Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates.

Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians.

1994 • 2,716 citations

The Human Hepatic Cytochromes P450 Involved in Drug Metabolism

1992 • 932 citations

Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism.

1997 • 767 citations

Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism.

1986 • 734 citations

Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4.

1989 • 528 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

Human liver carbamazepine metabolism

1994 • 428 citations

Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes.

1990 • 423 citations

Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat.

1992 • 382 citations

Activation of CYP3A4: Evidence for the Simultaneous Binding of Two Substrates in a Cytochrome P450 Active Site

1994 • 348 citations

Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes.

1996 • 342 citations

Oxidation of quinidine by human liver cytochrome P-450.

1986 • 296 citations

In vitro metabolism of simvastatin in humans [SBT]identification of metabolizing enzymes and effect of the drug on hepatic P450s.

1997 • 274 citations

Identification of human liver cytochrome P450 isoforms mediating omeprazole metabolism

1993 • 225 citations

Hepatic biotransformation of docetaxel (Taxotere) in vitro: involvement of the CYP3A subfamily in humans.

1996 • 224 citations

The involvement of CYP1A2 and CYP3A4 in the metabolism of clozapine

1997 • 219 citations

Speculations on the Substrate Structure-Activity Relationship (SSAR) of cytochrome P450 enzymes

1992 • 203 citations

Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cdna-expressed human cytochrome P450.

1996 • 191 citations

Identification of the cytochrome P450 IIIA family as the enzymes involved in the N-demethylation of tamoxifen in human liver microsomes

1991 • 185 citations

QSAR and 3D QSAR in drug design Part 2: applications and problems

1997 • 173 citations

Further characterization of the expression in liver and catalytic activity of CYP2B6.

1998 • 173 citations

Metabolism of fentanyl, a synthetic opioid analgesic, by human liver microsomes. Role of CYP3A4.

1996 • 171 citations

Involvement of cytochrome P450 3A4 in N-dealkylation of buprenorphine in human liver microsomes

1997 • 158 citations

Involvement of human liver cytochrome P450 3A in vinblastine metabolism: drug interactions.

1993 • 157 citations

Metabolism of irinotecan (CPT-11) by human hepatic microsomes: participation of cytochrome P-450 3A and drug interactions.

1998 • 157 citations

A predictive model for substrates of cytochrome P450-debrisoquine (2D6)

1992 • 152 citations

Alanine-scanning Mutagenesis of a Putative Substrate Recognition Site in Human Cytochrome P450 3A4

1997 • 148 citations

Species differences in the pharmacokinetics and metabolism of indinavir, a potent human immunodeficiency virus protease inhibitor.

1996 • 143 citations

Human cytochrome P450 3A4-catalyzed testosterone 6 beta-hydroxylation and erythromycin N-demethylation. Competition during catalysis.

1997 • 140 citations

Role of CYP3A4 in human hepatic diltiazem N-demethylation: inhibition of CYP3A4 activity by oxidized diltiazem metabolites.

1997 • 132 citations

Molecular modeling of cytochrome P450 3A4.

1997 • 129 citations

Metabolism of FK506, a potent immunosuppressive agent, by cytochrome P450 3A enzymes in rat, dog and human liver microsomes

1994 • 124 citations

Oxidative metabolism of clarithromycin in the presence of human liver microsomes. Major role for the cytochrome P4503A (CYP3A) subfamily.

1997 • 120 citations

Analysis of Four Residues within Substrate Recognition Site 4 of Human Cytochrome P450 3A4: Role in Steroid Hydroxylase Activity and α-Naphthoflavone Stimulation

1998 • 116 citations

Colchicine biotransformation by human liver microsomes

1997 • 114 citations

Properties of cytochrome P450 isoenzymes and their substrates part 2: properties of cytochrome P450 substrates

1997 • 113 citations

Dexamethasone metabolism by human liver in vitro. Metabolite identification and inhibition of 6-hydroxylation.

1996 • 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

MS-WHIM, new 3D theoretical descriptors derived from molecular surface properties: a comparative 3D QSAR study in a series of steroids.

1997 • 110 citations

Evidence for CYP3A-mediated N-deethylation of amiodarone in human liver microsomal fractions.

1993 • 97 citations

In Vivo Pharmacokinetics of Felodipine Predicted from in Vitro Studies in Rat, Dog and Man

1986 • 95 citations

Three-dimensional quantitative structure activity relationship analyses of substrates for CYP2B6.

1999 • 93 citations

Role of cytochrome P450IIIA4 in the metabolism of the pyrrolizidine alkaloid senecionine in human liver

1991 • 93 citations

Reconstitution Premixes for Assays Using Purified Recombinant Human Cytochrome P450, NADPH-Cytochrome P450 Reductase, and Cytochromeb5

1997 • 90 citations

Predictability of the in vivo metabolism of verapamil from in vitro data: contribution of individual metabolic pathways and stereoselective aspects.

