Induction of Drug Metabolism: The Role of Nuclear Receptors

The nuclear receptor superfamily: The second decade

1995 • 6,929 citations

The RXR heterodimers and orphan receptors

1995 • 3,168 citations

P450 superfamily: update on new sequences, gene mapping, accession numbers and nomenclature

1996 • 2,895 citations

Transcriptional co-activator PGC-1α drives the formation of slow-twitch muscle fibres

2002 • 2,422 citations

Nuclear Receptors and Lipid Physiology: Opening the X-Files

2001 • 2,040 citations

Peroxisome Proliferator-Activated Receptor-γ Coactivator 1α (PGC-1α): Transcriptional Coactivator and Metabolic Regulator

2003 • 1,964 citations

Steroid hormone receptors: Many Actors in search of a plot

1995 • 1,854 citations

A Regulatory Cascade of the Nuclear Receptors FXR, SHP-1, and LRH-1 Represses Bile Acid Biosynthesis

2000 • 1,801 citations

Control of hepatic gluconeogenesis through the transcriptional coactivator PGC-1

2001 • 1,782 citations

The Liver: Biology and Pathobiology.

1983 • 1,628 citations

The Aryl Hydrocarbon Receptor Complex

1995 • 1,586 citations

Towards a molecular understanding of adaptive thermogenesis

2000 • 1,560 citations

P450 GENES: STRUCTURE, EVOLUTION, AND REGULATION

1987 • 1,559 citations

The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.

1998 • 1,535 citations

An Orphan Nuclear Receptor Activated by Pregnanes Defines a Novel Steroid Signaling Pathway

1998 • 1,497 citations

Molecular Basis for Feedback Regulation of Bile Acid Synthesis by Nuclear Receptors

2000 • 1,426 citations

Clinical importance of the cytochromes P450

2002 • 1,356 citations

The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity

2001 • 1,271 citations

INDUCTION OF CYTOCHROME P4501A1

1999 • 1,124 citations

INSECT P450 ENZYMES

1999 • 979 citations

Genetic contribution to variable human CYP3A-mediated metabolism

2002 • 953 citations

St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor

2000 • 929 citations

SXR, a novel steroid and xenobioticsensing nuclear receptor

1998 • 903 citations

Regulation of Multidrug Resistance-associated Protein 2 (ABCC2) by the Nuclear Receptors Pregnane X Receptor, Farnesoid X-activated Receptor, and Constitutive Androstane Receptor

2002 • 888 citations

The Nuclear Pregnane X Receptor: A Key Regulator of Xenobiotic Metabolism

2002 • 885 citations

Cytochrome P-4502E1: its physiological and pathological role

1997 • 881 citations

Cytochromes P450: a success story.

2000 • 863 citations

Identification of a human nuclear receptor defines a new signaling pathway for CYP 3 A induction

1998 • 852 citations

Nuclear Receptor Response Elements Mediate Induction of Intestinal MDR1 by Rifampin

2001 • 843 citations

The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux

2001 • 830 citations

A Single P450 Allele Associated with Insecticide Resistance in Drosophila

2002 • 829 citations

Orphan Nuclear Receptors Constitutive Androstane Receptor and Pregnane X Receptor Share Xenobiotic and Steroid Ligands

2000 • 805 citations

The Human Nuclear Xenobiotic Receptor PXR: Structural Determinants of Directed Promiscuity

2001 • 738 citations

An essential role for nuclear receptors SXR/PXR in detoxification of cholestatic bile acids

2001 • 736 citations

P450 Gene Induction by Structurally Diverse Xenochemicals: Central Role of Nuclear Receptors CAR, PXR, and PPAR

1999 • 736 citations

The Role of Orphan Nuclear Receptors in the Regulation of Cholesterol Homeostasis

2000 • 734 citations

The Nuclear Orphan Receptor CAR-Retinoid X Receptor Heterodimer Activates the Phenobarbital-Responsive Enhancer Module of the CYP2B Gene

1998 • 697 citations

The Repressed Nuclear Receptor CAR Responds to Phenobarbital in Activating the Human CYP2B6 Gene

1999 • 658 citations

Humanized xenobiotic response in mice expressing nuclear receptor SXR

2000 • 655 citations

The Orphan Human Pregnane X Receptor Mediates the Transcriptional Activation ofCYP3A4by Rifampicin through a Distal Enhancer Module

1999 • 645 citations

Nuclear Pregnane X Receptor and Constitutive Androstane Receptor Regulate Overlapping but Distinct Sets of Genes Involved in Xenobiotic Detoxification

2002 • 642 citations

The nuclear receptor CAR mediates specific xenobiotic induction of drug metabolism

2000 • 641 citations

Evolution of Supergene Families Associated with Insecticide Resistance

2002 • 632 citations

Enzyme induction in the cytochrome P-450 system

1990 • 631 citations

Pharmacogenetics and adverse drug reactions

2000 • 605 citations

MOLECULAR MECHANISMS OF GENETIC POLYMORPHISMS OF DRUG METABOLISM

1997 • 540 citations

Phenobarbital-Responsive Nuclear Translocation of the Receptor CAR in Induction of the CYP2B Gene

1999 • 537 citations

An Orphan Nuclear Hormone Receptor That Lacks a DNA Binding Domain and Heterodimerizes with Other Receptors

1996 • 535 citations

Phenobarbital induction of cytochrome P-450 gene expression

1992 • 530 citations

Adaptive increases in drug-metabolizing enzymes induced by phenobarbital and other drugs.

