tyr845) phosphorylation and ERK activation. GW 4064 52-58 nuclear receptor subfamily 1 group H member 4 Homo sapiens 13-16 22178739-7 2012 In addition, EGCG suppressed FXR target gene expression induced by either GW4064 or chenodeoxycholic acid in vitro. GW 4064 74-80 nuclear receptor subfamily 1, group H, member 4 Mus musculus 29-32 22492528-5 2012 This effect was mimicked by the FXR agonist GW4064 and suppressed by the FXR antagonist guggulsterone. GW 4064 44-50 nuclear receptor subfamily 1, group H, member 4 Mus musculus 32-35 22197325-5 2012 Accordingly, pharmacological activation of Fxr with GW4064 overcomes the BA imbalance, restoring hepatic and plasma TG levels of FoxO1-deficient mice to normal levels. GW 4064 52-58 nuclear receptor subfamily 1, group H, member 4 Mus musculus 43-46 22197325-5 2012 Accordingly, pharmacological activation of Fxr with GW4064 overcomes the BA imbalance, restoring hepatic and plasma TG levels of FoxO1-deficient mice to normal levels. GW 4064 52-58 glucosidase beta 2 Mus musculus 73-75 22197325-5 2012 Accordingly, pharmacological activation of Fxr with GW4064 overcomes the BA imbalance, restoring hepatic and plasma TG levels of FoxO1-deficient mice to normal levels. GW 4064 52-58 forkhead box O1 Mus musculus 129-134 23119029-5 2012 In contrast, FXR overexpression and activation with GW4064 attenuated cell proliferation by down-regulating EGFR (Tyr845) phosphorylation and ERK activation. GW 4064 52-58 epidermal growth factor receptor Homo sapiens 108-112 23119029-5 2012 In contrast, FXR overexpression and activation with GW4064 attenuated cell proliferation by down-regulating EGFR (Tyr845) phosphorylation and ERK activation. GW 4064 52-58 mitogen-activated protein kinase 1 Homo sapiens 142-145 23119029-6 2012 Treatment with guggulsterone and GW4064 also caused dose-dependent changes in Src (Tyr416) phosphorylation. GW 4064 33-39 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 78-81 21564085-6 2011 FXR were activated by giving mice natural (chenodeoxycholic acid; CDCA) or synthetic (GW4064) FXR agonists. GW 4064 86-92 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-3 22952826-9 2012 However, wild-type mice treated with GW4064, a synthetic FXR ligand, showed that FXR activation induced mRNA and protein expression of Sqstm1/p62 in ileum, but not in liver. GW 4064 37-43 nuclear receptor subfamily 1, group H, member 4 Mus musculus 57-60 22952826-9 2012 However, wild-type mice treated with GW4064, a synthetic FXR ligand, showed that FXR activation induced mRNA and protein expression of Sqstm1/p62 in ileum, but not in liver. GW 4064 37-43 nuclear receptor subfamily 1, group H, member 4 Mus musculus 81-84 22952826-9 2012 However, wild-type mice treated with GW4064, a synthetic FXR ligand, showed that FXR activation induced mRNA and protein expression of Sqstm1/p62 in ileum, but not in liver. GW 4064 37-43 sequestosome 1 Mus musculus 135-141 22952826-9 2012 However, wild-type mice treated with GW4064, a synthetic FXR ligand, showed that FXR activation induced mRNA and protein expression of Sqstm1/p62 in ileum, but not in liver. GW 4064 37-43 sequestosome 1 Mus musculus 142-145 21564085-6 2011 FXR were activated by giving mice natural (chenodeoxycholic acid; CDCA) or synthetic (GW4064) FXR agonists. GW 4064 86-92 nuclear receptor subfamily 1, group H, member 4 Mus musculus 94-97 21564085-11 2011 FXR activation by GW4064 rescued mice from intestinal injury caused by naproxen. GW 4064 18-24 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-3 21660973-0 2011 A formulation-enabled preclinical efficacy assessment of a farnesoid X receptor agonist, GW4064, in hamsters and cynomolgus monkeys. GW 4064 89-95 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 69-79 21957312-8 2011 Second, CDCA, deoxycholic acid (DCA), and other synthetic FXR agonists, such as GW4064, significantly reduced rotavirus replication in cell culture in a dose-dependent manner. GW 4064 80-86 nuclear receptor subfamily 1 group H member 4 Homo sapiens 58-61 21660973-5 2011 We used a commercially available FXR agonist, GW4064, as a model compound to assess preclinical efficacy in two species (hamster and cynomolgus monkey). GW 4064 46-52 nuclear receptor subfamily 1 group H member 4 Homo sapiens 33-36 21632533-1 2011 We evaluated the metabolic impact of farnesoid X receptor (FXR) activation by administering a synthetic FXR agonist (GW4064) to mice in which obesity was induced by a high fat diet. GW 4064 117-123 nuclear receptor subfamily 1, group H, member 4 Mus musculus 59-62 21988803-6 2011 The FXR effect has been illustrated with the use of the FXR agonist GW4064 and the FXR antagonist GS. GW 4064 68-74 nuclear receptor subfamily 1 group H member 4 Homo sapiens 4-7 21988803-6 2011 The FXR effect has been illustrated with the use of the FXR agonist GW4064 and the FXR antagonist GS. GW 4064 68-74 nuclear receptor subfamily 1 group H member 4 Homo sapiens 56-59 21988803-6 2011 The FXR effect has been illustrated with the use of the FXR agonist GW4064 and the FXR antagonist GS. GW 4064 68-74 nuclear receptor subfamily 1 group H member 4 Homo sapiens 56-59 21988803-7 2011 More specifically, when the use of free bile acids combined with FXR agonist GW4064, the tumor cell inhibitory effect was even more pronounced. GW 4064 77-83 nuclear receptor subfamily 1 group H member 4 Homo sapiens 65-68 21988803-13 2011 We also found that FXR agonist GW4064 effectively blocked the stimulatory effect of GDCA on tumor growth. GW 4064 31-37 nuclear receptor subfamily 1 group H member 4 Homo sapiens 19-22 21988803-13 2011 We also found that FXR agonist GW4064 effectively blocked the stimulatory effect of GDCA on tumor growth. GW 4064 31-37 G protein subunit alpha transducin 3 Homo sapiens 84-88 21499302-4 2011 In this study, we show that activation of farnesoid X receptor (FXR), by the primary bile acid chenodeoxycholic acid (CDCA) or the synthetic agonist GW4064, inhibited growth of Tam-resistant breast cancer cells (termed MCF-7 TR1), which was used as an in vitro model of acquired Tam resistance. GW 4064 149-155 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 52-62 21499302-4 2011 In this study, we show that activation of farnesoid X receptor (FXR), by the primary bile acid chenodeoxycholic acid (CDCA) or the synthetic agonist GW4064, inhibited growth of Tam-resistant breast cancer cells (termed MCF-7 TR1), which was used as an in vitro model of acquired Tam resistance. GW 4064 149-155 nuclear receptor subfamily 1 group H member 4 Homo sapiens 64-67 21596890-6 2011 3-(2,6-Dichlorophenyl)-4-(3"-carboxy-2-chlorostilben-4-yl-)oxymethyl-5-isopropyl-isoxazole (GW4064), a synthetic FXR ligand, had similar effects. GW 4064 92-98 nuclear receptor subfamily 1 group H member 4 Homo sapiens 113-116 21632533-1 2011 We evaluated the metabolic impact of farnesoid X receptor (FXR) activation by administering a synthetic FXR agonist (GW4064) to mice in which obesity was induced by a high fat diet. GW 4064 117-123 nuclear receptor subfamily 1, group H, member 4 Mus musculus 104-107 21493670-0 2011 Bile acid receptor agonist GW4064 regulates PPARgamma coactivator-1alpha expression through estrogen receptor-related receptor alpha. GW 4064 27-33 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-18 21493670-8 2011 Using FXR-null [FXR knockout (FXRKO)] mice, we determined that GW4064 induction of PGC-1alpha expression is not affected in oxidative soleus muscles of FXRKO mice but is compromised in the FXRKO liver. GW 4064 63-69 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 83-93 21493670-8 2011 Using FXR-null [FXR knockout (FXRKO)] mice, we determined that GW4064 induction of PGC-1alpha expression is not affected in oxidative soleus muscles of FXRKO mice but is compromised in the FXRKO liver. GW 4064 63-69 nuclear receptor subfamily 1, group H, member 4 Mus musculus 16-19 21493670-0 2011 Bile acid receptor agonist GW4064 regulates PPARgamma coactivator-1alpha expression through estrogen receptor-related receptor alpha. GW 4064 27-33 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 44-72 21493670-3 2011 In our effort to identify new regulators of PGC-1alpha expression, we found that GW4064, a widely used synthetic agonist for the nuclear bile acid receptor [farnesoid X receptor (FXR)] strongly enhances PGC-1alpha promoter reporter activity, mRNA, and protein expression. GW 4064 81-87 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 44-54 21493670-3 2011 In our effort to identify new regulators of PGC-1alpha expression, we found that GW4064, a widely used synthetic agonist for the nuclear bile acid receptor [farnesoid X receptor (FXR)] strongly enhances PGC-1alpha promoter reporter activity, mRNA, and protein expression. GW 4064 81-87 nuclear receptor subfamily 1, group H, member 4 Mus musculus 137-155 21493670-3 2011 In our effort to identify new regulators of PGC-1alpha expression, we found that GW4064, a widely used synthetic agonist for the nuclear bile acid receptor [farnesoid X receptor (FXR)] strongly enhances PGC-1alpha promoter reporter activity, mRNA, and protein expression. GW 4064 81-87 nuclear receptor subfamily 1, group H, member 4 Mus musculus 179-182 21493670-3 2011 In our effort to identify new regulators of PGC-1alpha expression, we found that GW4064, a widely used synthetic agonist for the nuclear bile acid receptor [farnesoid X receptor (FXR)] strongly enhances PGC-1alpha promoter reporter activity, mRNA, and protein expression. GW 4064 81-87 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 203-213 21493670-5 2011 Using FXR-rich or FXR-nonexpressing cell lines and tissues, we found that this effect of GW4064 is not mediated directly by FXR but occurs via activation of estrogen receptor-related receptor alpha (ERRalpha). GW 4064 89-95 nuclear receptor