Cholesterol biosynthetic and metabolic pathways contain several branching points towards physiologically active molecules, such as coenzyme Q, vitamin D, glucocorticoid and steroid hormones, oxysterols, or bile acids. Sophisticated regulatory mechanisms are involved in maintenance of the homeostasis of not only cholesterol but also other cholesterogenic molecules. In addition to endogenous cues, cholesterol homeostasis needs to accommodate also to exogenous cues that are imported into the body, such as chemicals and medications. Steroid and nuclear receptors together with sterol regulatory element-binding protein (SREBP) mediate the fine tuning of biosynthetic and metabolic routes as well as transports of cholesterol and its derivatives. Similarly, drug/xenobiotic metabolism is the subject to the feedback regulation of cytochrome P450 enzymes and transporters. The regulatory mechanisms that maintain the homeostasis of cholesterogenic molecules and are involved in drug metabolism share similarities. Cholesterol and cholesterogenic compounds (bile acids, glucocorticoids, vitamin D, etc.) regulate the xenosensor signaling in drug-mediated induction of the major drug-metabolizing cytochrome P450 enzymes. The key cellular receptors,...Continue Reading
Paradoxical transcriptional activation of rat liver cytochrome P-450 3A1 by dexamethasone and the antiglucocorticoid pregnenolone 16 alpha-carbonitrile: analysis by transient transfection into primary monolayer cultures of adult rat hepatocytes
Glucocorticoid regulation of the rat cytochrome P450c (P450IA1) gene: receptor binding within intron I
Evidence that physiologic levels of circulating estrogens and neonatal sex-imprinting modify postpubertal hepatic microsomal 3-hydroxy-3-methylglutaryl coenzyme A reductase activity
Localization of a phenobarbital-responsive element (PBRE) in the 5'-flanking region of the rat CYP2B2 gene
Isolation of proteins that interact specifically with the retinoid X receptor: two novel orphan receptors
Modulation of xenobiotic-inducible cytochrome P450 gene expression by dexamethasone in primary rat hepatocytes
A new orphan member of the nuclear hormone receptor superfamily that interacts with a subset of retinoic acid response elements
The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions
Differential apoptotic response of human melanoma cells to 1 alpha,25-dihydroxyvitamin D3 and its analogues
Role of canonical glucocorticoid responsive elements in modulating expression of genes regulated by the arylhydrocarbon receptor
A reporter gene assay to assess the molecular mechanisms of xenobiotic-dependent induction of the human CYP3A4 gene in vitro
Evidence for the presence of a functional pregnane X receptor response element in the CYP3A7 promoter gene
Human white/murine ABC8 mRNA levels are highly induced in lipid-loaded macrophages. A transcriptional role for specific oxysterols
Insulin is the essential factor maintaining the constitutive expression of hepatic sterol 14-demethylase P450 (CYP51)
Molecular cloning and functional characterization of a novel nuclear receptor similar to an embryonic benzoate receptor BXR
A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis
Regulation of cholesterol 7alpha-hydroxylase gene (CYP7A1) transcription by the liver orphan receptor (LXRalpha)
The peptide near the C terminus regulates receptor CAR nuclear translocation induced by xenochemicals in mouse liver
The orphan nuclear receptor LRH-1 potentiates the sterol-mediated induction of the human CETP gene by liver X receptor
The phenobarbital response enhancer module in the human bilirubin UDP-glucuronosyltransferase UGT1A1 gene and regulation by the nuclear receptor CAR
Human hepatocyte culture systems for the in vitro evaluation of cytochrome P450 expression and regulation
Transcriptional regulation of CYP2C9 gene. Role of glucocorticoid receptor and constitutive androstane receptor
Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor
Differential effects of sterol regulatory binding proteins 1 and 2 on sterol 12 alpha-hydroxylase. SREBP-2 suppresses the sterol 12 alpha-hydroxylase promoter
Diverse roles of the nuclear orphan receptor CAR in regulating hepatic genes in response to phenobarbital
Regulation of ATP-binding cassette sterol transporters ABCG5 and ABCG8 by the liver X receptors alpha and beta
Induction of rat organic anion transporting polypeptide 2 by pregnenolone-16alpha-carbonitrile is via interaction with pregnane X receptor
Expression of CYP3A4, CYP2B6, and CYP2C9 is regulated by the vitamin D receptor pathway in primary human hepatocytes
Cholesterol and bile acids regulate xenosensor signaling in drug-mediated induction of cytochromes P450.
