CLINICAL AND TOXICOLOGICAL RELEVANCE OF CYP2C9: Drug-Drug Interactions and Pharmacogenetics

Pharmacogenomics: Translating Functional Genomics into Rational Therapeutics

1999 • 2,458 citations

Substrate recognition sites in cytochrome P450 family 2 (CYP2) proteins inferred from comparative analyses of amino acid and coding nucleotide sequences.

1992 • 1,168 citations

Association Between CYP2C9 Genetic Variants and Anticoagulation-Related Outcomes During Warfarin Therapy

2002 • 1,052 citations

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

1998 • 820 citations

Crystal structure of human cytochrome P450 2C9 with bound warfarin

2003 • 796 citations

Phosphorylation of Thr ⁴⁹⁵ Regulates Ca ²⁺ /Calmodulin-Dependent Endothelial Nitric Oxide Synthase Activity

2001 • 740 citations

Cytochrome P450 2C9 polymorphisms: a comprehensive review of the in-vitro and human data

2002 • 678 citations

Clinical relevance of genetic polymorphisms in the human CYP2C subfamily

2001 • 627 citations

The role of the CFP2C9-Leu 359 allelic variant in the tolbutamide polymorphism

1996 • 584 citations

Evaluation of Atypical Cytochrome P450 Kinetics with Two-Substrate Models: Evidence That Multiple Substrates Can Simultaneously Bind to Cytochrome P450 Active Sites

1998 • 508 citations

Endothelium-Derived Hyperpolarizing Factor Synthase (Cytochrome P450 2C9) Is a Functionally Significant Source of Reactive Oxygen Species in Coronary Arteries

2001 • 434 citations

The Structure of Human Cytochrome P450 2C9 Complexed with Flurbiprofen at 2.0-Å Resolution

2004 • 424 citations

In vitro-in vivo scaling of CYP kinetic data not consistent with the classical Michaelis-Menten model.

2000 • 388 citations

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

2002 • 350 citations

CYP2C9 allelic variants: ethnic distribution and functional significance

2002 • 333 citations

Effects of Prototypical Microsomal Enzyme Inducers on Cytochrome P450 Expression in Cultured Human Hepatocytes

2003 • 330 citations

Use of pharmacogenetics and clinical factors to predict the maintenance dose of warfarin

2003 • 326 citations

Developmental Expression of Human Hepatic CYP2C9 and CYP2C19

2003 • 312 citations

Genetic analysis of the human cytochrome P450 CYP2C9 locus

1996 • 300 citations

Structure of Mammalian Cytochrome P450 2B4 Complexed with 4-(4-Chlorophenyl)imidazole at 1.9-Å Resolution

2004 • 285 citations

The R144C change in the CYP2C9*2 allele alters interaction of the cytochrome P450 with NADPH:cytochrome P450 oxidoreductase

1997 • 269 citations

Transcriptional Regulation of CYP2C9 Gene

2002 • 260 citations

Atypical Kinetic Profiles in Drug Metabolism Reactions

2002 • 259 citations

Identification and Functional Characterization of a New CYP2C9 Variant (CYP2C9*5) Expressed among African Americans

2001 • 253 citations

Validation of Methods for CYP2C9 Genotyping: Frequencies of Mutant Alleles in a Swedish Population

1999 • 251 citations

Distribution of Soluble Epoxide Hydrolase and of Cytochrome P450 2C8, 2C9, and 2J2 in Human Tissues

2004 • 248 citations

Identification of a null allele of CYP2C9 in an African–American exhibiting toxicity to phenytoin

2001 • 237 citations

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

2003 • 218 citations

Metabolic Drug Interactions

2000 • 208 citations

Pharmacophore and three-dimensional quantitative structure activity relationship methods for modeling cytochrome p450 active sites.

2001 • 203 citations

Impact of CYP2C9 amino acid polymorphisms on glyburide kinetics and on the insulin and glucose response in healthy volunteers

2002 • 197 citations

Purification and characterization of six cytochrome P-450 isozymes from human liver microsomes

1983 • 192 citations

Population differences in S‐warfarin metabolism between CYP2C9 genotype‐matched Caucasian and Japanese patients

2003 • 191 citations

Gene structure ofCYP2C8 and extrahepatic distribution of the human CYP2Cs

1999 • 191 citations

Cytochrome P450 pathways of arachidonic acid metabolism

2002 • 188 citations

Cytochrome P450 oxidations in the generation of reactive electrophiles: epoxidation and related reactions

2002 • 185 citations

Structure of a Substrate Complex of Mammalian Cytochrome P450 2C5 at 2.3 Å Resolution: Evidence for Multiple Substrate Binding Modes^,