1992 • 90 citations

Properties of cytochrome P450 isoenzymes and their substrates Part 1: active site characteristics

1997 • 89 citations

Interaction of human liver cytochromes P450 in vitro with LY307640, a gastric proton pump inhibitor

1996 • 89 citations

Molecular modelling of CYP3A4 from an alignment with CYP102: Identification of key interactions between putative active site residues and CYP3A-specific chemicals

1996 • 88 citations

CO Binding Kinetics of Human Cytochrome P450 3A4

1995 • 88 citations

Molecular modelling of CYP1A subfamily members based on an alignment with CYP102: rationalization of CYP1A substrate specificity in terms of active site amino acid residues

1996 • 83 citations

Cytochrome P450 3A-mediated human liver microsomal taxol 6 alpha-hydroxylation.

1994 • 82 citations

Metabolism of rifabutin in human enterocyte and liver microsomes: Kinetic parameters, identification of enzyme systems, and drug interactions with macrolides and antifungal agents*

1997 • 82 citations

Overlapping substrate specificities of cytochrome P450 3A and P-glycoprotein for a novel cysteine protease inhibitor.

1998 • 82 citations

Human liver microsomal cytochrome P450 3A isozymes mediated vindesine biotransformation

1993 • 80 citations

Three-dimensional models of human and other mammalian microsomal P450s constructed from an alignment with P450102 (P450_bm3)

1995 • 78 citations

Identification of Three Key Residues in Substrate Recognition Site 5 of Human Cytochrome P450 3A4 by Cassette and Site-Directed Mutagenesis

1997 • 77 citations

Identification of human cytochrome P450 isoforms involved in the 3-hydroxylation of quinine by human live microsomes and nine recombinant human cytochromes P450.

1996 • 73 citations

Autoactivation and activation of the cytochrome P450s.

1998 • 72 citations

In vitro metabolism of terfenadine by a purified recombinant fusion protein containing cytochrome P4503A4 and NADPH-P450 reductase. Comparison to human liver microsomes and precision-cut liver tissue slices.

1995 • 69 citations

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

1996 • 66 citations

In vitro metabolism of dexamethasone (DEX) in human liver and kidney: The involvement of CYP3a4 and CYP17 (17,20 LYASE) and molecular modelling studies

1997 • 53 citations

Drug-drug interactions: Effect of quinidine on nifedipine binding to human cytochrome P450 3A4

1997 • 48 citations

Identification of CYP3A4 as the principal enzyme catalyzing mifepristone (RU 486) oxidation in human liver microsomes

1996 • 47 citations

Kinetic Characterization and Identification of the Enzymes Responsible for the Hepatic Biotransformation of Adinazolam and N-Desmethyladinazolam in Man

1998 • 46 citations

Characterization of Six in vitro Reactions Mediated by Human Cytochrome P450: Application to the Testing of Cytochrome P450-Directed Antibodies

1996 • 45 citations

Identification of the human liver cytochrome P450 enzymes involved in the metabolism of zileuton (ABT-077) and its N-dehydroxylated metabolite, Abbott-66193.

1995 • 43 citations

Biotransformation of tirilazad in human: 1. Cytochrome P450 3A-mediated hydroxylation of tirilazad mesylate in human liver microsomes.

1996 • 40 citations

Metabolism of fentanyl, A synthetic opioid analgesic, by human liver microsomes

1996 • 39 citations

Molecular modelling and quantitative structure-activity relationship studies on the interaction of omeprazole with cytochrome P450 isozymes

1998 • 38 citations

Metabolism of the new immunosuppressor cyclosporin G by human liver cytochromes P450

1996 • 32 citations

Cortisol metabolism in vitro—III. Inhibition of microsomal 6β—hydroxylase and cytosolic 4-ene-reductase

1993 • 28 citations

The active site of cytochrome P-450 nifedipine oxidase: a model-building study

1989 • 28 citations

In vitro metabolism of zatosetron. Interspecies comparison and role of CYP 3A.

1994 • 24 citations

Steady State Enzyme Velocities That Are Independent of [Enzyme]: An Important Behavior in Many Membrane and Particle-Bound States

1997 • 24 citations

Cytochrome P-450 3A4 (nifedipine oxidase) is responsible for the C-oxidative metabolism of 1-nitropyrene in human liver microsomal samples.

1992 • 23 citations

In vitro biotransformation and identification of human cytochrome P450 isozyme-dependent metabolism of tazofelone.

1997 • 19 citations

Monoacetyldapsone inhibition of dapsone N-hydroxylation by human and rat liver microsomes.

1994 • 12 citations

Cytochrome P4503A4-mediated N-demethylation of the antiprogestins lilopristone and onapristone.

1997 • 9 citations