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Encyclopedia of Drug Metabolism and Interactions, Volume 1, Fundamentals and Enzyme Systems

Encyclopedia of Drug Metabolism and Interactions, Volume 1, Fundamentals and Enzyme Systems

Alexander V. Lyubimov (Editor-in-Chief)

ISBN: 978-1-118-14975-1

Nov 2012

600 pages

Select type: Hardcover


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The ideal place to begin researching any question involving drug metabolism and interactions

The Encyclopedia of Drug Metabolism and Interactions provides essential support during all phases of drug development, from drug design to drug action and interaction within the human body. This six-volume work covers both preclinical and clinical aspects of drug metabolism and interactions. It also provides a wealth of toxicological, regulatory, and marketing information, all written and edited by leading international experts in the field.

By collecting and reviewing the current literature in the field in one expertly organized work, this encyclopedia is the ideal place to begin researching any question involving drug metabolism and interactions. Readers will find such important topics and working tools as:

  • Inhibited or induced enzymes and their impact on drug toxicity and altered response in both animal and human models
  • Effects of both genetic and non-genetic factors on drug metabolism
  • Relationships between a drug metabolism, its activation or inactivation, and a drug's potential toxicity/safety
  • Examples demonstrating all aspects of drug metabolism and interactions in silico, in vitro, in laboratory animals, and in humans
  • Methods and protocols enabling readers to perform seamless studies of metabolism and drug interactions

All articles are based on recent findings and standards of practice. By reviewing and contextualizing the current literature, the authors offer new perspectives on our current state of knowledge as well as future directions for research in drug metabolism and interactions. References at the end of each article serve as a gateway to the literature.

The Encyclopedia of Drug Metabolism and Interactions is recommended for researchers, physicians, and students at all levels. It introduces the basics to novices and explores the latest science and applications for more experienced investigators.

Contributors ix

Preface to the Encyclopedia xxiii

Preface—Volume 1 xxvii

PART I Basics Overview of Drug Metabolism 1

1 Review of Drug Metabolism in Drug Discovery and Development 3
Ronald E. White

2 In Vitro and In Vivo Models of Drug Metabolism 43
Michael A. Sinz

3 Enzyme Kinetics of Drug-Metabolizing Reactions and Drug–Drug Interactions 75
Melissa A. Kramer and Timothy S. Tracy

4 Sex Differences in Drug Metabolism 101
Thomas K. H. Chang and David J. Waxman

5 Species Differences of Drug-Metabolizing Enzymes 121
Joshua G. DeKeyser and Magang Shou

PART II Enzyme Systems Involved in Drug Metabolism and Interactions in Animals and Humans 159

6 Structure and Function of Cytochrome P450 Enzymes 161
Paul R. Ortiz de Montellano

7 Mechanisms of Cytochrome P450-Mediated Reactions 181
F. Peter Guengerich

8 Transcriptional Regulation of Cytochrome P450 Genes 205
Emily A. Fraser, Colin J. Henderson, and C. Roland Wolf

9 Cytochrome P450 Polymorphisms 239
Ulrich M. Zanger

10 Flavin-Containing Monooxygenase: The Role of Flavin-Containing Monooxgenase in Lead Design and Selection 275
John R. Cashman

11 Molybdenum-Containing Hydroxylases 305
Michael Zientek, Ping Kang, Matthew J. Hutzler, and Scott R. Obach

12 Amine Oxidases and Reductases 365
Ronald N. Hines and Russell A. Prough

13 Epoxide Hydrolases 393
Curtis J. Omiecinski, Xi Yang, and Elizabeth M. Laurenzana

14 Carboxylesterases 423
Bingfang Yan

15 UDP-Glucuronosyltransferases: Pharmacogenetics, Functional Characterization, and Clinical Relevance 457
Robert S. Foti and Michael B. Fisher

16 Sulfotransferases 529
Bennett Ma and Michael L. Schrag

17 Functional Genomics of the Human Glutathione Transferases 559
Philip G. Board

18 Amino Acid Conjugation: A Novel Route of Xenobiotic Carboxylic Acid Metabolism in Man 595
Kathleen M. Knights and John O. Miners

Index 611