Bile acids enhance low density lipoprotein receptor gene expression via a MAPK cascade-mediated stabilization of mRNA.
Squalestatin 1-inducible expression of rat CYP2B: evidence that an endogenous isoprenoid is an activator of the constitutive androstane receptor
Transcriptional analysis of the orphan nuclear receptor constitutive androstane receptor (NR1I3) gene promoter: identification of a distal glucocorticoid response element
The expression of CYP2B6, CYP2C9 and CYP3A4 genes: a tangle of networks of nuclear and steroid receptors
Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes.
Control of steroid, heme, and carcinogen metabolism by nuclear pregnane X receptor and constitutive androstane receptor
Genetic profiling defines the xenobiotic gene network controlled by the nuclear receptor pregnane X receptor
The normal liver harbors the vitamin D nuclear receptor in nonparenchymal and biliary epithelial cells
Insig-dependent ubiquitination and degradation of mammalian 3-hydroxy-3-methylglutaryl-CoA reductase stimulated by sterols and geranylgeraniol.
Sterol-responsive element-binding protein (SREBP) 2 down-regulates ATP-binding cassette transporter A1 in vascular endothelial cells: a novel role of SREBP in regulating cholesterol metabolism
Post-transcriptional regulation of low density lipoprotein receptor protein by proprotein convertase subtilisin/kexin type 9a in mouse liver.
AMP-activated protein kinase mediates phenobarbital induction of CYP2B gene expression in hepatocytes and a newly derived human hepatoma cell line.
The effect of synthetic glucocorticoid, dexamethasone on CYP1A1 inducibility in adult rat and human hepatocytes
The human ABCG1 gene: identification of LXR response elements that modulate expression in macrophages and liver.
Insig-mediated degradation of HMG CoA reductase stimulated by lanosterol, an intermediate in the synthesis of cholesterol
Schoenheimer effect explained--feedback regulation of cholesterol synthesis in mice mediated by Insig proteins
Liver X receptor activation controls intracellular cholesterol trafficking and esterification in human macrophages
Identification and characterization of two alternatively spliced transcript variants of human liver X receptor alpha.
Regulation of 3-hydroxy-3-methylglutaryl coenzyme A reductase promoter by nuclear receptors liver receptor homologue-1 and small heterodimer partner: a mechanism for differential regulation of cholesterol synthesis and uptake
Involvement of Akt in ER-to-Golgi transport of SCAP/SREBP: a link between a key cell proliferative pathway and membrane synthesis
Isolation and properties of the CYP2D25 promoter: transcriptional regulation by vitamin D3 metabolites
Evolution and function of the NR1I nuclear hormone receptor subfamily (VDR, PXR, and CAR) with respect to metabolism of xenobiotics and endogenous compounds
Stimulation of AMP-activated protein kinase is essential for the induction of drug metabolizing enzymes by phenobarbital in human and mouse liver
In the regulation of cytochrome P450 genes, phenobarbital targets LKB1 for necessary activation of AMP-activated protein kinase
Sterol-regulated transport of SREBPs from endoplasmic reticulum to Golgi: oxysterols block transport by binding to Insig
Phenobarbital suppresses vitamin D3 25-hydroxylase expression: a potential new mechanism for drug-induced osteomalacia
Bile acids and lipoprotein metabolism: effects of cholestyramine and chenodeoxycholic acid on human hepatic mRNA expression
Glucocorticoid-enhanced expression of dioxin target genes through regulation of the rat aryl hydrocarbon receptor
Microtubules-interfering agents restrict aryl hydrocarbon receptor-mediated CYP1A2 induction in primary cultures of human hepatocytes via c-jun-N-terminal kinase and glucocorticoid receptor
Cholesterol supply and SREBPs modulate transcription of the Niemann-Pick C-1 gene in steroidogenic tissues.