1960 • 511 citations

Coregulator Codes of Transcriptional Regulation by Nuclear Receptors

2001 • 507 citations

Reciprocal activation of Xenobiotic response genes by nuclear receptors SXR/PXR and CAR

2000 • 503 citations

Mammalian hepatocyte differentiation requires the transcription factor HNF-4alpha.

2000 • 489 citations

A new orphan member of the nuclear hormone receptor superfamily that interacts with a subset of retinoic acid response elements.

1994 • 470 citations

Androstane metabolites bind to and deactivate the nuclear receptor CAR-β

1998 • 466 citations

Redundant Pathways for Negative Feedback Regulation of Bile Acid Production

2002 • 462 citations

Diverse Roles of the Nuclear Orphan Receptor CAR in Regulating Hepatic Genes in Response to Phenobarbital

2002 • 455 citations

Regulation of cytochrome P450 (CYP) genes by nuclear receptors

2000 • 447 citations

Mammalian hepatocyte differentiation requires the transcription factor HNF-4α

2000 • 440 citations

The orphan nuclear receptor HNF4α determines PXR- and CAR-mediated xenobiotic induction of CYP3A4

2003 • 424 citations

The Xenobiotic Compound 1,4-Bis[2-(3,5-Dichloropyridyloxy)]Benzene Is an Agonist Ligand for the Nuclear Receptor CAR

2000 • 407 citations

Identification of a Novel Human Constitutive Androstane Receptor (CAR) Agonist and Its Use in the Identification of CAR Target Genes

2003 • 399 citations

Interactions of Herbs with Cytochrome P450

2003 • 387 citations

Disrupted Bile Acid Homeostasis Reveals an Unexpected Interaction among Nuclear Hormone Receptors, Transporters, and Cytochrome P450

2001 • 381 citations

Induction of bilirubin clearance by the constitutive androstane receptor (CAR)

2003 • 379 citations

The Phenobarbital Response Enhancer Module in the Human Bilirubin Udp–Glucuronosyltransferase Ugt1a1 Gene and Regulation by the Nuclear Receptor Car

2001 • 368 citations

Dexamethasone Induces Pregnane X Receptor and Retinoid X Receptor-α Expression in Human Hepatocytes: Synergistic Increase of CYP3A4 Induction by Pregnane X Receptor Activators

2000 • 367 citations

Phenobarbital Response Elements of Cytochrome P450 Genes and Nuclear Receptors

2001 • 357 citations

Control of steroid, heme, and carcinogen metabolism by nuclear pregnane X receptor and constitutive androstane receptor

2003 • 355 citations

Regulation of the human CYP2B6 gene by the nuclear pregnane X receptor.

2001 • 355 citations

Expression of CYP3A4, CYP2B6, andCYP2C9 Is Regulated by the Vitamin D Receptor Pathway in Primary Human Hepatocytes

2002 • 350 citations

Loss of Nuclear Receptor SHP Impairs but Does Not Eliminate Negative Feedback Regulation of Bile Acid Synthesis

2002 • 346 citations

Xenobiotic-inducible Transcription of Cytochrome P450 Genes

1995 • 343 citations

Pregnane X Receptor (PXR), Constitutive Androstane Receptor (CAR), and Benzoate X Receptor (BXR) Define Three Pharmacologically Distinct Classes of Nuclear Receptors

2002 • 336 citations

The expression of CYP2B6, CYP2C9 and CYP3A4 genes: a tangle of networks of nuclear and steroid receptors

2003 • 331 citations

Sharp, an inducible cofactor that integrates nuclear receptor repression and activation

2001 • 330 citations

Regulation ofCYP3AGene Transcription by the Pregnane X Receptor

2002 • 325 citations

Nuclear receptor coregulators: multiple modes of modification

2002 • 323 citations

Transcriptional Control of Intestinal Cytochrome P-4503A by 1α,25-Dihydroxy Vitamin D₃

2001 • 321 citations

2.1 Å Crystal Structure of Human PXR in Complex with the St. John's Wort Compound Hyperforin^,

2003 • 316 citations

Modulation of Acetaminophen-Induced Hepatotoxicity by the Xenobiotic Receptor CAR

2002 • 309 citations

The Orphan Nuclear Receptor SHP Inhibits Hepatocyte Nuclear Factor 4 and Retinoid X Receptor Transactivation: Two Mechanisms for Repression

2000 • 303 citations

Orphan nuclear receptors—new ligands and new possibilities: Figure 1.

1998 • 301 citations

The cytochrome P450 4 (CYP4) family

1997 • 299 citations

Dual effect of dexamethasone on CYP3A4 gene expression in human hepatocytes

2001 • 295 citations

The human pregnane X receptor: genomic structure and identification and functional characterization of natural allelic variants

2001 • 285 citations

HNF4: A central regulator of hepatocyte differentiation and function

2003 • 281 citations

Overview of enzymes of drug metabolism

1996 • 270 citations

Regulation of a xenobiotic sulfonation cascade by nuclear pregnane X receptor (PXR)

2002 • 269 citations

Differential Transactivation by Two Isoforms of the Orphan Nuclear Hormone Receptor CAR

1997 • 268 citations

The Pregnane X Receptor: A Promiscuous Xenobiotic Receptor That Has Diverged during Evolution

2000 • 260 citations

Transcriptional Regulation of CYP2C9 Gene

2002 • 260 citations

Coordinate regulation of xenobiotic and bile acid homeostasis by pregnane X receptor.

