(Q36749461)

16 August 2017

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title

The evolving role of drug metabolism in drug discovery and development (English)

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16 August 2017

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Lilian G Yengi

1

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16 August 2017

Louis Leung

series ordinal

2

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16 August 2017

John Kao

series ordinal

3

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16 August 2017

publication date

1 March 2007

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16 August 2017

published in

Pharmaceutical Research

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16 August 2017

volume

24

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16 August 2017

issue

5

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16 August 2017

page(s)

842-858

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Assessment of drug interactions in hepatobiliary transport using rhodamine 123 in sandwich-cultured rat hepatocytes.

16 August 2017

cites work

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12 December 2020

Pigments of rat liver microsomes

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12 December 2020

Mechanism of the cardiotoxic actions of terfenadine

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12 December 2020

Current Models of Steroid Hormone Action: A Critique

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12 December 2020

Detection of specific polymerase chain reaction product by utilizing the 5'----3' exonuclease activity of Thermus aquaticus DNA polymerase

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12 December 2020

A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes

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12 December 2020

Pharmacogenetic application in drug development and clinical trials

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12 December 2020

Gene expression profile in the livers of rats orally administered ethinylestradiol for 28 days using a microarray technique

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12 December 2020

The human intestinal cytochrome P450 "pie".

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12 December 2020

Inheritance and drug response

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12 December 2020

Troglitazone-induced intrahepatic cholestasis by an interference with the hepatobiliary export of bile acids in male and female rats. Correlation with the gender difference in troglitazone sulfate formation and the inhibition of the canalicular bile

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12 December 2020

The metabolism of 4-dimethylaminoazobenzene by rat liver homogenates

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12 December 2020

Biochemical and molecular pharmacological aspects of transporters as determinants of drug disposition

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12 December 2020

Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.

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12 December 2020

Selective downregulation of hepatic cytochrome P450 expression and activity in a rat model of inflammatory pain

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12 December 2020

On the protective action of certain polycyclic aromatic hydrocarbons against carcinogenesis by aminoazo dyes and 2-acetylaminofluorene.

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12 December 2020

Elucidating mechanisms of drug-induced toxicity.

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12 December 2020

Knowledge-based expert systems for toxicity and metabolism prediction: DEREK, StAR and METEOR.

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12 December 2020

Inflammation and drug idiosyncrasy--is there a connection?

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12 December 2020

Prescribing BiDil: is it black and white?

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12 December 2020

Nuclear receptor, pregname X receptor, is required for induction of UDP-glucuronosyltranferases in mouse liver by pregnenolone-16 alpha-carbonitrile

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12 December 2020

Acetaminophen-induced hepatic necrosis. II. Role of covalent binding in vivo

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12 December 2020

Identification of a novel route of extraction of sirolimus in human small intestine: roles of metabolism and secretion

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12 December 2020

Impact of parallel pathways of drug elimination and multiple cytochrome P450 involvement on drug-drug interactions: CYP2D6 paradigm.

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12 December 2020

Molecular and physical mechanisms of first-pass extraction

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12 December 2020

Aliphatic hydroxylation by highly purified liver microsomal cytochrome P-450. Evidence for a carbon radical intermediate

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12 December 2020

Induction of drug metabolism. II. Qualitative differences in the microsomal N-demethylating systems stimulated by polycyclic hydrocarbons and by phenobarbital

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12 December 2020

Functional characterization of single nucleotide polymorphisms with amino acid substitution in CYP1A2, CYP2A6, and CYP2B6 found in the Japanese population

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12 December 2020

Biochemistry and molecular biology of the human CYP2C subfamily

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12 December 2020

"Phase I and Phase II" drug metabolism: terminology that we should phase out?

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12 December 2020

Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs.

