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Validated All-in-One™ qPCR Primer for NR1I2(NM_022002.2) Search again
Product ID:
HQP021631
(click here to view gene annotation page)
Powered by BiozSpecies:
Human
Symbol:
Alias:
BXR, ONR1, PAR, PAR1, PAR2, PARq, PRR, PXR, SAR, SXR
Gene Description:
nuclear receptor subfamily 1 group I member 2
Target Gene Accession:
NM_022002.2(click here to view gene page)
Estimated Delivery:
Approximately 1-3 weeks, but may vary. Please email sales@genecopoeia.com or call 301-762-0888 to confirm ETA.
Important Note:
By default, qPCR primer pairs are designed to measure the expression level of the splice variant (accession number) you selected for this gene WITHOUT consideration of other possible variants of this gene. If this gene has multiple variants, and you would like to measure the expression levels of one particular variant, multiple variants, or all variants, please contact us for a custom service project at inquiry@genecopoeia.com.
Summary
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.
Gene References into function
- In-vitro transcription/translation studies show that translation of pregnane X receptor mRNA initiates at a non-AUG (CUG) codon.
- promiscuous nuclear receptor that responds to a wide variety of drugs, xenobiotics and endogenous compounds, and plays a critical role in mediating drug-drug interactions in humans
- Role of SXR in xenobiotic inhibition of CYP3A4 promotor activity
- mediates the proliferative action of mast-cell tryptase: possible relevance to human fibrotic disorders
- alternative splicings for hPXR may largely contribute to the interindividual variability in CYP3A4 and P-glycoprotein induction
- Pregnane X receptor mRNA expression levels are compared in a panel of 12 individual human liver samples; a 27-fold variability in PXR mRNA expression is found.
- human PXR requires a specific agonist different from that required in mice to induce cyp3A expression
- results provide evidence that the nuclear import of SXR is mediated by bipartite type of nuclear localization signal, which is recognized by three groups of importin adaptors for targeting the nuclear rim
- control of steroid, heme, and carcinogen metabolism by this protein in transgenic mice
- The present data indicate that SXR is a key system to induce, maintain and reverse a cisplatin-resistant phenotype in endometrial cancer cells.
- 2.0A crystal structure of the human PXR ligand-binding domain (LBD) in complex with the cholesterol-lowering compound SR12813 and a 25 amino acid residue fragment of the human steroid receptor coactivator-1 (SRC-1) containing one LXXLL motif
- steroid and xenobiotic receptor(SXR) has a novel role as a mediator of bone homeostasis in addition to its role as a xenobiotic sensor
- individual variation in pregnane X receptor expression may account for differential expression of some UDP-glucuronosyltransferase isoforms between subjects
- pregnane X receptor is a major determinant of CYP2B6-inducible expression
- pregnane X receptor (PXR) and constitutively activated receptor (CAR) mediate induction of CYP3A5 in human liver and intestine
- PXR-mediated gene regulation is affected by its DNA binding site
- ligand-activated PXR interferes with HNF-4 signaling by targeting the common coactivator PGC-1, which underlies physiologically relevant inhibitory cross-talk between drug metabolism and cholesterol/glucose metabolism
- expressed approximately 250-fold lower in peripheral blood mononuclear cells than in liver, and significantly correlated to MDR1 mRNA
- xenobiotics and drugs can modulate 25-hydroxyvitamin D(3)-24-hydroxylase gene expression and alter vitamin D(3) hormonal activity and calcium homeostasis through the activation of PXR
- findings demonstrated age-related differences in the body's capacity to metabolize steroids and xenobiotic compounds and suggest an important role for SXR and its target genes, CYP3A4 and MDR1 in this process
- pxr polymorphism is associated with decreased expression of MDR1 mRNA in intestinal villi
- there is cross talk between distal CAR/PXR sites and HNF4alpha binding sites in the CYP2C9 promoter and that the HNF4alpha sites are required for maximal induction of the CYP2C9 promoter.
