Results 31 to 40 of about 69,599 (292)

Constitutive androstane receptor, liver pathophysiology and chemical contaminants: current evidence and perspectives [PDF]

Frontiers in Endocrinology
IntroductionThe Constitutive Androstane Receptor (CAR) (NR1I3), a pivotal member of the xenosensor family, plays a key role in the hepatic detoxification of xenobiotic and endobiotic chemicals through the induction of the expression of drug-metabolizing ...
Francesca De Battistis, Aleksandra Buha Djordjevic, Luciano Saso, Alberto Mantovani, Alberto Mantovani   +4 more
doaj   +2 more sources

Constitutive androstane receptor and pregnane X receptor genotype influence efavirenz plasma concentration and CYP2B6 enzyme activity [PDF]

Scientific Reports, 2022
Efavirenz is metabolized by CYP2B6, an inducible enzyme whose expression is regulated by the constitutive androstane receptor and pregnane X receptor nuclear receptors. CAR and PXR are encoded by genetically polymorphic NR1I2 and NR1I3, respectively.
Zelalem Petros, Abiy Habtewold, Eyasu Makonnen, Eleni Aklillu   +3 more
doaj   +2 more sources

Characterization of DNA Complexes Formed by the Nuclear Receptor Constitutive Androstane Receptor [PDF]

Journal of Biological Chemistry, 2003
The nuclear receptor constitutive androstane receptor (CAR) acts as a xenobiotic sensor and regulates the expression of enzymes, such as several cytochromes P450s and the UDP-glucuronosyltransferase (UGT) type 1A1. CAR binds as a heterodimer with the retinoid X receptor (RXR) to specific DNA sites, called response elements (REs).
Manuel Macias Gonzalez, Christian Frank, Carita Oinonen, Carsten Carlberg, Thomas W. Dunlop   +4 more
openaire   +5 more sources

Polycyclic Aromatic Hydrocarbons Activate the Aryl Hydrocarbon Receptor and the Constitutive Androstane Receptor to Regulate Xenobiotic Metabolism in Human Liver Cells. [PDF]

Int J Mol Sci, 2020
Polycyclic aromatic hydrocarbons (PAHs) are environmental pollutants produced by incomplete combustion of organic matter. They induce their own metabolism by upregulating xenobiotic-metabolizing enzymes such as cytochrome P450 monooxygenase 1A1 (CYP1A1 ...
Goedtke L, Sprenger H, Hofmann U, Schmidt FF, Hammer HS, Zanger UM, Poetz O, Seidel A, Braeuning A, Hessel-Pras S.   +9 more
europepmc   +2 more sources

MicroRNA-122 down-regulation is involved in phenobarbital-mediated activation of the constitutive androstane receptor. [PDF]

PLoS ONE, 2012
Constitutive androstane receptor (CAR) is a nuclear receptor that regulates the transcription of target genes, including CYP2B and 3A. Phenobarbital activates CAR, at least in part, in an AMP-activated protein kinase (AMPK)-dependent manner. However, the
Ryota Shizu, Sawako Shindo, Takemi Yoshida, Satoshi Numazawa   +3 more
doaj   +3 more sources

Constitutive Androstane Receptor-Mediated Inhibition of Metformin on Phase II Metabolic Enzyme SULT2A1 [PDF]

International Journal of Endocrinology, 2021
Background. Metformin, as a first-line treatment for diabetes, interacts with many protein kinases and transcription factors which affect the expression of downstream target genes governing drug metabolism.
Xiaowen Hu, Mengsiyu Li, Chunxue Zhang, Shuguang Pang   +3 more
doaj   +2 more sources

Diazepam Promotes Translocation of Human Constitutive Androstane Receptor (CAR) via Direct Interaction with the Ligand-Binding Domain. [PDF]

Cells, 2020
The constitutive androstane receptor (CAR) is the essential regulator of genes involved both in xenobiotic and endobiotic metabolism. Diazepam has been shown as a potent stimulator of CAR nuclear translocation and is assumed as an indirect CAR activator ...
Skoda J, Dusek J, Drastik M, Stefela A, Dohnalova K, Chalupsky K, Smutny T, Micuda S, Gerbal-Chaloin S, Pavek P.   +9 more
europepmc   +2 more sources

Human constitutive androstane receptor represses liver cancer development and hepatoma cell proliferation by inhibiting erythropoietin signaling. [PDF]

J Biol Chem, 2022
Li Z, Kwon SM, Li D, Li L, Peng X, Zhang J, Sueyoshi T, Raufman JP, Negishi M, Wang XW, Wang H.   +10 more
europepmc   +2 more sources

Pharmacological activation of constitutive androstane receptor induces female-specific modulation of hepatic metabolism [PDF]

JHEP Reports
Background & Aims: The constitutive androstane receptor (CAR) is a nuclear receptor that binds diverse xenobiotics and whose activation leads to the modulation of the expression of target genes involved in xenobiotic detoxification and energy ...
Marine Huillet, Frédéric Lasserre, Marie-Pierre Gratacap, Beatrice Engelmann, Justine Bruse, Arnaud Polizzi, Tiffany Fougeray, Céline Marie Pauline Martin, Clémence Rives, Anne Fougerat, Claire Naylies, Yannick Lippi, Géraldine Garcia, Elodie Rousseau-Bacquie, Cécile Canlet, Laurent Debrauwer, Ulrike Rolle-Kampczyk, Martin von Bergen, Bernard Payrastre, Elisa Boutet-Robinet, Laurence Gamet-Payrastre, Hervé Guillou, Nicolas Loiseau, Sandrine Ellero-Simatos   +23 more
doaj   +2 more sources

Helix 11 Dynamics Is Critical for Constitutive Androstane Receptor Activity [PDF]

Structure, 2011
SummaryThe constitutive androstane receptor (CAR) transactivation can occur in the absence of exogenous ligand and this activity is enhanced by agonists TCPOBOP and meclizine.
Busby, Scott A., Fernandez, Elias J., Griffin, Patrick R., Vincent, Jeremy, Wisecarver, Sarah, Wright, Edward   +5 more
core   +5 more sources