Applied Biophysics for Drug Discovery
Donald Huddler, Edward R. Zartler, Donald Huddler, Edward R. Zartler
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Applied Biophysics for Drug Discovery
Donald Huddler, Edward R. Zartler, Donald Huddler, Edward R. Zartler
Ăber dieses Buch
Applied Biophysics for Drug Discovery is a guide to new techniques and approaches to identifying and characterizing small molecules in early drug discovery. Biophysical methods are reasserting their utility in drug discovery and through a combination of the rise of fragment-based drug discovery and an increased focus on more nuanced characterisation of small molecule binding, these methods are playing an increasing role in discovery campaigns.
This text emphasizes practical considerations for selecting and deploying core biophysical method, including but not limited to ITC, SPR, and both ligand-detected and protein-detected NMR.
Topics covered include:
âą Design considerations in biophysical-based lead screening
âą Thermodynamic characterization of protein-compound interactions
âą Characterizing targets and screening reagents with HDX-MS
âą Microscale thermophoresis methods (MST)
âą Screening with Weak Affinity Chromatography
âą Methods to assess compound residence time
âą 1D-NMR methods for hit identification
âą Protein-based NMR methods for SAR development
âą Industry case studies integrating multiple biophysical methods
This text is ideal for academic investigators and industry scientists planning hit characterization campaigns or designing and optimizing screening strategies.
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Information
Inhaltsverzeichnis
- Cover
- Title Page
- Table of Contents
- List of Contributors
- 1 Introduction
- 2 Thermodynamics in Drug Discovery
- 3 Tailoring Hit Identification and Qualification Methods for Targeting ProteinâProtein Interactions
- 4 HydrogenâDeuterium Exchange Mass Spectrometry in Drug Discovery â Theory, Practice and Future
- 5 Microscale Thermophoresis in Drug Discovery
- 6 SPR Screening: Applying the New Generation of SPR Hardware
- 7 Weak Affinity Chromatography (WAC)
- 8 1D NMR Methods for Hit Identification
- 9 ProteinâBased NMR Methods Applied to Drug Discovery
- 10 Applications of Ligand and ProteinâObserved NMR in Ligand Discovery
- 11 Using Biophysical Methods to Optimize Compound Residence Time
- 12 Applying Biophysical and Biochemical Methods to the Discovery of Allosteric Modulators of the AAA ATPase p97
- 13 Driving Drug Discovery with Biophysical Information: Application to Staphylococcus aureus Dihydrofolate Reductase (DHFR)
- 14 Assembly of Fragment Screening Libraries: Property and Diversity Analysis
- Index
- End User License Agreement