2001 • 255 citations

Regulation of CYP3A4 Expression in Human Hepatocytes by Pharmaceuticals and Natural Products

2003 • 248 citations

Dexamethasone Enhances Constitutive Androstane Receptor Expression in Human Hepatocytes: Consequences on Cytochrome P450 Gene Regulation

2000 • 246 citations

Transcriptional Regulation of the HumanCYP3A4Gene by the Constitutive Androstane Receptor

2002 • 244 citations

Specific and overlapping functions of the nuclear hormone receptors CAR and PXR in xenobiotic response

2002 • 236 citations

St John's wort, a herbal antidepressant, activates the steroid X receptor

2000 • 236 citations

Vitamin E activates gene expression via the pregnane X receptor

2002 • 226 citations

Hepatocyte-Specific Mutation Establishes Retinoid X Receptor α as a Heterodimeric Integrator of Multiple Physiological Processes in the Liver

2000 • 226 citations

The Acute Phase Response Is Associated with Retinoid X Receptor Repression in Rodent Liver

2000 • 225 citations

Interleukin-6 Negatively Regulates the Expression of Pregnane X Receptor and Constitutively Activated Receptor in Primary Human Hepatocytes

2000 • 223 citations

Induction of CYP1A1. The AhR / DRE Paradigm Transcription, Receptor Regulation, and Expanding Biological Roles

2001 • 221 citations

Enzyminduktion und Vermehrung von endoplasmatischem Reticulum in der Leberzelle w�hrend der Behandlung mit Phenobarbital (Luminal)

1963 • 221 citations

Natural protein variants of pregnane X receptor with altered transactivation activity toward CYP3A4.

2001 • 220 citations

Regulation of xenobiotic and bile acid metabolism by the nuclear pregnane X receptor

2002 • 217 citations

Orphan Nuclear Receptors: The Exotics of Xenobiotics

2001 • 216 citations

Down‐regulation of human CYP3A4 by the inflammatory signal interleukin 6: molecular mechanism and transcription factors involved

2002 • 212 citations

Organ Distribution of Multidrug Resistance Proteins 1, 2, and 3 (Mrp1, 2, and 3) mRNA and Hepatic Induction of Mrp3 by Constitutive Androstane Receptor Activators in Rats

2002 • 211 citations

Genetic Profiling Defines the Xenobiotic Gene Network Controlled by the Nuclear Receptor Pregnane X Receptor

2003 • 209 citations

A Novel Distal Enhancer Module Regulated by Pregnane X Receptor/Constitutive Androstane Receptor Is Essential for the Maximal Induction of CYP2B6 Gene Expression

2003 • 208 citations

Orphan nuclear receptors--the first eight years.

1996 • 206 citations

Rat Pregnane X Receptor: Molecular Cloning, Tissue Distribution, and Xenobiotic Regulation

1999 • 196 citations

Identification of bile acid precursors as endogenous ligands for the nuclear xenobiotic pregnane X receptor

2002 • 193 citations

Endocrine Disrupting Chemicals, Phthalic Acid and Nonylphenol, Activate Pregnane X Receptor-Mediated Transcription

2000 • 192 citations

Induction of drug metabolizing enzyme system in the liver

1972 • 191 citations

Rna Expression in the Early Characterization of Hepatotoxicants in Wistar Rats by High–Density Dna Microarrays

2001 • 190 citations

Peptide Mimetic HIV Protease Inhibitors Are Ligands for the Orphan Receptor SXR

2001 • 188 citations

Molecular Mechanisms of Polymorphic CYP3A7 Expression in Adult Human Liver and Intestine

2002 • 185 citations

Drug-Drug Interactions

2004 • 184 citations

NUBIScan, an in Silico Approach for Prediction of Nuclear Receptor Response Elements

2002 • 184 citations

Reduction in cytochrome P-450 enzyme expression is associated with repression of CAR (constitutive androstane receptor) and PXR (pregnane X receptor) in mouse liver during the acute phase response

2002 • 182 citations

Role of the peroxisome proliferator‐activated receptor in cytochrome P450 4A gene regulation

1996 • 178 citations

Drug-activated nuclear receptors CAR and PXR

2003 • 177 citations

Phenobarbital induction of cytochromes P-450. High-level long-term responsiveness of primary rat hepatocyte cultures to drug induction, and glucocorticoid dependence of the phenobarbital response

1990 • 171 citations

P450BM-3 and other Inducible Bacterial P450 Cytochromes: Biochemistry and Regulation

1991 • 170 citations

Nuclear receptor regulation of hepatic function

2002 • 169 citations

Cyp3A regulation: from pharmacology to nuclear receptors.

2001 • 163 citations

Activation by Diverse Xenochemicals of the 51-Base Pair Phenobarbital-Responsive Enhancer Module in theCYP2B10Gene

1998 • 160 citations

Mechanism of induction of cytochrome P-450 by phenobarbital.

