Nuclear Receptors and the Regulation of Drug‐Metabolizing Enzymes and Drug Transporters: Implications for Interindividual Variability in Response to Drugs

Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues.

1987 • 2,788 citations

BIOCHEMICAL, CELLULAR, AND PHARMACOLOGICAL ASPECTS OF THE MULTIDRUG TRANSPORTER

1999 • 2,049 citations

Targeted Disruption of the Nuclear Receptor FXR/BAR Impairs Bile Acid and Lipid Homeostasis

2000 • 1,704 citations

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

1998 • 1,535 citations

Human UDP-Glucuronosyltransferases: Metabolism, Expression, and Disease

2000 • 1,477 citations

Association of polymorphisms in the cytochrome P450 CYP2C9 with warfarin dose requirement and risk of bleeding complications

1999 • 1,263 citations

Multidrug resistance mediated by the breast cancer resistance protein BCRP (ABCG2)

2003 • 1,027 citations

A gene encoding a liver-specific ABC transporter is mutated in progressive familial intrahepatic cholestasis

1998 • 980 citations

The Sister of P-glycoprotein Represents the Canalicular Bile Salt Export Pump of Mammalian Liver

1998 • 933 citations

The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin

1999 • 911 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

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

Cytochrome P4502C9: an enzyme of major importance in human drug metabolism

1998 • 820 citations

Human Bile Salt Export Pump Promoter Is Transactivated by the Farnesoid X Receptor/Bile Acid Receptor

2001 • 753 citations

Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver

2001 • 722 citations

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

1998 • 697 citations

Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine*

1997 • 675 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

Enterohepatic bile salt transporters in normal physiology and liver disease

2003 • 641 citations

Nuclear Receptors and the Control of Metabolism

2003 • 631 citations

Drug and Bile Acid Transporters in Rosuvastatin Hepatic Uptake: Function, Expression, and Pharmacogenetics

2006 • 585 citations

OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.

1999 • 585 citations

Localization and Genomic Organization of a New Hepatocellular Organic Anion Transporting Polypeptide

2000 • 516 citations

Transporters and drug therapy: Implications for drug disposition and disease

2005 • 497 citations

CYP3A4 Induction by Drugs: Correlation between a Pregnane X Receptor Reporter Gene Assay and CYP3A4 Expression in Human Hepatocytes

2002 • 438 citations

Hepatocanalicular bile salt export pump deficiency in patients with progressive familial intrahepatic cholestasis

1999 • 431 citations

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

2003 • 424 citations

Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver

1995 • 419 citations

The breast cancer resistance protein BCRP (ABCG2) concentrates drugs and carcinogenic xenotoxins into milk

2005 • 412 citations

Intestinal Drug Transporter Expression and the Impact of Grapefruit Juice in Humans

2007 • 400 citations

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

2003 • 399 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

Polymorphisms in Human Organic Anion-transporting Polypeptide 1A2 (OATP1A2)

2005 • 351 citations

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

2002 • 350 citations

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

2003 • 331 citations

Expression of Enzymatically Active CYP3A4 by Caco-2 Cells Grown on Extracellular Matrix-Coated Permeable Supports in the Presence of 1α,25-Dihydroxyvitamin D₃

1997 • 326 citations

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

2001 • 321 citations

Induction of CYP2C genes in human hepatocytes in primary culture.

2001 • 316 citations

Possible involvement of pregnane X receptor–enhanced CYP24 expression in drug-induced osteomalacia

2005 • 300 citations

Differential Regulation of Sinusoidal and Canalicular Hepatic Drug Transporter Expression by Xenobiotics Activating Drug-Sensing Receptors in Primary Human Hepatocytes

2006 • 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

Inherited disorders of bilirubin metabolism

2002 • 275 citations

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

2002 • 269 citations

P-glycoprotein: a major determinant of rifampicin-inducible expression of cytochrome P4503A in mice and humans.

1996 • 266 citations

Effects of Ursodeoxycholic and Cholic Acid Feeding on Hepatocellular Transporter Expression in Mouse Liver

2001 • 262 citations

Transcriptional Regulation of CYP2C9 Gene

2002 • 260 citations

Importance of genetic factors in the regulation of diazepam metabolism: Relationship to S-mephenytoin, but not debrisoquin, hydroxylation phenotype

1989 • 257 citations

COMPARATIVE ANALYSIS OF CYP3A EXPRESSION IN HUMAN LIVER SUGGESTS ONLY A MINOR ROLE FOR CYP3A5 IN DRUG METABOLISM

2003 • 250 citations

The Nuclear Receptor Superfamily: A Rosetta Stone for Physiology

2005 • 247 citations

Polymorphic Gene Regulation and Interindividual Variation of UDP-glucuronosyltransferase Activity in Human Small Intestine

2000 • 247 citations

The role of individual human cytochrpmes P450 in drug metabolism and clinical response

1992 • 246 citations

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

2000 • 246 citations

Human CYP2B6: expression, inducibility and catalytic activities.

