Property Summary

NCBI Gene PubMed Count 208
Grant Count 247
R01 Count 157
Funding $32,326,672.24
PubMed Score 306.43
PubTator Score 566.77

Knowledge Summary

Patent (58,079)

Expression

Synonym

Accession Q96RI1 A1L4K5 B7Z412 B7ZM06 F8VYG8 Q8NFP5 Q8NFP6 Q92943
Symbols BAR
FXR
HRR1
HRR-1
PFIC5
RIP14

Gene

PDB

1OSH   1OSK   3BEJ   3DCT   3DCU   3FLI   3FXV   3GD2   3HC5   3HC6   3L1B   3OKH   3OKI   3OLF   3OMK   3OMM   3OOF   3OOK   3P88   3P89   3RUT   3RUU   3RVF   4OIV   4QE6   4QE8   4WVD  

Protein-protein Interaction (2)

MLP Assay (5)

AID Type Active / Inconclusive / Inactive Description
2117 screening 7 / 0 / 0 Late stage results from the probe development effort to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR).
2277 screening 14 / 0 / 0 Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors.
463145 screening 0 / 0 / 6 Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based cell-based assay to identify activators of the farnesoid X receptor (FXR)
504934 other 1 / 0 / 0 Late stage assay provider results from the probe development effort to identify inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors
624279 confirmatory 1 / 0 / 0 Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptor Gamma (RORC): luminescence-based cell-based dose response panel assay against ROR alpha, ROR gamma, LXR, FXR, and VP16

Gene RIF (171)

PMID Text
26888176 Mutations in NR1H4 cause progressive familial intrahepatic cholestasis.
26670557 FXR signalling in ileum biopsies of humans positively correlates with body mass index.
26607331 this is the first report of bile acid derivatives able to antagonize GPBAR1 and and farnesoid X receptor (FXR) modulatory activity.
26488943 FXR is decreased in obese animal models associated with INS resistance. Regulation of bile acids and FXR in the stage of obesity may prevent more metabolism disorders.
26416445 induction of SOCS3 may be a novel mechanism by which FXR exerts its anti-hepatocellular carcinoma effects
26305715 we drew a conclusion that curcumin attenuated Alcoholic liver disease by modulating lipid deposition in hepatocytes via a Nrf2/FXR activation-dependent mechanism
26302777 miR-122 is a novel target gene of FXR, and the upregulation of miR-122 by FXR represses the growth of hepatocellular carcinoma cells, suggesting that FXR may serve as a key transcriptional regulator for manipulating miR-122 expression
26292095 IL-18 repressed FXR mRNA and protein levels in HepG2 cells.
26241054 these data demonstrate that copper-mediated nuclear receptor dysfunction disrupts liver function in WD and potentially in other disorders associated with increased hepatic copper levels.
26134028 FXR activation in L cells decreases proglucagon expression by interfering with the glucose-responsive factor Carbohydrate-Responsive Element Binding Protein (ChREBP) and GLP-1 secretion by inhibiting glycolysis.
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AA Sequence

MVMQFQGLENPIQISPHCSCTPSGFFMEMMSMKPAKGVLTEQVAGPLGQNLEVEPYSQYSNVQFPQVQPQ      1 - 70
ISSSSYYSNLGFYPQQPEEWYSPGIYELRRMPAETLYQGETEVAEMPVTKKPRMGASAGRIKGDELCVVC     71 - 140
GDRASGYHYNALTCEGCKGFFRRSITKNAVYKCKNGGNCVMDMYMRRKCQECRLRKCKEMGMLAECMYTG    141 - 210
LLTEIQCKSKRLRKNVKQHADQTVNEDSEGRDLRQVTSTTKSCREKTELTPDQQTLLHFIMDSYNKQRMP    211 - 280
QEITNKILKEEFSAEENFLILTEMATNHVQVLVEFTKKLPGFQTLDHEDQIALLKGSAVEAMFLRSAEIF    281 - 350
NKKLPSGHSDLLEERIRNSGISDEYITPMFSFYKSIGELKMTQEEYALLTAIVILSPDRQYIKDREAVEK    351 - 420
LQEPLLDVLQKLCKIHQPENPQHFACLLGRLTELRTFNHHHAEMLMSWRVNDHKFTPLLCEIWDVQ        421 - 486
//

Publication (226)

PMID Year Title
26888176 2016 Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis.
26670557 2015 Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction.
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.
26488943 2015 Farnesoid X Receptor Expression Reduced in Obese Rat Model With Insulin Resistance.
26416445 2015 FXR induces SOCS3 and suppresses hepatocellular carcinoma.
26305715 2015 Curcumin attenuates ethanol-induced hepatic steatosis through modulating Nrf2/FXR signaling in hepatocytes.
26302777 2015 Upregulation of microRNA-122 by farnesoid X receptor suppresses the growth of hepatocellular carcinoma cells.
26292095 2015 Interleukin-18 Down-Regulates Multidrug Resistance-Associated Protein 2 Expression through Farnesoid X Receptor Associated with Nuclear Factor Kappa B and Yin Yang 1 in Human Hepatoma HepG2 Cells.
26241054 2015 Elevated copper impairs hepatic nuclear receptor function in Wilson's disease.
26134028 2015 Farnesoid X receptor inhibits glucagon-like peptide-1 production by enteroendocrine L cells.
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