1981 • 159 citations

Regulation of HumanCYP2C9by the Constitutive Androstane Receptor: Discovery of a New Distal Binding Site

2002 • 156 citations

Localization of a phenobarbital-responsive element (PBRE) in the 5′-flanking region of the rat CYP2B2 gene

1995 • 156 citations

Estrogen Activation of the Nuclear Orphan Receptor CAR (Constitutive Active Receptor) in Induction of the MouseCyp2b10Gene

2000 • 155 citations

A Pharmacophore for Human Pregnane X Receptor Ligands

2002 • 152 citations

Environmental Xenobiotics and the Antihormones Cyproterone Acetate and Spironolactone Use the Nuclear Hormone Pregnenolone X Receptor to Activate theCYP3A23Hormone Response Element

1998 • 150 citations

Monitoring expression of genes involved in drug metabolism and toxicology using DNA microarrays

2001 • 150 citations

The Peptide Near the C Terminus Regulates Receptor CAR Nuclear Translocation Induced by Xenochemicals in Mouse Liver

2001 • 146 citations

The human orphan receptor PXR messenger RNA is expressed in both normal and neoplastic breast tissue.

1999 • 139 citations

Characterization of a Phenobarbital-responsive Enhancer Module in Mouse P450 Cyp2b10 Gene

1997 • 139 citations

Regulation of Drug Transporter Gene Expression by Nuclear Receptors

2003 • 138 citations

Role of the hepatocyte nuclear factor 4α in control of the pregnane X receptor during fetal liver development

2003 • 137 citations

Trans-species gene transfer for analysis of glucocorticoid-inducible transcriptional activation of transiently expressed human CYP3A4 and rabbit CYP3A6 in primary cultures of adult rat and rabbit hepatocytes.

1996 • 134 citations

CXR, a chicken xenobiotic-sensing orphan nuclear receptor, is related to both mammalian pregnane X receptor (PXR) and constitutive androstane receptor (CAR)

2000 • 126 citations

Putative Role of the Orphan Nuclear Receptor SXR (Steroid and Xenobiotic Receptor) in the Mechanism of CYP3A4 Inhibition by Xenobiotics

2002 • 125 citations

Regulation of the rat glutathione S-transferase A2 gene by glucocorticoids: involvement of both the glucocorticoid and pregnane X receptors.

2001 • 125 citations

Induction of Rat Organic Anion Transporting Polypeptide 2 by Pregnenolone-16α-carbonitrile Is via Interaction with Pregnane X Receptor

2002 • 124 citations

Cloning of DNA complementary to rat liver NADPH-cytochrome c (P-450) oxidoreductase and cytochrome P-450b mRNAs. Evidence that phenobarbital augments transcription of specific genes.

1982 • 120 citations

TheDrosophilaCytochrome P450 GeneCyp6a2: Structure, Localization, Heterologous Expression, and Induction by Phenobarbital

1997 • 119 citations

Phenobarbital-Elicited Activation of Nuclear Receptor CAR in Induction of Cytochrome P450 Genes

2000 • 117 citations

Regulation of P450 genes by liver-enriched transcription factors and nuclear receptors

2003 • 117 citations

Identification of an endogenous ligand that activates pregnane X receptor-mediated sterol clearance

2003 • 116 citations

Pregnane X Receptor (PXR), Constitutive Androstane Receptor (CAR), and Benzoate X Receptor (BXR) Define Three Pharmacologically Distinct Classes of Nuclear Receptors

2002 • 115 citations

Evidence for the Presence of a Functional Pregnane X Receptor Response Element in the CYP3A7 Promoter Gene

1999 • 115 citations

Alternatively spliced isoforms of the human constitutive androstane receptor

2003 • 115 citations

Mechanisms of Hepatic Transport of Drugs: Implications for Cholestatic Drug Reactions

2002 • 114 citations

The Small Heterodimer Partner Interacts with the Pregnane X Receptor and Represses Its Transcriptional Activity

2003 • 114 citations

Functional and structural comparison of PXR and CAR

2003 • 113 citations

A barbiturate-regulated protein binding to a common sequence in the cytochrome P450 genes of rodents and bacteria.

1991 • 112 citations

Hepatic Cytochrome P450 Regulation in Disease States

2001 • 111 citations

PXR-dependent induction of human CYP3A4 gene expression by organochlorine pesticides

2002 • 110 citations

Characterization of Phenobarbital-inducible Mouse Cyp2b10 Gene Transcription in Primary Hepatocytes

1996 • 109 citations

Transcriptional Analysis of the Orphan Nuclear Receptor Constitutive Androstane Receptor (NR1I3) Gene Promoter: Identification of a Distal Glucocorticoid Response Element

2003 • 109 citations

Chemical genomics: Functional analysis of orphan nuclear receptors in the regulation of bile acid metabolism

2001 • 109 citations

Orphan Receptor Promiscuity in the Induction of Cytochromes P450 by Xenobiotics

2001 • 107 citations

A Structural Model of the Constitutive Androstane Receptor Defines Novel Interactions That Mediate Ligand-Independent Activity

2002 • 107 citations

Molecular Mechanisms of Cytochrome P-450 Induction by Xenobiotics: An Expanded Role for Nuclear Hormone Receptors

1999 • 107 citations

Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes.

