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EGF suppresses specifically CAR signaling mainly through transcriptional regulation and drives the xenobiotic response toward a pregnane X receptor (PXR)-mediated mechanism.
The bosutinib C0 in patients with the NR1I2 7635G/G or 8055T/T genotype was significantly lower than those in patients with the 7635A allele or 8055C allele.
An overview of NR1I2 and NR1I3 pharmacogenetic studies in various therapeutic fields.
We demonstrated that small interfering RNA (siRNA)-mediated knockdown of PRR, Nox2 and Nox4 significantly reduced the HG-induced stimulation of VEGF. On the other hand, Nox4 overexpression significantly potentiated PRR-induced stimulation of VEGF under hyperglycemia in ARPE-19 cells.
The pregnane X receptor (PXR) and the nuclear receptor corepressor 2 (NCoR2) modulate cell growth in head and neck squamous cell carcinoma.
High endogenous pregnane X receptor (PXR) level is associated with poor sorafenib therapy outcome.
A total of six studies with 4248 cases and 3853 controls were included in this meta-analysis. Three PXR gene polymorphisms were evaluated: rs1523127, rs2276707, and rs6785049. Our analyses of rs1523127, rs2276707, and rs6785049 suggested that PXR gene polymorphism had no obvious influence on the risk of inflammatory bowel disease in Caucasians.
genotypes and haplotypes of PXR rs3814057, rs3814058 and rs6785049 have impact on the major adverse cardiovascular events in clopidogrel treated patients after percutaneous coronary intervention
replication confirmed at genome-wide significance the association of loci at FOXE1 with hypothyroidism, and PDE8B, CAPZB and PDE10A with serum TSH. A total of 12 SNPs seemed to explain nearly 7% of the serum TSH variation
NR1I2 has a role in promoting stem cell-mediated colon cancer relapse
Dual ligands of CAR/PXR show distinct gene regulation patterns by regulating cross-talk between CAR and PXR.
High PXR expression is associated with multidrug resistance in breast cancer.
PXR, CYP3A4, and VIL1 expression was decreased only in the actively inflamed small intestinal tissue in children with Crohn's disease.
NR1I2 g.7635A>G had a significant interaction with time, but the dose-adjusted tacrolimus concentration did not significantly differ over 5 years post-transplantation, except for the GG genotype of NR1I2 g.7635A>G.
Together, our results suggest that protection of the endothelial barrier by APC/TR47-mediated signaling pathways might be a valuable therapeutic approach to prevent metastasis
Mulberroside A significantly suppressed PXR-mediated P-gp luciferase activity induced by rifampicin (Rif).
This data indicates that 14-3-3sigma contributes to P-gp overexpression through interaction with PXR with rifampin and paclitaxel treatment.
Data suggest both PXR and CAR are expressed in testis/Sertoli cells; exposure of Sertoli cells (in vitro model of blood-testis barrier) to PXR or CAR ligands (including antiretroviral drugs) up-regulates expression of Pgp/ABCB1, BCRP, and MRP4. (PXR = pregnane X receptor; CAR = constitutive androstane receptor; Pgp/ABCB1 = P-glycoprotein ABCB1; BCRP = breast cancer resistance protein; MRP4 =multidrug resistance protein 4)
Genetic variations in PXR affect induction of Bupropion hydroxylation by sodium ferulate.
The pregnane X receptor down-regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for ("squelching") SRC-1 coactivator.
Data suggest that expression of pregnane X receptor (PXR) is correlated with expression of CYP3A29 in hepatocytes. (CYP3A29 = cytochrome P450 family 3 subfamily A polypeptide 29)
The regulatory effect of IFN-gamma on CYP3A29 expression is mediated via PXR.
Pregnane X receptor is required for interferon-alpha-mediated CYP3A29 expression, and its expression before CYP3A29.
In conclusion, PXR and FXR both responded to ligands that activated their human orthologs, and some of the alternatively spliced variants significantly altered PXR and FXR transactivation at in vivo expression levels.
the PXR gene revealed multiple splice variants in the ligand-binding domain
Selected zebrafish CYP1, CYP2 and CYP3 genes appear to be under the regulation of both pregnane X receptor and aryl hydrocarbon receptor 2.
CYP3A65 and PXR may be involved in the metabolization and detoxification of microcystins in zebrafish, which may be regulated by dre-miR-27b.
similar pattern of mRNA expression of PXR, cytochrome P4503A and multiple drug resistance 1 genes found in fish treated with different PXR inducers suggests that the intrinsic association between these three genes is conserved in zebrafish
This gene product belongs to the nuclear receptor superfamily, members of which are transcription factors characterized by a ligand-binding domain and a DNA-binding domain. The encoded protein is a transcriptional regulator of the cytochrome P450 gene CYP3A4, binding to the response element of the CYP3A4 promoter as a heterodimer with the 9-cis retinoic acid receptor RXR. It is activated by a range of compounds that induce CYP3A4, including dexamethasone and rifampicin. Several alternatively spliced transcripts encoding different isoforms, some of which use non-AUG (CUG) translation initiation codon, have been described for this gene. Additional transcript variants exist, however, they have not been fully characterized.
nuclear receptor subfamily 1 group I member 2
, orphan nuclear receptor PAR1
, orphan nuclear receptor PXR
, pregnane X nuclear receptor variant 2
, pregnane X receptor
, steroid and xenobiotic receptor
, Pregnane X receptor
, nuclear receptor subfamily 1, group 1, member 2
, pregnane X receptor (nuclear receptor sub family 1, group I, member 2)
, nuclear receptor subfamily 1 group I member 2 S homeolog
, nuclear receptor subfamily 1, group I, member 2
, orphan nuclear receptor BXR-beta