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Drug−Protein Adducts: An Industry Perspective on Minimizing the Potential for Drug Bioactivation in Drug Discovery and Development

Chemical research in toxicology, 2004-01, Vol.17 (1), p.3-16

2004

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Drug Metabolites in Safety Testing

Toxicology and applied pharmacology, 2002-08, Vol.182 (3), p.188-196

2002

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Organic Chemistry in Drug Discovery

Science (American Association for the Advancement of Science), 2004-03, Vol.303 (5665), p.1810-1813

2004

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Is the role of the small intestine in first-pass metabolism overemphasized?

Pharmacological reviews, 1999-06, Vol.51 (2), p.135

1999

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Studies on the Metabolism of Troglitazone to Reactive Intermediates in Vitro and in Vivo. Evidence for Novel Biotransformation Pathways Involving Quinone Methide Formation and Thiazolidinedione Ring Scission

Chemical research in toxicology, 2001-01, Vol.14 (1), p.62-70

2001

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Metabolism and Toxicity of Drugs. Two Decades of Progress in Industrial Drug Metabolism

Chemical research in toxicology, 2008-01, Vol.21 (1), p.129-137

Baillie, Thomas A

2008

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Studies on cytochrome P-450-mediated bioactivation of diclofenac in rats and in human hepatocytes: identification of glutathione conjugated metabolites

Drug metabolism and disposition, 1999-03, Vol.27 (3), p.365

1999

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Bioactivation of diclofenac via benzoquinone imine intermediates-identification of urinary mercapturic acid derivatives in rats and humans

Drug metabolism and disposition, 2001-12, Vol.29 (12), p.1608

2001

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Zafirlukast Metabolism by Cytochrome P450 3A4 Produces an Electrophilic α,β-Unsaturated Iminium Species That Results in the Selective Mechanism-Based Inactivation of the Enzyme

Chemical research in toxicology, 2005-09, Vol.18 (9), p.1427-1437

2005

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Cytochrome P450 3A4-Mediated Bioactivation of Raloxifene: Irreversible Enzyme Inhibition and Thiol Adduct Formation

Chemical research in toxicology, 2002-07, Vol.15 (7), p.907-914

2002

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Assessing and minimizing time-dependent inhibition of cytochrome P450 3A in drug discovery: A case study with melanocortin-4 receptor agonists

Xenobiotica, 2008-11, Vol.38 (11), p.1437-1451

2008

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Evaluation of microdosing strategies for studies in preclinical drug development: demonstration of linear pharmacokinetics in dogs of a nucleoside analog over a 50-fold dose range

Drug metabolism and disposition, 2004-11, Vol.32 (11), p.1254

2004

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Tumour vasculature - a potential therapeutic target

British journal of cancer, 1995-08, Vol.72 (2), p.257-267

1995

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Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats

Xenobiotica, 2008-02, Vol.38 (2), p.223-237

2008

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Influence of different recombinant systems on the cooperativity exhibited by cytochrome P4503A4

Xenobiotica, 2004-05, Vol.34 (5), p.473-486

2004

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Metabolism of the Chemoprotective Agent Diallyl Sulfide to Glutathione Conjugates in Rats

Chemical research in toxicology, 1997-03, Vol.10 (3), p.318-327

1997

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Mechanistic studies on the reversible metabolism of rofecoxib to 5-hydroxyrofecoxib in the rat: evidence for transient ring opening of a substituted 2-furanone derivative using stable isotope-labeling techniques

Drug metabolism and disposition, 2001-12, Vol.29 (12), p.1614

2001

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Metabolic Activation of a 1,3-Disubstituted Piperazine Derivative: Evidence for a Novel Ring Contraction to an Imidazoline

Chemical research in toxicology, 2005-02, Vol.18 (2), p.271-276

2005

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Mechanistic Studies on the Metabolic Scission of Thiazolidinedione Derivatives to Acyclic Thiols

Chemical research in toxicology, 2005-05, Vol.18 (5), p.880-888

2005

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Enzyme kinetics of cytochrome P450-mediated reactions

Current drug metabolism, 2001-03, Vol.2 (1), p.17-36

2001

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Taurine conjugation of ibuprofen in humans and in rat liver in vitro. Relationship to metabolic chiral inversion