subfamily 1, group H, member 4 Mus musculus 6-9 21493670-5 2011 Using FXR-rich or FXR-nonexpressing cell lines and tissues, we found that this effect of GW4064 is not mediated directly by FXR but occurs via activation of estrogen receptor-related receptor alpha (ERRalpha). GW 4064 89-95 nuclear receptor subfamily 1, group H, member 4 Mus musculus 18-21 21493670-5 2011 Using FXR-rich or FXR-nonexpressing cell lines and tissues, we found that this effect of GW4064 is not mediated directly by FXR but occurs via activation of estrogen receptor-related receptor alpha (ERRalpha). GW 4064 89-95 nuclear receptor subfamily 1, group H, member 4 Mus musculus 18-21 21493670-5 2011 Using FXR-rich or FXR-nonexpressing cell lines and tissues, we found that this effect of GW4064 is not mediated directly by FXR but occurs via activation of estrogen receptor-related receptor alpha (ERRalpha). GW 4064 89-95 estrogen related receptor, alpha Mus musculus 199-207 21493670-6 2011 Cell-based, biochemical and biophysical assays indicate GW4064 as an agonist of ERR proteins. GW 4064 56-62 solute carrier family 7 (cationic amino acid transporter, y+ system), member 1 Mus musculus 80-83 21493670-7 2011 Interestingly, FXR disruption alters GW4064 induction of PGC-1alpha mRNA in a tissue-dependent manner. GW 4064 37-43 nuclear receptor subfamily 1, group H, member 4 Mus musculus 15-18 21493670-7 2011 Interestingly, FXR disruption alters GW4064 induction of PGC-1alpha mRNA in a tissue-dependent manner. GW 4064 37-43 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 57-67 21493670-8 2011 Using FXR-null [FXR knockout (FXRKO)] mice, we determined that GW4064 induction of PGC-1alpha expression is not affected in oxidative soleus muscles of FXRKO mice but is compromised in the FXRKO liver. GW 4064 63-69 nuclear receptor subfamily 1, group H, member 4 Mus musculus 6-9 21364590-6 2011 The function of FXR was studied by small interfering RNA and treatment with FXR antagonist guggulsterone and FXR agonist GW4064. GW 4064 121-127 nuclear receptor subfamily 1 group H member 4 Homo sapiens 16-19 21364590-10 2011 Moreover, GW4064-mediated FXR activation increased cell migration and invasion. GW 4064 10-16 nuclear receptor subfamily 1 group H member 4 Homo sapiens 26-29 20675645-5 2010 Treatment of DKO mice with the farnesoid X receptor (FXR) agonist GW4064 did not alter the intestinal cholesterol absorption, suggesting that the action of CA in this process is confined mainly to formation of intraluminal micelles and less to its ability to activate the nuclear receptor FXR. GW 4064 66-72 nuclear receptor subfamily 1, group H, member 4 Mus musculus 53-56 21291553-6 2011 RESULTS: Tetraodon FXR has a ligand selectivity profile very similar to human FXR, with strong activation by the synthetic ligand GW4064 and by the primary bile acid chenodeoxycholic acid. GW 4064 130-136 nuclear receptor subfamily 1 group H member 4 Homo sapiens 19-22 21085652-5 2010 We report in this study that treatment of quiescent HSCs with GW4064, a synthetic FXR agonist, significantly inhibited the HSC transdifferentiation, which was associated with an inhibition of the upregulation of ET-1 expression. GW 4064 62-68 nuclear receptor subfamily 1 group H member 4 Homo sapiens 82-85 21085652-5 2010 We report in this study that treatment of quiescent HSCs with GW4064, a synthetic FXR agonist, significantly inhibited the HSC transdifferentiation, which was associated with an inhibition of the upregulation of ET-1 expression. GW 4064 62-68 endothelin 1 Homo sapiens 212-216 21085652-6 2010 These GW4064-treated cells also showed reduced contractile response to ET-1 in comparison to HSCs without GW4064 treatment. GW 4064 6-12 endothelin 1 Homo sapiens 71-75 21085652-7 2010 We have further shown that GW4064 treatment inhibited the ET-1-mediated contraction in fully activated HSCs. GW 4064 27-33 endothelin 1 Homo sapiens 58-62 21085652-8 2010 To elucidate the potential mechanism we showed that GW4064 inhibited ET-1-mediated activation of Rho/ROCK pathway in activated HSCs. GW 4064 52-58 endothelin 1 Homo sapiens 69-73 21319191-8 2011 Treatment of mouse or human hepatocytes with a farnesoid X receptor (FXR) agonist GW4064 or bile acids induced hepatic Abcg5/g8 expression. GW 4064 82-88 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 57-67 21319191-8 2011 Treatment of mouse or human hepatocytes with a farnesoid X receptor (FXR) agonist GW4064 or bile acids induced hepatic Abcg5/g8 expression. GW 4064 82-88 nuclear receptor subfamily 1 group H member 4 Homo sapiens 69-72 21319191-8 2011 Treatment of mouse or human hepatocytes with a farnesoid X receptor (FXR) agonist GW4064 or bile acids induced hepatic Abcg5/g8 expression. GW 4064 82-88 ATP binding cassette subfamily G member 5 Homo sapiens 119-124 21291553-6 2011 RESULTS: Tetraodon FXR has a ligand selectivity profile very similar to human FXR, with strong activation by the synthetic ligand GW4064 and by the primary bile acid chenodeoxycholic acid. GW 4064 130-136 nuclear receptor subfamily 1 group H member 4 Homo sapiens 78-81 20185821-4 2010 Activation of FXR by the synthetic agonist GW4064 decreases hepatic miR-34a levels in normal mice, and consistently, hepatic miR-34a levels are elevated in FXR-null mice. GW 4064 43-49 nuclear receptor subfamily 1, group H, member 4 Mus musculus 14-17 20185821-4 2010 Activation of FXR by the synthetic agonist GW4064 decreases hepatic miR-34a levels in normal mice, and consistently, hepatic miR-34a levels are elevated in FXR-null mice. GW 4064 43-49 microRNA 34a Mus musculus 68-75 20026603-5 2010 We found, in rat Leydig tumor cells, R2C, that FXR activation by the primary bile acid chenodeoxycholic acid (CDCA) or a synthetic agonist GW4064, through a SHP-independent mechanism, down-regulates aromatase expression in terms of mRNA, protein levels, and its enzymatic activity. GW 4064 139-145 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 47-50 20091679-5 2010 This study analyzed genome-wide FXR binding in liver and intestine of mice treated with a synthetic FXR ligand (GW4064) by chromatin immunoprecipitation coupled to massively parallel sequencing (ChIP-seq). GW 4064 112-118 nuclear receptor subfamily 1, group H, member 4 Mus musculus 32-35 20091679-5 2010 This study analyzed genome-wide FXR binding in liver and intestine of mice treated with a synthetic FXR ligand (GW4064) by chromatin immunoprecipitation coupled to massively parallel sequencing (ChIP-seq). GW 4064 112-118 nuclear receptor subfamily 1, group H, member 4 Mus musculus 100-103 20189675-10 2010 The FXR inducer GW4064 activated UGT1A3 transcription, and electrophoretic mobility shift assays identified UGT1A3 as a FXR target gene. GW 4064 16-22 nuclear receptor subfamily 1 group H member 4 Homo sapiens 4-7 20189675-10 2010 The FXR inducer GW4064 activated UGT1A3 transcription, and electrophoretic mobility shift assays identified UGT1A3 as a FXR target gene. GW 4064 16-22 UDP glucuronosyltransferase family 1 member A3 Homo sapiens 33-39 20189675-10 2010 The FXR inducer GW4064 activated UGT1A3 transcription, and electrophoretic mobility shift assays identified UGT1A3 as a FXR target gene. GW 4064 16-22 UDP glucuronosyltransferase family 1 member A3 Homo sapiens 108-114 20189675-10 2010 The FXR inducer GW4064 activated UGT1A3 transcription, and electrophoretic mobility shift assays identified UGT1A3 as a FXR target gene. GW 4064 16-22 nuclear receptor subfamily 1 group H member 4 Homo sapiens 120-123 19605523-5 2009 We report here that treatment of mice with an FXR agonist 3-(2,6-dichlorophenyl)-4-(3"-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole; GW4064) led to increased expression of DDAH-1 and CAT-1 in both liver and kidney. GW 4064 148-154 nuclear receptor subfamily 1, group H, member 4 Mus musculus 46-49 20104269-8 2010 The effects of CDCA and GW4064 on expression of Cdx2 and MUC2 were abolished by guggulsterone. GW 4064 24-30 caudal type homeo box 2 Rattus norvegicus 48-52 20104269-8 2010 The effects of CDCA and GW4064 on expression of Cdx2 and MUC2 were abolished by guggulsterone. GW 4064 24-30 mucin 2, oligomeric mucus/gel-forming Rattus norvegicus 57-61 19605523-6 2009 In cultured human hepatocytes and kidney proximal tubular epithelial cells, GW4064 increased CAT-1 expression, and this was associated with a significant increase in the cellular uptake of ADMA. GW 4064 76-82 solute carrier family 7 member 1 Homo sapiens 93-98 19586769-1 2009 Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. GW 4064 70-77 nuclear receptor subfamily 1 group H member 4 Homo sapiens 58-61 19608735-10 2009 In vitro experiments show reduced induction of mRNA expression of relevant genes upon chenodeoxycholic acid and a selective FXR agonist GW4064 stimulation in EFA-deficient Caco-2 cells. GW 4064 136-142 nuclear receptor subfamily 1 group H member 4 Homo sapiens 124-127 19410460-0 2009 Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064. GW 4064 68-74 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 43-53 19410460-0 2009 Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064. GW 4064 68-74 nuclear receptor subfamily 1 group H member 4 Homo sapiens 55-58 19118524-3 2009 In this study, we report that two synthetic FXR agonists, WAY-362450 and GW4064, suppressed interleukin-6-induced CRP expression in human Hep3B hepatoma cells. GW 4064 73-79 nuclear receptor subfamily 1 group H member 4 Homo sapiens 44-47 19228886-0 2009 Knockdown of ATP8B1 expression leads to specific downregulation of the bile acid sensor FXR in HepG2 cells: effect of the FXR agonist GW4064. GW 4064 134-140 ATPase phospholipid transporting 8B1 Homo sapiens 13-19 19228886-0 2009 Knockdown of ATP8B1 expression leads to specific downregulation of the bile acid sensor FXR in HepG2 cells: effect of the FXR agonist