Xenobiotic CAR activators induce Dlk1-Dio3 locus non-coding RNA expression in mouse liver [PDF]
Predicting the impact of human exposure to chemicals such as pharmaceuticals and agrochemicals requires the development of reliable and predictive biomarkers suitable for the detection of early events potentially leading to adverse outcomes.
Dubost, Valérie +20 more
core +2 more sources
A brief history of the discovery of PXR and CAR as xenobiotic receptors
The nuclear receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR) were cloned and/or established as xenobiotic receptors in 1998.
Jiong Yan, Wen Xie
doaj +1 more source
A Targeted in Vivo SILAC Approach for Quantification of Drug Metabolism Enzymes:Regulation by the Constitutive Androstane Receptor [PDF]
The modulation of drug metabolism enzyme (DME) expression by therapeutic agents is a central mechanism of drug-drug interaction and should be assessed as early as possible in preclinical drug development.
Henderson, Colin J. +5 more
core +5 more sources
Activation of Constitutive Androstane Receptor Prevents Cholesterol Gallstone Formation [PDF]
Cholesterol gallstone disease (CGD) is one of the most common gastrointestinal diseases. Lithogenic hepatic bile secretion precedes the formation of cholesterol gallstones. Constitutive androstane receptor (CAR), a member of nuclear family, plays an important role in cholesterol and bile acid metabolism. To examine whether activation of CAR can prevent
Shihai, Cheng +13 more
openaire +2 more sources
Triclocarban (3,4,4'-trichlorocarbanilide, TCC) is used as a broad-based antimicrobial agent that is commonly added to personal hygiene products. Because of its extensive use in the health care industry and resistance to degradation in sewage treatment ...
Mei-Fei Yueh +4 more
doaj +1 more source
Cross-species comparison of CAR-mediated procarcinogenic key events in a 3D liver microtissue model [PDF]
Characterisation of the mode of action (MOA) of constitutive androstane receptor (CAR)-mediated rodent liver tumours involves measurement 5 key events including activation of the CAR receptor, altered gene expression, hepatocellular proliferation, clonal
Ball, Graeme +8 more
core +2 more sources
Stereoisomerization of human constitutive androstane receptor agonist CITCO
Abstract CITCO (6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde-O-(3,4-dichlorobenzyl) oxime) is a widely used agonist of the human constitutive androstane receptor (hCAR), a key hepatic xenobiotic sensor protein with emerging therapeutic indications. To address the insufficient stability of CITCO, which limits its therapeutic potential,
Benjamin Diethelm-Varela +8 more
openaire +2 more sources
Phenobarbital-mediated tumor promotion in transgenic mice with humanized CAR and PXR [PDF]
The nuclear receptors CAR (constitutive androstane receptor) and possibly PXR (pregnane X receptor) mediate the hepatic effects of phenobarbital (PB) and similar-acting compounds.
Braeuning, Albert +5 more
core +2 more sources
The Concise Guide to PHARMACOLOGY 2015/16:Nuclear hormone receptors [PDF]
The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org),
Aldrich, R +151 more
core +4 more sources
Pharmacokinetic Herb-Drug Interactions: Insight into Mechanisms and Consequences [PDF]
Herbal medicines are currently in high demand, and their popularity is steadily increasing. Because of their perceived effectiveness, fewer side effects and relatively low cost, they are being used for the management of numerous medical conditions ...
Horie, Toshiharu +3 more
core +1 more source