2001 • 103 citations

Constitutive Androstane Receptor and Pregnane X Receptor Gene Expression in Human Liver: Interindividual Variability and Correlation with CYP2B6 mRNA Levels

2003 • 101 citations

Phenobarbital Induction Mediated by a Distal CYP2B2 Sequence in Rat Liver Transiently Transfected in Situ

1996 • 101 citations

Induction of CYP3A4 by 1 alpha,25-dihydroxyvitamin D3 is human cell line-specific and is unlikely to involve pregnane X receptor.

2001 • 100 citations

Protein serine/threonine phosphatase inhibitors suppress phenobarbital-induced Cyp2b10 gene transcription in mouse primary hepatocytes

1998 • 99 citations

The glucocorticoid receptor is essential for induction of cytochrome P-4502B by steroids but not for drug or steroid induction of CYP3A or P-450 reductase in mouse liver.

2000 • 98 citations

Role of Constitutive Androstane Receptor in the In Vivo Induction of Mrp3 and CYP2B1/2 by Phenobarbital

2002 • 94 citations

Activation of Orphan Nuclear Constitutive Androstane Receptor Requires Subnuclear Targeting by Peroxisome Proliferator-activated Receptor γ Coactivator-1α

2003 • 94 citations

Transport of Drugs Across the Hepatic Sinusoidal Membrane: Sinusoidal Drug Influx and Efflux in the Liver

2000 • 92 citations

cAMP-associated Inhibition of Phenobarbital-inducible Cytochrome P450 Gene Expression in Primary Rat Hepatocyte Cultures

1995 • 92 citations

A C. elegans orphan nuclear receptor contributes to xenobiotic resistance

2001 • 91 citations

A ligand-based approach to understanding selectivity of nuclear hormone receptors PXR, CAR, FXR, LXRalpha, and LXRbeta.

2002 • 90 citations

Guggulsterone antagonizes farnesoid X receptor induction of bile salt export pump but activates pregnane X receptor to inhibit cholesterol 7α-hydroxylase gene

2003 • 89 citations

Vitamin E and drug metabolism

2003 • 89 citations

Xenobiotic induction of cytochrome P450 2B1 (CYP2B1) is mediated by the orphan nuclear receptor constitutive androstane receptor (CAR) and requires steroid co-activator 1 (SRC-1) and the transcription factor Sp1

2001 • 88 citations

The CYP2B2 Phenobarbital Response Unit Contains an Accessory Factor Element and a Putative Glucocorticoid Response Element Essential for Conferring Maximal Phenobarbital Responsiveness

1998 • 88 citations

Phenobarbital induction and tissue-specific expression of the rat CYP2B2 gene in transgenic mice.

1993 • 86 citations

Organ clearance concepts: new perspectives on old principles.

1997 • 84 citations

Inhibitory Cross-talk between Estrogen Receptor (ER) and Constitutively Activated Androstane Receptor (CAR)

2002 • 83 citations

Glucocorticoid Receptor Enhancement of Pregnane X Receptor-Mediated CYP2B6 Regulation in Primary Human Hepatocytes

2003 • 83 citations

Nuclear Receptor CAR as a Regulatory Factor for the Sexually Dimorphic Induction ofCYP2B1Gene by Phenobarbital in Rat Livers

2001 • 83 citations

The Role of Barbie Box Sequences as cis-Acting Elements Involved in the Barbiturate-mediated Induction of Cytochromes P450BM−1 and P450BM−3 in Bacillus megaterium

1995 • 82 citations

A Nuclear Receptor-Mediated Xenobiotic Response and Its Implication in Drug Metabolism and Host Protection

2003 • 81 citations

Glucocorticoid Receptor-interacting Protein 1 Mediates Ligand-independent Nuclear Translocation and Activation of Constitutive Androstane Receptor in Vivo

2002 • 81 citations

TRANSCRIPTIONAL ACTIVATION OF CYTOCHROME P450 GENES BY DIFFERENT CLASSES OF CHEMICAL INDUCERS

1998 • 80 citations

Effects of Dexamethasone on Aryl (SULT1A1)- and Hydroxysteroid (SULT2A1)-Sulfotransferase Gene Expression in Primary Cultured Human Hepatocytes

2002 • 79 citations

A Novel cis-Acting Element in a Liver Cytochrome P450 3A Gene Confers Synergistic Induction by Glucocorticoids plus Antiglucocorticoids

1995 • 79 citations

Modulation of Mouse and Human Phenobarbital-Responsive Enhancer Module by Nuclear Receptors

2002 • 78 citations

Orphan nuclear receptors--the first eight years

1996 • 76 citations

Drug-mediated induction of cytochrome(s) P-450 and drug metabolism in cultured hepatocytes maintained in chemically defined medium.

1979 • 75 citations

Dexamethasone responsiveness of a major glucocorticoid-inducible CYP3A gene is mediated by elements unrelated to a glucocorticoid receptor binding motif.

1996 • 74 citations

BXR, an embryonic orphan nuclear receptor activated by a novel class of endogenous benzoate metabolites

1998 • 73 citations

Role reversal: new insights from new ligands for the xenobiotic receptor CAR

2001 • 72 citations

The role of hepatocyte RXRα in xenobiotic-sensing nuclear receptor-mediated pathways

2002 • 70 citations

An okadaic acid-sensitive pathway involved in the phenobarbital-mediated induction of CYP2B gene expression in primary rat hepatocyte cultures.

