Recombinant Human Bile acid receptor (NR1H4)

1. FXR pathway activation increases XBP1 splicing and enhances p-IRE1alpha expression in liver PMID: 29377207
2. Activation of FXR inhibits, whereas TGR5 activation may promote, cholangiocarcinoma progression by regulating proliferation, migration and mitochondrial energy metabolism. PMID: 28916388
3. study demonstrated for the first time a novel target for farnesoid X-activated receptor (FXR) and that the activated receptor alters the acquisition of sperm fertilising ability PMID: 29921626
4. Low FXR expression is associated with colorectal cancer. PMID: 30106441
5. Studies indicate that the deregulation of farnesoid X receptor (FXR) may lead to abnormalities of specific organs and metabolic dysfunction [Review]. PMID: 30013008
6. FXR agonist treatment enhanced TGF-beta-induced epithelial mesenchymal transition(EMT) morphologic changes and FXR antagonist inhibited the effect of TGF-beta;. Thus, FXR activation enhances EMT in hepatocellular carcinoma (HCC) and FXR antagonists may be EMT-suppressing drug candidates. PMID: 29958417
7. This study provides some data suggesting the possible involvement of FXR in the pathophysiology and development of thyroid neoplasms. In particular, we found that there are differences regarding FXR expression between papillary carcinomas and hyperplastic nodules, being also correlated with some patients' clinicopathological parameters. PMID: 28762281
8. Data suggest that TGR5 and FXR in intestinal mucosa are important for glucose homeostasis, in particular in metabolic disorders such as type 2 diabetes and obesity. (TGR5 = membrane-type receptor for bile acids TGR5; FXR = farnesoid X receptor) [REVIEW; Congress as Topic] PMID: 27846919
9. These results suggested that FXR may serve as an important negative regulator for manipulating Smad3 expression, and the FXR/Smad3 pathway may be a novel target for the treatment of renal fibros PMID: 27853248
10. Loss of FXR or its down-regulation is associated with higher bile acids concentrations and with a pro-tumorigenic phenotype. (Review) PMID: 28400119
11. Lys-325 is a non-canonical site of SUMOylation of human FXR.CK2 is the priming effector that phosphorylates Ser-327, resulting in enhanced SUMO2 conjugation, which then directs the ubiquitination and degradation of FXR through the recruitment of the SUMO-dependent ubiquitin E3 ligase RNF4. PMID: 28201649
12. we proposed a model to link FXR to Sp1, which included triggered FXR, p38/MAPK and/or PI3K/AKT signaling and phosphorylated Sp1, to illustrate the potential crosstalk between the two factors. PMID: 28402278
13. the presented evidence suggested that WA can inhibit HCC cell proliferationand tumorigenesis through miR-22-repressed CCNA2, which was at least partially through FXR regulation PMID: 27738335
14. The results indicated that epigenetically regulated miR-449a targets CREB5 to increase FXRalpha expression, thereby promoting HBV replication and gene expression. Our findings provide a new understanding of the role of miRNAs in HBV replication PMID: 27138288
15. In diabetic humans, there is decreased FXR expression in the kidney. FXR plays an important role in Diabetic Kidney Disease. PMID: 27045028
16. FXR regulates serum triglyceride level in part through PLA2G12B. PMID: 27471003
17. It regulates the growth of renal adenocarcinoma cells. PMID: 28496032
18. we conclude that FXR-Gank-TSPs-Stem cells pathway is a key determinant of liver cancer in animal models and in pediatric liver cancer. Our data provide a strong basis for development of FXR-Gank-based therapy for treatment of patients with hepatoblastoma PMID: 28535186
19. PPARalpha and FXR function coordinately to integrate liver energy balance. PMID: 28287408
20. These studies investigated in differentiated HepaRG cells and in primary human hepatocytes (PHHs) effects of FXR activation on HBV replication and of infection on the FXR pathway. PMID: 27251172
21. Treatment with LXR and FXR ligands initiates coated platelet formation, which is thought to support coagulation but results in desensitization to platelet stimuli through inhibition of alphaIIbbeta3 consistent with their ability to inhibit platelet function and stable thrombus formation in vivo. PMID: 28619996
22. FXR ligands to inhibit platelet activation. PMID: 27758768
