Enzyme Inhibition in Drug Discovery and Development
The Good and the Bad
Published on 28. January 2010
752 pages
978-0-470-53894-4 (ISBN)
Description
The science and applied approaches of enzyme inhibition in drugdiscovery and development
Offering a unique approach that includes both the pharmacologicand pharmaco-kinetic aspects of enzyme inhibition, EnzymeInhibition in Drug Discovery and Development examines thescientific concepts and experimental approaches related to enzymeinhibition as applied in drug discovery and drug development.
With chapters written by over fifty leading experts in theirfields, Enzyme Inhibition in Drug Discovery and Developmentfosters a cross-fertilization of pharmacology, drug metabolism,pharmacokinetics, and toxicology by understanding the "good"inhibitions--desirable pharmacological effects--and "bad"inhibitions--drug-drug interactions and toxicity. Thebook discusses:
* The drug discovery process, including drug discovery strategy,medicinal chemistry, analytical chemistry, drug metabolism,pharmacokinetics, and safety biomarker assessment
* The manipulations of drug metabolizing enzymes and transportersas well as the negative consequences, such as drug-druginteractions
* The inhibition of several major drug target pathways, such asthe GPCR pathway, the NFkB pathway, and the ion channel pathway
Through this focused, single-source reference on thefundamentals of drug discovery and development, researchers in drugmetabolism and pharmacokinetics (DMPK) will learn and appreciatetarget biology in drug discovery; discovery biologists andmedicinal chemists will also broaden their understanding ofDMPK.
Reviews / Votes
"The description of each topic is clear, well organized andinformative, making the book a useful or even essential high-levelhandbook." (ChemMedChem, November 2010)More details
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Chuang Lu | Albert P. Li
Enzyme Inhibition in Drug Discovery and t: The Good and the Bad
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02/2010
Wiley
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Persons
Chuang Lu, PhD, is the Associate Director in the Drug Safetyand Disposition Department of Millennium Pharmaceuticals. Hiscurrent research interests include drug-metabolizing enzymes,drug-drug interaction, and in vitro-in vivocorrelation.
Albert P. Li, PhD, is the President and CEO of In VitroADMET Laboratories, LLC and Advanced Pharmaceutical Sciences, Inc.,and the cofounder, Chairman, and CSO of the ADMET Group. Hisexperience spans over twenty-five years in the drug developmentindustry, with over 150 publications. He is the editor of severalbooks, including Drug-Drug Interactions in PharmaceuticalDevelopment, published by Wiley.
Content
PREFACE.
CONTRIBUTORS.
PART I. DRUG DISCOVERY APPROACHES AND TECHNOLOGIES.
1. The Drug Discovery Process (Gerald T. Miwa).
2. Medicinal Chemistry of the Optimization of Enzyme Inhibitors(Geraldine Harriman, Amy Elder, and Indranath Ghosh).
3. Bioanalytical Technologies in Drug Discovery (Jing-TaoWu).
4. Safety Biomarkers in Drug Development: Emerging Trends andImplications (Eric R. Fedyk).
5. The Role of Drug Metabolism in Drug Discovery (TonikaBohnert and Liang-Shang Gan).
6. Applied Pharmacokinetics in Drug Discovery and Development(Hua Yang, Xingrong Liu, Anjaneya Chimalakonda, Zheng Lu,Cuiping Chen, Frank Lee, and Wen Chyi Shyu).
PART II. INHIBITION OF THE DRUG METABOLIZINGENZYMES--THE UNDESIRABLE INHIBITION.
7. Enzyme Inhibition and Inactivation: Cytochrome P450 Enzymes(R. Scott Obach).
8. Cytochrome P450 Induction (Edward L. LeCluyse, Michael W.Sinz, Nicola Hewitt, Stephen S. Ferguson, and JasminderSahi).
9. Inhibition of Drug-Metabolizing Enzymes in GastrointestinalTract and Its Influence on the Drug-Drug InteractionPrediction (Aleksandra Galetin and J. Brian Houston).
10. Enzyme Inhibition in Various In Vitro Systems(Ping Zhou).
11. Cytochrome P450 Degradation and Its Clinical Relevance(Mingxiang Liao, Ping Kang, Bernard P. Murray, and Maria AlmiraCorreia).
12. Complexities of Working withUDP-Glucuronosyltransferases (UGTs): Focus on Enzyme Inhibition(Michael B. Fisher).
13. Evaluation of Inhibitors of Drug Metabolism in HumanHepatocytes (Albert P. Li and Chuang Lu).
14. Grapefruit Juice and Its Constituents as New EsteraseInhibitors (Suresh K. Balani).
15. Transporter-Xenobiotic Interactions: An ImportantAspect of Drug Development Studies (Gang Luo, Richard Ridgewell,and Thomas Guenthner).
16. Polymorphisms of Drug Transporters and Their ClinicalImplications (Cindy Q. Xia and Johnny J. Yang).
17. Clinical Drug Interactions Due to Metabolic Inhibition:Prediction, Assessment, and Interpretation (Lisa L. von Moltkeand David J. Greenblatt).
18. Predicting Interindividual Variability of MetabolicDrug-Drug Interactions: Identifying the Causes and Accountingfor Them Using Systems Approach (Amin Rostami-Hodjegan).
PART III. INHIBITION OF THE DRUG TARGET ENZYMES--THEDESIRABLE INHIBITION.
19. NF-kappaB: Mechanism, Tumor Biology, and Inhibitors(Lenny Dang).
20. G-Protein-Coupled Receptors as Drug Targets (Wenyan Miaoand Lijun Wu).
21. Pharmacological Modulation of Ion Channels for the Treatmentof Chronic Pain (Yi Liu and Ning Qin).
22. Targeting the mTOR Pathway for Tumor Therapeutics (WeiChen).
23. HIV-1 Protease Inhibitors as Antiretroviral Agents(Sergei V. Gulnik, Elena Afonina, and MichaelEissenstat).
INDEX.