GW4064. GW 4064 134-140 nuclear receptor subfamily 1 group H member 4 Homo sapiens 122-125 19228886-9 2009 Treatment with the synthetic FXR agonist GW4064 was able to partially neutralize ATP8B1 siRNA-mediated FXR downregulation and fully counteract inhibition of FXR target genes. GW 4064 41-47 nuclear receptor subfamily 1 group H member 4 Homo sapiens 29-32 19228886-9 2009 Treatment with the synthetic FXR agonist GW4064 was able to partially neutralize ATP8B1 siRNA-mediated FXR downregulation and fully counteract inhibition of FXR target genes. GW 4064 41-47 ATPase phospholipid transporting 8B1 Homo sapiens 81-87 19228886-9 2009 Treatment with the synthetic FXR agonist GW4064 was able to partially neutralize ATP8B1 siRNA-mediated FXR downregulation and fully counteract inhibition of FXR target genes. GW 4064 41-47 nuclear receptor subfamily 1 group H member 4 Homo sapiens 103-106 19228886-9 2009 Treatment with the synthetic FXR agonist GW4064 was able to partially neutralize ATP8B1 siRNA-mediated FXR downregulation and fully counteract inhibition of FXR target genes. GW 4064 41-47 nuclear receptor subfamily 1 group H member 4 Homo sapiens 103-106 19328688-0 2009 Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist. GW 4064 38-44 nuclear receptor subfamily 1 group H member 4 Homo sapiens 64-67 19328688-1 2009 According to the docking studies and the analysis of a co-crystal structure of GW4064 with FXR, a series of 3-aryl heterocyclic isoxazole analogs were designed and synthesized. GW 4064 79-85 nuclear receptor subfamily 1 group H member 4 Homo sapiens 91-94 19118524-3 2009 In this study, we report that two synthetic FXR agonists, WAY-362450 and GW4064, suppressed interleukin-6-induced CRP expression in human Hep3B hepatoma cells. GW 4064 73-79 interleukin 6 Homo sapiens 92-105 19118524-3 2009 In this study, we report that two synthetic FXR agonists, WAY-362450 and GW4064, suppressed interleukin-6-induced CRP expression in human Hep3B hepatoma cells. GW 4064 73-79 C-reactive protein Homo sapiens 114-117 18755856-1 2008 The farnesoid X receptor (FXR, NR1H4) belongs to the nuclear receptor superfamily and is activated by bile acids such as chenodeoxycholic acid, or synthetic ligands such as GW4064. GW 4064 173-179 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 14-24 19085950-3 2009 Chenodeoxycholic acid (CDCA) and the farnesoid X receptor (FXR)-specific agonist GW4064 strongly induced FGF19 but inhibited CYP7A1 messenger RNA (mRNA) levels in primary human hepatocytes. GW 4064 81-87 nuclear receptor subfamily 1 group H member 4 Homo sapiens 37-57 19085950-3 2009 Chenodeoxycholic acid (CDCA) and the farnesoid X receptor (FXR)-specific agonist GW4064 strongly induced FGF19 but inhibited CYP7A1 messenger RNA (mRNA) levels in primary human hepatocytes. GW 4064 81-87 nuclear receptor subfamily 1 group H member 4 Homo sapiens 59-62 19085950-3 2009 Chenodeoxycholic acid (CDCA) and the farnesoid X receptor (FXR)-specific agonist GW4064 strongly induced FGF19 but inhibited CYP7A1 messenger RNA (mRNA) levels in primary human hepatocytes. GW 4064 81-87 fibroblast growth factor 19 Homo sapiens 105-110 19085950-3 2009 Chenodeoxycholic acid (CDCA) and the farnesoid X receptor (FXR)-specific agonist GW4064 strongly induced FGF19 but inhibited CYP7A1 messenger RNA (mRNA) levels in primary human hepatocytes. GW 4064 81-87 cytochrome P450 family 7 subfamily A member 1 Homo sapiens 125-131 19085950-8 2009 FGF19 antibody and siRNA specific to FGFR4 abrogated GW4064 inhibition of CYP7A1. GW 4064 53-59 fibroblast growth factor 19 Homo sapiens 0-5 19085950-8 2009 FGF19 antibody and siRNA specific to FGFR4 abrogated GW4064 inhibition of CYP7A1. GW 4064 53-59 fibroblast growth factor receptor 4 Homo sapiens 37-42 19085950-8 2009 FGF19 antibody and siRNA specific to FGFR4 abrogated GW4064 inhibition of CYP7A1. GW 4064 53-59 cytochrome P450 family 7 subfamily A member 1 Homo sapiens 74-80 18755856-1 2008 The farnesoid X receptor (FXR, NR1H4) belongs to the nuclear receptor superfamily and is activated by bile acids such as chenodeoxycholic acid, or synthetic ligands such as GW4064. GW 4064 173-179 nuclear receptor subfamily 1 group H member 4 Homo sapiens 26-29 18755856-1 2008 The farnesoid X receptor (FXR, NR1H4) belongs to the nuclear receptor superfamily and is activated by bile acids such as chenodeoxycholic acid, or synthetic ligands such as GW4064. GW 4064 173-179 nuclear receptor subfamily 1 group H member 4 Homo sapiens 31-36 17988216-5 2008 In the present study, we report the expression of FXR in normal and cancer prostate epithelial cells, and we demonstrate that its activation by chenodeoxycholic acid or GW4064 negatively interferes with the levels of UGT2B15 and UGT2B17 mRNA and protein in prostate cancer LNCaP cells. GW 4064 169-175 nuclear receptor subfamily 1 group H member 4 Homo sapiens 50-53 18436567-4 2008 Two FXR ligands, chenodeoxycholic acid (CDCA) and GW4064, rescued HepG2 cells from serum deprivation-induced apoptosis in a dose-dependent manner. GW 4064 50-56 nuclear receptor subfamily 1 group H member 4 Homo sapiens 4-7 18436567-6 2008 Similarly, the effects of both CDCA and GW4064 were abolished after inhibition of the MAPK pathway by a specific inhibitor of MAPK kinase 1/2. GW 4064 40-46 mitogen-activated protein kinase 1 Mus musculus 86-90 18436567-7 2008 Immunoblotting results indicated that FXR activation by CDCA and GW4064 induced ERK1/2 phosphorylation, which was attenuated by serum deprivation. GW 4064 65-71 nuclear receptor subfamily 1, group H, member 4 Mus musculus 38-41 18436567-7 2008 Immunoblotting results indicated that FXR activation by CDCA and GW4064 induced ERK1/2 phosphorylation, which was attenuated by serum deprivation. GW 4064 65-71 mitogen-activated protein kinase 3 Mus musculus 80-86 18385139-7 2008 Treatment of mice with GW4064, a synthetic agonist for farnesoid X receptor, induced SHP expression and decreased both the recruitment of PGC-1alpha to the Cyp7A1 promoter and the fasting-induced expression of CYP7A1 mRNA. GW 4064 23-29 nuclear receptor subfamily 0, group B, member 2 Mus musculus 85-88 18385139-7 2008 Treatment of mice with GW4064, a synthetic agonist for farnesoid X receptor, induced SHP expression and decreased both the recruitment of PGC-1alpha to the Cyp7A1 promoter and the fasting-induced expression of CYP7A1 mRNA. GW 4064 23-29 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 138-148 18385139-7 2008 Treatment of mice with GW4064, a synthetic agonist for farnesoid X receptor, induced SHP expression and decreased both the recruitment of PGC-1alpha to the Cyp7A1 promoter and the fasting-induced expression of CYP7A1 mRNA. GW 4064 23-29 cytochrome P450, family 7, subfamily a, polypeptide 1 Mus musculus 156-162 18385139-7 2008 Treatment of mice with GW4064, a synthetic agonist for farnesoid X receptor, induced SHP expression and decreased both the recruitment of PGC-1alpha to the Cyp7A1 promoter and the fasting-induced expression of CYP7A1 mRNA. GW 4064 23-29 cytochrome P450, family 7, subfamily a, polypeptide 1 Mus musculus 210-216 18298956-4 2008 Moreover, activation of the BA-activated farnesoid X receptor (FXR) by its synthetic specific agonist GW4064 also decreased PCSK9 expression. GW 4064 102-108 nuclear receptor subfamily 1 group H member 4 Homo sapiens 41-61 18298956-4 2008 Moreover, activation of the BA-activated farnesoid X receptor (FXR) by its synthetic specific agonist GW4064 also decreased PCSK9 expression. GW 4064 102-108 nuclear receptor subfamily 1 group H member 4 Homo sapiens 63-66 18298956-4 2008 Moreover, activation of the BA-activated farnesoid X receptor (FXR) by its synthetic specific agonist GW4064 also decreased PCSK9 expression. GW 4064 102-108 proprotein convertase subtilisin/kexin type 9 Homo sapiens 124-129 17988216-5 2008 In the present study, we report the expression of FXR in normal and cancer prostate epithelial cells, and we demonstrate that its activation by chenodeoxycholic acid or GW4064 negatively interferes with the levels of UGT2B15 and UGT2B17 mRNA and protein in prostate cancer LNCaP cells. GW 4064 169-175 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 217-224 17988216-5 2008 In the present study, we report the expression of FXR in normal and cancer prostate epithelial cells, and we demonstrate that its activation by chenodeoxycholic acid or GW4064 negatively interferes with the levels of UGT2B15 and UGT2B17 mRNA and protein in prostate cancer LNCaP cells. GW 4064 169-175 UDP glucuronosyltransferase family 2 member B17 Homo sapiens 229-236 17720959-4 2007 Treatment with the FXR-selective agonist GW4064 significantly repressed CYP7A1 in Fxr DeltaL mice but not Fxr DeltaIE mice, demonstrating that activation of FXR in intestine but not liver is required for short-term repression of CYP7A1 in liver. GW 4064 41-47 nuclear receptor subfamily 1, group H, member 4 Mus musculus 19-22 18029909-4 2007 METHODS AND RESULTS: The FXR target gene, small heterodimer partner (SHP), was induced in vascular smooth muscle cells after treatment with synthetic FXR ligands, GW4064, or 6alpha-ethyl-chenodeoxycholic acid. GW 4064 163-169 nuclear receptor subfamily 1 group H member 4 Homo sapiens 25-28 18029909-4 2007 METHODS AND RESULTS: The FXR target gene, small heterodimer partner (SHP), was induced in vascular smooth muscle cells after treatment with synthetic FXR ligands, GW4064, or 6alpha-ethyl-chenodeoxycholic acid. GW 4064 163-169 nuclear receptor subfamily 0 group B member 2 Homo sapiens 42-67 18029909-4 2007 METHODS AND RESULTS: The FXR target gene, small heterodimer partner (SHP), was induced in vascular smooth muscle cells after treatment with synthetic FXR ligands, GW4064, or 6alpha-ethyl-chenodeoxycholic acid. GW 4064 163-169 nuclear receptor subfamily 0 group B member 2 Homo