1997 • 69 citations

Regulatory DNA elements of phenobarbital-responsive cytochrome P450 CYP2B genes

1998 • 69 citations

Functionally Conserved Xenobiotic Responsive Enhancer in Cytochrome P450 3A7

2001 • 68 citations

Induction of CYP1A2 by phenobarbital in the livers of aryl hydrocarbon-responsive and -nonresponsive mice.

1999 • 67 citations

Inhibition by barbiturates of the binding of Bm3R1 repressor to its operator site on the barbiturate-inducible cytochrome P450BM-3 gene of Bacillus megaterium.

1993 • 67 citations

The role of the nuclear receptor CAR as a coordinate regulator of hepatic gene expression in defense against chemical toxicity

2002 • 66 citations

Identification of the novel splicing variants for the hPXR in human livers

2002 • 65 citations

Endocrine Disrupting Chemicals, Phthalic Acid and Nonylphenol, Activate Pregnane X Receptor-Mediated Transcription

2000 • 65 citations

Homology modelling of the nuclear receptors: human oestrogen receptorβ (hERβ), the human pregnane-X-receptor (PXR), the Ah receptor (AhR) and the constitutive androstane receptor (CAR) ligand binding domains from the human oestrogen receptor α (hERα) crystal structure, and the human peroxisome proliferator activated receptor α (PPARα) ligand binding domain from the human PPARγ crystal structure

2003 • 64 citations

CYP6B cytochrome P450 monooxygenases from Papilio canadensis and Papilio glaucus: potential contributions of sequence divergence to host plant associations

2002 • 63 citations

Phenobarbital induction of drug/steroid-metabolizing enzymes and nuclear receptor CAR

2003 • 63 citations

Cholesterol and Bile Acids Regulate Xenosensor Signaling in Drug-mediated Induction of Cytochromes P450

2002 • 62 citations

CYP3A4 inducible model for in vitro analysis of human drug metabolism using a bioartificial liver

2003 • 61 citations

Induction ofCYP3AExpression by Dehydroepiandrosterone: Involvement of the Pregnane X Receptor

2002 • 60 citations

Extent and character of phenobarbital-mediated changes in gene expression in the liver.

1997 • 59 citations

Physiological and pathophysiological regulation of cytochrome P450.

1998 • 59 citations

Sex difference in the proliferative response of mouse hepatocytes to treatment with the CAR ligand, TCPOBOP

2003 • 57 citations

I. Nuclear receptors and bile acid homeostasis

2002 • 57 citations

NUBIScan, an in Silico Approach for Prediction of Nuclear Receptor Response Elements

2002 • 57 citations

Transcriptional Control of Hepatocanalicular Transporter Gene Expression

2000 • 57 citations

Orphan nuclear receptor binding site in the human inducible nitric oxide synthase promoter mediates responsiveness to steroid and xenobiotic ligands

2002 • 57 citations

Bile acid and xenobiotic transporters in liver

1998 • 55 citations

Drugs Mediate the Transcriptional Activation of the 5-Aminolevulinic Acid Synthase (ALAS1) Gene via the Chicken Xenobiotic-sensing Nuclear Receptor (CXR)

2002 • 55 citations

Protein Synthesis Inhibitors Exhibit a Nonspecific Effect on Phenobarbital-inducible Cytochome P450 Gene Expression in Primary Rat Hepatocytes

1998 • 55 citations

ROLE OF GLUCOCORTICOID RECEPTOR AND CONSTITUTIVE ANDROSTANE RECEPTOR

2002 • 54 citations

Regulation of Hepatic Drug Metabolism: Role of the Nuclear Receptors PXR and CAR

2002 • 52 citations

Transcriptional response elements in the promoter of CYP6B1, an insect P450 gene regulated by plant chemicals

2003 • 52 citations

Nuclear Receptor Involvement in the Regulation of Rat Cytochrome P450 3A23 Expression

1998 • 52 citations

Conservation of Signaling Pathways of Xenobiotic-Sensing Orphan Nuclear Receptors, Chicken Xenobiotic Receptor, Constitutive Androstane Receptor, and Pregnane X Receptor, from Birds to Humans

2001 • 51 citations

Pharmaceutical use of mouse models humanized for the xenobiotic receptor

2002 • 50 citations

The Peroxisome Proliferator Response Element of the Gene Encoding the Peroxisomal β-Oxidation Enzyme Enoyl-CoA Hydratase/3-Hydroxyacyl-CoA Dehydrogenase Is a Target for Constitutive Androstane Receptor β/9-cis-Retinoic Acid Receptor-mediated Transactivation

2000 • 50 citations

Squalestatin 1-Inducible Expression of Rat CYP2B: Evidence That an Endogenous Isoprenoid Is an Activator of the Constitutive Androstane Receptor

2002 • 47 citations

Estrogen Activation of the Nuclear Orphan Receptor CAR (Constitutive Active Receptor) in Induction of the Mouse Cyp2b10 Gene

2000 • 46 citations

Rabbit pregnane X receptor is activated by rifampicin.

2000 • 46 citations

Transcriptional regulation of the chicken CYP2H1 gene. Localization of a phenobarbital-responsive enhancer domain.

