Fragment-based Approaches in Drug Discovery
Methods and Principles in Medicinal Chemistry (Series Nr. 34)
1. Edition July 2006
XXII, 369 Pages, Hardcover
136 Pictures (48 Colored Figures)
18 tables
Handbook/Reference Book
Short Description
Discover the modular approach to ligand design! Latest technologies and strategies for fragment-based approaches in the screening and design of pharmaceutically active compounds are discussed here, including numerous case studies.
- Out of print -
Further versions
This first systematic summary of the impact of fragment-based approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this represents a book by professionals for professionals, tailor-made for drug developers in the pharma and biotech sector who need to keep up-to-date on the latest technologies and strategies in pharmaceutical ligand design. The book is clearly divided into three sections on ligand design, spectroscopic techniques, and screening and drug discovery, backed by numerous case studies.
The concept of fragment-based ligand design
Multivalency in Ligand Design
Entropic consequences of linking ligands
Location of Binding Sites on Proteins by the Multiple Solvent Crystal Structure Method
PART 2: FRAGMENT LIBRARY DESIGN AND COMPUTATIONAL APPROACHES
Cheminformatics approaches to fragment-based lead discovery
Structural fragments from marketed oral drugs
Fragment docking to proteins with the multi-copy simultaneous search (MCSS) methodology
PART 3: EXPERIMENTAL TECHNIQUES
NMR - guided fragment assembly
SAR by NMR: an analysis of ptency gains realized through fragment-linking and fragment-elaboration strategies for lead generation
Pyramid: an integrated platform for fragment-based drug discovery
Fragment-based lead discovery and optimization using X-ray crystallography
Synergistic use of protein crystallography and solution-phase NMR spectroscopy in structure-based drug design: strategies and tactics
Ligand SAR using electrospray ionization mass spectrometry
Tethering
PART 4: EMERGING TECHNOLOGIES
Click chemistry for drug discovery
Dynamic combinatorial diversity in drug discovery
Daniel A. Erlanson joined Sunesis Pharmaceuticals at its inception in 1998. He has been instrumental in inventing its drug-discovery technologies and using these to design leads against a variety of disease targets. Prior to Sunesis, Dr. Erlanson developed methods to conformationally constrain peptides as a post-doctoral fellow with James A. Wells at Genentech. Dr. Erlanson received his PhD in chemistry from Harvard University in the laboratory of Gregory L. Verdine, and his BA in chemistry from Carleton College, MN.