1999 • 245 citations

Transcriptional Regulation of the HumanCYP3A4Gene by the Constitutive Androstane Receptor

2002 • 244 citations

Interactions between Hepatic Mrp4 and Sult2a as Revealed by the Constitutive Androstane Receptor and Mrp4 Knockout Mice

2004 • 229 citations

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

2001 • 220 citations

Antimalarial Artemisinin Drugs Induce Cytochrome P450 and MDR1 Expression by Activation of Xenosensors Pregnane X Receptor and Constitutive Androstane Receptor

2005 • 220 citations

Drug transport proteins in the liver

2003 • 220 citations

Breast cancer resistance protein (BCRP/ABCG2)

2004 • 218 citations

Induction of Human CYP2C9 by Rifampicin, Hyperforin, and Phenobarbital Is Mediated by the Pregnane X Receptor

2003 • 218 citations

Inhibition of drug metabolism by blocking the activation of nuclear receptors by ketoconazole

2006 • 205 citations

Human CYP2B6

1999 • 203 citations

Dehydroepiandrosterone Sulfotransferase Gene Induction by Bile Acid Activated Farnesoid X Receptor

2001 • 201 citations

PXR (NR1I2): splice variants in human tissues, including brain, and identification of neurosteroids and nicotine as PXR activators

2004 • 198 citations

In Vivo Activation of Human Pregnane X Receptor Tightens the Blood-Brain Barrier to Methadone through P-Glycoprotein Up-Regulation

2006 • 187 citations

Effect of Grapefruit Juice Volume on the Reduction of Fexofenadine Bioavailability: Possible Role of Organic Anion Transporting Polypeptides*

2005 • 187 citations

Lopinavir/Ritonavir Induces the Hepatic Activity of Cytochrome P450 Enzymes CYP2C9, CYP2C19, and CYP1A2 But Inhibits the Hepatic and Intestinal Activity of CYP3A as Measured by a Phenotyping Drug Cocktail in Healthy Volunteers

2006 • 186 citations

Lithocholic Acid Decreases Expression of Bile Salt Export Pump through Farnesoid X Receptor Antagonist Activity

2002 • 182 citations

genotype–related efficacy of omeprazole for the treatment of infection caused by

1999 • 180 citations

Involvement of the Xenobiotic Response Element (XRE) in Ah Receptor-mediated Induction of Human UDP-glucuronosyltransferase 1A1

2003 • 173 citations

Identification of Constitutive Androstane Receptor and Glucocorticoid Receptor Binding Sites in the CYP2C19 Promoter

2003 • 171 citations

Peroxisome Proliferator-activated Receptor γ-regulated ABCG2 Expression Confers Cytoprotection to Human Dendritic Cells

2006 • 171 citations

Human organic anion transporting polypeptide 8 promoter is transactivated by the farnesoid X receptor/bile acid receptor

2002 • 167 citations

The human drug metabolizing cytochromes P450

1996 • 166 citations

Variations of the human glucocorticoid receptor gene (NR3C1): Pathological and in vitro mutations and polymorphisms

2003 • 165 citations

Chlorambucil-taurocholate is transported by bile acid carriers expressed in human hepatocellular carcinomas

1997 • 165 citations

ATP-DEPENDENT TRANSPORT OF ROSUVASTATIN IN MEMBRANE VESICLES EXPRESSING BREAST CANCER RESISTANCE PROTEIN

2006 • 164 citations

Regulation of CYP3A4 by the bile acid receptor FXR

2004 • 162 citations

Dehydroepiandrosterone Sulfotransferase Is a Target for Transcriptional Induction by the Vitamin D Receptor

2004 • 159 citations

Hepatic uptake of cholecystokinin octapeptide by organic anion-transporting polypeptides OATP4 and OATP8 of rat and human liver

2001 • 157 citations

Breast Cancer Resistance Protein (Bcrp/abcg2) Is a Major Determinant of Sulfasalazine Absorption and Elimination in the Mouse

2006 • 153 citations

HUMAN PXR VARIANTS AND THEIR DIFFERENTIAL EFFECTS ON THE REGULATION OF HUMAN UDP-GLUCURONOSYLTRANSFERASE GENE EXPRESSION

2004 • 152 citations

A role for constitutive androstane receptor in the regulation of human intestinal MDR1 expression

2005 • 150 citations

Induction of Drug Metabolism by Forskolin: The Role of the Pregnane X Receptor and the Protein Kinase A Signal Transduction Pathway

2004 • 146 citations

Multispecific amphipathic substrate transport by an organic anion transporter of human liver

1996 • 140 citations

Expression and Induction of CYP2C P450 Enzymes in Primary Cultures of Human Hepatocytes

