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Microbial polymers. --- Plastics --- Biotransformation (Metabolism) --- Biotransformation (Métabolisme) --- Microbiology.

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Enzymes --- Biotransformation (Metabolism) --- Biotechnology --- Biotransformation --- Catalysis --- Industrial applications --- Biotechnologies --- Biocatalysts --- Catalyses --- Activation, Metabolic --- Bioactivation (Metabolism) --- Biodegradation (Metabolism) --- Metabolic activation --- Ferments --- Soluble ferments --- Molecular Mechanisms of Pharmacological Action --- Metabolism --- Pharmacology --- Catalysts --- Proteins --- Enzymology --- Biocatalyst --- Enzyme --- Catalysis. --- Enzymes. --- Biotechnology. --- Biotransformation. --- Biology

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I have always been interested in chemistry and biology. My undergraduate, graduate, and postdoctoral trainings in pharmacy, medicinal chemistry and pharmacology, respectively, have strengthened this interest and led me to realize that significant advances in medicine have frequently been realized because of research at the chem- try–biology interface. I am hoping that this comprehensive volume on recent advances in bioactivation research will stimulate pharmacologists, medicinal chemists, phar- ceutical scientists, and graduate students in these fields and related areas to consider and use bioactivation research when they explore and chart new frontiers in drug design and drug development and when they consider ways to reduce the side effects of existing drugs by making prodrugs. As for the toxicologists and environmental health scientists, I hope this volume will help them generate the knowledge needed to understand better mechanisms of toxicity to improve human risk assessments and intervention methods after occupational or environmental exposure to various hazardous chemicals. Adnan A. Elfarra, Ph. D. vii Part I General Concepts and Basic Mechanisms 1 Metabolic Concerns in Drug Design Jeffrey P. Jones Department of Chemistry, Washington State University, Pullman, WA 99164, USA e-mail: jpj@wsu. edu Keywords: Cytochrome P450 Aldehyde Oxidase Drug–Drug Interactions Mechanism-based Virtual Screening ADMET Regioselectivity 1. 1. Introduction Due to recent technological innovations, such as genomics, combinatorial chemistry, and high-throughput screening, the identification of disease targets and of compounds that are active against these targets (‘‘leads’’) can now be carried out efficiently.

Biomedicine. --- Pharmacology/Toxicology. --- Immunology. --- Medicine. --- Toxicology. --- Médecine --- Immunologie --- Toxicologie --- Biotransformation (Metabolism). --- Biotransformation. --- Drug activation. --- Biotransformation (Metabolism) --- Drug activation --- Pharmacological Processes --- Metabolism --- Metabolic Phenomena --- Pharmacological Phenomena --- Physiological Processes --- Physiological Phenomena --- Phenomena and Processes --- Biotransformation --- Human Anatomy & Physiology --- Health & Biological Sciences --- Animal Biochemistry --- Activation, Metabolic --- Bioactivation (Metabolism) --- Biodegradation (Metabolism) --- Metabolic activation --- Activation of drugs --- Drugs --- Activation --- Pharmacology. --- Pharmacology --- Immunobiology --- Life sciences --- Serology --- Chemicals --- Medicine --- Poisoning --- Poisons --- Toxicology --- Drug effects --- Medical pharmacology --- Medical sciences --- Chemotherapy --- Pharmacy --- Physiological effect

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The use of biocatalysts, employed either as isolated enzymes or whole microbial cells, offers a remarkable arsenal of highly selective transformations for state-of-the-art synthetic organic chemistry. Over the last two decades, this methodology has become an indispensable tool for asymmetric synthesis, not only at the academic level, but also on an industrial scale. This well-established textbook on biocatalysis provides a basis for undergraduate and graduate courses in modern organic chemistry, as well as a condensed introduction into this field. After a basic introduction into the use of biocatalysts—principles of stereoselective transformations, enzyme properties and kinetics—the different types of reactions are explained according to the 'reaction principle', such as hydrolysis, reduction, oxidation, C–C bond formation, etc. Special techniques, such as the use of enzymes in organic solvents, immobilization techniques and modified or artificial enzymes, are treated in a separate section. A final chapter deals with thebasic rules for the safe and practical handling of biocatalysts. In this completely revised 6th edition, emphasis has been given to an improved didactic style including colored graphics in order to facilitate a deeper understanding of the underlying principles. New developments, such as transamination, enzyme promiscuity and applications on industrial scale within the field of 'white biotechnology' are included.

Biotransformation (Metabolism). --- Enzymes -- Biotechnology. --- Organic compounds -- Synthesis. --- Chemistry --- Physical Sciences & Mathematics --- Biochemistry --- Enzymes --- Biotransformation (Metabolism) --- Organic compounds --- Biotechnology. --- Synthesis. --- Chemistry, Organic --- Chemistry, Synthetic organic --- Organic synthesis (Chemistry) --- Synthetic organic chemistry --- Activation, Metabolic --- Bioactivation (Metabolism) --- Biodegradation (Metabolism) --- Metabolic activation --- Synthesis --- Chemistry. --- Organic chemistry. --- Biochemistry. --- Organic Chemistry. --- Biochemistry, general. --- Metabolism --- Pharmacology --- Chemistry, Organic. --- Biological chemistry --- Chemical composition of organisms --- Organisms --- Physiological chemistry --- Biology --- Medical sciences --- Chemical engineering --- Genetic engineering --- Organic chemistry --- Composition

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Metabolic Detoxication, Drug --- Enzymes --- Xenobiotics --- Metabolism --- Xénobiotiques --- Métabolisme --- Inactivation, Metabolic. --- -Metabolic detoxification --- Chemicals --- Detoxication, Metabolic --- Detoxification, Metabolic --- Metabolic detoxication --- Biotransformation (Metabolism) --- Metabolic conjugation --- Foreign chemical compounds --- Foreign compounds --- Xenobiotic compounds --- Biochemistry --- Biocatalysts --- Ferments --- Soluble ferments --- Catalysts --- Proteins --- Enzymology --- Detoxification, Drug, Metabolic --- Metabolic Detoxification, Drug --- Metabolic Drug Inactivation --- Detoxication, Drug, Metabolic --- Drug Detoxication, Metabolic --- Detoxication, Drug Metabolic --- Detoxication, Metabolic Drug --- Detoxification, Drug Metabolic --- Drug Inactivation, Metabolic --- Drug Metabolic Detoxication --- Drug Metabolic Detoxification --- Inactivation, Metabolic Drug --- Metabolic Drug Detoxication --- Metabolic Inactivation --- metabolism. --- Metabolic detoxification --- Xénobiotiques --- Métabolisme --- Inactivation, Metabolic --- metabolism