Details

Autor(en) / Beteiligte

• Giralt, Ernest,
• Peczuh, Mark W.,
• Salvatella, Xavier,

Titel

Protein surface recognition : approaches for drug discovery

Ort / Verlag

West Sussex, England : Wiley,

Erscheinungsjahr

2011

Link zum Volltext

• Wiley Online Library - AutoHoldings Books

Beschreibungen/Notizen

• Includes index.
• Cover; Title; Copyright; Preface; List of Contributors; Part I: Principles; 1: The Discovery and Characterization of Protein-Protein Interactions; 1.1 Introduction; 1.2 Techniques to Identify Protein-Protein Interactions; 1.3 Techniques to Characterize Protein-Protein Interactions; 1.4 Structure and Dynamics of Protein Complexes; 1.5 Protein-Protein Complexes as Therapeutic Targets; 1.6 Conclusions; 2: Biophysics of Protein-Protein Interactions; 2.1 Introduction; 2.2 Intermolecular Forces in Protein Recognition; 2.3 Basic Binding Thermodynamics; 2.4 Thermodynamically Driven Drug Design
• 2.5 Measurement of Binding Energetics2.6 Structure-based Calculation of Protein Binding Energetics; 2.7 Interfacial Water Molecules in Protein Recognition; 2.8 The Linkage Between Binding and Conformational Equilibrium in Proteins; Part II: Approaches; 3: On the Logic of Natural Product Binding in Protein-Protein Interactivity; 3.1 Introduction; 3.2 Structural Logic; 3.3 Functional Logic; 3.4 The Need for Programmers; 3.5 Compiling the NPPI Mapper; 4: Interface Peptides; 4.1 Interface Peptides Defined; 4.2 Unmodified Peptides; 4.3 Modified Peptides; 4.4 Summary/Perspective
• 5: Inhibition of Protein-Protein Interactions by Peptide Mimics5.1 Introduction; 5.2 Inhibition of Calmodulin; 5.3 Inhibition of HIV-1 Fusion; 5.4 Inhibition of the Nuclear Estrogen Receptor; 5.5 Inhibition of the Bcl-xL/Bak Interaction; 5.6 Inhibition of the p53/MDM2 Interaction; 5.7 Miscellaneous Protein Targets; 5.8 Conclusion; 6: Discovery of Inhibitors of Protein-Protein Interactions by Screening Chemical Libraries; 6.1 Introduction; 6.2 Screening Strategies to Identify and Develop Antagonists of Protein-Protein Interactions
• 6.3 Mimetics of Common Protein Structure Motifs and Structure-based Design of Peptidomimetics6.4 Conclusions and Outlook; Part III: Techniques; 7: High-throughput Methods of Chemical Synthesis Applied to the Preparation of Inhibitors of Protein-Protein Interactions; 7.1 Introduction; 7.2 Survey of High-throughput Organic Synthesis; 7.3 Synthesis of 'Peptide-Inspired' Compounds and Libraries; 7.4 Synthesis of 'Natural Product-Inspired' Compounds and Libraries; 7.5 Diversity Oriented Synthesis (DOS) in the Discovery of PPI Inhibitors; 7.6 Summary and Outlook; 8: In Silico Screening
• 8.1 Introduction8.2 Methods for Virtual Ligand Screening; 8.3 Binding Site Characterization; 8.4 Case Studies; 8.5 Outlook and Conclusions; 9.1: In Vitro Screening: Screening by Nuclear Magnetic Resonance; 9.1.1 Saturation Transfer Difference (STD); 9.1.2 STD in Fragment-based Drug Design; 9.1.3 Chemical Shift Perturbation (CSP); 9.1.4 19F-NMR in Molecular Recognition Studies; 9.2: In Vitro Screening: Methods of High-throughput Screening; 9.2.1 Introduction; 9.2.2 Statistical Evaluation of the HTS Assay Performance; 9.2.3 Biochemical Assays; 9.2.4 Cell-based Assays; 9.2.5 Conclusion
• Part IV: Case Studies
• A new perspective on the design of molecular therapeutics is emerging. This new strategy emphasizes the rational complementation of functionality along extended patches of a protein surface with the aim of inhibiting protein/protein interactions. The successful development of compounds able to inhibit these interactions offers a unique chance to selectively intervene in a large number of key cellular processes related to human disease. Protein Surface Recognition presents a detailed treatment of this strategy, with topics including:an extended survey of protein-protein interac
• English
• Description based on print version record.