Fragment-Based Drug Discovery: A Practical Approach - Hardcover

Hardcover

ISBN 10: 0470058137 ISBN 13: 9780470058138

Publisher: Wiley, 2008

Synopsis

Fragment-based drug discovery (FBDD) is a new paradigm in drug discovery that utilizes very small molecules - fragments of larger molecules. It is a faster, cheaper, smarter way to do drug discovery, as shown by the number of pharmaceutical companies that have embraced this approach and the biotechnology companies who use fragments as their sole source of drug discovery.

Fragment-Based Drug Discovery: A Practical Approach is a guide to the techniques and practice of using fragments in drug screening. The emphasis is on practical guidance, with procedures, case studies, practical tips, and contributions from industry. Topics covered include:

• an introduction to  fragment based drug discovery, why using fragments is a more efficient process than predominant models, and what it means to have a successful FBDD effort.
• setting up an FBDD project
• library building and production
• NMR in fragment screening and follow up

• application of protein-ligand NOE matching to the rapid evaluation of fragment binding poses
• target immobilized NMR screening: validation and extension to membrane proteins
• in situ fragment-based medicinal chemistry: screening by mass spectrometry
• computational approaches to fragment and substructure discovery and evaluation
• virtual fragment scanning:  current trends, applications and web based tools
• fragment-based lead discovery using covalent capture methods
• case study from industry: the identification of high affinity beta-secretase inhibitors using fragment-based lead generation

With contributions from industry experts who have successfully set up an industrial fragment-based research program, Fragment-Based Drug Discovery: A Practical Approach offers essential advice to anyone embarking on drug discovery using fragments and those looking for a new approach to screening for drugs.

About this title

About the Author:

Edward R. Zartler, Strategy Consultant, Eli Lilly & Co.; Established the Fragment-based Drug Design paradigm at Eli Lilly.

Michael J. Shapiro, Associate Professor of Pharmacy, University of Maryland School of Pharmaceutical Sciences; Industry experience at Lilley, Novartis and Sandoz.

Review:

"This is a useful book for readers already familiar with the basic aspects of drug design and discovery." (ChemMedChem, October 2009)

"This book provides an excellent resource for those in pharmaceutical research who are interested in fragment-based drug discovery. Most of the topics are covered in enough detail that this book could be used as a guide for those initiating a program in fragment-based drug discovery." (Journal of the American Chemical Society, April 29, 2009)

"As the authors eloquently state in Chapter 2, 'Where there is a validated target and a will, there is a (drug discovery) way.'" (Journal of Medicinal Chemistry, 2009)

About this edition

• Publisher: Wiley
• Publication date: 2008
• ISBN 10: 0470058137
• ISBN 13: 9780470058138
• Binding: Hardcover
• Edition number: 1
• Number of pages: 296
• Editor: Zartler Edward R., Shapiro Michael