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 +8 more sources
A novel panel of mouse models to evaluate the role of human pregnane X receptor and constitutive androstane receptor in drug response [PDF]
The pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are closely related orphan nuclear hormone receptors that play a critical role as xenobiotic sensors in mammals.
Anja Rode+19 more
core +5 more sources
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 +3 more sources
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 +4 more sources
Canvass: a crowd-sourced, natural-product screening library for exploring biological space [PDF]
NCATS thanks Dingyin Tao for assistance with compound characterization. This research was supported by the Intramural Research Program of the National Center for Advancing Translational Sciences, National Institutes of Health (NIH). R.B.A.
Andrade, Rodrigo B.+94 more
core +4 more sources
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
1I. Vitamin D receptor-like receptors in GtoPdb v.2023.1 [PDF]
Vitamin D (VDR), Pregnane X (PXR) and Constitutive Androstane (CAR) receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Nuclear Hormone Receptors [50, 1]) are members of the NR1I family of nuclear receptors, which form heterodimers with ...
Christakos, Sylvia
core +2 more sources
Unsaturated fatty acid regulation of cytochrome P450 expression via a CAR-dependent pathway. [PDF]
The liver is responsible for key metabolic functions, including control of normal homoeostasis in response to diet and xenobiotic metabolism/detoxification.
Finn, Robert+3 more
core +4 more sources
Importance of Ethnicity, CYP2B6 and ABCB1 Genotype for Efavirenz Pharmacokinetics and Treatment Outcomes: A Parallel-group Prospective Cohort Study in two sub-Saharan Africa Populations. [PDF]
We evaluated the importance of ethnicity and pharmacogenetic variations in determining efavirenz pharmacokinetics, auto-induction and immunological outcomes in two African populations. ART naïve HIV patients from Ethiopia (n = 285) and Tanzania (n = 209)
A Habtewold+48 more
core +7 more sources
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