04284nam 2200637Ia 450 991013952270332120170810190549.01-282-49134-297866124913440-470-53895-30-470-53894-5(CKB)2550000000007143(EBL)484843(OCoLC)587380806(SSID)ssj0000337317(PQKBManifestationID)11253889(PQKBTitleCode)TC0000337317(PQKBWorkID)10289234(PQKB)11188224(MiAaPQ)EBC484843(PPN)243318391(EXLCZ)99255000000000714320090401d2010 uy 0engur|n|---|||||txtccrEnzyme inhibition in drug discovery and development[electronic resource] the good and the bad /edited by Chuang Lu, Albert P. LiHoboken, NJ John Wileyc20101 online resource (878 p.)Description based upon print version of record.0-470-28174-X Includes bibliographical references and index.ENZYME INHIBITION IN DRUG DISCOVERY AND DEVELOPMENT; CONTENTS; PREFACE; CONTRIBUTORS; PART I. DRUG DISCOVERY APPROACHES AND TECHNOLOGIES; 1. The Drug Discovery Process; 2. Medicinal Chemistry of the Optimization of Enzyme Inhibitors; 3. Bioanalytical Technologies in Drug Discovery; 4. Safety Biomarkers in Drug Development: Emerging Trends and Implications; 5. The Role of Drug Metabolism in Drug Discovery; 6. Applied Pharmacokinetics in Drug Discovery and Development; PART II. INHIBITION OF THE DRUG METABOLIZING ENZYMES-THE UNDESIRABLE INHIBITION7. Enzyme Inhibition and Inactivation: Cytochrome P450 Enzymes8. Cytochrome P450 Induction; 9. Inhibition of Drug-Metabolizing Enzymes in the Gastrointestinal Tract and Its Influence on the Drug-Drug Interaction Prediction; 10. Enzyme Inhibition in Various In Vitro Systems; 11. Cytochrome P450 Degradation and Its Clinical Relevance; 12. Complexities of Working with UDP-Glucuronosyltransferases (UGTs): Focus on Enzyme Inhibition; 13. Evaluation of Inhibitors of Drug Metabolism in Human Hepatocytes; 14. Grapefruit Juice and Its Constituents as New Esterase Inhibitors15. Transporter-Xenobiotic Interactions: An Important Aspect of Drug Development Studies16. Polymorphisms of Drug Transporters and Their Clinical Implications; 17. Clinical Drug Interactions Due to Metabolic Inhibition: Prediction, Assessment, and Interpretation; 18. Predicting Interindividual Variability of Metabolic Drug-Drug Interactions: Identifying the Causes and Accounting for Them Using a Systems Approach; PART III. INHIBITION OF THE DRUG TARGET ENZYMES-THE DESIRABLE INHIBITION; 19. NF-κB: Mechanism, Tumor Biology, and Inhibitors; 20. G-Protein-Coupled Receptors as Drug Targets21. Pharmacological Modulation of Ion Channels for the Treatment of Chronic Pain22. Targeting the mTOR Pathway for Tumor Therapeutics; 23. HIV-1 Protease Inhibitors as Antiretroviral Agents; INDEXThe science and applied approaches of enzyme inhibition in drug discovery and development Offering a unique approach that includes both the pharmacologic and pharmaco-kinetic aspects of enzyme inhibition, Enzyme Inhibition in Drug Discovery and Development examines the scientific concepts and experimental approaches related to enzyme inhibition as applied in drug discovery and drug development. With chapters written by over fifty leading experts in their fields, Enzyme Inhibition in Drug Discovery and Development fosters a cross-fertilization of pharmacology, drug metabolism,Enzyme inhibitorsDrug developmentDrugsMetabolismEnzyme inhibitors.Drug development.DrugsMetabolism.615.35615/.19Lu Chuang989479Li A. P946693MiAaPQMiAaPQMiAaPQBOOK9910139522703321Enzyme inhibition in drug discovery and development2263021UNINA