The Journal of pharmacology and experimental therapeutics, 1994-06, Vol.269 (3), p.1166

1994

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Identification of Novel Glutathione Conjugates of Disulfiram and Diethyldithiocarbamate in Rat Bile by Liquid Chromatography-Tandem Mass Spectrometry. Evidence for Metabolic Activation of Disulfiram in vivo

Chemical research in toxicology, 1994-07, Vol.7 (4), p.526-533

1994

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Interaction of diclofenac and quinidine in monkeys: stimulation of diclofenac metabolism

The Journal of pharmacology and experimental therapeutics, 1999-12, Vol.291 (3), p.1068

1999

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Studies on the beta-oxidation of valproic acid in rat liver mitochondrial preparations

Drug metabolism and disposition, 1991-07, Vol.19 (4), p.823

1991

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Cytochrome P-450-mediated dehydrogenation of 2-n-propyl-2(E)-pentenoic acid, a pharmacologically-active metabolite of valproic acid, in rat liver microsomal preparations

Drug metabolism and disposition, 1993-03, Vol.21 (2), p.242

1993

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Drug−Protein Adducts: An Industry Perspective on Minimizing the Potential for Drug Bioactivation in Drug Discovery and Development

Drug Metabolites in Safety Testing

Organic Chemistry in Drug Discovery

Is the role of the small intestine in first-pass metabolism overemphasized?

Studies on the Metabolism of Troglitazone to Reactive Intermediates in Vitro and in Vivo. Evidence for Novel Biotransformation Pathways Involving Quinone Methide Formation and Thiazolidinedione Ring Scission

Metabolism and Toxicity of Drugs. Two Decades of Progress in Industrial Drug Metabolism

Studies on cytochrome P-450-mediated bioactivation of diclofenac in rats and in human hepatocytes: identification of glutathione conjugated metabolites

Bioactivation of diclofenac via benzoquinone imine intermediates-identification of urinary mercapturic acid derivatives in rats and humans

Zafirlukast Metabolism by Cytochrome P450 3A4 Produces an Electrophilic α,β-Unsaturated Iminium Species That Results in the Selective Mechanism-Based Inactivation of the Enzyme

Cytochrome P450 3A4-Mediated Bioactivation of Raloxifene: Irreversible Enzyme Inhibition and Thiol Adduct Formation

Assessing and minimizing time-dependent inhibition of cytochrome P450 3A in drug discovery: A case study with melanocortin-4 receptor agonists

Evaluation of microdosing strategies for studies in preclinical drug development: demonstration of linear pharmacokinetics in dogs of a nucleoside analog over a 50-fold dose range

Tumour vasculature - a potential therapeutic target

Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats

Influence of different recombinant systems on the cooperativity exhibited by cytochrome P4503A4

Metabolism of the Chemoprotective Agent Diallyl Sulfide to Glutathione Conjugates in Rats

Mechanistic studies on the reversible metabolism of rofecoxib to 5-hydroxyrofecoxib in the rat: evidence for transient ring opening of a substituted 2-furanone derivative using stable isotope-labeling techniques

Metabolic Activation of a 1,3-Disubstituted Piperazine Derivative: Evidence for a Novel Ring Contraction to an Imidazoline

Mechanistic Studies on the Metabolic Scission of Thiazolidinedione Derivatives to Acyclic Thiols

Enzyme kinetics of cytochrome P450-mediated reactions

Taurine conjugation of ibuprofen in humans and in rat liver in vitro. Relationship to metabolic chiral inversion

Identification of Novel Glutathione Conjugates of Disulfiram and Diethyldithiocarbamate in Rat Bile by Liquid Chromatography-Tandem Mass Spectrometry. Evidence for Metabolic Activation of Disulfiram in vivo

Interaction of diclofenac and quinidine in monkeys: stimulation of diclofenac metabolism

Studies on the beta-oxidation of valproic acid in rat liver mitochondrial preparations

Cytochrome P-450-mediated dehydrogenation of 2-n-propyl-2(E)-pentenoic acid, a pharmacologically-active metabolite of valproic acid, in rat liver microsomal preparations

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