- role in transcriptional regulation of CYP2C8
- May be involved in metabolic detoxification in drug-induced osteomalacia.
- PXR expression is required for Bcl-2 and Bcl-xL up-regulation upon PXR activators treatment in human and rat hepatocytes.
- PXR was observed to be a predominantly nuclear protein maintaining a dynamic equilibrium between the nuclear and cytoplasmic compartments of interphase cells.
- The minimal essential region for promoter activity has been mapped to a 160 bp region upstream of the transcription initiation site, an area that also showed nuclear protein binding.
- structural models of the pregnane X receptor (PXR)complexes PXR-LBD/SMRT-ID1 and PXR-LBD/SMRT-ID2 reveal key interactions that account for binding preferences.
- genetic variation in the PXR encoding gene, which has been associated with altered activity of PXR, is strongly associated with susceptibility to inflammatory bowel disease, crohn disease and ulcerative colitis.
- cross-regulation of CD36 by PXR and PPARgamma suggests that this fatty acid transporter may function as a common target of orphan nuclear receptors in their regulation of lipid homeostasis
- SXR mediates vitamin K2-activated transcription of extracellular matrix-related genes and collagen accumulation in osteoblastic cells
- NF-kappaB p65 directly interacted with the DNA-binding domain of RXRalpha and may prevent its binding to the consensus DNA sequences, thus inhibiting the transactivation by the PXR.RXRalpha complex.
- Data show that activation of steroid and xenobiotic receptor does not induce cytochrome P450, family 24 (CYP24)-mediated expression, but inhibits vitamin D receptor-mediated CYP24 promoter activity.
- The pregnane X receptor is transcriptionally functional in human hepatic stellate cells and activators inhibit transdifferentiation and proliferation.
- These results suggest that the unique Trp-Zip-mediated PXR homodimer plays a role in the function of this nuclear xenobiotic receptor.
- hPXR activation in vivo increased P-glycoprotein activity and tightened the blood-brain barrier to methadone, reducing the drug's CNS efficacy. This is the first demonstration of the ability of PXR to alter the efficacy of a CNS-acting drug.
- clinical consequences for individuals undergoing therapeutic exposure to the wide variety of drugs that are also SXR agonists
- CYP2A6 is induced via PXR and PGC-1alpha through the DR4-like element at the distal response region.
- Functional SXR gene variants appear to modify disease course in PSC.
- PXR is a potential endocrine disrupting factor that may have broad implications in steroid homeostasis and drug-hormone interactions
- Dietary isothiocyanate sulforaphane is the first identified naturally occurring antagonist for SXR.
- Human pregnane X receptor gene polymorphisms and alternative mRNA splicing were investigated as possible contributors to individual variability in CYP3A metabolic activity.
- there may be an intestine-specific PXR/CYP27A1/LXRalpha pathway that regulates intestine cholesterol efflux and HDL assembly.
- PXR protein levels were equal in uninflamed and inflamed tissue of CD and UC patients despite low PXR mRNA levels in inflamed tissue.
- PXR plays a critical role in the regulation of P450 3A4 expression in osteosarcoma and that its expression and activation in these tumors may influence the effect of chemotherapeutic agents on the induction of target genes implicated in drug resistance
- Study of molecular structure provides detailed insights into the manner in which human PXR responds to a wide range of endobiotic compou
- In comparison with previously published data, we identified 13 novel polymorphisms. Genetic variation contributing to altered NR1I2 function may have an important clinical impact.
- T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity.
- not only the Q158K variant found in Chinese, but also in native pregnane X receptor variants in other ethnic groups (D163G, A370T, R381W, and I403V) affect CYP3A4 induction by altering steroid receptor coactivator-1 recruitment
- Comparative genomics of xenobiotic metabolism: a porcine-human PXR gene comparison.
- Some azole anticancer agents repress the coordinated activation of genes involved in drug metabolism by blocking PXR activation.
