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Studies indicate that the deregulation of farnesoid X receptor (zeige xpr1 Proteine) (FXR) may lead to abnormalities of specific organs and metabolic dysfunction [Review].
FXR agonist treatment enhanced TGF-beta (zeige TGFB1 Proteine)-induced epithelial mesenchymal transition(EMT (zeige ITK Proteine)) morphologic changes and FXR antagonist inhibited the effect of TGF-beta (zeige TGFB1 Proteine);. Thus, FXR activation enhances EMT (zeige ITK Proteine) in hepatocellular carcinoma (HCC (zeige FAM126A Proteine)) and FXR antagonists may be EMT (zeige ITK Proteine)-suppressing drug candidates.
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.
Data suggest that TGR5 (zeige GPBAR1 Proteine) and FXR in intestinal mucosa are important for glucose homeostasis, in particular in metabolic disorders such as type 2 diabetes and obesity. (TGR5 (zeige GPBAR1 Proteine) = membrane-type receptor for bile acids TGR5 (zeige GPBAR1 Proteine); FXR = farnesoid X receptor (zeige xpr1 Proteine)) [REVIEW; Congress as Topic]
These results suggested that FXR may serve as an important negative regulator for manipulating Smad3 (zeige SMAD3 Proteine) expression, and the FXR/Smad3 (zeige SMAD3 Proteine) pathway may be a novel target for the treatment of renal fibros
Loss of FXR or its down-regulation is associated with higher bile acids concentrations and with a pro-tumorigenic phenotype. (Review)
Lys (zeige LYZ Proteine)-325 is a non-canonical site of SUMOylation of human FXR.CK2 is the priming effector that phosphorylates Ser (zeige SIGLEC1 Proteine)-327, resulting in enhanced SUMO2 (zeige SUMO2 Proteine) conjugation, which then directs the ubiquitination and degradation of FXR through the recruitment of the SUMO-dependent ubiquitin E3 ligase RNF4 (zeige RNF4 Proteine).
we proposed a model to link FXR to Sp1 (zeige PSG1 Proteine), which included triggered FXR, p38/MAPK (zeige MAPK14 Proteine) and/or PI3K (zeige PIK3CA Proteine)/AKT (zeige AKT1 Proteine) signaling and phosphorylated Sp1 (zeige PSG1 Proteine), to illustrate the potential crosstalk between the two factors.
the presented evidence suggested that WA can inhibit HCC (zeige FAM126A Proteine) cell proliferationand tumorigenesis through miR (zeige MLXIP Proteine)-22-repressed CCNA2 (zeige CCNA2 Proteine), which was at least partially through FXR regulation
The results indicated that epigenetically regulated miR (zeige MLXIP Proteine)-449a targets CREB5 (zeige CREB5 Proteine) 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
results suggest that hypothyroidism induces a moderate non-alcoholic steatohepatitis, alllowing the hepatic regeneration. The FXRalpha may be involved in the development of non-alcoholic steatohepatitis in hypothyroid subjects.
FXR is expressed in the ovary, in all regions of the oviduct, and all portions of the vagina of rabbits.
The role of the CAR signaling pathways within testis was validated using specific CAR agonist (TCPOBOP) and inverse agonist (androstanol) that respectively inhibited or reproduced the phenotype observed in Fxralpha-/- males fed Bile acids (BAs)-diet. These data open interesting perspectives to better define how BA homeostasis contributes to physiological or pathophysiological conditions via the modulation of CAR activity.
Study identified an FXR/beta-catenin (zeige CTNNB1 Proteine) interaction whose modulation through beta-catenin (zeige CTNNB1 Proteine) suppression promotes FXR activation and decreases hepatic bile acids, which may provide unique therapeutic opportunities in cholestatic liver diseases
Farnesoid X receptor (zeige xpr1 Proteine) gene deficiency impairs urine concentration in renal medulla.
Data, including data from studies using knockout mice, suggest that control of whole-body energy expenditure by Gcgr (zeige GCGR Proteine) agonism requires intact Fxr signaling and Fgf21 (zeige FGF21 Proteine) secretion in liver. (Gcgr (zeige GCGR Proteine) = glucagon receptor (zeige GCGR Proteine) glucagon (zeige GCG Proteine); Fxr = farnesoid X receptor (zeige xpr1 Proteine); Fgf21 (zeige FGF21 Proteine) = fibroblast growth factor-21 (zeige FGF21 Proteine))
FXR exerts its function in L cells through interacting with CREB (zeige CREB1 Proteine), a crucial transcriptional regulator of cAMP-CREB (zeige CREB1 Proteine) signaling pathway, to inhibit its transcriptional activity. Targeting FXR to rescue GLP-1 (zeige GCG Proteine) secretion may be a promising strategy for type II diabetes.
The underlying mechanism of curcumin against cholestasis was restoring bile acid homeostasis and antagonizing inflammatory responses in a FXR-dependent manner and in turn contributed to overall cholestasis attenuation.
FXR alpha helps establish and maintain an undifferentiated germ cell pool and in turn influences male fertility. FXR alpha controls the expression of the pluripotency marker Lin28 (zeige LIN28A Proteine) in the germ cells.
FXR signaling is a bile acid nuclear receptor that regulates lipids and glucose homeostasis and lack of it causes hepatomegaly and liver dysfunction.
These results suggest that lack of FXR impaired FoxO3a (zeige FOXO3 Proteine)-mediated autophagy and in turn exacerbated alcohol-induced liver injury
alterations in bile acid composition may have contributed to the observed disturbance in FXR-mediated signalling pathways in short bowel syndrome-associated liver disease
FXR splice variant has a dominant positive effect on wild type FXR.
In conclusion, PXR (zeige NR1I2 Proteine) and FXR both responded to ligands that activated their human orthologs, and some of the alternatively spliced variants significantly altered PXR (zeige NR1I2 Proteine) and FXR transactivation at in vivo expression levels.
This gene encodes a ligand-activated transcription factor, which shares structural features in common with nuclear hormone receptor family, such as a DNA-binding domain that targets the receptor to specific DNA sequences, and a ligand-binding domain, which interacts directly with the ligand and contains a ligand-dependent transcriptional activation domain. This protein functions as a receptor for bile acids, and when bound to bile acids, regulates the expression of genes involved in bile acid synthesis and transport. Alternatively spliced transcript variants encoding different isoforms have been described for this gene.
nuclear receptor subfamily 1, group H, member 4
, orphan nuclear receptor FOR2
, bile acid receptor
, farnesoid X activated receptor
, bile acid receptor-like
, RXR-interacting protein 14
, farnesoid X nuclear receptor
, farnesoid X-activated receptor
, farnesol receptor HRR-1
, retinoid X receptor-interacting protein 14
, nuclear receptor subfamily 1 group H member 4