The Biochemistry of Drug Metabolism
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Bernard Testa and Stefanie D. Krämer

The Biochemistry of Drug Metabolism: Principles, Redox Reactions, Hydrolyses

Volume 1




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March 2008
319 Pages, Softcover
ISBN-10: 3-906390-53-5
ISBN-13: 978-3-906390-53-6



In this first of this two-volume work, the authors draw on their extensive experience as researchers and graduate teachers to offer a vivid, richly informative and, above all, instructive presentation of three major aspects of drug and xenobiotic metabolism. Divided into three parts, the first presents general principles and an overview of this fast evolving field, providing an initial overview of pharmacokinetic, pharmacological and toxicological consequences. The second part covers metabolic reactions of oxidation and reduction, with a strong emphasis on cytochromes P450, their catalytic mechanisms and the various types of reactions they catalyze. Part Three is dedicated to the innumerable hydrolases known or suspected to play a role in xenobiotic metabolism, and the many types of substrates they hydrolyze.


Part 1: Principles and Overview
1.1. Drugs and Xenobiotics
1.2. What Are Drug Disposition and Metabolism?
1.3. Where Does Drug Metabolism Occur?
1.4. Consequences of Drug Metabolism – An Overview
1.5. Drug Metabolism and Drug Research

Part 2: Redox Reactions and Their Enzymes
2.1. Cytochromes P450 (CYPs) and Flavin Monooxygenases (FMOs)
2.2. CYP-Catalyzed sp3-C-Oxidations
2.3. CYP-Catalyzed sp2-C- and sp-C-Oxidations
2.4. Oxidations of N- and S-Atoms Catalyzed by CYPs and/or FMOs
2.5. Other Reactions Catalyzed by CYPs
2.6. Other Oxidoreductases and Their Reactions

Part 3: Reactions of Hydrolysis and Their Enzymes
3.1. A Survey of Hydrolases
3.2. The Hydrolysis of Carboxylic Esters
3.3. Synthetic Reactions of Esterases
3.4. The Hydrolysis of Amides and Peptides
3.5. Hydrolytic Ring Opening
3.6. The Hydrolysis of Esters of Inorganic Acids
3.7. The Hydration of Epoxides
3.8. Miscellaneous Reactions