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characterized activity profile of CAR and compared with hCAR (zeige CXADR ELISA Kits) and mCAR (zeige CXADR ELISA Kits); related this to structural homology among the 3 orthologues; 5 alternative splice variants identified and sequenced each of which generated a truncated protein product
CAR is important for hepatic clearance of several widely prescribed drugs metabolized by P450 (zeige POR ELISA Kits) enzymes, however the fasting-induced (zeige C10orf10 ELISA Kits) alterations in P450 (zeige POR ELISA Kits)-mediated drug clearance are largely independent of CAR.
The present study has revealed known and novel, as well as common and unique targets of PXR (zeige NR1I2 ELISA Kits) and CAR in mouse liver following pharmacological activation using their prototypical ligands.
Results show that circadian disruption activates CAR via sympathetic dysfunction and cholestasis. The nuclear receptor CAR drives NAFLD (zeige TSC2 ELISA Kits) to NASH (zeige SAMSN1 ELISA Kits), fibrosis, and hepatocellular carcinoma progression
data indicate that DE might be a potential therapeutic agent for obese pregnant patients with insulin (zeige INS ELISA Kits) resistance through CAR to prevent the perinatal outcomes such as preeclampsia, gestational diabetes, and macrosomia. Further analysis of possible complications and side effects using animal models is required.
Combining CAR activation with limited beta-catenin (zeige CTNNB1 ELISA Kits) activation induces tumorigenesis, and the tumours share a conserved gene expression signature with beta-catenin (zeige CTNNB1 ELISA Kits)-positive human hepatocellular carcinoma.
Constitutive androstane receptor is the main mediator of liver hypertrophy induced by cyproconazole and fluconazole, but not tebuconazole; constitutive androstane receptor played a crucial role in liver tumor development induced by all three triazoles.
CAR activation decreases miR (zeige MLXIP ELISA Kits)-122 levels through suppression of HNF4alpha (zeige HNF4A ELISA Kits) transcriptional activity and indirectly regulates the promitogenic protein cMyc (zeige MYC ELISA Kits).
The induction of CYP2B by PB or CFA (zeige TBCA ELISA Kits) was comparable to nuclear CAR levels. CAR nuclear translocation was induced by CFA (zeige TBCA ELISA Kits) in both rat strains.
The nuclear receptor constitutive androstane receptor/NR1I3 enhances the profibrotic effects of transforming growth factor beta and contributes to the development of experimental dermal fibrosis.
ubiquitin-proteasomal regulation of CCRP (zeige DNAJC7 ELISA Kits) and HSP70 (zeige HSP70 ELISA Kits) are important contributors to the regulation of cytoplasmic CAR levels, and hence the ability of CAR to respond to PB or PB-like inducers
Data suggest both PXR (zeige NR1I2 ELISA Kits) and CAR are expressed in testis/Sertoli cells; exposure of Sertoli cells (in vitro model of blood-testis barrier) to PXR (zeige NR1I2 ELISA Kits) or CAR ligands (including antiretroviral drugs) up-regulates expression of Pgp/ABCB1 (zeige ABCB4 ELISA Kits), BCRP (zeige ABCG2 ELISA Kits), and MRP4 (zeige ABCC4 ELISA Kits). (PXR (zeige NR1I2 ELISA Kits) = pregnane X receptor (zeige NR1I2 ELISA Kits); CAR = constitutive androstane receptor; Pgp/ABCB1 (zeige ABCB4 ELISA Kits) = P-glycoprotein ABCB1 (zeige ABCB1 ELISA Kits); BCRP (zeige ABCG2 ELISA Kits) = breast cancer resistance protein (zeige ABCG2 ELISA Kits); MRP4 (zeige ABCC4 ELISA Kits) =multidrug resistance protein 4)
Genome-wide comparison of the inducible transcriptomes of nuclear receptors CAR, PXR (zeige NR1I2 ELISA Kits) and PPARalpha (zeige PPARA ELISA Kits) in primary human hepatocytes has been presented.
Integrative analysis of four RNA-Seq datasets and differential expression revealed for the first time, splicing alterations of SLC39A14 (zeige SLC39A14 ELISA Kits) and NR1I3 in hepatocellular carcinoma.
These results reveal both novel and known targets of hCAR (zeige CXADR ELISA Kits) and support the role of hCAR (zeige CXADR ELISA Kits) in maintaining the homeostasis of metabolism and cell proliferation in the liver.
Around 42.5% of the overall interindividual variability in warfarin dose requirements was explained : VKORC1 (zeige VKORC1 ELISA Kits) genotype accounted for 29.6%, CYP2C9 (zeige CYP2C9 ELISA Kits) genotype for 4.3%, age for 3.6%, the CYP4F2 (zeige CYP4F2 ELISA Kits) genotype for 3.3%, and CAR/HNF4alpha (zeige HNF4A ELISA Kits) (rs2501873/rs3212198) for 1.7%
It is suggested that the functions of PXR (zeige NR1I2 ELISA Kits), CAR and AhR (zeige AHR ELISA Kits) may be closely implicated in the pathogeneses of metabolic vascular diseases, such as hyperlipidemia, atherogenesis, and hypertension.
Suggest that PXR (zeige NR1I2 ELISA Kits) and CAR double humanized mice are more sensitive rifampcin induction of cytochrome P450 (zeige CYP ELISA Kits) and UDP-glucuronosyltransferases.
PRMT5 (zeige PRMT5 ELISA Kits) enhances transcriptional activity of constitutive androstane receptor.PRMT5 is a gene-selective co-activator for CAR.
Donor CYP3A5 (zeige CYP3A5 ELISA Kits), NR1I3 gene polymorphisms.
This gene encodes a member of the nuclear receptor superfamily, and is a key regulator of xenobiotic and endobiotic metabolism. The protein binds to DNA as a monomer or a heterodimer with the retinoid X receptor and regulates the transcription of target genes involved in drug metabolism and bilirubin clearance, such as cytochrome P450 family members. Unlike most nuclear receptors, this transcriptional regulator is constitutively active in the absence of ligand but is regulated by both agonists and inverse agonists. Ligand binding results in translocation of this protein to the nucleus, where it activates or represses target gene transcription. These ligands include bilirubin, a variety of foreign compounds, steroid hormones, and prescription drugs. Multiple transcript variants encoding different isoforms have been found for this gene.
constitutive androstane receptor
, constitutively transactivates RAREs
, nuclear receptor subfamily 1 group I member 3
, orphan nuclear receptor MB67
, constitutive androstane receptor NR1I3
, nuclear receptor constitutive active receptor
, strain Fischer nuclear receptor (CAR)
, constitutive activator of retinoid response
, constitutive active receptor
, constitutive active response
, constitutive androstane nuclear receptor variant 2
, constitutive androstane nuclear receptor variant 3
, constitutive androstane nuclear receptor variant 4
, constitutive androstane nuclear receptor variant 5
, orphan nuclear hormone receptor
, xenobiotic receptor