Search Results - "NEGISHI, Masahiko"
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Phenobarbital Meets Phosphorylation of Nuclear Receptors
Published in Drug metabolism and disposition (01-05-2017)“…Phenobarbital was the first therapeutic drug to be characterized for its induction of hepatic drug metabolism. Essentially at the same time, cytochrome P450,…”
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Phosphorylated nuclear receptors as drug-targets
Published in Drug metabolism and pharmacokinetics (01-01-2019)Get full text
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Nuclear receptor phosphorylation in xenobiotic signal transduction
Published in The Journal of biological chemistry (06-11-2020)“…Nuclear pregnane X receptor (PXR, NR1I2) and constitutive active/androstane receptor (CAR, NR1I3) are nuclear receptors characterized in 1998 by their…”
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Statin-activated nuclear receptor PXR promotes SGK2 dephosphorylation by scaffolding PP2C to induce hepatic gluconeogenesis
Published in Scientific reports (22-09-2015)“…Statin therapy is known to increase blood glucose levels in humans. Statins utilize pregnane X receptor (PXR) and serum/glucocorticoid regulated kinase 2…”
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Phenobarbital indirectly activates the constitutive active androstane receptor (CAR) by inhibition of epidermal growth factor receptor signaling
Published in Science signaling (07-05-2013)“…Phenobarbital is a central nervous system depressant that also indirectly activates nuclear receptor constitutive active androstane receptor (CAR), which…”
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CAR and PXR: The xenobiotic-sensing receptors
Published in Steroids (01-03-2007)“…The xenobiotic receptors CAR and PXR constitute two important members of the NR1I nuclear receptor family. They function as sensors of toxic byproducts derived…”
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Regulation of gene expression by CAR: an update
Published in Archives of toxicology (01-07-2015)“…The constitutive androstane receptor (CAR), a member of the nuclear receptor superfamily, is a well-known xenosensor that regulates hepatic drug metabolism and…”
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Phosphorylation of nuclear receptors: Novelty and therapeutic implications
Published in Pharmacology & therapeutics (Oxford) (01-08-2023)“…Nuclear receptors (NR) collectively regulate several biological functions in various organs. While NRs can be characterized by activation of the transcription…”
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Glucose elicits serine/threonine kinase VRK1 to phosphorylate nuclear pregnane X receptor as a novel hepatic gluconeogenic signal
Published in Cellular signalling (01-12-2017)“…Low glucose stimulated phosphorylation of pregnane X receptor (PXR) at Ser350 in correlation with an increased gluconeogenesis in human hepatoma-derived HepG2…”
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Serum- and glucocorticoid-regulated kinase 2 determines drug-activated pregnane X receptor to induce gluconeogenesis in human liver cells
Published in The Journal of pharmacology and experimental therapeutics (01-01-2014)“…Drug activation of the human nuclear pregnane X receptor (PXR) induced gluconeogenic genes and increased glucose production. In this study, we have determined…”
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Ligand induced dissociation of the AR homodimer precedes AR monomer translocation to the nucleus
Published in Scientific reports (13-11-2019)“…The androgen receptor (AR) regulates male sexual development. We have now investigated AR homodimerization, hormone-dependent monomerization and nuclear…”
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Nuclear Pregnane X Receptor Cross-talk with FoxA2 to Mediate Drug-induced Regulation of Lipid Metabolism in Fasting Mouse Liver
Published in The Journal of biological chemistry (30-03-2007)“…Upon drug activation, the nuclear pregnane X receptor (PXR) regulates not only hepatic drug but also energy metabolism. Using Pxr–/– mice, we have now…”
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Nuclear Receptor CAR Suppresses GADD45B-p38 MAPK Signaling to Promote Phenobarbital-induced Proliferation in Mouse Liver
Published in Molecular cancer research (01-08-2018)“…Phenobarbital, a nongenotoxic hepatocarcinogen, induces hepatic proliferation and promotes development of hepatocellular carcinoma (HCC) in rodents. Nuclear…”
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Phosphorylated Nuclear Receptor CAR Forms a Homodimer To Repress Its Constitutive Activity for Ligand Activation
Published in Molecular and cellular biology (01-05-2017)“…The nuclear receptor CAR (NR1I3) regulates hepatic drug and energy metabolism as well as cell fate. Its activation can be a critical factor in drug-induced…”
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CAR requires Gadd45β to promote phenobarbital-induced mouse liver tumors in early stage
Published in Frontiers in oncology (07-09-2023)“…Phenobarbital (PB) is an archetypal substance used as a mouse hepatocellular carcinoma (HCC) promotor in established experimental protocols. Our previous…”
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Nuclear receptor CAR-ERα signaling regulates the estrogen sulfotransferase gene in the liver
Published in Scientific reports (19-03-2020)“…Estrogen sulfotransferase (SULT1E1) inactivates estrogen and regulates its metabolic homeostats. Whereas SULT1E1 is expressed low in the liver of adult mice,…”
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The Roles of Nuclear Receptors CAR and PXR in Hepatic Energy Metabolism
Published in DRUG METABOLISM AND PHARMACOKINETICS (01-01-2008)“…Nuclear receptors constitutive active/androstane receptor (CAR) and pregnane X receptor (PXR) were originally characterized as transcription factors regulating…”
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A phosphorylation-deficient mutant of retinoid X receptor α at Thr 167 alters fasting response and energy metabolism in mice
Published in Laboratory investigation (01-10-2019)“…Retinoid X receptor α (RXRα) has a conserved phosphorylation motif at threonine 162 (humans) and threonine 167 (mice) within the DNA-binding domain. Here we…”
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Coordinated regulation of nuclear receptor CAR by CCRP/DNAJC7, HSP70 and the ubiquitin-proteasome system
Published in PloS one (02-05-2014)“…The constitutive active/androstane receptor (CAR) plays an important role as a coordinate transcription factor in the regulation of various hepatic metabolic…”
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Serine 216 phosphorylation of estrogen receptor α in neutrophils: migration and infiltration into the mouse uterus
Published in PloS one (26-12-2013)“…Whereas estrogen receptors are present in immune cells, it is not known if they are phosphorylated to regulate immune cell functions. Here we determined the…”
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