23. Taken together, our data provide the first evidence that FXR suppresses proliferation of human liver cancer cells via the inhibition of the mTOR/S6K signaling pathway. FXR expression can be used as a biomarker of personalized mTOR inhibitor treatment assessment for liver cancer patients. PMID: 27109477
24. Activated FXR inhibits leptin signaling and counteracts tumor-promoting activities of cancer-associated fibroblasts in breast malignancy. PMID: 26899873
25. FXR may promote the proliferation of tumor cells and the hepatocytes in the process of liver regeneration by activating the PDK4-mediated metabolic reprogramming to generate glycolytic intermediates essential for rapid biomass generation, establishing a mechanistic link between cell proliferation and metabolic switch. PMID: 26728993
26. this is the first report of bile acid derivatives able to antagonize GPBAR1 and and farnesoid X receptor (FXR) modulatory activity. PMID: 26607331
27. induction of SOCS3 may be a novel mechanism by which FXR exerts its anti-hepatocellular carcinoma effects PMID: 26416445
28. Mutations in NR1H4 cause progressive familial intrahepatic cholestasis. PMID: 26888176
29. we drew a conclusion that curcumin attenuated Alcoholic liver disease by modulating lipid deposition in hepatocytes via a Nrf2/FXR activation-dependent mechanism PMID: 26305715
30. 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 PMID: 26302777
31. IL-18 repressed FXR mRNA and protein levels in HepG2 cells. PMID: 26292095
32. FXR signalling in ileum biopsies of humans positively correlates with body mass index. PMID: 26670557
33. 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. PMID: 26134028
34. 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. PMID: 26488943
35. These results provide important information to prioritize chemicals for further investigation, and suggest possible modes of action of compounds in FXR signaling. PMID: 25257666
36. FXR may regulate SOD3 expression to suppress reactive oxygen species production, resulting in decreasing JNK activity. PMID: 25496033
37. Liver nuclear receptors, FXR and SHP, and bile acid transporters, NTCP and BSEP, are associated with the progression of NAFLD. PMID: 26019035
38. Three FXR gene variants (rs35724, rs11110385, rs11110386) were identified as potential susceptibility factors for cholelithiasis in a German cohort in gender- and weight-dependent manners PMID: 25242139
39. 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. PMID: 26241054
40. FXR agonist, GW4064, upregulates adipokine expression in preadipocytes and HepG2 cells. PMID: 25400456
41. NHR1H4 genotype increases the risk for spontaneous bacterial peritonitis in live cirrhosis patients. PMID: 25086996
42. Results show that HRG is a novel transcriptional target gene of FXR in human hepatoma cells, human upcyteVR primary hepatocytes and 3D human liver microtissues in vitro and in mouse liver in vivo. PMID: 25363753
43. established genome-wide human FXR binding and transcriptome profiles. These results will aid in determining the human FXR functions, as well as judging to what level the mouse models could be used to study human FXR functions PMID: 25198545
44. our data showed that bile acid-activated FXR stimulates miR-22-silenced CCNA2, a novel pathway for FXR to exert its protective effect in the gastrointestinal tract. PMID: 25596928
45. AB23A produces protective effect against ANIT-induced hepatotoxity and cholestasis, due to FXR-mediated regulation of transporters and enzymes. PMID: 25655198
46. Compared with normal gallbladder tissues, FXR expression was decreased and MCL1 expression was increased in GBC, during progression of tumor node metastasis (TNM) stage PMID: 25043081
47. Intestinal nuclear bile acid farnesoid X receptor is regulated transcriptionally by CDX2. PMID: 25138215
48. significant differences at the distal (-1890) and proximal promoter (-358) CpG sites of the FXR/NR1H4 and at the distal PXR/NR1I2 (-1224) promoter, which were consistently less methylated in ICP cases when compared with controls. PMID: 24498169
49. show that FXR interacts with and is O-GlcNAcylated by O-GlcNAc transferase in its N-terminal AF1 domain PMID: 24037988
50. NR1H4 methylation is associated with colon cancer. PMID: 24169962

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HGNC: 7967

OMIM: 603826

KEGG: hsa:9971

STRING: 9606.ENSP00000447149

UniGene: Hs.282735