Property Summary

NCBI Gene PubMed Count 43
Grant Count 36
R01 Count 28
Funding $3,032,478.84
PubMed Score 315.65
PubTator Score 141.14

Knowledge Summary

Patent (31,189)

Expression

  Differential Expression (2)

Disease log2 FC p
tuberculosis 1.700 0.000
fibroadenoma -1.100 0.024

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.
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AA Sequence

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