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12 December 2020

Transcriptomics in predictive toxicology

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12 December 2020

CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: studies with sirolimus and midazolam

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12 December 2020

Selective serotonin reuptake inhibitors and cytochrome P-450 mediated drug-drug interactions: an update

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12 December 2020

Geographical/interracial differences in polymorphic drug oxidation. Current state of knowledge of cytochromes P450 (CYP) 2D6 and 2C19

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12 December 2020

Implications of pharmacogenomics for drug development and clinical practice

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12 December 2020

Orphan nuclear receptors: shifting endocrinology into reverse

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12 December 2020

The conduct of in vitro and in vivo drug-drug interaction studies: a Pharmaceutical Research and Manufacturers of America (PhRMA) perspective

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12 December 2020

Human drug metabolising cytochrome P450 enzymes: properties and polymorphisms

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12 December 2020

Evidence for superoxide generation by NADPH-cytochrome c reductase of rat liver microsomes

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12 December 2020

Integrating in vitro kinetic data from compounds exhibiting induction, reversible inhibition and mechanism-based inactivation: in vitro study design

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12 December 2020

Pharmacogenomics and individualized drug therapy

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12 December 2020

Predicting drug disposition via application of BCS: transport/absorption/ elimination interplay and development of a biopharmaceutics drug disposition classification system

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12 December 2020

Evolutionarily conserved sequences on human chromosome 21

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12 December 2020

Time course of hepatic changes produced by medroxyprogesterone acetate in the rat

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12 December 2020

Sex difference in induction of hepatic CYP2B and CYP3A subfamily enzymes by nicardipine and nifedipine in rats

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12 December 2020

Apical/basolateral surface expression of drug transporters and its role in vectorial drug transport

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12 December 2020

Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction

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12 December 2020

Polymorphisms in human organic anion-transporting polypeptide 1A2 (OATP1A2): implications for altered drug disposition and central nervous system drug entry

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12 December 2020

Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios

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12 December 2020

Use of a low-density microarray for studying gene expression patterns induced by hepatotoxicants on primary cultures of rat hepatocytes

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12 December 2020

THE LIGHT REVERSIBLE CARBON MONOXIDE INHIBITION OF THE STEROID C21-HYDROXYLASE SYSTEM OF THE ADRENAL CORTEX

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12 December 2020

Aryl hydrocarbon hydroxylase induction in mammalian liver cell culture. I. Stimulation of enzyme activity in nonhepatic cells and in hepatic cells by phenobarbital, polycyclic hydrocarbons, and 2,2-bis(p-chlorophenyl)-1,1,1-trichloroethane

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12 December 2020

Effect of superoxide generation and dismutation on hydroxylation reactions catalyzed by liver microsomal cytochrome P-450

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12 December 2020

On the formation of carbamate glucuronides

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12 December 2020

Adipsin, a biomarker of gastrointestinal toxicity mediated by a functional gamma-secretase inhibitor

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12 December 2020

Correlation between genotype and phenotype of the human arylamine N-acetyltransferase type 1 (NAT1).

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12 December 2020

Mechanism-based inactivation of human cytochrome P4502C8 by drugs in vitro

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12 December 2020

Congenital adrenal hyperplasia

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12 December 2020

Substrate depletion approach for determining in vitro metabolic clearance: time dependencies in hepatocyte and microsomal incubations

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12 December 2020

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12 December 2020

Quantitation of cytochrome P450 mRNA levels in human skin

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12 December 2020

Therapeutic drugs that behave as mechanism-based inhibitors of cytochrome P450 3A4

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12 December 2020

Relevance of pheno- and genotyping in clinical drug development.

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12 December 2020

Mechanism-based inactivation of human recombinant P450 2C9 by the nonsteroidal anti-inflammatory drug suprofen

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12 December 2020

A passion for P450s (rememberances of the early history of research on cytochrome P450).

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12 December 2020

Apparent mechanism-based inhibition of human CYP2D6 in vitro by paroxetine: comparison with fluoxetine and quinidine

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12 December 2020

Rational use of in vitro P-glycoprotein assays in drug discovery

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12 December 2020

Multiple forms of inducible drug-metabolizing enzymes: A reasonable mechanism by which any organism can cope with adversity

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12 December 2020

Studies on pig liver microsomes. I. Enzymic and pigment composition of different microsomal fractions

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12 December 2020

The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module

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12 December 2020

Application of pharmacogenomics in drug discovery and development: correlations between transcriptional modulation and preclinical safety observations

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12 December 2020

Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: An examination of in vitro half-life approach and nonspecific binding to microsomes.