- There were significant phytoestrogen interactions with polymorphisms in ESR1 and NR1I2 genes in affecting estrone levels; we conclude that phytoestrogens modulate sex hormone and SHBG levels in postmenopausal women.
- Tamoxifen activated the SXR-mediated transcription through CYP3A4 and MDR1 promoters in a ligand- and receptor concentration-dependent manner.
- Discovery of a highly active ligand of human pregnane X receptor is reported.
- Human pregnane X receptor antagonists and agonists define molecular requirements for different binding sites.
- Nuclear PXR represses the transcription of the glucose-6-phosphatase gene by inhibiting the DNA-binding ability of cAMP-response element-binding protein (CREB).
- Reduction of sperm motility by tryptase through the PAR-2 receptor involves epidermal growth factor receptor pathways.
- CYP3A4 enhancers co-ordinate the proximal promoter in responding similarly to the pregnane X receptor but differentially to hepatocyte nuclear factor-4alpha
- we have utilized a target selective human pregnane X receptor-siRNA (hPXR-siRNA)-adenovirus expression system to examine the contribution of hPXR on the gene regulation of drug-metabolizing P450s in human hepatocytes
- The data seem to support the association of the PXR locus with extensive ulcerative colitis and the interaction between PXR and MDR1 genes.
- Inter-individual/inter-ethnic variations of docetaxel and doxorubicin pharmacokinetics or pharmacodynamics exist, but genotypic variability of PAR cannot account for this variability.
- Polymorphisms in the NR1I2 gene are not significantly associated with epilepsy treatment responses.
- PXR promoter and intron 1 SNPs associated with PXR target gene expression (CYP3A4)
- PAR2 up-regulates cyclooxygenase-2 expression via an ERK1/2-mediated activation.
- Besides functioning as a xenobiotic biosensor, our findings show that SXR is also a vitamin K2 target and an important transcriptional factor that regulates bone homeostasis in bone cells[review]
- miR-148a post-transcriptionally regulated human PXR, resulting in the modulation of the inducible and/or constitutive levels of CYP3A4 in human liver.
- These results extend the 5'UTR sequence of PXR1 and PXR2 and define new proximal promoters for both; in addition, PXR2 has transcriptional activity comparable to that of PXR1.
- In this review, pregnane X receptor (PXR) is a nuclear receptor that plays a critical role in modulating hepatic energy metabolism.
- The activities of the human pregnane X receptor promoter are significantly increased by co-expression of hepatocyte nuclear factor 4 alpha.
- NR1I2 gene haplotype is not associated with Crohn's disease
- there are marked differences in the mutant frequencies of A11156C and T11193C of PXR between Han Chinese and other ethnic groups. The mutant frequency in the coding region (exons 2 and 4) of PXR was very low in Han Chinese
- Influence of NR1I2 polymorphism on prednisolone pharmacokinetics in renal transplant recipients was evaluated. Those carrying the allele possessed higher intestinal metabolic activity for prednisolone, greatly reducing its maximal plasma concentration.
- PXR activation, regardless of the type of ligand agonist present, promotes the "malignant" phenotype of cancer cells.
- Cdk2 negatively regulates the activity of hPXR, and suggest an important role for Cdk2 in regulating hPXR activity and CYP3A4 expression in hepatocytes passing through the cell cycle
- The purpose of this study was to evaluate the role of coding variation in hPXR (NR1I2) in intrahepatic cholestasis of pregnancy (ICP) and to functionally asses the response of PXR variants to ligands of interest in ICP.
- investigated pregnane X receptor polymorphisms in relation to unboosted atazanavir plasma concentrations in 2 cohorts of patients. The polymorphism 63396T-->C predicted concentrations below the minimum effective concentration with odds ratios of 18
- This study showed that PXR*1B was associated with reduced hepatic mRNA expression of PXR and its downstream targets, CYP3A4 and ABCB1
- the interplay between a xenobiotic nuclear receptor PXR and OATP1A2 that could contribute to the pathogenesis of breast cancer.