Cortese, Riccardo.

Combinatorial Libraries : Synthesis, Screening and Application Potential. - 1st ed. - 1 online resource (248 pages)

Intro -- A Synthetic Peptide Libraries -- 1 Soluble Synthetic Combinatorial Libraries: The Use of Molecular Diversities for Drug Discovery -- 1.1 Introduction -- 1.2 Synthetic Combinatorial Libraries (SCLs) -- 1.3 Synthetic Methods for the Generation of SCLs -- 1.4 SCLs in Drug Discovery and Basic Research -- 1.5 Conclusion -- 2 Combinatorial Libraries of Synthetic Structures: Synthesis, Screening, and Structure Determination -- 2.1 Introduction -- 2.2 One-Bead One-Structure Concept -- 2.3 Design and Synthesis of Non-Peptide Libraries -- 2.4 Release Assay -- 2.5 Stucture Determination -- 2.6 Conclusion -- 3 Peptide Libraries Bound to Continuous Cellulose Membranes: Tools to study Molecular Recognition -- 3.1 Introduction -- 3.2 Detection of antibody epitopes -- 3.3 Mutational analyses of peptide epitopes -- 3.4 Positional scanning combinatorial library -- 3.5 Indentification of metal binding peptides -- 3.6 Summary -- B Nucleic Acids Libraries -- 4 In Vitro Selection of Nucleic Acid Sequences that Bind Small Molecules -- 4.1 Introduction -- 4.2 Natural RNA Receptors -- 4.3 In Vitro Selection -- 4.4 Amino Acid Aptamers -- 4.5 Cofactors -- 4.6 DNA Aptamers -- 4.7 The Complexity of Complexity -- 4.8 Aptamer Structures -- 4.9 Transition State Stabilization and Tight Binding -- 4.10 Conclusions -- 5 Discovery and Characterization of a Thrombin Aptamer Selected from a Combinatorial ssDNA Library -- 5.1 Introduction -- 5.2 Discovery and Initial Characterization -- 5.3 Structure -- 5.4 Binding Site on Thrombin -- 5.5 Determination of Kd and Ki -- 5.6 In vitro Activity -- 5.7 In Vitro Activity -- 5.8 Conclusions -- C Phage Display of Peptide Libraries -- 6 Structural and Functional Constraints in the Display of Peptides on Filamentous Phage Capsids -- 6.1 Introduction -- 6.2 The Phage Life Cycle -- 6.3 A Low Resolution Model. 6.4 Extending the Amino-Terminus of pVIII -- 6.5 Modifying the Surface of Filamentous Phage by Amino Acid Substitution -- 6.6 Can the Remaining Minor Proteins Support Modification? -- 7 Conformationally Defined Peptide Libraries on Phage: Selectable Templates for the Design of Pharmacological Agents -- 7.1 Introduction -- 7.2 From Peptides to Peptidomimetics -- 7.3 Building Constraints in Phage-Displayed Polypeptides -- 7.4 The Minibody: An Engineered ß-Pleated Scaffold for the Display of Reverse-Turn Motifs -- 7.5 The Zinc Finger: A Small Domain for the Display of Structurally Homogeneous α-Helical Motifs -- 7.6 Future Developments: Progressing Toward Non-Peptide Pharmaceuticals -- 8 Discovery of Disease-Specific Mimotopes by Screening Phage Libraries with Human Serum Samples -- 8.1 Introduction -- 8.2 Using Polyclonal Antibodies as a Ligate for the Selection of RPL -- 8.3 Immunofingerprint of the Individual Humoral Response to an Infectious Agent: The Hepatitis C Virus -- 8.4 Phagotope-Based Vaccines -- 8.5 Toward the Indentification of the Pathological Antigens of Autoimmune Diseases -- 8.6 Conclusions -- 9 The Utilization of Platelets and Whole Cells for the Selection of Peptides Ligands from Phage Display Libraries -- 9.1 Introduction -- 9.2 Platelets -- 9.3 Urokinase Plasminogen Activator Receptor -- 9.4 Fibroblast Growth Factor Receptor 1 -- 10 Identification of MHC Binding Motifs with Synthetic and Phage Displayed Peptide Libraries -- 10.1 Introduction -- 10.2 Identification of MHC Class II Peptide Binding Motifs -- 10.3 Conserved and Allele-Specific Anchor Residues Explain Promiscuity and Allele Specificity of HLA-DR/Peptide Interaction -- 10.4 High-Stringency Screening and the Design of Short Peptide Antagonists -- 10.5 Anchor Residues Interact with Pockets of the MHC Class II Peptide Binding Cleft. 10.6 Refinement of Peptide Motifs and Prediction of MHC Class II/Peptide Interaction -- 10.7 Changing the Fine Specificity of a Class II MHC Pocket -- 10.8 Peptide Libraries and MHC: An Outlook -- D Phage Display of Protein Domains -- 11 Isolating High Affinity Human Antibodies from Phage Repertoires -- 11.1 Introduction -- 11.2 High Affinity Human Antibodies to RT3 -- 11.3 Discussion -- 11.4 Conclusion -- 12 Altering the Function of Enzymes and Macromolecular Inhibitors by Phage Display -- 12.1 Introduction -- 12.2 Background -- 12.3 Filamentous Phage Display System -- 12.4 Enzymes Displayed on Phage -- 12.5 Macromolecular Protease Inhibitors Displayed on Phage -- 12.6 Conclusions -- Authors -- Index.

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9783110808902


Electronic books.

QP620.C64 1996eb