Pharmacogenetics of the Constitutive Androstane Receptor
Pharmacogenomics, 2007The constitutive androstane receptor (CAR), a member of the NR1I group of nuclear hormone receptors, has been implicated in regulating the expression of genes that are critical in xenobiotic and endobiotic metabolism, uptake and elimination as well as genes involved in various other physiological processes. Hence, functional variation in CAR associated
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Role of the constitutive androstane receptor (CAR) in human liver cancer
Biochimica Et Biophysica Acta: Reviews on Cancer, 2021The constitutive androstane receptor (CAR) is a member of the nuclear receptor superfamily (subfamily 1, group I, member 3, also known as NR1I3) that is almost exclusively expressed in the liver. CAR interacts with key signalling pathways such as those involved in drug, energy and bilirubin metabolism.
Liang Qiao, Jacob George
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Constitutive androstane receptor (CAR) is a xenosensor and target for therapy
Biochemistry (Moscow), 2011Constitutive androstane receptor (CAR, NR1I3), which is under consideration in this review, is a member of the superfamily of nuclear receptors. However, certain features distinguish CAR from the variety of nuclear receptors. First, this receptor has structural features that allow it to display constitutive activity in the absence of a ligand and to ...
E M, Kachaylo +3 more
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Isolation and characterization of Schistosoma mansoni constitutive androstane receptor
Molecular and Biochemical Parasitology, 2006Full length cDNA clones encoding a Schistosoma mansoni homologue of vertebrate CAR/PXR/VDR group nuclear receptor, termed SmCAR were isolated from screening a S. mansoni adult worm cDNA library. SmCAR is a 702 amino acid protein which retains a typical domain organization of nuclear receptor superfamily members.
Rong, Hu +3 more
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Transcriptional Regulation of the Human CYP3A4Gene by the Constitutive Androstane Receptor
Molecular Pharmacology, 2002Cytochrome P450 3A4 (CYP3A4), the predominant P450 expressed in adult human liver, is both constitutively expressed and transcriptionally activated by a variety of structurally diverse xenochemicals. In this study, we examined the role of the constitutive androstane receptor (CAR), a member of the steroid/retinoid/thyroid hormone receptor superfamily ...
Bryan, Goodwin +4 more
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Constitutive androstane/active receptor is a target of retinoic acid receptor in humans
Biochemical Pharmacology, 2010Nuclear receptor constitutive androstane/active receptor (CAR) is well known as a transcription factor regulating many genes that encode drug-metabolizing enzymes and factors modulating hepatic gluconeogenesis. However, there have been few studies on regulation of the CAR gene itself. In this study, we examined the involvement of retinoic acid receptor
Kosuke, Saito +4 more
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Constitutive androstane receptor activation evokes the expression of glycolytic genes
Biochemical and Biophysical Research Communications, 2016It is well-known that constitutive androstane receptor (CAR) activation by 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene (TCPOBOP) increases the liver-to-body weight ratio. CAR-mediated liver growth is correlated with increased expression of the pleiotropic transcription factor cMyc, which stimulates cell cycle regulatory genes and drives proliferating ...
Andrei A. Yarushkin +5 more
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Constitutive Androstane Receptor Expression in the Rat Cervix During Gestation
Journal of the Society for Gynecologic Investigation, 2000To investigate expression of the constitutive androstane receptor (CAR) in the pregnant rat cervix.Rat uterine tissue was obtained on gestational days 12, 16, 20, 21, and 22 (the day of parturition), and postpartum day 1. In addition, liver, lung, kidney, heart, and skeletal muscle tissue were obtained.
D F, Rychlik, E, Bieber, M, Phillippe
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The Constitutive Active/Androstane Receptor Regulates Phenytoin Induction of Cyp2c29
Molecular Pharmacology, 2004Many cytochrome P450 isoforms are known to be drug-inducible. The anticonvulsant phenytoin has been reported to be an inducer of human CYP2B6, CYP3A4, and murine CYP2C29. However, the molecular mechanism mediating phenytoin induction remains unclear.
Jonathan P, Jackson +4 more
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Molecular Determinants of Steroid Inhibition for the Mouse Constitutive Androstane Receptor
Journal of Medicinal Chemistry, 2003The constitutive androstane receptor (CAR) regulates drug and steroid metabolism through binding to cytochrome P450 2B, 2C, and 3A gene enhancers. Uniquely among nuclear receptors, mouse CAR (mCAR) can be suppressed by androstenol and activated by structurally diverse drugs, pesticides, and environmental pollutants.
Johanna, Jyrkkärinne +5 more
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