The Biochemistry of Drug Metabolism: Volume 1: Principles, Redox Reactions, Hydrolyses by Bernard Testa, Stefanie D. Kramer

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The Biochemistry of Drug Metabolism: Volume 1: Principles, Redox Reactions, Hydrolyses

Bernard Testa, Stefanie D. Kramer
332 pages
February 2008
The first of the two volumes is divided into three parts. Part One begins by introducing xenobiotics in the broad context of physiological metabolism, and continues with an overview of the processes of drug disposition and metabolism. It then goes on to summarize the macroscopic and microscopic locations of drug metabolism in animals and humans. This is followed by an introduction to the all-important issue of the consequences of drug and xenobiotic metabolism, providing an initial overview of pharmacokinetic, pharmacological and toxicological consequences. The last chapter examines drug metabolism in the context of drug research, with a focus on medicinal chemistry.
The second part is a major component of the book, corresponding to the role of oxidoreductases as major agents of metabolism. Cytochromes P450 receive particular attention, namely their multiplicity, structure, catalytic mechanisms, and the various reactions they catalyze, while other oxidoreductases are also presented, such as flavin monooxygenases, monoamine oxidases and other amine oxidases, aldehyde oxidase and xanthine dehydrogenase, peroxidases, and dehydrogenases-reductases. Each drug-metabolizing enzyme or enzyme family begins with an Enzyme Identity Card summarizing its nomenclature and biochemical essentials.
Part Three begins with a survey of the classification, properties and catalytic mechanism of the innumerable hydrolases known or suspected to play a role in xenobiotic metabolism. The focus then shifts to a systematic presentation of the various substrate classes, namely carboxylic esters, amides and peptides, lactams and lactones, esters of inorganic acids, alkene and arene epoxides, and some miscellaneous hydrolyzable moieties.

With a foreword by Prof Leslie Z. Benet, the world's best and best-known biopharmaceutical scientist
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 Discovery

Part 2: Redox Reactions and Their Enzymes
2.1. Cytochromes P450 (CYPs) and Flavin-Containing Monooxygenases (FMOs)
2.2. CYP-Catalyzed sp3-C-Oxidations
2.2. 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
"These two volumes provide a comprehensive scientific basis for the study of the biochemistry of drug metabolism. The text is practically organized with extensive literature and information figures. As well as providing fundamental knowledge towards understanding the principles of drug metabolism, to those new
to the subject, both volumes represent an invaluable reference for researchers in the field of biochemistry, pharmacology and new drug development". (Anticancer Research, 1 August 2010)

Many readers will find the concise way that information can be communicated very time saving and helpful." (BTS Newsletter, Summer 2010)

"As for the book, if you are interested in teaching, studying or are already a drug metabolism professional my advice to you is buy it, and snap up volume 2 as soon as it becomes available." (Chromatographia, March 2009)

"An excellent book ... .Extraordinarily detailed, yet presented in a clear and attractive manner." (Journal of Medical Chemistry, July 2009)

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