Fragment-Based Drug Discovery

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.

• 1. Introduction to Fragment based Drug Discovery (Tim Mitchell and Mike Cherry). 2. Building the Perfect Beast: Designing a Fragment Process to Fit Your Needs (Edward Zartler and Michael Shapiro).3. Assembling a Fragment Library (Mark Brewer, Osamu Ichihara, Christian Kirchhoff, Markus Schade, and Mark Whittaker).4. The Practical Aspects of Using NMR in Fragment Based Screening (Johan Schultz).5. Application of Protein-Ligand NOE Matching to the Rapid Evaluation of Fragment Binding Poses (William J. Metzler, Brian L. Claus, Patricia McDonnell, Stephen R. Johnson, Valentina Goldfarb, Malcolm E. Davis, Luciano Mueller, and Keith L. Constantine).6. Target Immobilized NMR Screening: Validation and Extension to Membrane Proteins (Virginie Früh, Robert J. Heetebrij and Gregg Siegal).7. In situ fragment-based medicinal chemistry: screening by mass spectrometry (Sally-Ann Poulsen and Gary H. Kruppa).8. Computational approaches to fragment and substructure discovery and evaluation (Eelke van der Horst and Adriaan P. IJzerman).9. In Silico Design Chapter (Bradley Feuston, M. Katharine Holloway, Georgia McGaughey and J. Chris Culberson).10. Fragment-based lead discovery using covalent capture methods (Stig K. Hansen and Daniel A. Erlanson).11. Identification of high affinity beta-secretase inhibitors using fragment-based lead generation.Jeffrey S. Albert and Philip D. Edwards.

"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)