2002 • 140 citations

Human Constitutive Androstane Receptor Mediates Induction of CYP2B6 Gene Expression by Phenytoin

2004 • 139 citations

Liganded VDR induces CYP3A4 in small intestinal and colon cancer cells via DR3 and ER6 vitamin D responsive elements

2002 • 135 citations

Expression of the Steroid and Xenobiotic Receptor and Its Possible Target Gene, Organic Anion Transporting Polypeptide-A, in Human Breast Carcinoma

2006 • 134 citations

The Human Na+-Taurocholate Cotransporting Polypeptide Gene Is Activated by Glucocorticoid Receptor and Peroxisome Proliferator-Activated Receptor-γ Coactivator-1α, and Suppressed by Bile Acids via a Small Heterodimer Partner-Dependent Mechanism

2005 • 127 citations

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

2001 • 125 citations

Orphan Nuclear Receptor Pregnane X Receptor Sensitizes Oxidative Stress Responses in Transgenic Mice and Cancerous Cells

2005 • 112 citations

NUCLEAR RECEPTOR, PREGNANE X RECEPTOR, IS REQUIRED FOR INDUCTION OF UDP-GLUCURONOSYLTRANSFERASES IN MOUSE LIVER BY PREGNENOLONE-16α-CARBONITRILE

2003 • 109 citations

Expression of Constitutive Androstane Receptor Splice Variants in Human Tissues and Their Functional Consequences

2004 • 108 citations

The Nuclear Receptors Constitutive Androstane Receptor and Pregnane X Receptor Cross-Talk with Hepatic Nuclear Factor 4α to Synergistically Activate the HumanCYP2C9Promoter

2005 • 107 citations

MRP2 and 3 in health and disease

2006 • 106 citations

CYP2C9 genotypes and dose requirements during the induction phase of oral anticoagulant therapy

2004 • 104 citations

MDR1 genotype is associated with hepatic cytochrome P450 3A4 basal and induction phenotype

2006 • 103 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

Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase

2005 • 101 citations

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

2003 • 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

Genetic analysis of the interethnic difference between Chinese and Caucasians in the polymorphic metabolism of debrisoquine and codeine

1991 • 95 citations

Pharmacological interventions for the treatment of neonatal jaundice

2002 • 94 citations

Association Between Peroxisome Proliferator–Activated Receptor γ Haplotypes and the Metabolic Syndrome in French Men and Women

2005 • 93 citations

Identification of a Novel Polymorphic Enhancer of the HumanCYP3A4Gene

2004 • 90 citations

A Cell-Based Reporter Gene Assay for Determining Induction of CYP3A4 in a High-Volume System

2002 • 85 citations

Molecular and functional comparison of 1,25‐dihydroxyvitamin D₃ and the novel vitamin D receptor ligand, lithocholic acid, in activating transcription of cytochrome P450 3A4

2004 • 85 citations

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

2003 • 83 citations

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

2002 • 79 citations

Evaluation of Human Liver Slices and Reporter Gene Assays as Systems for Predicting the Cytochrome P450 Induction Potential of Drugs in Vivo in Humans

2005 • 68 citations

Activation of the Steroid and Xenobiotic Receptor (Human Pregnane X Receptor) by Nontaxane Microtubule-Stabilizing Agents

2005 • 67 citations

IDENTIFICATION OF HMG-CoA REDUCTASE INHIBITORS AS ACTIVATORS FOR HUMAN, MOUSE AND RAT CONSTITUTIVE ANDROSTANE RECEPTOR

2005 • 66 citations

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

2002 • 65 citations

Phenotype and genotype analysis of debrisoquine hydroxylase (CYP2D6) in a black Zimbabwean population

1996 • 58 citations

The Mycoestrogen Zearalenone Induces CYP3A through Activation of the Pregnane X Receptor

2006 • 56 citations

Induction of Cytochrome P450 3A4 and P-Glycoprotein by the Isoxazolyl- Penicillin Antibiotic Flucloxacillin

2006 • 53 citations

Functional analysis of four naturally occurring variants of human constitutive androstane receptor

2005 • 52 citations

A simultaneous assessment of CYP3A4 metabolism and induction in the DPX-2 cell line

2005 • 51 citations

Development of A Real-Time in Vivo Transcription Assay: Application Reveals Pregnane X Receptor-Mediated Induction of CYP3A4 by Cancer Chemotherapeutic Agents

2002 • 51 citations

Pharmaceutical use of mouse models humanized for the xenobiotic receptor

2002 • 50 citations

Cytochrome P450 3A pharmacogenetics: the road that needs traveled

2003 • 48 citations

Functional characterization of a novel polymorphism of pregnane X receptor, Q158K, in Chinese subjects

2005 • 38 citations

Variability of human hepatic UDP-glucuronosyltransferase activity.

1999 • 13 citations