2003 • 182 citations

Inhibitory effects of amiodarone and its N‐deethylated metabolite on human cytochrome P450 activities: Prediction of in vivo drug interactions

2000 • 179 citations

Drug-activated nuclear receptors CAR and PXR

2003 • 177 citations

Structure of Mammalian Cytochrome P450 2C5 Complexed with Diclofenac at 2.1 Å Resolution: Evidence for an Induced Fit Model of Substrate Binding^,

2003 • 167 citations

Extrapolation of Diclofenac Clearance from in Vitro Microsomal Metabolism Data: Role of Acyl Glucuronidation and Sequential Oxidative Metabolism of the Acyl Glucuronide

2002 • 166 citations

Regio- and stereoselective epoxidation of arachidonic acid by human cytochromes P450 2C8 and 2C9.

1994 • 163 citations

Impact of CYP2C9 and CYP2C19 polymorphisms on tolbutamide kinetics and the insulin and glucose response in healthy volunteers.

2002 • 163 citations

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

2002 • 156 citations

The mechanism of the interaction between amiodarone and warfarin in humans

1992 • 155 citations

Cytochrome P450 enzyme polymorphisms and adverse drug reactions

2003 • 151 citations

Characterization of CYP2C19 and CYP2C9 from Human Liver: Respective Roles in Microsomal Tolbutamide,S-Mephenytoin, and Omeprazole Hydroxylations

1998 • 150 citations

Discovery of new potentially defective alleles of human CYP2C9

2004 • 142 citations

Analysis of Mammalian Cytochrome P450 Structure and Function by Site-Directed Mutagenesis

2001 • 140 citations

Combined phenotypic assessment of cytochrome P450 1A2, 2C9, 2C19, 2D6, and 3A, N-acetyltransferase-2, and xanthine oxidase activities with the “Cooperstown 5+1 cocktail”

2003 • 139 citations

Predicting Drug Metabolism: A Site of Metabolism Prediction Tool Applied to the Cytochrome P450 2C9

2003 • 137 citations

Frequency of cytochrome P450 2C9 mutant alleles in a Korean population

2001 • 135 citations

Re‐expression of C/EBPα induces CYP2B6, CYP2C9 and CYP2D6 genes in HepG2 cells

1998 • 131 citations

Polymorphism of the cytochrome P450 (CYP) 2C9 gene in Japanese epileptic patients: genetic analysis of the CYP2C9 locus

2000 • 130 citations

Nifedipine Increases Cytochrome P4502C Expression and Endothelium-Derived Hyperpolarizing Factor–Mediated Responses in Coronary Arteries

2000 • 128 citations

Interaction of Sulfaphenazole Derivatives with Human Liver Cytochromes P450 2C: Molecular Origin of the Specific Inhibitory Effects of Sulfaphenazole on CYP 2C9 and Consequences for the Substrate Binding Site Topology of CYP 2C9

1996 • 121 citations

Allelic variants of cytochromes P450 2C modify the risk for acute myocardial infarction

2003 • 111 citations

The Substrate Binding Site of Human Liver Cytochrome P450 2C9: An Approach Using Designed Tienilic Acid Derivatives and Molecular Modeling

1995 • 111 citations

Development of a Combined Protein and Pharmacophore Model for Cytochrome P450 2C9

2002 • 109 citations

The mechanism of the warfarin-rifampin drug interaction in humans

1987 • 109 citations

Study of P450 function using gene knockout and transgenic mice

2002 • 106 citations

Crystal structures of ligand complexes of P450eryF exhibiting homotropic cooperativity

2000 • 103 citations

Substrate selectivity of human cytochrome P450 2C9: importance of residues 476, 365, and 114 in recognition of diclofenac and sulfaphenazole and in mechanism-based inactivation by tienilic acid

2002 • 101 citations

Allosteric Behavior in Cytochrome P450-Dependent in Vitro Drug−Drug Interactions: A Prospective Based on Conformational Dynamics

2001 • 101 citations

A common genetic basis for idiosyncratic toxicity of warfarin and phenytoin

1999 • 100 citations

Uncommon P450-Catalyzed Reactions

2001 • 100 citations

Three- and four-dimensional-quantitative structure activity relationship (3D/4D-QSAR) analyses of CYP2C9 inhibitors.

2000 • 95 citations

A Refined 3-Dimensional QSAR of Cytochrome P450 2C9: Computational Predictions of Drug Interactions

2000 • 89 citations

Three-dimensional quantitative structure-activity relationship for inhibitors of cytochrome P4502C9.

