Introduction: Drug Discovery in the 21st Century.

1. Natural Products (Charles B. Spainhour).

2. Cancer Cell Proteomics Using Molecular Aptamers (Weihong Tan, Zehui Cao, Dihua Shangguan, Ying Li, Zhiwen Tang, Prabodhika Mallikratchy, and Hui Chen).

3. Molecular Similarity Methods and QSAR Models as Tools for Virtual Screening (Jürgen Bajorath).

4. Systems Biology: Applications in Drug Discovery (Sean Ekins, Andrej Bugrim, Yuri Nikolsky, and Tatiana Nikolskaya).

5. High-Throughput Flow Cytometry (Larry A. Sklar, Peter C. Simons, Anna Waller, Sean M. Biggs, Susan M. Young, Marius Olah, Cristian Bologa, Tudor I. Oprea, Eric R. Prossnitz, and Bruce S. Edwards).

6. Combining NMR Spectral Information with Associated Structural Features to Form Computationally Nonintensive, Rugged, and Objective Models of Biological Activity (Richard D. Beger, Dan A. Buzatu, and Jon G.Wilkes).

7. Using Microsoft Excel® as a Laboratory Data Management Tool (A. Erik Rubin, Mark F. Russo, and William Neil).

8. Age of Regulation (Sandy Weinberg and Gerald J. Whartenby).

9. Simultaneous Screening of Multiple Cell Lines Using the CellCard System (Oren E. Beske).

10. Protein X-ray Crystallography in Drug Discovery (Peter Nollert, Michael D. Feese, Bart L. Staker, and Hidong Kim).

11. Biological and Chemistry Assays Available During Drug Discovery and Developability Assessment (Duane B. Lakings).

12. Strategies and Methods in Monitoring and Targeting Protein–Protein Interactions (Arianna Loregian and Giorgio Palù)

13. High-Throughput Screening: Evolution of Technology and Methods (Martyn N. Banks, Angela M. Cacace, Jonathan O’Connell, and John G. Houston).

14. Metal-Enhanced Fluorescence: Application to High-Throughput Screening and Drug Discovery (Kadir Aslan, Ignacy Gryczynski, Joanna Malicka, Joseph R. Lakowicz, and Chris D. Geddes).

15. Methods for the Design and Analysis of Replicate-Experiment Studies to Establish Assay Reproducibility and the Equivalence of Two Potency Assays (Brian J. Eastwood, Amy K. Chesterfield, Mary C.Wolff, and Christian C. Felder).

16. Coupled Luminescent Methods in Drug Discovery: 3-Min Assays for Cytotoxicity and Phosphatase Activity (Michael J. Corey and Robert J. Kinders).

17. Design and Pharmaceutical Applications of Prodrugs (Tomi Järvinen, Jarkko Rautio, Mar Masson, and Thorsteinn Loftsson).

18. GABA and Glutamate Receptor Ligands and Their Therapeutic Potential in CNS Disorders (Ulf Madsen, Hans Bräuner-Osborne, Jeremy R. Greenwood, Tommy N. Johansen, Povl Krogsgaard-Larsen, Tommy Liljefors, Mogens Nielsen, and Bente Frølund).

19. Cardiac Sarcolemmal ATP-Sensitive Potassium Channel Antagonists: Novel Ischemia-Selective Antiarrhythmic Agents (George E. Billman).

20. Factors Influencing the Efficacy of Mediator-Specific Anti-Inflammatory, Glucocorticoid, and Anticoagulant Therapies for Sepsis (Peter C. Minneci, Katherine J. Deans, Michael Haley, Xizhong Cui, Charles Natanson, and Peter Q. Eichacker).

21. Combinatorial Chemistry in the Drug Discovery Process (Nathan T. Ross, Brian R. McNaughton, and Benjamin L. Miller).

22. Herbal Medicines and Animal Models of Gastrointestinal Diseases (C.H. Cho and J.K.S. Ko).

23. Endocrine and Metabolic Agents (Brian L. Furman).

24. Respiratory Viruses (Paul D. Olivo).

25. Strategies in the Design of Antiviral Drugs (Erik De Clercq and Piet Herdewijn).

26. Protein Kinase Inhibitors in Drug Discovery (Keykavous Parang and Gongqin Sun).

27. RNA-Based Therapies (Steve Pascolo).

28. Novel Imaging Agents for Molecular MR Imaging of Cancer (Dmitri Artemov and Zaver M. Bhujwalla).

29. Targets and Approches for Cancer Drug Discovery (Susan L. Mooberry).

Index.