Pregnane X receptor and constitutive androstane receptor modulate differently CYP3A-mediated metabolism in earlyand late-stage cholestasis [PDF]
AIM: To ascertain whether cholestasis affects the expression of two CYP3A isoforms (CYP3A1 and CYP3A2) and of pregnane X receptor (PXR) and constitutive androstane receptor (CAR).
Albertoni, Laura +9 more
core +1 more source
Differential effects of clinically used derivatives and metabolites of artemisinin in the activation of constitutive androstane receptor isoforms [PDF]
BACKGROUND AND PURPOSE Widespread resistance to antimalarial drugs requires combination therapies with increasing risk of pharmacokinetic drugdrug interactions.
Alexander +51 more
core +1 more source
Constitutive androstane receptor 1 is constitutively bound to chromatin and ‘primed’ for transactivation in hepatocytes [PDF]
The constitutive androstane receptor (CAR) is a xenobiotic sensor expressed in hepatocytes that activates genes involved in drug metabolism, lipid homeostasis, and cell proliferation.
Acosta-Jimenez, Lourdes +8 more
core +2 more sources
The Environmental Estrogen, Nonylphenol, Activates the Constitutive Androstane Receptor [PDF]
Nonylphenol (NP) and its parent compounds, the nonylphenol ethoxylates are some of the most prevalent chemicals found in U.S. waterways. NP is also resistant to biodegradation and is a known environmental estrogen, which makes NP a chemical of concern.
Juan P, Hernandez +5 more
openaire +2 more sources
Inhaled glucocorticoids are the first-line treatment for patients with persistent asthma. However, approximately thirty percent of patients exhibit glucocorticoid insensitivity, which may involve excess metabolic clearance of the glucocorticoids by ...
Jessica K Roberts +5 more
doaj +1 more source
Functional constraints on the constitutive androstane receptor inferred from human sequence variation and cross-species comparisons [PDF]
Members of the NR1I subfamily of nuclear receptors play a role in the transcriptional activation of genes involved in drug metabolism and transport. NR1I3, the constitutive androstane receptor (CAR), mediates the induction of several genes involved in ...
Di Rienzo Anna +3 more
core +2 more sources
Alternatively spliced isoforms of the human constitutive androstane receptor [PDF]
The nuclear receptor CAR (NR1I3) regulates transcription of genes encoding xenobiotic- and steroid-metabolizing enzymes. Regulatory processes that are mediated by CAR are modulated by a structurally diverse array of chemicals including common pharmaceutical and environmental agents.
Scott S, Auerbach +5 more
openaire +2 more sources
Inhaled glucocorticoids are the first-line treatment for patients with persistent asthma. However, approximately thirty percent of patients exhibit glucocorticoid insensitivity, which may involve excess metabolic clearance of the glucocorticoids by ...
Jessica K Roberts +5 more
doaj +1 more source
Regulation of cytochrome P450 mRNA expression in primary porcine hepatocytes by selected secondary plant metabolites from chicory (Cichorium intybus L.) [PDF]
Chicory (Cichorium intybus) has been shown to induce enzymes of pharmacokinetic relevance (cytochrome P450; CYP). The aim of this study was to investigate the effects of selected secondary plant metabolites with a global extract of chicory root, on the ...
Ekstrand, Bo +2 more
core +1 more source
Dehydroepiandrosterone Induces Human CYP2B6 through the Constitutive Androstane Receptor [PDF]
Dehydroepiandrosterone (DHEA), the major precursor of androgens and estrogens, has several beneficial effects on the immune system, on memory function, and in modulating the effects of diabetes, obesity, and chemical carcinogenesis. Treatment of rats with DHEA influences expression of cytochrome P450 (P450) genes, including peroxisome proliferator ...
Krisztina, Kohalmy +9 more
openaire +2 more sources