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12 December 2020

Identification of the polymorphically expressed CYP2C19 and the wild-type CYP2C9-ILE359 allele as low-Km catalysts of cyclophosphamide and ifosfamide activation.

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12 December 2020

Pharmacogenomics: translating functional genomics into rational therapeutics

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12 December 2020

Screening for the potential of a drug candidate to cause idiosyncratic drug reactions

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12 December 2020

Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor

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12 December 2020

The role of multidrug transporters in drug availability, metabolism and toxicity

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12 December 2020

PHOTOCHEMICAL ACTION SPECTRUM OF THE TERMINAL OXIDASE OF MIXED FUNCTION OXIDASE SYSTEMS

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12 December 2020

Isosorbide dinitrate and hydralazine hydrochloride: a review of efficacy and safety

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12 December 2020

Drug uptake systems in liver and kidney

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12 December 2020

Absorption properties and P-glycoprotein activity of modified Caco-2 cell lines

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12 December 2020

Pharmacokinetic drug interactions

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12 December 2020

Current pharmacogenomic approaches to clinical drug development

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12 December 2020

Simple strategies for reducing sample loads in in vitro metabolic stability high-throughput screening experiments: a comparison between traditional, two-time-point and pooled sample analyses

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12 December 2020

The Paton Prize Award. The discovery of the debrisoquine hydroxylation polymorphism: scientific and clinical impact and consequences

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12 December 2020

Gene expression analysis of the acute phase response using a canine microarray

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12 December 2020

Can the pharmaceutical industry reduce attrition rates?

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12 December 2020

Cross-species sequence comparisons: a review of methods and available resources

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12 December 2020

Genetic variation as a guide to drug development

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12 December 2020

Mechanism-based inactivation and reversibility: is there a new trend in the inactivation of cytochrome p450 enzymes?

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12 December 2020

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12 December 2020

Pharmacogenetics goes genomic

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12 December 2020

The relevance of chemico-biological interactions for the toxic and carcinogenic effects of aromatic amines. V. The pharmacokinetics of related aromatic amines in blood

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12 December 2020

High-resolution whole-genome association study of Parkinson disease.

1 reference

12 December 2020

Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver

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12 December 2020

Prediction of hepatic clearance and availability by cryopreserved human hepatocytes: an application of serum incubation method

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12 December 2020

In vitro-in vivo extrapolation of CYP2D6 inactivation by paroxetine: prediction of nonstationary pharmacokinetics and drug interaction magnitude

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12 December 2020

Development of a DNA microarray for toxicology based on hepatotoxin-regulated sequences

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12 December 2020

Utility of Hepatocytes in Predicting Drug Metabolism: Comparison of Hepatic Intrinsic Clearance in Rats and Humans in Vivo and in Vitro

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12 December 2020

Role of hemoprotein P-450 in fatty acid omega-hydroxylation in a soluble enzyme system from liver microsomes

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12 December 2020

Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.

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12 December 2020

Searches for ultimate chemical carcinogens and their reactions with cellular macromolecules.

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12 December 2020

Pharmacogenetics and pharmacogenomics: why is this relevant to the clinical geneticist?

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12 December 2020

A method for the simultaneous evaluation of the activities of seven major human drug-metabolizing cytochrome P450s using an in vitro cocktail of probe substrates and fast gradient liquid chromatography tandem mass spectrometry

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12 December 2020

Challenges in current drug delivery from the potential application of pharmacogenomics and personalized medicine in clinical practice

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12 December 2020

The Gerhard Zbinden memorial lecture: application of biochemical and genetic approaches to understanding pathways of chemical toxicity

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12 December 2020

Cytosolic receptor for aryl hydrocarbon hydroxylase induction by polycyclic aromatic compounds. Evidence for structural and regulatory variants among established cell cultured lines