sapiens 69-72 17720959-4 2007 Treatment with the FXR-selective agonist GW4064 significantly repressed CYP7A1 in Fxr DeltaL mice but not Fxr DeltaIE mice, demonstrating that activation of FXR in intestine but not liver is required for short-term repression of CYP7A1 in liver. GW 4064 41-47 cytochrome P450, family 7, subfamily a, polypeptide 1 Mus musculus 72-78 17720959-4 2007 Treatment with the FXR-selective agonist GW4064 significantly repressed CYP7A1 in Fxr DeltaL mice but not Fxr DeltaIE mice, demonstrating that activation of FXR in intestine but not liver is required for short-term repression of CYP7A1 in liver. GW 4064 41-47 nuclear receptor subfamily 1, group H, member 4 Mus musculus 82-85 17720959-4 2007 Treatment with the FXR-selective agonist GW4064 significantly repressed CYP7A1 in Fxr DeltaL mice but not Fxr DeltaIE mice, demonstrating that activation of FXR in intestine but not liver is required for short-term repression of CYP7A1 in liver. GW 4064 41-47 nuclear receptor subfamily 1, group H, member 4 Mus musculus 157-160 17720959-4 2007 Treatment with the FXR-selective agonist GW4064 significantly repressed CYP7A1 in Fxr DeltaL mice but not Fxr DeltaIE mice, demonstrating that activation of FXR in intestine but not liver is required for short-term repression of CYP7A1 in liver. GW 4064 41-47 cytochrome P450, family 7, subfamily a, polypeptide 1 Mus musculus 229-235 17660268-8 2007 In renal mesangial cells, overexpression of FXR or treatment with GW4064 also inhibited SREBP-1c and other lipogenic genes, transforming growth factor-beta, and interleukin-6, suggesting a direct role of FXR in modulating renal lipid metabolism and modulation of fibrosis and inflammation. GW 4064 66-72 sterol regulatory element binding transcription factor 1 Mus musculus 88-96 17975826-3 2007 Experiments in primary human hepatocytes and in human liver slices showed that ALAS1 messenger RNA (mRNA) and activity is increased upon exposure to chenodeoxycholic acid (CDCA), the most potent natural FXR ligand, or the synthetic FXR-specific agonist GW4064. GW 4064 253-259 5'-aminolevulinate synthase 1 Homo sapiens 79-84 17660268-8 2007 In renal mesangial cells, overexpression of FXR or treatment with GW4064 also inhibited SREBP-1c and other lipogenic genes, transforming growth factor-beta, and interleukin-6, suggesting a direct role of FXR in modulating renal lipid metabolism and modulation of fibrosis and inflammation. GW 4064 66-72 interleukin 6 Mus musculus 161-174 17660268-8 2007 In renal mesangial cells, overexpression of FXR or treatment with GW4064 also inhibited SREBP-1c and other lipogenic genes, transforming growth factor-beta, and interleukin-6, suggesting a direct role of FXR in modulating renal lipid metabolism and modulation of fibrosis and inflammation. GW 4064 66-72 nuclear receptor subfamily 1, group H, member 4 Mus musculus 204-207 17545158-5 2007 Treatment of wild-type mice with GW4064, a synthetic Fxralpha agonist, induced Slc13a1 mRNA in the intestine and kidney. GW 4064 33-39 solute carrier family 13 (sodium/sulfate symporters), member 1 Mus musculus 79-86 17047076-6 2006 At lower concentrations that had no direct effect on viability, the FXR agonist GW4064 induced expression of mRNA for the FXR target genes, small heterodimer partner (SHP), intestinal bile acid binding protein, and multidrug resistance-associated protein 2 (MRP-2), and repressed the expression of the SHP target gene aromatase. GW 4064 80-86 nuclear receptor subfamily 1 group H member 4 Homo sapiens 68-71 17065154-2 2006 By microarray analysis of hepatic genes from female Zucker diabetic fatty (ZDF) rats treated with the FXR agonist GW4064, we have identified dimethylarginine dimethylaminohydrolase-1 (DDAH1) as an FXR target gene. GW 4064 114-120 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 102-105 17065154-2 2006 By microarray analysis of hepatic genes from female Zucker diabetic fatty (ZDF) rats treated with the FXR agonist GW4064, we have identified dimethylarginine dimethylaminohydrolase-1 (DDAH1) as an FXR target gene. GW 4064 114-120 dimethylarginine dimethylaminohydrolase 1 Rattus norvegicus 141-182 17065154-2 2006 By microarray analysis of hepatic genes from female Zucker diabetic fatty (ZDF) rats treated with the FXR agonist GW4064, we have identified dimethylarginine dimethylaminohydrolase-1 (DDAH1) as an FXR target gene. GW 4064 114-120 dimethylarginine dimethylaminohydrolase 1 Rattus norvegicus 184-189 17065154-2 2006 By microarray analysis of hepatic genes from female Zucker diabetic fatty (ZDF) rats treated with the FXR agonist GW4064, we have identified dimethylarginine dimethylaminohydrolase-1 (DDAH1) as an FXR target gene. GW 4064 114-120 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 197-200 17065154-5 2006 Functional analysis of the putative FXRE demonstrated GW4064 dose-dependent transcriptional activation from the element, and we have demonstrated that the FXRE sequence binds the FXR-RXR heterodimer. GW 4064 54-60 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 36-39 17065154-6 2006 In vivo administration of GW4064 to female ZDF rats promoted a dose-dependent and >6-fold increase in hepatic DDAH1 gene expression. GW 4064 26-32 dimethylarginine dimethylaminohydrolase 1 Rattus norvegicus 113-118 17047076-6 2006 At lower concentrations that had no direct effect on viability, the FXR agonist GW4064 induced expression of mRNA for the FXR target genes, small heterodimer partner (SHP), intestinal bile acid binding protein, and multidrug resistance-associated protein 2 (MRP-2), and repressed the expression of the SHP target gene aromatase. GW 4064 80-86 nuclear receptor subfamily 1 group H member 4 Homo sapiens 122-125 17047076-6 2006 At lower concentrations that had no direct effect on viability, the FXR agonist GW4064 induced expression of mRNA for the FXR target genes, small heterodimer partner (SHP), intestinal bile acid binding protein, and multidrug resistance-associated protein 2 (MRP-2), and repressed the expression of the SHP target gene aromatase. GW 4064 80-86 nuclear receptor subfamily 0 group B member 2 Homo sapiens 140-165 17047076-6 2006 At lower concentrations that had no direct effect on viability, the FXR agonist GW4064 induced expression of mRNA for the FXR target genes, small heterodimer partner (SHP), intestinal bile acid binding protein, and multidrug resistance-associated protein 2 (MRP-2), and repressed the expression of the SHP target gene aromatase. GW 4064 80-86 nuclear receptor subfamily 0 group B member 2 Homo sapiens 167-170 17047076-6 2006 At lower concentrations that had no direct effect on viability, the FXR agonist GW4064 induced expression of mRNA for the FXR target genes, small heterodimer partner (SHP), intestinal bile acid binding protein, and multidrug resistance-associated protein 2 (MRP-2), and repressed the expression of the SHP target gene aromatase. GW 4064 80-86 ATP binding cassette subfamily C member 2 Homo sapiens 215-256 17047076-6 2006 At lower concentrations that had no direct effect on viability, the FXR agonist GW4064 induced expression of mRNA for the FXR target genes, small heterodimer partner (SHP), intestinal bile acid binding protein, and multidrug resistance-associated protein 2 (MRP-2), and repressed the expression of the SHP target gene aromatase. GW 4064 80-86 ATP binding cassette subfamily C member 2 Homo sapiens 258-263 17047076-6 2006 At lower concentrations that had no direct effect on viability, the FXR agonist GW4064 induced expression of mRNA for the FXR target genes, small heterodimer partner (SHP), intestinal bile acid binding protein, and multidrug resistance-associated protein 2 (MRP-2), and repressed the expression of the SHP target gene aromatase. GW 4064 80-86 nuclear receptor subfamily 0 group B member 2 Homo sapiens 302-305 16446356-9 2006 Treatment of differentiated 3T3-L1 adipocytes with the FXR-specific synthetic agonist GW4064 enhanced insulin signaling and insulin-stimulated glucose uptake. GW 4064 86-92 nuclear receptor subfamily 1, group H, member 4 Mus musculus 55-58 16946559-9 2006 Human SULT2A1 protein and mRNA levels were decreased in HepG2 cells treated with the FXR agonists, CDCA or GW4064 in dose-dependent manners, although SHP mRNA levels were increased. GW 4064 107-113 sulfotransferase family 2A member 1 Homo sapiens 6-13 16946559-9 2006 Human SULT2A1 protein and mRNA levels were decreased in HepG2 cells treated with the FXR agonists, CDCA or GW4064 in dose-dependent manners, although SHP mRNA levels were increased. GW 4064 107-113 nuclear receptor subfamily 1 group H member 4 Homo sapiens 85-88 16682417-5 2006 Feeding mice with cholic acid or the synthetic farnesoid X receptor (FXR) agonist GW4064 resulted in a robust PXR induction. GW 4064 82-88 nuclear receptor subfamily 1, group H, member 4 Mus musculus 69-72 16682417-5 2006 Feeding mice with cholic acid or the synthetic farnesoid X receptor (FXR) agonist GW4064 resulted in a robust PXR induction. GW 4064 82-88 nuclear receptor subfamily 1, group I, member 2 Mus musculus 110-113 16357058-8 2006 As predicted from the promoter analyses, ileal Ostalpha and Ostbeta mRNA expressions were increased in wild-type mice administered the FXR agonist GW4064 and decreased in FXR-null mice. GW 4064 147-153 solute carrier family 51, alpha subunit Mus musculus 47-55 16357058-8 2006 As predicted from the promoter analyses, ileal Ostalpha and Ostbeta mRNA expressions were increased in wild-type mice administered the FXR agonist GW4064 and decreased in FXR-null mice. GW 4064 147-153 solute carrier family 51, beta subunit Mus musculus 60-67 16357058-8 2006 As predicted from the promoter analyses, ileal Ostalpha and Ostbeta mRNA expressions were increased in wild-type mice administered the FXR agonist GW4064 and decreased in FXR-null