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Integrating the findings from several disciplines, Nuclear Receptors in Drug Metabolism enables readers to more accurately predict drug metabolism and drug-drug interactions as well as physiological outcomes. It offers a comprehensive review of the role of nuclear hormone receptors as transcriptional regulators of drug-metabolizing enzymes and transporters, helping readers understand what’s known, what’s in development, and what’s on the horizon. In addition to drug metabolism and drug development, the book also emphasizes clinical drug use, therapeutic potentials, and pharmacogenetics. Nuclear Receptors in Drug Metabolism features a team of expert authors. Their contributions are based not only on a thorough analysis and synthesis of the primary literature, but also their own firsthand experiences in the drug development labs. With their guidance, readers gain a deep understanding of how nuclear hormone receptors function in regulating drug-metabolizing enzymes and transporters. Among the topics covered are: * Establishing orphan nuclear receptors PXR and CAR as xenobiotic receptors * Nuclear receptor-mediated regulation of phase II conjugating enzymes and drug transporters * Structure and function of PXR and CAR * Animal models of xenobiotic nuclear receptors and their utility in drug development * Nuclear receptors and drug-drug interactions of prescription drugs and herbal medicines * Genetic variants of xenobiotic receptors and their implications in drug metabolism and pharmacogenetics * Regulation of drug-metabolizing enzymes and transporters by nuclear receptors other than PXR and CAR Drug development scientists will find a wealth of new information and approaches to support their efforts to develop new drugs that effectively treat such diseases as cancer, coronary heart disease, diabetes, and liver diseases. Wen Xie, MD, PHD, directs the Center for Pharmacogenetics at the University of Pittsburgh’s School of Pharmacy. Among the courses he teaches are Pharmaceutical Analysis: Nucleic Acid Techniques; Pharmacogenomics: Pharmacogenetics of Drug Metabolizing Enzymes; and Drug Development. Dr. Xie is the author or coauthor of nearly seventy journal articles and more than seventy invited lectures. Preface. Abbreviations. Contributors. Chapter 1. Drug Metabolism: Significance and Challenges (Chandra Prakash and Alfin D.N. Vaz). Chapter 2. Establishing Orphan Nuclear Receptors PXR and CAR as Xenobiotic Receptors (Tao Li, Junichiro Sonoda, and Ronald M. Evans). Chapter 3. Nuclear Receptor-Mediated Regulation of Phase II Conjugating Enzymes (Olivier Barbier). Chapter 4. Nuclear Receptor-Mediated Regulation of Drug Transporters (Oliver Burk). Chapter 5. Structure and Function of PXR and CAR (X. Edward Zhou and H. Eric Xu). Chapter 6. Xenobiotic Receptor CoFactors and Coregulators (John Y. L. Chiang). Chapter 7. Animal Models of Xenobiotic Nuclear Receptors and Their Utility in Drug Development (Haibiao Gong and Wen Xie). Chapter 8. Nuclear Receptors and Drug-Drug Interactions with Prescription Drugs and Herbal Medicines (Rommel G. Tirona and Richard B. Kim). Chapter 9. Genetic Variants of Xenobiotic Receptors and Their Implications in Drug Metabolism and Pharmacogenetics (Jatinder Lamba and Erin G. Schuetz). Chapter 10. Beyond PXR and CAR, Regulation of Xenobiotic Metabolism by Other Nuclear Receptors (Martin Wagner, Gernot Zollner, and Michael Trauner). Chapter 11. Emerging Role of Retinoid-Related Orphan Receptor (ROR) and Its Crosst alk With LXR(Liver X Receptor) in the Regulation Of Drug-Metabolizing Enzymes (Taira Wada and Wen Xie). Index.

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