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12 December 2020

Metabolic interactions between mibefradil and HMG-CoA reductase inhibitors: an in vitro investigation with human liver preparations

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12 December 2020

Science, medicine, and the future: Pharmacogenetics

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12 December 2020

An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway

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12 December 2020

Polymorphic oxidation of debrisoquine and sparteine

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12 December 2020

Genetic Differences in the Extent of Aryl Hydrocarbon Hydroxylase Induction in Mouse Fetal Cell Cultures

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12 December 2020

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

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12 December 2020

Concurrent induction and mechanism-based inactivation of CYP3A4 by an L-valinamide derivative

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12 December 2020

The enzymatic deamination of amphetamine (benzedrine)

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12 December 2020

Functional polymorphisms of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo

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12 December 2020

Are chemically reactive metabolites responsible for adverse reactions to drugs?

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12 December 2020

Merits and limitations of recombinant models for the study of human P450-mediated drug metabolism and toxicity: an intralaboratory comparison.

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12 December 2020

Amino terminal sequence analysis of human placenta aromatase

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12 December 2020

A comparison of the covalent binding of clozapine, procainamide, and vesnarinone to human neutrophils in vitro and rat tissues in vitro and in vivo

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12 December 2020

Metabolic polymorphisms

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12 December 2020

Tissue distribution and pharmacodynamics: a complicated relationship

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12 December 2020

A simplified method for the culturing of primary adult rat and human hepatocytes as multicellular spheroids

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12 December 2020

Drug bioactivation, covalent binding to target proteins and toxicity relevance

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12 December 2020

Systems biology in drug safety and metabolism: integration of microarray, real-time PCR and enzyme approaches

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12 December 2020

The metabolism of methylated aminoazo dyes. II. Oxidative demethylation by rat liver homogenates

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12 December 2020

Pharmacokinetics and metabolic disposition of sirolimus in healthy male volunteers after a single oral dose

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12 December 2020

Methotrexate is excreted into the bile by canalicular multispecific organic anion transporter in rats

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12 December 2020

A new cytochrome in liver microsomes

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12 December 2020

Automated screening with confirmation of mechanism-based inactivation of CYP3A4, CYP2C9, CYP2C19, CYP2D6, and CYP1A2 in pooled human liver microsomes

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12 December 2020

High density synthetic oligonucleotide arrays

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12 December 2020

Plasma levels of monomethylated tricyclic antidepressants during treatment with imipramine-like compounds

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12 December 2020

Kinetic values for mechanism-based enzyme inhibition: assessing the bias introduced by the conventional experimental protocol.

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12 December 2020

Purified liver microsomal cytochrome P-450. Separation and characterization of multiple forms

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12 December 2020

Six-base deletion occurring in messages of human cytochrome P-450 in the CYP2C subfamily results in reduction of tolbutamide hydroxylase activity

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12 December 2020

Use of canalicular membrane vesicles (CMVs) from rats, dogs, monkeys and humans to assess drug transport across the canalicular membrane

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12 December 2020

Prediction of in vivo biliary clearance from the in vitro transcellular transport of organic anions across a double-transfected Madin-Darby canine kidney II monolayer expressing both rat organic anion transporting polypeptide 4 and multidrug resista

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12 December 2020

Polymorphic hydroxylation of Debrisoquine in man.

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12 December 2020

Molecular mechanisms of genetic polymorphisms of drug metabolism

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12 December 2020

Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity

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12 December 2020

Conversion of androstenedione to estrone by placental microsomes

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12 December 2020

An in vitro model for predicting in vivo inhibition of cytochrome P450 3A4 by metabolic intermediate complex formation.

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12 December 2020

Pharmacogenetic diagnostics of cytochrome P450 polymorphisms in clinical drug development and in drug treatment

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12 December 2020

Inactivation of the hepatic cytochrome P450 system by conditional deletion of hepatic cytochrome P450 reductase.

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12 December 2020

Effects of freezing, thawing, and storing human liver microsomes on cytochrome P450 activity.