mice. GW 4064 147-153 nuclear receptor subfamily 1, group H, member 4 Mus musculus 135-138 16625821-3 2006 The C57L mouse is also susceptible to gallstone formation when fed a lithogenic diet, and in this model, the small-molecule FXR agonist GW-4064 prevents the precipitation of cholesterol. GW 4064 136-143 nuclear receptor subfamily 1, group H, member 4 Mus musculus 124-127 16410358-3 2006 Activation of FXR by the synthetic agonist GW4064 or hepatic overexpression of constitutively active FXR by adenovirus-mediated gene transfer significantly lowered blood glucose levels in both diabetic db/db and wild-type mice. GW 4064 43-49 nuclear receptor subfamily 1, group H, member 4 Mus musculus 14-17 16037943-7 2005 In these cells, the FXR pharmacological agonist GW4064 upregulated VPAC1 expression in a dose-dependent manner, and this effect was antagonized by the RXRalpha ligand, 9-cis retinoic acid. GW 4064 48-54 nuclear receptor subfamily 1 group H member 4 Homo sapiens 20-23 16012168-4 2005 AlphaA-crystallin was identified in a microarray screen as one of the most highly induced genes after treatment of HepG2 cells with the synthetic FXR ligand GW4064. GW 4064 157-163 nuclear receptor subfamily 1 group H member 4 Homo sapiens 146-149 16037943-7 2005 In these cells, the FXR pharmacological agonist GW4064 upregulated VPAC1 expression in a dose-dependent manner, and this effect was antagonized by the RXRalpha ligand, 9-cis retinoic acid. GW 4064 48-54 vasoactive intestinal peptide receptor 1 Homo sapiens 67-72 16037943-7 2005 In these cells, the FXR pharmacological agonist GW4064 upregulated VPAC1 expression in a dose-dependent manner, and this effect was antagonized by the RXRalpha ligand, 9-cis retinoic acid. GW 4064 48-54 retinoid X receptor alpha Homo sapiens 151-159 15692145-8 2005 Treatment of Huh7 cells with CDCA or the synthetic farnesoid X receptor (FXR) agonist GW4064 decreased mRNA and protein levels and also nuclear binding activity of HNF-4 alpha. GW 4064 86-92 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 61-71 15817812-5 2005 In addition, ICAM-1 and SHP mRNA levels were also induced in primary human hepatocytes when treated with chenodeoxycholic acid or GW4064, a FXR-selective agonist. GW 4064 130-136 intercellular adhesion molecule 1 Homo sapiens 13-19 15817812-5 2005 In addition, ICAM-1 and SHP mRNA levels were also induced in primary human hepatocytes when treated with chenodeoxycholic acid or GW4064, a FXR-selective agonist. GW 4064 130-136 nuclear receptor subfamily 0 group B member 2 Homo sapiens 24-27 15817812-5 2005 In addition, ICAM-1 and SHP mRNA levels were also induced in primary human hepatocytes when treated with chenodeoxycholic acid or GW4064, a FXR-selective agonist. GW 4064 130-136 nuclear receptor subfamily 1 group H member 4 Homo sapiens 140-143 15817812-7 2005 Both ICAM-1 and SHP expression were induced in a dose- and time-dependent manner by treatment with the FXR-selective agonist GW4064. GW 4064 125-131 intercellular adhesion molecule 1 Homo sapiens 5-11 15817812-7 2005 Both ICAM-1 and SHP expression were induced in a dose- and time-dependent manner by treatment with the FXR-selective agonist GW4064. GW 4064 125-131 nuclear receptor subfamily 0 group B member 2 Homo sapiens 16-19 15817812-7 2005 Both ICAM-1 and SHP expression were induced in a dose- and time-dependent manner by treatment with the FXR-selective agonist GW4064. GW 4064 125-131 nuclear receptor subfamily 1 group H member 4 Homo sapiens 103-106 15817812-8 2005 Moreover, the induction of ICAM-1 by GW4064 was inhibited by the FXR antagonist guggulsterone or with transfection of FXR siRNA. GW 4064 37-43 intercellular adhesion molecule 1 Homo sapiens 27-33 15817812-8 2005 Moreover, the induction of ICAM-1 by GW4064 was inhibited by the FXR antagonist guggulsterone or with transfection of FXR siRNA. GW 4064 37-43 nuclear receptor subfamily 1 group H member 4 Homo sapiens 65-68 15817812-8 2005 Moreover, the induction of ICAM-1 by GW4064 was inhibited by the FXR antagonist guggulsterone or with transfection of FXR siRNA. GW 4064 37-43 nuclear receptor subfamily 1 group H member 4 Homo sapiens 118-121 15644430-8 2005 These changes were reproduced by GW4064, a synthetic FXR ligand. GW 4064 33-39 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 53-56 15692145-8 2005 Treatment of Huh7 cells with CDCA or the synthetic farnesoid X receptor (FXR) agonist GW4064 decreased mRNA and protein levels and also nuclear binding activity of HNF-4 alpha. GW 4064 86-92 nuclear receptor subfamily 1 group H member 4 Homo sapiens 73-76 15692145-8 2005 Treatment of Huh7 cells with CDCA or the synthetic farnesoid X receptor (FXR) agonist GW4064 decreased mRNA and protein levels and also nuclear binding activity of HNF-4 alpha. GW 4064 86-92 hepatocyte nuclear factor 4 alpha Homo sapiens 164-175 15882126-2 2005 The nuclear farnesoid X receptor (FXR) is the receptor for bile acids, and GW4064 is a synthetic agonist at the FXR. GW 4064 75-81 nuclear receptor subfamily 1, group H, member 4 Mus musculus 34-37 15882126-2 2005 The nuclear farnesoid X receptor (FXR) is the receptor for bile acids, and GW4064 is a synthetic agonist at the FXR. GW 4064 75-81 nuclear receptor subfamily 1, group H, member 4 Mus musculus 112-115 15882126-8 2005 As FXR agonism with GW4064 has been shown to be useful in a mouse model of cholesterol gallstone disease, it should undergo further development for the treatment of this condition. GW 4064 20-26 nuclear receptor subfamily 1, group H, member 4 Mus musculus 3-6 15564327-7 2005 Consistent with these observations, treatment of C57BL6 mice with GW4064 significantly increased hepatic PEPCK expression. GW 4064 66-72 phosphoenolpyruvate carboxykinase 1, cytosolic Mus musculus 105-110 15810635-6 2005 When the same experiment was performed in the presence of a synthetic FXR ligand (GW4064), cPLA2 expression and activity were reduced, although COX-2 expression was unchanged. GW 4064 82-88 nuclear receptor subfamily 1, group H, member 4 Mus musculus 70-73 12754200-8 2003 Finally, Fisher rats treated with the synthetic FXR ligand GW4064 clearly show increased transcript levels of both the BACS and BAT mRNA. GW 4064 59-65 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 48-51 15810635-6 2005 When the same experiment was performed in the presence of a synthetic FXR ligand (GW4064), cPLA2 expression and activity were reduced, although COX-2 expression was unchanged. GW 4064 82-88 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 91-96 15810635-6 2005 When the same experiment was performed in the presence of a synthetic FXR ligand (GW4064), cPLA2 expression and activity were reduced, although COX-2 expression was unchanged. GW 4064 82-88 prostaglandin-endoperoxide synthase 2 Mus musculus 144-149 15810635-9 2005 A synthetic FXR ligand (GW4064) inhibited the induction of COX-2 activity (detected as PG production) by GCDC, suggesting its anticarcinogenic potential. GW 4064 24-30 nuclear receptor subfamily 1, group H, member 4 Mus musculus 12-15 15810635-9 2005 A synthetic FXR ligand (GW4064) inhibited the induction of COX-2 activity (detected as PG production) by GCDC, suggesting its anticarcinogenic potential. GW 4064 24-30 prostaglandin-endoperoxide synthase 2 Mus musculus 59-64 15342685-5 2004 The nonsteroidal synthetic FXR agonist GW4064 also decreases HL mRNA levels in HepG2 cells and in primary human hepatocytes. GW 4064 39-45 nuclear receptor subfamily 1 group H member 4 Homo sapiens 27-30 15342685-7 2004 In addition, FXR-specific gene silencing using small interfering RNAs demonstrated that CDCA- and GW4064-mediated downregulation of HL transcript levels occurs via an FXR-dependent mechanism. GW 4064 98-104 nuclear receptor subfamily 1 group H member 4 Homo sapiens 13-16 15342685-7 2004 In addition, FXR-specific gene silencing using small interfering RNAs demonstrated that CDCA- and GW4064-mediated downregulation of HL transcript levels occurs via an FXR-dependent mechanism. GW 4064 98-104 nuclear receptor subfamily 1 group H member 4 Homo sapiens 167-170 14684751-6 2004 Similar results were also obtained from a glutathione S-transferase pull-down assay in which only CDCA and the synthetic FXR agonist GW4064 significantly increased the interaction of SRC-1 with FXR. GW 4064 133-139 nuclear receptor subfamily 1 group H member 4 Homo sapiens 121-124 14684751-6 2004 Similar results were also obtained from a glutathione S-transferase pull-down assay in which only CDCA and the synthetic FXR agonist GW4064 significantly increased the interaction of SRC-1 with FXR. GW 4064 133-139 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 183-188 14684751-6 2004 Similar results were also obtained from a glutathione S-transferase pull-down assay in which only CDCA and the synthetic FXR agonist GW4064 significantly increased the interaction of SRC-1 with FXR. GW 4064 133-139 nuclear receptor subfamily 1 group H member 4 Homo sapiens 194-197 14527955-5 2003 In FXR trans-activation assays, both the endogenous FXR agonist chenodeoxycholate and the synthetic agonist GW4064 activated the MDR3 promoter. GW 4064 108-114 nuclear receptor subfamily 1 group H member 4 Homo sapiens 3-6 14527955-5 2003 In FXR trans-activation assays, both the endogenous FXR agonist chenodeoxycholate and the synthetic agonist GW4064 activated the MDR3 promoter. GW 4064 108-114 ATP binding cassette subfamily B member 4 Homo sapiens 129-133 14527955-7 2003 Consistent with these data, MDR3 mRNA was significantly induced by both chenodeoxycholate and GW4064 in primary human hepatocytes in time- and dose-dependent fashions. GW 4064 94-100 ATP binding cassette subfamily B member 4 Homo sapiens 28-32 14623915-4 2003 We investigated whether the synthetic FXR agonist GW4064 could protect against cholestatic liver damage