1991 • 46 citations

Induction of drug metabolism by nuclear receptor CAR: molecular mechanisms and implications for drug research

2000 • 46 citations

Chromatin Assembly Enhances Binding to the CYP2B1Phenobarbital-responsive Unit (PBRU) of Nuclear Factor-1, Which Binds Simultaneously with Constitutive Androstane Receptor (CAR)/Retinoid X Receptor (RXR) and Enhances CAR/RXR-mediated Activation of the PBRU

2001 • 46 citations

Regulation of Rat Hepatic Cytochrome P450 Expression by Sterol Biosynthesis Inhibition: Inhibitors of Squalene Synthase Are Potent Inducers of CYP2B Expression in Primary Cultured Rat Hepatocytes and Rat Liver

1998 • 46 citations

Comparing nuclear receptors in worms, flies and humans

2001 • 44 citations

Identification of residues in the PXR ligand binding domain critical for species specific and constitutive activation

2002 • 43 citations

Mechanism of induction of cytochrome p450 enzymes by the proestrogenic endocrine disruptor pesticide-methoxychlor: interactions of methoxychlor metabolites with the constitutive androstane receptor system.

2001 • 43 citations

A Conserved Nuclear Receptor Consensus Sequence (DR-4) Mediates Transcriptional Activation of the Chicken CYP2H1 Gene by Phenobarbital in a Hepatoma Cell Line

2000 • 42 citations

Regulation of phenobarbital induction of the cytochrome P450 2b9/10 genes in primary mouse hepatocyte culture

2000 • 41 citations

Cytochrome P4502A5 Expression and Inducibility by Phenobarbital Is Modulated by cAMP in Mouse Primary Hepatocytes

1994 • 41 citations

Benzoate X Receptors α and β Are Pharmacologically Distinct and Do Not Function as Xenobiotic Receptors

2002 • 39 citations

Phenobarbital Alters Protein Binding to the CYP2B1/2Phenobarbital-responsive Unit in Native Chromatin

1997 • 38 citations

Transcriptional Activation of Cytochrome P450 CYP2C45 by Drugs Is Mediated by the Chicken Xenobiotic Receptor (CXR) Interacting with a Phenobarbital Response Enhancer Unit

2002 • 38 citations

Phenobarbital responsiveness conferred by the 5′-flanking region of the rat CYP2B2 gene in transgenic mice

1999 • 37 citations

Gene Induction by Phenobarbital: An Update on an Old Question that Receives Key Novel Answers

2001 • 37 citations

Phosphorylation/Dephosphorylation Steps Are Crucial for the Induction of CYP2B1 and CYP2B2 Gene Expression by Phenobarbital

1999 • 37 citations

A model for the transcriptional regulation of the CYP2B1/B2 gene in rat liver.

1995 • 37 citations

Transcriptional Elements Directing a Liver-Specific Expression of P450/6βA (CYP3A2) Gene-Encoding Testosterone 6β-Hydroxylase

1995 • 36 citations

Effect of Phenobarbital on Hepatic CYP1A1 and CYP1A2 in the Ahr-Null Mouse

1998 • 36 citations

Divergent effects of cycloheximide on the induction of Class II and Class III cytochrome P450 mRNAs in cultures of adult rat hepatocytes

1990 • 36 citations

Regulation of Cytochrome P450 Gene Transcription by Phenobarbital

1998 • 35 citations

Microsomal ethanol oxidizing system: transcriptional and posttranscriptional regulation of cytochrome P450, CYP2E1.

1991 • 34 citations

Insights from a Three-Dimensional Model into Ligand Binding to Constitutive Active Receptor

2002 • 32 citations

Phenobarbital Induction of CYP2B1/2 in Primary Hepatocytes: Endocrine Regulation and Evidence for a Single Pathway for Multiple Inducers

1999 • 32 citations

Use of dominant negative nuclear receptors to study xenobiotic-inducible gene expression in primary cultured hepatocytes

2002 • 31 citations

Involvement of Synthesis and Phosphorylation of Nuclear Protein Factors That Bind to the Positivecis-Acting Element in the Transcriptional Activation of the CYP2B1/B2 Gene by Phenobarbitonein Vivo

1996 • 30 citations

Forskolin-mediated induction of CYP3A1 mRNA expression in primary rat hepatocytes is independent of elevated intracellular cyclic AMP.

1996 • 29 citations

The Critical Role of Carboxy-Terminal Amino Acids in Ligand-Dependent and -Independent Transactivation of the Constitutive Androstane Receptor

2003 • 29 citations

Expression and Replication Timing Patterns of Wildtype and Translocated BCL2 Genes

2001 • 29 citations

Nuclear Factor-1 Motif and Redundant Regulatory Elements Comprise Phenobarbital-Responsive Enhancer inCYP2B1/2

1998 • 28 citations

Mutational Analysis of the CYP2B2 Phenobarbital Response Unit and Inhibitory Effect of the Constitutive Androstane Receptor on Phenobarbital Responsiveness

2000 • 27 citations

Taurine modulates induction of cytochrome P450 3A4 mRNA by rifampicin in the HepG2 cell line

2002 • 25 citations

Multiple enhancer units mediate drug induction of CYP2H1 by xenobiotic-sensing orphan nuclear receptor chicken xenobiotic receptor.