1996 • 87 citations

Genetic polymorphisms and functional characterization of the 5′-flanking region of the human CYP2C9 gene: In vitro and in vivo studies

2001 • 86 citations

Structural Forms of Phenprocoumon and Warfarin That Are Metabolized at the Active Site of CYP2C9

1999 • 86 citations

Enzymatic Determinants of the Substrate Specificity of CYP2C9: Role of B‘−C Loop Residues in Providing the π-Stacking Anchor Site for Warfarin Binding

1999 • 83 citations

Transcriptional Regulation of Human CYP2C Genes: Functional Comparison of CYP2C9 and CYP2C18 Promoter Regions

1995 • 79 citations

Allosteric phenomena in cytochrome P450‐catalyzed monooxygenations

2001 • 74 citations

Activation of cytochrome P450 2C9-mediated metabolism: mechanistic evidence in support of kinetic observations

2003 • 71 citations

Catalytic Activity of Three Variants (Ile, Leu, and Thr) at Amino Acid Residue 359 in Human CYP2C9 Gene and Simultaneous Detection Using Single-Strand Conformation Polymorphism Analysis

2000 • 71 citations

Arginines 97 and 108 in CYP2C9 Are Important Determinants of the Catalytic Function

2000 • 69 citations

Putative active site template model for cytochrome P4502C9 (tolbutamide hydroxylase).

1996 • 66 citations

Differences in flurbiprofen pharmacokinetics between CYP2C9*1/*1, *1/*2, and *1/*3 genotypes

2003 • 63 citations

Homology modeling and substrate binding study of human CYP2C9 enzyme

1999 • 60 citations

Pharmacogenetics of acenocoumarol pharmacodynamics

2004 • 59 citations

Conformer- and Alignment-Independent Model for Predicting Structurally Diverse Competitive CYP2C9 Inhibitors

2004 • 54 citations

Differential Roles of Arg97, Asp293, and Arg108 in Enzyme Stability and Substrate Specificity of CYP2C9

2004 • 54 citations

Generation and Evaluation of a CYP2C9 Heteroactivation Pharmacophore

2003 • 53 citations

Analysis of CYP2C9*5 in Caucasian, Oriental and Black-African populations

2002 • 53 citations

Identification of Residues 286 and 289 as Critical for Conferring Substrate Specificity of Human CYP2C9 for Diclofenac and Ibuprofen

1998 • 50 citations

Identification of Amino Acid Substitutions that Confer a High Affinity for Sulfaphenazole Binding and a High Catalytic Efficiency for Warfarin Metabolism To P450 2C19

1998 • 49 citations

Minimal in vivo activation of CYP2C9-mediated flurbiprofen metabolism by dapsone

2001 • 47 citations

Potentiation of anticoagulant effect of warfarin caused by enantioselective metabolic inhibition by the uricosuric agent benzbromarone

1999 • 47 citations

5′-Flanking region polymorphisms of CYP2C9 and their relationship to S-warfarin metabolism in white and Japanese patients

2004 • 46 citations

Effector-Mediated Alteration of Substrate Orientation in Cytochrome P450 2C9

2004 • 46 citations

Relationships between the levels of cytochrome P4502C9 and its prototypic catalytic activities in human liver microsomes.

1994 • 45 citations

Identification of CYP2C9 as a Human Liver Microsomal Linoleic Acid Epoxygenase

2000 • 44 citations

Quantitative Binding Models for CYP2C9 Based on Benzbromarone Analogues

2004 • 37 citations

Targeted Antipeptide Antibodies to Cytochrome P450 2C18 Based on Epitope Mapping of an Inhibitory Monoclonal Antibody to P450 2C51

1997 • 35 citations

Introductory remarks on human CYPs

2002 • 35 citations

5‐Hydroxytryptamine is biotransformed by CYP2C9, 2C19 and 2B6 to hydroxylamine, which is converted into nitric oxide

2004 • 33 citations

A NEW CLASS OF CYP2C9 INHIBITORS: PROBING 2C9 SPECIFICITY WITH HIGH-AFFINITY BENZBROMARONE DERIVATIVES

2003 • 30 citations

Role of conserved Asp293 of cytochrome P450 2C9 in substrate recognition and catalytic activity

2003 • 28 citations

Enhancement of Anticoagulant Action by Warfarin—Benzbromarone Interaction

1996 • 16 citations

ASSESSMENT OF ARGININE 97 AND LYSINE 72 AS DETERMINANTS OF SUBSTRATE SPECIFICITY IN CYTOCHROME P450 2C9 (CYP2C9)

2004 • 14 citations