in rat models of extrahepatic and intrahepatic cholestasis. GW 4064 50-56 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 38-41 14623915-5 2003 In the bile duct-ligation and alpha-naphthylisothiocyanate models of cholestasis, GW4064 treatment resulted in significant reductions in serum alanine aminotransferase, aspartate aminotransferase, and lactate dehydrogenase, as well as other markers of liver damage. GW 4064 82-88 glutamic-oxaloacetic transaminase 2 Rattus norvegicus 169-195 14623915-7 2003 Analysis of gene expression in livers from GW4064-treated cholestatic rats revealed decreased expression of bile acid biosynthetic genes and increased expression of genes involved in bile acid transport, including the phospholipid flippase MDR2. GW 4064 43-49 ATP binding cassette subfamily B member 4 Rattus norvegicus 240-244 12891557-7 2003 Incubation of human primary hepatocytes and HepG2 cells with bile acids or the nonsteroidal synthetic FXR agonist GW4064 resulted in a dose-dependent down-regulation of Apo CIII gene expression. GW 4064 114-120 nuclear receptor subfamily 1 group H member 4 Homo sapiens 102-105 12891557-7 2003 Incubation of human primary hepatocytes and HepG2 cells with bile acids or the nonsteroidal synthetic FXR agonist GW4064 resulted in a dose-dependent down-regulation of Apo CIII gene expression. GW 4064 114-120 apolipoprotein C3 Homo sapiens 169-177 15309887-6 2004 Intestinal bile acid binding protein was activated by chenodeoxycholic acid and the synthetic FXR agonist GW4064 in Caco-2 and HT-29 but not in SW cells unless FXR was transfected. GW 4064 106-112 nuclear receptor subfamily 1 group H member 4 Homo sapiens 94-97 12761213-5 2003 In primary human hepatocytes, both the endogenous FXR agonist chenodeoxycholate and synthetic FXR agonist GW4064 increased kininogen mRNA with a maximum induction of 8-10-fold. GW 4064 106-112 nuclear receptor subfamily 1 group H member 4 Homo sapiens 94-97 12754200-8 2003 Finally, Fisher rats treated with the synthetic FXR ligand GW4064 clearly show increased transcript levels of both the BACS and BAT mRNA. GW 4064 59-65 solute carrier family 27 member 5 Rattus norvegicus 119-123 12754200-8 2003 Finally, Fisher rats treated with the synthetic FXR ligand GW4064 clearly show increased transcript levels of both the BACS and BAT mRNA. GW 4064 59-65 bile acid CoA:amino acid N-acyltransferase Rattus norvegicus 128-131 12052824-6 2002 Both the endogenous FXR agonist chenodeoxycholate (CDCA) and synthetic FXR ligand GW4064 effectively increased BSEP mRNA in both cell types. GW 4064 82-88 nuclear receptor subfamily 1 group H member 4 Homo sapiens 71-74 12525500-5 2003 In HepG2 cells, in the presence of an FXR agonist such as chenodeoxycholate or GW4064, GS enhanced endogenous BSEP expression with a maximum induction of 400-500% that induced by an FXR agonist alone. GW 4064 79-85 nuclear receptor subfamily 1 group H member 4 Homo sapiens 38-41 12525500-5 2003 In HepG2 cells, in the presence of an FXR agonist such as chenodeoxycholate or GW4064, GS enhanced endogenous BSEP expression with a maximum induction of 400-500% that induced by an FXR agonist alone. GW 4064 79-85 ATP binding cassette subfamily B member 11 Homo sapiens 110-114 12525500-5 2003 In HepG2 cells, in the presence of an FXR agonist such as chenodeoxycholate or GW4064, GS enhanced endogenous BSEP expression with a maximum induction of 400-500% that induced by an FXR agonist alone. GW 4064 79-85 nuclear receptor subfamily 1 group H member 4 Homo sapiens 182-185 12660231-2 2003 Treatment of human hepatocytes with either naturally occurring (chenodeoxycholic acid) or synthetic (GW4064) FXR ligands resulted in both induction of SDC1 mRNA and enhanced binding, internalization, and degradation of low density lipoprotein. GW 4064 101-107 nuclear receptor subfamily 1 group H member 4 Homo sapiens 109-112 12660231-2 2003 Treatment of human hepatocytes with either naturally occurring (chenodeoxycholic acid) or synthetic (GW4064) FXR ligands resulted in both induction of SDC1 mRNA and enhanced binding, internalization, and degradation of low density lipoprotein. GW 4064 101-107 syndecan 1 Homo sapiens 151-155 12519787-4 2003 Using real-time quantitative PCR and cotransfection reporter assays, we demonstrate that the RXR agonist LG100268 antagonizes induction of BSEP expression mediated by endogenous and synthetic FXR ligands, CDCA and GW4064, respectively. GW 4064 214-220 retinoid X receptor alpha Homo sapiens 93-96 12519787-4 2003 Using real-time quantitative PCR and cotransfection reporter assays, we demonstrate that the RXR agonist LG100268 antagonizes induction of BSEP expression mediated by endogenous and synthetic FXR ligands, CDCA and GW4064, respectively. GW 4064 214-220 ATP binding cassette subfamily B member 11 Homo sapiens 139-143 12554753-6 2003 Incubation of human hepatoma HepG2 cells with the natural FXR ligand chenodeoxycholic acid (CDCA) as well as with the nonsteroidal FXR agonist GW4064 resulted in a significant induction of PPARalpha mRNA levels. GW 4064 143-149 nuclear receptor subfamily 1 group H member 4 Homo sapiens 131-134 12554753-6 2003 Incubation of human hepatoma HepG2 cells with the natural FXR ligand chenodeoxycholic acid (CDCA) as well as with the nonsteroidal FXR agonist GW4064 resulted in a significant induction of PPARalpha mRNA levels. GW 4064 143-149 peroxisome proliferator activated receptor alpha Homo sapiens 189-198 12052824-11 2002 In an in vitro co-activator association assay, LCA decreased CDCA- and GW4064-induced FXR activation with an IC(50) of 1 microm. GW 4064 71-77 nuclear receptor subfamily 1 group H member 4 Homo sapiens 86-89 12052824-12 2002 In HepG2 cells, LCA also effectively antagonized GW4064-enhanced FXR transactivation. GW 4064 49-55 nuclear receptor subfamily 1 group H member 4 Homo sapiens 65-68 12052824-6 2002 Both the endogenous FXR agonist chenodeoxycholate (CDCA) and synthetic FXR ligand GW4064 effectively increased BSEP mRNA in both cell types. GW 4064 82-88 ATP binding cassette subfamily B member 11 Homo sapiens 111-115 11706036-3 2002 MRP2 mRNA levels were induced following treatment of human or rat hepatocytes with either naturally occurring (chenodeoxycholic acid) or synthetic (GW4064) FXR ligands. GW 4064 148-154 ATP binding cassette subfamily C member 2 Homo sapiens 0-4 11927623-9 2002 The nonsteroidal synthetic FXR agonist GW4064 likewise decreased apoA-I mRNA levels and promoter activity in HepG2 cells. GW 4064 39-45 nuclear receptor subfamily 1 group H member 4 Homo sapiens 27-30 11927623-9 2002 The nonsteroidal synthetic FXR agonist GW4064 likewise decreased apoA-I mRNA levels and promoter activity in HepG2 cells. GW 4064 39-45 apolipoprotein A1 Homo sapiens 65-71 11706036-3 2002 MRP2 mRNA levels were induced following treatment of human or rat hepatocytes with either naturally occurring (chenodeoxycholic acid) or synthetic (GW4064) FXR ligands. GW 4064 148-154 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 156-159 25599407-7 2015 Interestingly, in contrast to its effect on islets from lean mice, the FXR agonist GW4064 was ineffective in stimulating insulin secretion of islets from wild type mice fed a HFD or isolated islets kept in a glucolipotoxic medium. GW 4064 83-89 nuclear receptor subfamily 1, group H, member 4 Mus musculus 71-74 11607932-3 2001 GW4064 is a potent and selective nonsteroidal ligand for the nuclear bile acid receptor FXR (NR1H4). GW 4064 0-6 nuclear receptor subfamily 1 group H member 4 Homo sapiens 88-91 11607932-3 2001 GW4064 is a potent and selective nonsteroidal ligand for the nuclear bile acid receptor FXR (NR1H4). GW 4064 0-6 nuclear receptor subfamily 1 group H member 4 Homo sapiens 93-98 11607932-4 2001 Using GW4064 as a chemical tool, we have identified genes regulated by FXR in the liver, including those involved in bile acid synthesis and transport. GW 4064 6-12 nuclear receptor subfamily 1 group H member 4 Homo sapiens 71-74 34870866-15 2021 The FXR agonist GW4064 almost completely restored the dysregulated bile acid signaling and metabolic syndrome in iron-fed mice. GW 4064 16-22 nuclear receptor subfamily 1, group H, member 4 Mus musculus 4-7 34387888-4 2022 METHODS: To induce PNAC, male C57BL/6 mice were subjected to intestinal injury (2% dextran sodium sulfate for 4 days) followed by central venous catheterization and 14 day-infusion of PN with or without the FXR agonist GW4064. GW 4064 219-225 nuclear receptor subfamily 1, group H, member 4 Mus musculus 207-210 34387888-6 2022 RESULTS: GW4064 (30mg/kg/day) added to PN on days 4-14 prevented hepatic injury and cholestasis, reversed the suppressed mRNA expression of Nr1h4/FXR, Abcb11/BSEP, Abcc2, Abcb4, and Abcg5/8, and normalized serum bile acids. GW 4064 9-15 nuclear receptor subfamily 1, group H, member 4 Mus musculus 140-145 34387888-6 2022 RESULTS: GW4064 (30mg/kg/day) added to PN on days 4-14 prevented hepatic injury and cholestasis, reversed the suppressed mRNA expression of Nr1h4/FXR, Abcb11/BSEP, Abcc2, Abcb4, and Abcg5/8, and normalized serum bile acids. GW 4064 9-15 nuclear receptor subfamily 1, group H, member 4 Mus musculus 146-149 34387888-6 2022 RESULTS: GW4064 (30mg/kg/day) added to PN on days 4-14 prevented hepatic injury and cholestasis, reversed the suppressed mRNA expression of Nr1h4/FXR, Abcb11/BSEP, Abcc2, Abcb4, and Abcg5/8, and normalized serum bile acids. GW 4064 9-15 ATP-binding cassette, sub-family B (MDR/TAP), member 11 Mus musculus 151-157 34387888-6 2022 RESULTS: GW4064 (30mg/kg/day) added to PN on days 4-14 prevented hepatic injury and cholestasis, reversed the suppressed mRNA expression of Nr1h4/FXR, Abcb11/BSEP, Abcc2, Abcb4, and Abcg5/8, and normalized serum bile acids. GW 4064 9-15 ATP-binding cassette, sub-family B (MDR/TAP), member 11 Mus musculus 158-162 