2001 • 23 citations

Die Beschleunigung des Abbaues als Ursache der Gewöhnung an Barbiturate

1959 • 23 citations

Retinoic Acids Repress Constitutive Active Receptor-Mediated Induction by 1,4-bis[2-(3,5-Dichloropyridyloxy)]benzene of theCyp2b10 Gene in Mouse Primary Hepatocytes

2002 • 23 citations

A component of the 26S proteasome binds an orphan member of the nuclear hormone receptor superfamily

1996 • 23 citations

Residue Threonine 350 Confers Steroid Hormone Responsiveness to the Mouse Nuclear Orphan Receptor CAR

2002 • 22 citations

The PXR crystal structure: the end of the beginning

2002 • 22 citations

A Link between Cholesterol Levels and Phenobarbital Induction of Cytochromes P450

2002 • 22 citations

Involvement of cyclic nucleotide- and calcium-regulated pathways in phenobarbital-induced cytochrome P-450 3A expression in mouse primary hepatocytes.

1999 • 21 citations

PHENOBARBITAL-MEDIATED CHANGES IN GENE EXPRESSION IN THE LIVER

1999 • 20 citations

Transcriptional analysis in vivo of the hepatic genes, Cyp2b9 and Cyp2b10, by intravenous administration of plasmid DNA in mice

2003 • 20 citations

A 65-kDa Protein Mediates the Positive Role of Heme in Regulating the Transcription of CYP2B1/B2 Gene in Rat Liver

1997 • 20 citations

Evidence against the Bm1P1 Protein as a Positive Transcription Factor for Barbiturate-mediated Induction of Cytochrome P450BM-1 in Bacillus megaterium

1998 • 19 citations

Superinduction by Cycloheximide of Cytochrome P4502H1 and 5-Aminolevulinate Synthase Gene Transcription in Chick Embryo Liver

1993 • 19 citations

Mechanisms of phenobarbital-type induction of cytochrome P-450 isozymes

1987 • 18 citations

Phenobarbital-Induced Activation ofCYP2H1and 5-Aminolevulinate Synthase Genes in Chick Embryo Hepatocytes Is Blocked by an Inhibitor of Protein Phosphorylation

1996 • 18 citations

Liver-Enriched Transcription Factors, HNF-1, HNF-3, and C/EBP, Are Major Contributors to the Strong Activity of the ChickenCYP2H1Promoter in Chick Embryo Hepatocytes

1997 • 17 citations

Identification of phenobarbitone‐modulated genes in mouse liver by differential display

1999 • 17 citations

Identification of phenobarbitone-modulated genes in mouse liver by differential display

2000 • 16 citations

Molecular Cloning and Functional Characterization of a Novel Nuclear Receptor Similar to an Embryonic Benzoate Receptor BXR

2000 • 15 citations

Analysis of a Phenobarbital-Responsive Enhancer Sequence Located in the 5′ Flanking Region of the ChickenCYP2H1Gene: Identification and Characterization of Functional Protein-Binding Sites

1999 • 15 citations

Tissue-specific chromatin structure of the phenobarbital- responsive unit and proximal promoter of CYP2B1/2 and modulation by phenobarbital

2000 • 13 citations

The Liver-Specific Response to Phenobarbital Involves a Transient Increase in Phosphorylation of a 34-kDa Nuclear-Protein in Rat Liver and in Hepatocytes in Culture

1995 • 11 citations

Expression pattern of BXR suggests a role for benzoate ligand-mediated signalling in hatching gland function.

2000 • 11 citations

Repression of Phenobarbital-Dependent CYP2B1 mRNA Induction by Reactive Oxygen Species in Primary Rat Hepatocyte Cultures

2001 • 11 citations

Positive regulation of the rat CYP2B2 phenobarbital response unit by the nuclear receptor hexamer half-site·nuclear factor 1 complex

1999 • 10 citations

Conservation of Signaling Pathways of Xenobiotic-Sensing Orphan Nuclear Receptors, Chicken Xenobiotic Receptor, Constitutive Androstane Receptor, and Pregnane X Receptor, from Birds to Humans

2001 • 10 citations

The PXR ligand-binding domain: how to be picky and promiscuous at the same time

2001 • 9 citations

Functional analysis of the phenobarbital-responsive unit in rat CYP2B211Abbreviations: P450, cytochrome P450; PB, phenobarbital; CYP, P450 gene; NR, nuclear receptor; NF-1, nuclear factor-1; GRE, glucocorticoid response element; CAR, constitutive androgen receptor; RXR, retinoid X receptor; PBRU, PB response element

2001 • 9 citations

Biochemical and genetic analysis of AMP deaminase deficiency in cultured mammalian cells.

1981 • 6 citations

A duplicated HNF-3 binding site in the CYP2H2 promoter underlies the weak phenobarbital induction response

2001 • 5 citations

Phenobarbitone-Mediated Translocation of the Cytosolic Proteins Interacting with the 5′-Proximal Region of Rat Liver CYP2B1/B2 Gene into the Nucleus

2002 • 3 citations

The Basal-Level Expression of the Cytochrome P450 BM-1 Gene Is Negatively Affected by the bm1P1 Gene of Bacillus megaterium

2000 • 3 citations

Evidence That the Coactivator CBP/p300 Is Important for Phenobarbital-Induced but Not Basal Expression of theCYP2H1Gene

2003 • 3 citations

‘S-SXR-RMs’? Selective SXR response modulators – the future of designer drug interactions?

2002 • 1 citations

Besprechungen

1958 • 1 citations