Property Summary

NCBI Gene PubMed Count 43
PubMed Score 315.65
PubTator Score 141.14

Knowledge Summary

Patent (31,189)

Expression

  Differential Expression (2)

Disease log2 FC p
tuberculosis 1.700 8.0e-06
fibroadenoma -1.100 2.4e-02

Protein-protein Interaction (8)

Gene RIF (38)

PMID Text
26607331 this is the first report of bile acid derivatives able to antagonize GPBAR1 and and farnesoid X receptor (FXR) modulatory activity.
26420419 TGR5 is a mediator of bile acid-induced cholangiocyte proliferation and protects cholangiocytes from apoptosis but may trigger proliferation and apoptosis resistance in malignantly transformed cholangiocytes, promoting cholangiocarcinoma.
26417930 These findings identify TGR5 as a suppressor of gastric cancer cell proliferation and migration
26045278 Collectively, these data suggest the involvement of TGR5 in PLD and that TGR5 targeting in cystic cholangiocytes may have therapeutic potential.
25934094 GPBAR1 plays a role in secondary bile acid induced vasodilation via reglation of cystathionine gamma-lyase. The GPBAR1/CSE pathway might contribute to endothelial dysfunction and hyperdynamic circulation in liver cirrhosis.
25418122 Because elevated levels of circulatory LPS may contribute to the development of insulin resistance, the results from this study suggest that bile acids through the activation of TGR5 may have a role in the development of insulin resistance as well.
25283506 Study demonstrates that highly lipophilic 3-epi-betulinic acid derivatives can be potent and selective TGR5 agonists with improved cellular efficacy.
25012842 GPBAR1 SNP is associated with symptoms and pathobiology in IBS-D and IBS-C.
24465162 Our findings strongly suggested the combination of serum TGR5 promoter methylation and AFP enhanced the diagnostic value of AFP alone in discriminating HCC from CHB patients.
24338481 the secondary structure of the TGR5 membrane-proximal C terminus is the determining factor for plasma membrane localization and responsiveness towards extracellular ligands.
23849932 Data suggest that TGR5 is expressed in 2 cell types of term placenta, macrophage/trophoblast; TGR5 expression is low in maternal cholestasis; TGR5 appears to trigger different responses to bile acid/progesterone metabolites depending on cell type.
23818521 DCA, taurolithocholic acid, and oleanolic acid did not stimulate TGR5 association with beta-arrestin 1/2 or G protein-coupled receptor kinase (GRK) 2/5/6, as determined by bioluminescence resonance energy transfer
23619297 TGR5 agonism induces NO production via Akt activation and intracellular Ca(2+) increase in vascular endothelial cells, and this function inhibits monocyte adhesion in response to inflammatory stimuli.
23566200 TGR5 signalling inhibits the production of pro-inflammatory cytokines by in vitro differentiated inflammatory and intestinal macrophages in Crohn's disease.
23523790 Human adipose tissue TGR5 expression is positively correlated to obesity and reduced during diet-induced weight loss.
23238937 TGR5 is overexpressed in most gastric intestinal-type adenocarcinomas, and moderate to strong TGR5 staining is associated with decreased patient survival in all gastric adenocarcinomas.
23022524 this study demonstrates that the TGR5 expressed in the pancreatic beta cells regulates insulin secretion and highlights the importance of ongoing therapeutic strategies targeting TGR5 in the control of glucose homeostasis.
22550135 the mechanisms of metabolic regulation by FXR and TGR5
22236403 These results indicate that bile acids induce the differentiation of IL-12 hypo-producing dendritic cells from monocytes via the TGR5-cAMP pathway.
21883702 Data suggest that variation in bile acid receptor TGR5 may contribute to altered small bowel transit and colonic transit in lower functional gastrointestinal disorders.
21754919 TGR5 is a key factor in energy expenditure by regulating metabolism.
21691110 The TGR5 gene is localized at chromosome 2q35, close to a genetic variant associated with both primary sclerosing cholangitis and ulcerative colitis in recent genome-wide association studies.
21691103 The aim of the present study was to determine the localization and function of the receptor in biliary epithelial cells.
21691102 The current knowledge on BA receptors is reviewed, with a strong focus on the cell membrane receptor TGR5, which has emerged as a promising target for intervention in metabolic diseases.
21212509 The ability of the bile acid analogues obtained by chemical modification of ursodeoxycholic acid (UDCA) for TGR5 activation in HEK 293 cells is reported.
20811628 resequencing of TGR5 along with functional investigations of novel variants
20811628 Observational study of gene-disease association. (HuGE Navigator)
20623999 The TGR5 is localized in the primary cilium of human cholangiocytes and the receptor could play an important role in coupling biliary bile acid concentration and composition to ductular bile formation.
19944697 Observational study and genome-wide association study of gene-disease association. (HuGE Navigator)
19723493 TGR5 signaling pathway is critical in regulating intestinal glucagon-like peptide-1 secretion in CHO cells transiently transfected hTGR5 gene.
19716570 Our data suggest that a common genetic variation within the GPBAR1 gene may not play a major role in the development of prediabetic phenotypes in our white population
19716570 Observational study of gene-disease association. (HuGE Navigator)
19582812 TGR5 mediates chloride secretion via activation of CFTR. The presence of the receptor in both the plasma membrane and the recycling endosome indicate that TGR5 can be regulated by translocation.
17326144 This is the first report on the expression of TGR5 in sinusoidal endothelial cells. Regulation of eNOS by TGR5 connects bile salts with hepatic hemodynamics.
17214962 These results suggest that in AGS cells, DC transactivates EGFR through M-BAR- and ADAM/HB-EGF-dependent mechanisms.
17178880 Combined blockade of both epidermal growth factor receptors and GPCRs may be a rational strategy to treat cancers, including head and neck squamous cell carcinoma that shows cross-talk between GPCR and EGFR signaling pathways.
12524422 TGR5 is implicated in the suppression of macrophage functions by bile acids
12419312 Expression of BG37 was detected in various specific tissues, suggesting its physiological role.