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12 December 2020

Protein targets of xenobiotic reactive intermediates

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12 December 2020

Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites

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12 December 2020

Stereospecific, high affinity binding of 2,3,7,8-tetrachlorodibenzo-p-dioxin by hepatic cytosol. Evidence that the binding species is receptor for induction of aryl hydrocarbon hydroxylase

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12 December 2020

Clinical importance of the cytochromes P450

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12 December 2020

Utility of recombinant cytochrome p450 enzymes: a drug metabolism perspective.

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12 December 2020

Transgenic analysis of human drug-metabolizing enzymes: preclinical drug development and toxicology

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12 December 2020

Pharmacogenetics: a laboratory tool for optimizing therapeutic efficiency.

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12 December 2020

Pharmacogenomics, regulation and signaling pathways of phase I and II drug metabolizing enzymes

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12 December 2020

Common and uncommon cytochrome P450 reactions related to metabolism and chemical toxicity

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12 December 2020

DNA microarrays in drug discovery and development

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12 December 2020

Acetaminophen-induced hepatic necrosis. 3. Cytochrome P-450-mediated covalent binding in vitro

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12 December 2020

Gene expression in two hepatic cell lines, cultured primary hepatocytes, and liver slices compared to the in vivo liver gene expression in rats: possible implications for toxicogenomics use of in vitro systems

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12 December 2020

Mechanisms of oxygen metabolism

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12 December 2020

Detoxication of Drugs and Other Foreign Compounds by Liver Microsomes

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12 December 2020

Prediction of a new drug's potential to cause idiosyncratic reactions

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12 December 2020

Temperature-dependent cytosol-to-nucleus translocation of the Ah receptor for 2,3,7,8-tetrachlorodibenzo-p-dioxin in continuous cell culture lines

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12 December 2020

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

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12 December 2020

Resolution of the cytochrome P-450-containing omega-hydroxylation system of liver microsomes into three components

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12 December 2020

The effect of medroxyprogesterone acetate on the hepatic drug-metabolizing enzymes in normal and protein-deficient female rats

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12 December 2020

Diclofenac acyl glucuronide, a major biliary metabolite, is directly involved in small intestinal injury in rats

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12 December 2020

Species differences in the transport activity for organic anions across the bile canalicular membrane.

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12 December 2020

P-glycoprotein-mediated in vitro biliary excretion in sandwich-cultured rat hepatocytes.

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12 December 2020

Prediction of hepatic clearance from microsomes, hepatocytes, and liver slices

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12 December 2020

The cytochrome P450 superfamily: biochemistry, evolution and drug metabolism in humans

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12 December 2020

Cytochrome P450: what have we learned and what are the future issues?

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12 December 2020

Metabolic gene polymorphism frequencies in control populations

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12 December 2020

Challenges and limitations of gene expression profiling in mechanistic and predictive toxicology

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12 December 2020

CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes

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12 December 2020

Monitoring gene expression using DNA microarrays

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12 December 2020

Antimycotic drug discovery in the age of genomics

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12 December 2020

Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine

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12 December 2020

SXR, a novel steroid and xenobiotic-sensing nuclear receptor

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12 December 2020

Impact of drug transporter studies on drug discovery and development

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12 December 2020

Cytochrome P-450 of liver microsomes--one pigment or many

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12 December 2020

The role of orphan nuclear receptors in the regulation of cholesterol homeostasis

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12 December 2020

Steady-state plasma levels of nortriptyline in twins: influence of genetic factors and drug therapy

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12 December 2020

Enzyme kinetics for clinically relevant CYP inhibition

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12 December 2020

A comprehensive listing of bioactivation pathways of organic functional groups

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12 December 2020

Expression and regulation of cytochrome P450 enzymes in primary cultures of human hepatocytes

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12 December 2020

Substrates of human hepatic cytochrome P450 3A4.

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12 December 2020

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

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12 December 2020

The drugs don't work: expectations and the shaping of pharmacogenetics

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12 December 2020

Transporters and their impact on drug disposition

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12 December 2020

10.1007/S11095-006-9217-9

Identifiers

DOI

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16 August 2017

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