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Drug Discovery Handbook

Shayne Cox Gad (Editor)
ISBN: 978-0-471-72877-1
1496 pages
July 2005
Drug Discovery Handbook (0471728772) cover image


The Drug Discovery Handbook gives professionals a tool to facilitate drug discovery by bringing together, for the first time in one resource, a compendium of methods and techniques that need to be considered when developing new drugs.

This comprehensive, practical guide presents an explanation of the latest techniques and methods in drug discovery, including:
  • Genomics, proteomics, high-throughput screening, and systems biology
  • Summaries of how these techniques and methods are used to discover new central nervous system agents, antiviral agents, respiratory drugs, oncology drugs, and more
  • Specific approaches to drug discovery, including problems that are encountered, solutions to these problems, and limitations of various methods and techniques
The thorough coverage and practical, scientifically valid problem-solving approach of Drug Discovery Handbook will serve as an invaluable aid in the complex task of developing new drugs.
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Table of Contents


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).


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Author Information

SHAYNE C. GAD, PHD, DABT, ATS, is the Principal of Gad Consulting Services. He has more than twenty-eight years of experience as a toxicologist, statistical consultant, manager, and consultant on research and development in the chemical, consumer product, contract testing, biotechnology, medical device, and pharmaceutical industries. He is the author of twenty-nine books and numerous papers, presentations, and other publications.
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"...provides in one volume most of the currently used and emerging technologies available...presents a wealth of information on topics that are difficult to find elsewhere...a very useful handbook." (Journal of Medicinal Chemistry, November 2005)

"…will be of great value to medicinal chemists and organic chemists, pharmacologists, physicians, researchers, and everyone interested in the development of therapeutic drugs." (Chemical Educator, September/October 2005)

"...the quality and breadth of the 'Drug Discovery Handbook' make it indispensable for professionals, and endlessly engaging for those interested in discovering more about new drugs..." (Kirkus Reviews, The 2005 Reference Review)

“…an authoritative, comprehensive, and state-of-the-art reference source...thorough coverage and practical, scientifically valid problem-solving approach make it an indispensable aid to anyone involved in the complex task of developing new drugs.” (The Chemical Educator, Vol. 10, No. 5, September/October 2005)

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