Fragment-based Approaches in Drug Discovery
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Based on recent successes in the modular design of pharmaceutically active ligands, the concept and technology of fragment-based design has quickly pervaded the research departments of pharma companies, large and small. Drug developers everywhere are currently struggling to keep ahead of the competition by applying these methods to speed up the drug discovery.This first systematic summary of the impact of such approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this book by professionals for professionals is indispensable for drug developers in the pharma and biotech sector who need to keep abreast of the latest technologies and strategies in pharmaceutical ligand design. Clearly divided into sections on ligand design, spectroscopic techniques, and screening and drug discovery, the text is backed by numerous case studies.
Wolfgang Jahnke is a Senior Research Investigator at the Novartis Institutes for Biomedical Research in Basel, Switzerland, where he leads the Fragment-Based Screening technology platform. During his ten years at Novartis, he has received several honors, among them the appointment as Scientific Expert, and the Leading Scientist Award. Dr. Jahnke received his PhD from the TU München, working with Horst Kessler on the development and application of novel NMR methods. He subsequently carried out research with Peter Wright at the Scripps Research Institute in La Jolla. 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.
PART 1: CONCEPT AND THEORY
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
'...this is indispensable reading for drug discovery researchers in the pharma and biotech sector.' ( Anticancer Research , 2007)
| Erscheint lt. Verlag | 20.7.2006 |
|---|---|
| Reihe/Serie | Methods and Principles in Medicinal Chemistry ; 34 |
| Mitarbeit |
Herausgeber (Serie): Raimund Mannhold, Hugo Kubinyi, Gerd Folkers |
| Sprache | englisch |
| Maße | 170 x 240 mm |
| Gewicht | 865 g |
| Themenwelt | Medizin / Pharmazie ► Pharmazie |
| Naturwissenschaften ► Chemie | |
| Schlagworte | Arzneimittel • Chemie • Chemistry • Computational Chemistry & Molecular Modeling • Computational Chemistry & Molecular Modeling • Computational Chemistry u. Molecular Modeling • Drug Discovery & Development • Drug Discovery & Development • Methods - Synthesis & Techniques • Methods - Synthesis & Techniques • Organic Chemistry • Organische Chemie • Organische Chemie / Methoden, Synthesen, Verfahren • Pharmazeutische Chemie • Wirkstoffforschung u. -entwicklung |
| ISBN-13 | 9783527312917 / 9783527312917 |
| Zustand | Neuware |
| Informationen gemäß Produktsicherheitsverordnung (GPSR) | |
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