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OverviewThis second edition further develops the principles of applying kinetic principles to drug metabolizing enzymes and transporters. Chapters are divided into six sections detailing fundamental principles of enzyme kinetics, enzyme and transporter structures, highlighting specific oxidative and conjugative drug metabolizing enzymes and drug transporters, modeling approaches for drug metabolizing enzymes and transporters, understanding of variability both experimental and interindividual (pharmacogenomic), and expanded case studies that provide real life examples of applying these principles. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, in some cases step-by-step instructions with readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls with extensive cross referencing to assist in learning. Authoritativeand fully updated, Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications, Second Edition serves as a practical teaching tool for novice and advanced scientists interested in the fundamental concepts. Full Product DetailsAuthor: Swati Nagar , Upendra A. Argikar , Donald TweediePublisher: Springer-Verlag New York Inc. Imprint: Springer-Verlag New York Inc. Edition: 2nd ed. 2021 Volume: 2342 Weight: 1.701kg ISBN: 9781071615560ISBN 10: 1071615564 Pages: 881 Publication Date: 18 July 2022 Audience: Professional and scholarly , Professional & Vocational Format: Paperback Publisher's Status: Active Availability: Manufactured on demand ![]() We will order this item for you from a manufactured on demand supplier. Table of ContentsPART I: UNDERLYING PRINCIPLES OF ENZYME KINETICS 1. Fundamentals of Enzyme Kinetics – Michaelis-Menten and Non-Michaelis Type (Atypical) Enzyme Kinetics Eleanore Seibert and Timothy S. Tracy 2. Reversible Mechanisms of Enzyme Inhibition and Resulting Clinical Significance Barbara Ring, Steven A. Wrighton, and Michael Mohutsky 3. Irreversible Enzyme Inhibition Kinetics and Drug-Drug Interactions Michael Mohutsky and Stephen D. Hall 4. Multi-enzyme Kinetics and Sequential Metabolism Larry C. Wienkers and Brooke Rock 5. Consideration of the Unbound Drug Concentration in Enzyme Kinetics Nigel J Waters, R Scott Obach, and Li Di 6. Numerical Methods for Modeling Enzyme Kinetics Jaydeep Yadav, Ken Korzekwa, and Swati Nagar Part II: Crystal Structure, Biochemistry, and Impact On Enzyme Kinetics 7. Crystal Structures of Drug-Metabolizing CYPs D. Fernando Estrada, Amit Kumar, Christopher S. Campomizzi, and Natalie Jay 8. The Structure and Mechanism of Drug Transporters Arthur G. Roberts PART III: KINETICS OF DRUG METABOLIZING ENZYMES AND TRANSPORTERS 9. Enzyme Kinetics of Oxidative Metabolism – Cytochromes P450 Ken Korzekwa 10. Enzyme Kinetics, Pharmacokinetics, and Inhibition of Aldehyde oxidase Erickson M. Paragas, Kanika Choughule, Jeffrey P. Jones, and John T. Barr 11. Enzyme Kinetics of PAPS-sulfotransferase Margaret O. James 12. Enzyme Kinetics of Uridine Diphosphate Glucuronosyltransferases (UGTs) Jin Zhou, Upendra Argikar, and John O. Miners 13. Principles and Experimental Considerations for In Vitro Transporter Interaction Assays Sid Bhoopathy, Chris Bode, Vatsala Naageshwaran, Erica Weiskircher-Hildebrandt, Venkata Mukkavilli, and Ismael J. Hidal PART IV: MODELING CONSIDERATIONS 14. Prediction of Drug Clearance from Enzyme and Transporter Kinetics Priyanka R. Kulkarni, Amir S. Youssef, and Aneesh A. Argikar 15. Systems Biology Approaches to Enzyme Kinetics Nnenna A. Finn, Andrew D. Raddatz, and Melissa L. Kemp PART V: APPLICATION TO THE CLINIC AND REGULATORY CONSIDERATIONS 16. Variability in Human In Vitro Enzyme Kinetics Christopher R. Gibson, Ying-Hong Wang, Ninad Varkhede, and Bennett Ma 17. Sources of Interindividual Variability Yvonne S. Lin,Kenneth E. Thummel, Brice D. Thompson, Rheem A. Totah, and Christi W. Cho 18. Ontogeny of Drug Metabolizing Enzymes Aarzoo Thakur, Md Masud Parvez, J. Steven Leeder, and Bhagwat Prasad 19. How Science is Driving Regulatory Guidances Xinning Yang, Jianghong Fan, and Lei Zhang PART VI: CASE STUDIES 20. Case Study 1: Practical Considerations with Experimental Design and Interpretation John T Barr and Otito Iwuchukwu 21. Case Study # 2: Practical Analytical Considerations for Conducting In Vitro Enzyme Kinetic Studies Upendra A. Argikar and Swati Nagar 22. Case Study 3: Criticality of High-Quality Curve Fitting: Getting a Km,app isn’t as Simple as it May Seem David M. Stresser and Arian Emami-Riedmaier 23. Case Study 4 Application of Basic Enzyme Kinetics To Metabolism Studies – Real Life Examples Yongmei Li, Michelle McCabe, Lalitha Podila, Timothy S. Tracy, and Donald Tweedie 24. Case Study 5. Predicting the Drug Interaction Potential for Inhibition of CYP2C8 by Montelukast Ken Korzekwa 25 Case Study 6: Deconvoluting Hyperbilirubinemia: Differentiating between Hepatotoxicity and Reversible Inhibition of UGT1A1, MRP2 or OATP1B1 in Drug Development Ian Templeton, Gary Eichenbaum, Rucha Sane, Jin Zhou 26. Case Study 7. Transporters Case Studies: In Vitro Solutions for Translatable Outcomes Sid Bhoopathy, Chris Bode, Vatsala Naageshwaran, Erica Weiskircher-Hildebrandt, Venkata Mukkavilli, and Ismael J. Hidalgo 27. Case Study 8: Status of the Structural Mass Action Kinetic Model of P-gp Mediated Transport through Confluent Cell Monolayers Joe Bentz and Harma Ellens 28. Case Study 9: Probe-Dependent Binding Explains Lack of CYP2C9 Inactivation by 1-Aminobenzotriazole (ABT) Jasleen K. Sodhi and Jason S. Halladay 29. Case Study 10: A Case to Investigate Acetyl Transferase Kinetics Jennifer L Dumouchel and Valerie M Kramlinger 30. Case Study 11. Considerations for Enzyme Mapping Experiments: Interaction between the Aldehyde Oxidase Inhibitor Hydralazine and Glutathione Rachel D. Crouch, Jessica L. Beers, and Klarissa D. Jackson2 31. Case Study 12: Roadmap to Quantifying Ago2-Mediated siRNA Metabolic Activation Kinetics Sara C. Humphreys, Babak Basiri, Armina Abbasi and Brooke M. RockReviewsAuthor InformationTab Content 6Author Website:Countries AvailableAll regions |