AA Sequence

MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLAGLLTGLALPT      1 - 70
LPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQPPGSIRLALLLTWAGPLLFAS     71 - 140
LPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGAAAFLSVRVLATAHRQLQDICRLERAVCRDE    141 - 210
PSALARALTWRQARAQAGAMLLFGLCWGPYVATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAM    211 - 280
GLGDQRYTAPWRAAAQRCLQGLWGRASRDSPGPSIAYHPSSQSSVDLDLN                        281 - 330
//

Text Mined References (43)

PMID Year Title
26607331 2016 Investigation on bile acid receptor regulators. Discovery of cholanoic acid derivatives with dual G-protein coupled bile acid receptor 1 (GPBAR1) antagonistic and farnesoid X receptor (FXR) modulatory activity.
26420419 2016 TGR5 is essential for bile acid-dependent cholangiocyte proliferation in vivo and in vitro.
26417930 2015 The G-protein-coupled bile acid receptor Gpbar1 (TGR5) suppresses gastric cancer cell proliferation and migration through antagonizing STAT3 signaling pathway.
26045278 2015 TGR5 in the Cholangiociliopathies.
25934094 2015 Cystathionine ?-lyase, a H2S-generating enzyme, is a GPBAR1-regulated gene and contributes to vasodilation caused by secondary bile acids.
25418122 2015 Activation of the bile acid receptor TGR5 enhances LPS-induced inflammatory responses in a human monocytic cell line.
25283506 2014 Highly lipophilic 3-epi-betulinic acid derivatives as potent and selective TGR5 agonists with improved cellular efficacy.
25012842 2014 Genetic variation in GPBAR1 predisposes to quantitative changes in colonic transit and bile acid excretion.
24465162 2014 Aberrant DNA methylation of G-protein-coupled bile acid receptor Gpbar1 (TGR5) is a potential biomarker for hepatitis B Virus associated hepatocellular carcinoma.
24338481 2014 A membrane-proximal, C-terminal ?-helix is required for plasma membrane localization and function of the G Protein-coupled receptor (GPCR) TGR5.
23849932 2013 Effect of maternal cholestasis on TGR5 expression in human and rat placenta at term.
23818521 2013 The bile acid receptor TGR5 does not interact with ?-arrestins or traffic to endosomes but transmits sustained signals from plasma membrane rafts.
23619297 2013 Bile acid receptor TGR5 agonism induces NO production and reduces monocyte adhesion in vascular endothelial cells.
23566200 2013 TGR5 signalling inhibits the production of pro-inflammatory cytokines by in vitro differentiated inflammatory and intestinal macrophages in Crohn's disease.
23523790 2013 The TGR5 gene is expressed in human subcutaneous adipose tissue and is associated with obesity, weight loss and resting metabolic rate.
23238937 2013 Expression of bile acid receptor TGR5 in gastric adenocarcinoma.
23022524 2012 Activation of transmembrane bile acid receptor TGR5 stimulates insulin secretion in pancreatic ? cells.
22550135 2012 Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease.
22236403 2012 Bile acids induce monocyte differentiation toward interleukin-12 hypo-producing dendritic cells via a TGR5-dependent pathway.
21883702 2011 Association of bile acid receptor TGR5 variation and transit in health and lower functional gastrointestinal disorders.
21754919 2011 TGR5: a novel target for weight maintenance and glucose metabolism.
21691110 2011 TGR5 sequence variation in primary sclerosing cholangitis.
21691103 2011 TGR5 in the biliary tree.
21691102 2011 The bile acid membrane receptor TGR5: a valuable metabolic target.
21212509 2011 Effects of chemical modification of ursodeoxycholic acid on TGR5 activation.
20811628 2010 Mutational characterization of the bile acid receptor TGR5 in primary sclerosing cholangitis.
20623999 2010 The membrane-bound bile acid receptor TGR5 (Gpbar-1) is localized in the primary cilium of cholangiocytes.
19944697 2010 Genome-wide association analysis in primary sclerosing cholangitis.
19723493 2009 TGR5-mediated bile acid sensing controls glucose homeostasis.
19716570 2009 Preliminary report: genetic variation within the GPBAR1 gene is not associated with metabolic traits in white subjects at an increased risk for type 2 diabetes mellitus.
19582812 2009 The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders.
18577758 2008 Dissociation of heterotrimeric g proteins in cells.
17326144 2007 The G-protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells.
17214962 2007 Involvement of membrane-type bile acid receptor M-BAR/TGR5 in bile acid-induced activation of epidermal growth factor receptor and mitogen-activated protein kinases in gastric carcinoma cells.
17178880 2006 Cross-talk between G protein-coupled receptor and epidermal growth factor receptor signaling pathways contributes to growth and invasion of head and neck squamous cell carcinoma.
16400329 2006 Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
14702039 2004 Complete sequencing and characterization of 21,243 full-length human cDNAs.
12524422 2003 A G protein-coupled receptor responsive to bile acids.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12419312 2002 Identification of membrane-type receptor for bile acids (M-BAR).
12044878 2002 Identification of G protein-coupled receptor genes from the human genome sequence.
12036966 2002 Selective inhibition of heterotrimeric Gs signaling. Targeting the receptor-G protein interface using a peptide minigene encoding the Galpha(s) carboxyl terminus.