LEADER 04286nam 2200637Ia 450 001 9910830438803321 005 20170810190549.0 010 $a1-282-49134-2 010 $a9786612491344 010 $a0-470-53895-3 010 $a0-470-53894-5 035 $a(CKB)2550000000007143 035 $a(EBL)484843 035 $a(OCoLC)587380806 035 $a(SSID)ssj0000337317 035 $a(PQKBManifestationID)11253889 035 $a(PQKBTitleCode)TC0000337317 035 $a(PQKBWorkID)10289234 035 $a(PQKB)11188224 035 $a(MiAaPQ)EBC484843 035 $a(PPN)243318391 035 $a(EXLCZ)992550000000007143 100 $a20090401d2010 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aEnzyme inhibition in drug discovery and development$b[electronic resource] $ethe good and the bad /$fedited by Chuang Lu, Albert P. Li 210 $aHoboken, NJ $cJohn Wiley$dc2010 215 $a1 online resource (878 p.) 300 $aDescription based upon print version of record. 311 $a0-470-28174-X 320 $aIncludes bibliographical references and index. 327 $aENZYME 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 INHIBITION 327 $a7. 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 Inhibitors 327 $a15. 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-?B: Mechanism, Tumor Biology, and Inhibitors; 20. G-Protein-Coupled Receptors as Drug Targets 327 $a21. 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; INDEX 330 $aThe 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, 606 $aEnzyme inhibitors 606 $aDrug development 606 $aDrugs$xMetabolism 615 0$aEnzyme inhibitors. 615 0$aDrug development. 615 0$aDrugs$xMetabolism. 676 $a615.35 676 $a615/.19 701 $aLu$b Chuang$01701146 701 $aLi$b A. P$01616272 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910830438803321 996 $aEnzyme inhibition in drug discovery and development$94084702 997 $aUNINA