34387888-6 2022 RESULTS: GW4064 (30mg/kg/day) added to PN on days 4-14 prevented hepatic injury and cholestasis, reversed the suppressed mRNA expression of Nr1h4/FXR, Abcb11/BSEP, Abcc2, Abcb4, and Abcg5/8, and normalized serum bile acids. GW 4064 9-15 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 164-169 34387888-6 2022 RESULTS: GW4064 (30mg/kg/day) added to PN on days 4-14 prevented hepatic injury and cholestasis, reversed the suppressed mRNA expression of Nr1h4/FXR, Abcb11/BSEP, Abcc2, Abcb4, and Abcg5/8, and normalized serum bile acids. GW 4064 9-15 ATP-binding cassette, sub-family B (MDR/TAP), member 4 Mus musculus 171-176 34387888-6 2022 RESULTS: GW4064 (30mg/kg/day) added to PN on days 4-14 prevented hepatic injury and cholestasis, reversed the suppressed mRNA expression of Nr1h4/FXR, Abcb11/BSEP, Abcc2, Abcb4, and Abcg5/8, and normalized serum bile acids. GW 4064 9-15 ATP binding cassette subfamily G member 5 Mus musculus 182-189 34387888-7 2022 Chromatin-immunoprecipitation of liver showed that GW4064 increased FXR binding to the Abcb11 promoter. GW 4064 51-57 nuclear receptor subfamily 1, group H, member 4 Mus musculus 68-71 34387888-7 2022 Chromatin-immunoprecipitation of liver showed that GW4064 increased FXR binding to the Abcb11 promoter. GW 4064 51-57 ATP-binding cassette, sub-family B (MDR/TAP), member 11 Mus musculus 87-93 34387888-8 2022 Furthermore, GW4064 prevented DSS-PN-induced hepatic macrophage accumulation, hepatic expression of genes associated with macrophage recruitment and activation (ll1b, Ccr2, Itgam, Ly6C), and hepatic macrophage cytokine transcription in response to LPS in vitro. GW 4064 13-19 chemokine (C-C motif) receptor 2 Mus musculus 167-171 34387888-8 2022 Furthermore, GW4064 prevented DSS-PN-induced hepatic macrophage accumulation, hepatic expression of genes associated with macrophage recruitment and activation (ll1b, Ccr2, Itgam, Ly6C), and hepatic macrophage cytokine transcription in response to LPS in vitro. GW 4064 13-19 integrin alpha M Mus musculus 173-178 34387888-8 2022 Furthermore, GW4064 prevented DSS-PN-induced hepatic macrophage accumulation, hepatic expression of genes associated with macrophage recruitment and activation (ll1b, Ccr2, Itgam, Ly6C), and hepatic macrophage cytokine transcription in response to LPS in vitro. GW 4064 13-19 lymphocyte antigen 6 complex, locus C1 Mus musculus 180-184 34387888-9 2022 In primary mouse hepatocytes, GW4064 activated transcription of FXR canonical targets, irrespective of IL-1beta exposure. GW 4064 30-36 nuclear receptor subfamily 1, group H, member 4 Mus musculus 64-67 34387888-10 2022 Intestinal inflammation and ileal mRNAs (Nr1h4, Fgf15 and Ostalpha) were not different among groups, supporting a liver specific effect of GW4064 in this model CONCLUSION: GW4064 prevents PNAC in mice through restoration of hepatic FXR signaling resulting in increased expression of canalicular bile, sterol and phospholipid transporters, and suppression of macrophage recruitment and activation. GW 4064 172-178 nuclear receptor subfamily 1, group H, member 4 Mus musculus 41-46 34387888-10 2022 Intestinal inflammation and ileal mRNAs (Nr1h4, Fgf15 and Ostalpha) were not different among groups, supporting a liver specific effect of GW4064 in this model CONCLUSION: GW4064 prevents PNAC in mice through restoration of hepatic FXR signaling resulting in increased expression of canalicular bile, sterol and phospholipid transporters, and suppression of macrophage recruitment and activation. GW 4064 172-178 fibroblast growth factor 15 Mus musculus 48-53 34387888-10 2022 Intestinal inflammation and ileal mRNAs (Nr1h4, Fgf15 and Ostalpha) were not different among groups, supporting a liver specific effect of GW4064 in this model CONCLUSION: GW4064 prevents PNAC in mice through restoration of hepatic FXR signaling resulting in increased expression of canalicular bile, sterol and phospholipid transporters, and suppression of macrophage recruitment and activation. GW 4064 172-178 solute carrier family 51, alpha subunit Mus musculus 58-66 34387888-10 2022 Intestinal inflammation and ileal mRNAs (Nr1h4, Fgf15 and Ostalpha) were not different among groups, supporting a liver specific effect of GW4064 in this model CONCLUSION: GW4064 prevents PNAC in mice through restoration of hepatic FXR signaling resulting in increased expression of canalicular bile, sterol and phospholipid transporters, and suppression of macrophage recruitment and activation. GW 4064 172-178 nuclear receptor subfamily 1, group H, member 4 Mus musculus 232-235 34881818-7 2022 Application of GW4064, an activator of FXR, to microbiota eliminated mice markedly mitigated IR-induced intestinal damage, reduced intestinal epithelial cell death and promoted the survival of IR mice. GW 4064 15-21 nuclear receptor subfamily 1, group H, member 4 Mus musculus 39-42 34870866-8 2021 Mice fed an iron-rich diet were co-administered the FXR agonist GW4064. GW 4064 64-70 nuclear receptor subfamily 1, group H, member 4 Mus musculus 52-55 34888230-6 2021 Importantly, FXR agonist (GW4064) can synergize with anti-PD-1 antibody (Ab) to inhibit HCC growth in tumor-bearing models. GW 4064 26-32 nuclear receptor subfamily 1 group H member 4 Homo sapiens 13-16 35451003-6 2022 Agonistic activation of Fxr (GW4064) in the LShpKO did not alter the elevated basal expression of Cyp8b1 but lowered Cyp7a1 expression. GW 4064 29-35 nuclear receptor subfamily 1, group H, member 4 Mus musculus 24-27 34145381-4 2021 HepG2 cells and primary hepatocytes were incubated with chenodeoxycholic acid (CDCA), glycochenodeoxycholic acid (GCDCA), ursodeoxycholic acid (UCDA), or the synthetic FXR agonist GW4064 for 24 h. MTT tests demonstrated cell viability throughout experiments. GW 4064 180-186 nuclear receptor subfamily 1 group H member 4 Homo sapiens 168-171 34145381-6 2021 Increased TF activity alongside enhanced thrombin generation was observed with CDCA and GW4064 but not with GCDCA and UDCA. GW 4064 88-94 coagulation factor II, thrombin Homo sapiens 41-49 34145381-8 2021 Quantitative polymerase chain reaction revealed upregulation of FXR target genes only by CDCA and GW4064. GW 4064 98-104 nuclear receptor subfamily 1 group H member 4 Homo sapiens 64-67 34406989-7 2021 Functional studies in vitro showed that activation of the FXR in primary cultured astrocytes by chenodeoxycholic acid or GW4064 induced a marked increase in expression levels of small heterodimer partner mRNA and protein. GW 4064 121-127 nuclear receptor subfamily 1, group H, member 4 Mus musculus 58-61 34256254-5 2021 Thus, we decided to develop non-steroidal FXR agonists and discovered a series of novel FXR agonists which were synthesized from GW4064 by replacing the stilbene group with ketoxime ether. GW 4064 129-135 nuclear receptor subfamily 1 group H member 4 Homo sapiens 42-45 34256254-5 2021 Thus, we decided to develop non-steroidal FXR agonists and discovered a series of novel FXR agonists which were synthesized from GW4064 by replacing the stilbene group with ketoxime ether. GW 4064 129-135 nuclear receptor subfamily 1 group H member 4 Homo sapiens 88-91 34366680-5 2021 In vitro, FXR synthetic ligand GW4064 was used to detect the effects on ESCC cell proliferation, migration, apoptosis and cell cycles. GW 4064 31-37 nuclear receptor subfamily 1, group H, member 4 Mus musculus 10-13 34366680-8 2021 Results: FXR synthetic ligand GW4064 impaired esophageal squamous cell carcinoma (ESCC) proliferation and migration, induced apoptosis and cell cycle arrest in vitro, accompanied by inhibition of some inflammatory genes and promotion of pro-apoptotic genes. GW 4064 30-36 nuclear receptor subfamily 1, group H, member 4 Mus musculus 9-12 34366680-10 2021 Consistent with these results, GW4064 suppressed ESCC tumorigenesis in a xenograft model and suppressed the phosphorylation of ERK1/2 in tumors. GW 4064 31-37 mitogen-activated protein kinase 3 Mus musculus 127-133 35451003-6 2022 Agonistic activation of Fxr (GW4064) in the LShpKO did not alter the elevated basal expression of Cyp8b1 but lowered Cyp7a1 expression. GW 4064 29-35 cytochrome P450, family 7, subfamily a, polypeptide 1 Mus musculus 117-123 33311703-7 2020 Importantly, molecular modeling-based screening confirmed the action of the miR-21-targeting drug ivermectin and led to the identification of a new effective derivative, GW4064, for inhibiting oncogenic DDX23-miR-21 signaling. GW 4064 170-176 microRNA 21 Homo sapiens 76-82 35224661-7 2022 Exposure to DON downregulates expression of the genes coding for the apical sodium-dependent bile acid transporter (ASBT), the ileal bile acid-binding protein (IBABP) and the organic solute transporter alpha (OSTalpha), and it counteracts the agonist activity of Farnesoid X receptor (FXR) agonist GW4064 on these genes. GW 4064 298-304 solute carrier family 10 member 2 Homo sapiens 69-114 35224661-7 2022 Exposure to DON downregulates expression of the genes coding for the apical sodium-dependent bile acid transporter (ASBT), the ileal bile acid-binding protein (IBABP) and the organic solute transporter alpha (OSTalpha), and it counteracts the agonist activity of Farnesoid X receptor (FXR) agonist GW4064 on these genes. GW 4064 298-304 solute carrier family 10 member 2 Homo sapiens 116-120 35224661-7 2022 Exposure to DON downregulates expression of the genes coding for the apical sodium-dependent bile acid transporter (ASBT), the ileal bile acid-binding protein (IBABP) and the organic solute transporter alpha (OSTalpha), and it counteracts the agonist activity of Farnesoid X receptor (FXR) agonist GW4064 on these genes. GW 4064 298-304 fatty acid binding protein 6 Homo sapiens 127-158 35224661-7 2022 Exposure to DON downregulates expression of the genes coding for the apical sodium-dependent bile acid transporter (ASBT), the ileal bile acid-binding protein (IBABP) and the organic solute transporter alpha (OSTalpha), and it counteracts the agonist activity of Farnesoid X receptor (FXR) agonist GW4064 on these genes. GW 4064 298-304 fatty acid binding protein 6 Homo sapiens 160-165 35224661-7 2022 Exposure to DON downregulates expression of the genes coding for the apical sodium-dependent bile acid transporter (ASBT), the ileal bile acid-binding protein (IBABP) and the organic solute transporter alpha (OSTalpha), and it counteracts the agonist activity of Farnesoid X receptor (FXR) agonist GW4064 on these genes. GW 4064 298-304 solute carrier family 51 subunit alpha Homo sapiens 175-207 35224661-7 2022 Exposure to DON downregulates expression of the genes coding for the apical sodium-dependent bile acid transporter (ASBT), the ileal bile acid-binding protein (IBABP) and the organic solute transporter alpha (OSTalpha), and it counteracts the agonist activity of Farnesoid X receptor (FXR) agonist GW4064 on these genes. GW 4064 298-304 solute carrier family 51 subunit alpha Homo sapiens 209-217 35224782-7 2022 We showed that GW4064 obviously ameliorated subchondral bone deterioration, associated with reduction in tartrate-resistant acid phosphatase (TRAP) positive multinuclear osteoclast number, as well as articular cartilage degradation, which were blocked by the treatment with FXR antagonist Guggulsterone. GW 4064 15-21 acid phosphatase 5, tartrate resistant Mus musculus 105-140 35224782-7 2022 We showed that GW4064 obviously ameliorated subchondral bone deterioration, associated with reduction in tartrate-resistant acid phosphatase (TRAP) positive multinuclear osteoclast number, as well as articular cartilage degradation, which were blocked by the treatment with FXR antagonist Guggulsterone. GW 4064 15-21 acid phosphatase 5, tartrate resistant Mus musculus 142-146 35224782-7 2022 We showed that GW4064 obviously ameliorated subchondral bone deterioration, associated with reduction in tartrate-resistant acid phosphatase (TRAP) positive multinuclear osteoclast number, as well as articular cartilage degradation, which were blocked by the treatment with FXR antagonist Guggulsterone. GW 4064 15-21 nuclear receptor subfamily 1, group H, member 4 Mus musculus 274-277 35224782-8 2022 Mechanistically, GW4064 impeded osteoclastogenesis through inhibiting subchondral bone osteoclast fusion via suppressing c-Jun N-terminal kinase (JNK) 1/2/nuclear factor of activated T-cells 1 (NFATc1) pathway. GW 4064 17-23 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 194-200 34998040-5 2022 Here we report the synthesis and characterization of compound HEC96719 a novel tricyclic FXR agonist based on a prior high-affinity nonsteroidal molecule GW4064. GW 4064 154-160 nuclear receptor subfamily 1 group H member 4 Homo sapiens 89-92 34998040-6 2022 HEC96719 exhibits excellent potency superior to GW4064 and obeticholic acid in in vitro and in vivo assays of FXR activation. GW 4064 48-54 nuclear receptor subfamily 1 group H member 4 Homo sapiens 110-113 35216094-7 2022 FXR expressed in the intestinal epithelial cells is absolutely required for sustaining a basal expression of intestinal Trpm6 that can be robustly induced by the treatment of GW4064, a synthetic FXR agonist. GW 4064 175-181 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-3 35216094-7 2022 FXR expressed in the intestinal epithelial cells is absolutely required for sustaining a basal expression of intestinal Trpm6 that can be robustly induced by the treatment of GW4064, a synthetic FXR agonist. GW 4064 175-181 transient receptor potential cation channel, subfamily M, member 6 Mus musculus 120-125 35216094-7 2022 FXR expressed in the intestinal epithelial cells is absolutely required for sustaining a basal expression of intestinal Trpm6 that can be robustly induced by the treatment of GW4064, a synthetic FXR agonist. GW 4064 175-181 nuclear receptor subfamily 1, group H, member 4 Mus musculus 195-198 35058750-5 2021 We studied the role of FXR in brain control of energy homeostasis by treating wild-type and FXR-deficient mice by intracerebroventricular (ICV) injection with the reference FXR agonist GW4064. GW 4064 185-191 nuclear receptor subfamily 1, group H, member 4 Mus musculus 173-176 33895309-7 2021 FRET-based real-time monitoring of FXR activity revealed that isoCDCA>CDCA stimulated FXR, and isoDCA and isoUDCA allowed fully activated FXR to be re-stimulated by a second dose of GW4064. GW 4064 182-188 nuclear receptor subfamily 1, group H, member 4 Mus musculus 35-38 33895309-8 2021 In vivo co-administration of a single dose of isoBAs followed by GW4064 cooperatively activated FXR, as did feeding of UDCA in a background of endogenous FXR ligands. GW 4064 65-71 nuclear receptor subfamily 1, group H, member 4 Mus musculus 96-99 34045606-7 2021 Finally, using the synthetic, non-bile acid, FXR-agonist GW4064, we show that some of these effects are mediated through direct or indirect activation of FXR. GW 4064 57-63 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 45-48 34045606-7 2021 Finally, using the synthetic, non-bile acid, FXR-agonist GW4064, we show that some of these effects are mediated through direct or indirect activation of FXR. GW 4064 57-63 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 154-157 35614513-13 2022 Moreover, the FXR agonist GW4064 decreased the proliferation of CC cells by repressing the expression of beta-catenin. GW 4064 26-32 nuclear receptor subfamily 1, group H, member 4 Mus musculus 14-17 35614513-13 2022 Moreover, the FXR agonist GW4064 decreased the proliferation of CC cells by repressing the expression of beta-catenin. GW 4064 26-32 catenin (cadherin associated protein), beta 1 Mus musculus 105-117 33968024-5 2021 Since CDCA is a well-known natural high-affinity ligand for the bile acid receptor farnesoid-x-receptor (FXR) while GW4064 is the synthetic specific agonist of this receptor, we then revealed that GW4064 significantly decreased IL-6 expression in RAW 264.7 cells and bone marrow-derived macrophages but not in FXR-/- macrophages upon LPS stimulation. GW 4064 197-203 nuclear receptor subfamily 1, group H, member 4 Mus musculus 83-103 33968024-5 2021 Since CDCA is a well-known natural high-affinity ligand for the bile acid receptor farnesoid-x-receptor (FXR) while GW4064 is the synthetic specific agonist of this receptor, we then revealed that GW4064 significantly decreased IL-6 expression in RAW 264.7 cells and bone marrow-derived macrophages but not in FXR-/- macrophages upon LPS stimulation. GW 4064 197-203 nuclear receptor subfamily 1, group H, member 4 Mus musculus 105-108 33968024-5 2021 Since CDCA is a well-known natural high-affinity ligand for the bile acid receptor farnesoid-x-receptor (FXR) while GW4064 is the synthetic specific agonist of this receptor, we then revealed that GW4064 significantly decreased IL-6 expression in RAW 264.7 cells and bone marrow-derived macrophages but not in FXR-/- macrophages upon LPS stimulation. GW 4064 197-203 interleukin 6 Mus musculus 228-232 33968024-5 2021 Since CDCA is a well-known natural high-affinity ligand for the bile acid receptor farnesoid-x-receptor (FXR) while GW4064 is the synthetic specific agonist of this receptor, we then revealed that GW4064 significantly decreased IL-6 expression in RAW 264.7 cells and bone marrow-derived macrophages but not in FXR-/- macrophages upon LPS stimulation. GW 4064 197-203 nuclear receptor subfamily 1, group H, member 4 Mus musculus 310-313 33399988-4 2021 METHODS: We treated db/db mice with the FXR agonist GW4064 for 3 months and evaluated insulin resistance, lipid metabolism, renal functional changes, and structural changes in organs including those of the kidney, liver, pancreas, adipose tissue, aorta, and heart. GW 4064 52-58 nuclear receptor subfamily 1, group H, member 4 Mus musculus 40-43 33311703-7 2020 Importantly, molecular modeling-based screening confirmed the action of the miR-21-targeting drug ivermectin and led to the identification of a new effective derivative, GW4064, for inhibiting oncogenic DDX23-miR-21 signaling. GW 4064 170-176 DEAD-box helicase 23 Homo sapiens 203-208 33311703-7 2020 Importantly, molecular modeling-based screening confirmed the action of the miR-21-targeting drug ivermectin and led to the identification of a new effective derivative, GW4064, for inhibiting oncogenic DDX23-miR-21 signaling. GW 4064 170-176 microRNA 21 Homo sapiens 209-215 32341465-8 2020 Farnesoid X receptor (FXR) inhibitor glycine-beta-muricholic acid or FXR knockdown reversed the downregulation of PepT1 expression by CDCA and GW4064 (another FXR agonist). GW 4064 143-149 nuclear receptor subfamily 1, group H, member 4 Rattus norvegicus 0-20 32341465-8 2020 Farnesoid X receptor (FXR) inhibitor glycine-beta-muricholic acid or FXR knockdown reversed the downregulation of PepT1 expression by CDCA and GW4064 (another FXR agonist). GW 4064 143-149 nuclear receptor subfamily 1 group H member 4 Homo sapiens 22-25 32341465-8 2020 Farnesoid X receptor (FXR) inhibitor glycine-beta-muricholic acid or FXR knockdown reversed the downregulation of PepT1 expression by CDCA and GW4064 (another FXR agonist). GW 4064 143-149 nuclear receptor subfamily 1 group H member 4 Homo sapiens 69-72 32341465-8 2020 Farnesoid X receptor (FXR) inhibitor glycine-beta-muricholic acid or FXR knockdown reversed the downregulation of PepT1 expression by CDCA and GW4064 (another FXR agonist). GW 4064 143-149 solute carrier family 15 member 1 Homo sapiens 114-119 32341465-8 2020 Farnesoid X receptor (FXR) inhibitor glycine-beta-muricholic acid or FXR knockdown reversed the downregulation of PepT1 expression by CDCA and GW4064 (another FXR agonist). GW 4064 143-149 nuclear receptor subfamily 1 group H member 4 Homo sapiens 69-72