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A compendium of proven experimental approaches and strategies for studying the bioactivation, detoxification, tissue distribution, and elimination of xenobiotics in the metabolism and/or transport of various chemicals. The authors address several of the major drug metabolizing systems, including the cytochrome P450 family, flavin-containing monooxygenases, glutathione, S-transferase, glucuronidation, N-acetylation, and sulfotransferases. Additional chapters present novel approaches to the study of: signaling pathways in the regulation of drug metabolism enzymes, how the modulation of thiols and other low molecular-weight cofactors can alter drug metabolism, and how modulation of drug metabolism pathways can influence antiviral therapy.Remarkable advances in molecular and cell biology and the development of novel in vitro model systems have greatly expanded our knowledge of the processes involved in metabolism and transport and led to numerous new therapeutic approaches. In Drug Metabolism and Transport: Molecular Methods and Mechanisms, well-established investigators describe their best experimental approaches and strategies for studying the bioactivation, detoxification, tissue distribution, and elimination of xenobiotics in the metabolism and/or transport of various chemicals. The authors address several of the major drug metabolizing systems, including the cytochrome P450 family, flavin-containing monooxygenases, glutathione, glucuronidation, N-acetylation, and sulfotransferases. Additional chapters present novel approaches to the study of: signaling pathways in the regulation of drug metabolism enzymes, how the modulation of thiols and other low-molecular-weight cofactors can alter drug metabolism, and how modulation of drug metabolism pathways can influence antiviral therapy. The strategies detailed for transport phenomena cover the multidrug resistance proteins, the reduced folate carrier, the plasma membrane, and mitochondrial glutathione transporters, and can be applied to numerous other transport systems. Many chapters contain step-by-step methods for investigating metabolism and transport.§Insightful and broad-ranging, Drug Metabolism and Transport: Molecular Methods and Mechanisms offers novice and experienced investigators alike a highly useful compendium of key strategies and approaches to successful research on drug metabolism and transport pathways.