Sterol regulators of cholesterol homeostasis and beyond: the oxysterol hypothesis revisited and revised
Dexamethasone controls aryl hydrocarbon receptor (AhR)-mediated CYP1A1 and CYP1A2 expression and activity in primary cultures of human hepatocytes
Intestinal cell-specific vitamin D receptor (VDR)-mediated transcriptional regulation of CYP3A4 gene
Tumor necrosis factor-alpha and lymphotoxin-alpha increase macrophage ABCA1 by gene expression and protein stabilization via different receptors
The effect of anti epileptic drug therapy on serum 25-hydroxyvitamin D and parameters of calcium and bone metabolism--a longitudinal study
The bladder tumor suppressor protein TERE1 (UBIAD1) modulates cell cholesterol: implications for tumor progression
Effects of intravascular laser irradiation of blood in mitochondria dysfunction and oxidative stress in adults with chronic spinal cord injury
In-vivo quantitative proteomics reveals a key contribution of post-transcriptional mechanisms to the circadian regulation of liver metabolism
Longitudinal trajectories of cholesterol from midlife through late life according to apolipoprotein E allele status
The evolution of our understanding of endo-xenobiotic crosstalk and cytochrome P450 regulation and the therapeutic implications
Defects in cholesterol synthesis genes in mouse and in humans: lessons for drug development and safer treatments
MicroRNAs from biology to future pharmacotherapy: regulation of cytochrome P450s and nuclear receptors
Revisiting Human Cholesterol Synthesis and Absorption: The Reciprocity Paradigm and its Key Regulators
MicroRNAs as regulators of drug transporters, drug-metabolizing enzymes, and tight junctions: implication for intestinal barrier function
Modulation of cytochrome P450 enzymes in response to continuous or intermittent high-fat diet in pigs
The effects of antiepileptic inducers in neuropsychopharmacology, a neglected issue. Part II: Pharmacological issues and further understanding
Aflatoxins upregulate CYP3A4 mRNA expression in a process that involves the PXR transcription factor
In vitro effects of aldehydes present in tobacco smoke on gene expression in human lung alveolar epithelial cells
Quantification of cholesterol solubilized in bile salt micellar aqueous solutions using (13)C nuclear magnetic resonance
Birth Cohort, Age, and Sex Strongly Modulate Effects of Lipid Risk Alleles Identified in Genome-Wide Association Studies
Farnesyltransferase Inhibition Exacerbates Eosinophilic Inflammation and Airway Hyperreactivity in Mice with Experimental Asthma: The Complex Roles of Ras GTPase and Farnesylpyrophosphate in Type 2 Allergic Inflammation
Effects of cross-fostering and developmental exposure to mixtures of environmental contaminants on hepatic gene expression in prepubertal 21 days old and adult male Sprague-Dawley rats
Liver and the defects of cholesterol and bile acids biosynthesis: Rare disorders many diagnostic pitfalls
Investigation of the interactions between methadone and elvitegravir-cobicistat in subjects receiving chronic methadone maintenance
Cytochrome P450 genetic polymorphism in neonatal drug metabolism: role and practical consequences towards a new drug culture in neonatology
The TERE1 protein interacts with mitochondrial TBL2: regulation of trans-membrane potential, ROS/RNS and SXR target genes
Genetically regulated expression underlies cellular sensitivity to chemotherapy in diverse populations.
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