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.

Topics covered include:

• 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 transporters as well as the negative consequences, such as drug–drug interactions
• The inhibition of several major drug target pathways, such as the GPCR pathway, the NFkB pathway, and the ion channel pathway

Contents

Part 1: 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

7. Enzyme Inhibition and Inactivation: Cytochrome P450 Enzymes
8. Cytochrome P450 Induction (
9. Inhibition of Drug-Metabolizing Enzymes in 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
15. Transporter–Xenobiotic Interactions: An Important Aspect of Drug Development Studies
16. 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 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 Targets
21. Pharmacological Modulation of Ion Channels for the Treatment of Chronic Pain
22. Targeting the mTOR Pathway for Tumor Therapeutics
23. HIV-1 Protease Inhibitors as Antiretroviral Agents

Index

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