Stilbene compound trans-3,4,5,4´-tetramethoxystilbene, a potential anticancer drug, regulates constitutive androstane receptor (Car) target genes, but does not possess proliferative activity in mouse liver.
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DOI: 10.1016/j.toxlet.2019.05.024
Abstract: The constitutive androstane receptor(CAR) activation is connected with mitogenic effects leading to liver hyperplasia and tumorigenesis in rodents. CAR activators, including phenobarbital, are considered rodent non-genotoxic carcinogens. Recently, trans-3,4,5,4´-tetramethoxystilbene(TMS), a potential anticancer drug (DMU-212), have… read more here.
Keywords: target genes; constitutive androstane; car target; car ... See more keywords
Regulatory Mechanics of Constitutive Androstane Receptors: Basal and Ligand-Directed Actions
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DOI: 10.1021/acs.jcim.9b00695
Abstract: Constitutive androstane receptor (CAR) is a nuclear hormone receptor that primarily functions in sensing and metabolizing xenobiotics. The basal activity of this receptor is relatively high, and CAR is deemed active in the absence of… read more here.
Keywords: constitutive androstane; car; ligand; activity ... See more keywords
Potent and Selective Human Constitutive Androstane Receptor Activator DL5055 Facilitates Cyclophosphamide-Based Chemotherapies.
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DOI: 10.1021/acs.jmedchem.4c02064
Abstract: Enhancement of the metabolic conversion of cyclophosphamide (CPA) increases its therapeutic effects. Activation of the human constitutive androstane receptor (hCAR) induces CYP2B6, a key enzyme responsible for CPA bioactivation. Based on our previous hCAR activator… read more here.
Keywords: constitutive androstane; androstane receptor; human constitutive; hcar ... See more keywords
Porcine interleukin-6 enhances the expression of CYP2C33 through a constitutive androstane receptor/retinoid X receptor-mediated pathway
Sign Up to like & getrecommendations! Published in 2019 at "Xenobiotica"
DOI: 10.1080/00498254.2018.1438686
Abstract: Abstract Cytochrome P450, which is expressed in humans and other animals, is a superfamily of drug-metabolizing enzymes that play important roles in the metabolism of endogenous and xenobiotic substrates via oxidation, peroxidation and reduction. Of… read more here.
Keywords: cyp2c33 expression; constitutive androstane; expression cyp2c33; expression ... See more keywords
Chemical Activation of the Constitutive Androstane Receptor Leads to Activation of Oxidant-Induced Nrf2
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DOI: 10.1093/toxsci/kfy231
Abstract: Exposure to environmentally relevant chemicals that activate the xenobiotic receptors aryl hydrocarbon receptor (AhR), constitutive androstane receptor (CAR), and peroxisome proliferator-activated receptor alpha (PPARα) in rodent test systems often leads to increases in oxidative stress… read more here.
Keywords: activation oxidant; androstane receptor; constitutive androstane; activation ... See more keywords
Constitutive androstane receptor regulates the intestinal mucosal response to injury
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DOI: 10.1111/bph.13787
Abstract: The pathogenesis of the inflammatory bowel diseases (IBD), comprising Crohn's disease (CD) and ulcerative colitis (UC), involves aberrant interactions between a genetically susceptible individual, their microbiota and environmental factors. Alterations in xenobiotic receptor expression and… read more here.
Keywords: receptor; androstane receptor; intestinal mucosal; constitutive androstane ... See more keywords
Constitutive androstane receptor (CAR) mediates pyrene‐induced inflammatory responses in mouse liver, with increased serum amyloid A proteins and Th17 cells
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DOI: 10.1111/bph.15934
Abstract: The constitutive androstane receptor (CAR), a known xenobiotic sensor, plays an important role in drug metabolism by regulating numerous genes. The polycyclic aromatic hydrocarbon pyrene, an environmental pollutant, is a CAR activator and induces mouse… read more here.
Keywords: car; receptor car; constitutive androstane; androstane receptor ... See more keywords
Mouse Hepatomas with Ha-ras and B-raf Mutations Differ in Mitogen-Activated Protein Kinase Signaling and Response to Constitutive Androstane Receptor Activation
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DOI: 10.1124/dmd.118.083014
Abstract: Nuclear receptors mediate the hepatic induction of drug-metabolizing enzymes by xenobiotics. Not much is known about enzyme induction in liver tumors. Here, we treated tumor-bearing mice with phenobarbital, an activator of the constitutive androstane receptor… read more here.
Keywords: androstane receptor; constitutive androstane; ras raf; activation ... See more keywords
Clinical Relevance of the Constitutive Androstane Receptor
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DOI: 10.1124/dmd.121.000483
Abstract: Constitutive androstane receptor (CAR) (NR1I3), a xenobiotic receptor, has long been considered a master mediator of drug disposition and detoxification. Accumulating evidence indicates that CAR also participates in various physiologic and pathophysiological pathways regulating the… read more here.
Keywords: clinical relevance; car; constitutive androstane; androstane receptor ... See more keywords
Deletion of Constitutive Androstane Receptor Led to Intestinal Alterations and Increased Imidacloprid in Murine Liver
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DOI: 10.1210/jendso/bvac145
Abstract: Abstract Imidacloprid (IMI) is the most frequently detected neonicotinoid pesticide in the environment. Despite typically low toxicity in vertebrates, IMI exposure is associated with liver and gastrointestinal toxicity. The mechanism underlying IMI toxicity in mammals… read more here.
Keywords: car; intestinal alterations; constitutive androstane; androstane receptor ... See more keywords
Timosaponin AⅢ induces drug-metabolizing enzymes by activating constitutive androstane receptor (CAR) via dephosphorylation of the EGFR signaling pathway
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DOI: 10.7555/jbr.38.20240055
Abstract: The current study aimed to assess the effect of timosaponin AⅢ (T-AⅢ) on drug-metabolizing enzymes during anticancer therapy. The in vivo experiments were conducted on nude and ICR mice. Following a 24-day administration of T-AⅢ,… read more here.
Keywords: egfr; car; constitutive androstane; expression ... See more keywords