| Description |
1 online resource (336 pages). |
| Physical Medium |
polychrome |
| Description |
text file |
| Series |
ISSN
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ISSN.
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| Note |
Description based upon print version of record. |
| Contents |
Intro -- HalfTitle -- Chemical Biology -- Title -- Copyright -- Preface -- Contents -- Chapter 1 Introduction to Chemical Probes 1 -- 1.1 Why Make and Use Chemical Probes? -- 1.2 What Is a Chemical Probe? -- 1.3 How "Good" Must Chemical Probes Be? -- 1.4 How Can One Discover and Use Chemical Probes? -- 1.5 Where Can One Find Chemical Probes? -- References -- Chapter 2 DNA-encoded Chemistry and Its Use in Discovering Chemical Probes 14 -- 2.1 Introduction to DNA-encoded Chemical Synthesis -- 2.2 Comparison with Other Methods -- 2.3 Examples of Challenging Targets -- Acknowledgements |
| Bibliography |
References -- Chapter 3 Computational Methods for the Discovery of Chemical Probes 39 -- 3.1 Introduction to Computational Methods in Drug Discovery and Discovery of Chemical Probes -- 3.2 Molecular Docking -- 3.2.1 Molecular Docking Background -- 3.2.2 Rigid and Ensemble Docking -- 3.2.3 Flexible Docking -- 3.2.4 Scoring Functions -- 3.3 Target Databases for Structure-based Drug Design -- 3.4 Molecular Dynamics Simulations -- 3.5 Quantitative Structure-Activity Relationship (QSAR) -- 3.6 Pharmacophore Modelling -- 3.7 Screening in Virtual Chemical Space -- 3.8 De Novo Design and Big Data. |
| Contents |
3.9 Selected Examples of Chemical Probe Development -- 3.10 Database of Known and Potential Probes -- 3.11 The Future: A Probe for Every Protein -- Acknowledgements -- References -- Chapter 4 Best Practices for Design and Characterization of Covalent Chemical Probes 69 -- 4.1 Introduction -- 4.2 Discovery of Covalent Chemical Probes -- 4.2.1 Target Residues for Covalent Probes -- 4.2.2 Development of Covalent Binders Starting from Non-covalent Binders -- 4.2.3 Covalent Docking and Virtual Screening -- 4.2.4 Covalent Fragment Screening and Disulfide Tethering |
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4.3 Characterization of Covalent Chemical Probes -- 4.3.1 Proof of Covalency or Irreversibility -- 4.3.2 Characterization of the Potency of Irreversible Covalent Probes -- 4.3.3 Evaluation of Reactivity -- 4.3.4 Proof of Cellular Engagement -- 4.3.5 Evaluation of Selectivity -- 4.4 Summary and Suggested Covalent Chemical Probe Criteria -- References -- Chapter 5 Cyclic Peptides as Chemical Probes 100 -- 5.1 Introduction -- 5.2 Advantages and Disadvantages of Peptides as Probes -- 5.3 Selection Methods for Cyclic Peptides -- 5.3.1 Phage Display -- 5.3.2 mRNA Display |
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5.3.3 Split-intein Circular Ligation of Peptides and Proteins (SICLOPPS) -- 5.3.4 Split and Mix Chemical Synthesis -- 5.3.5 Comparison of Methods -- 5.4 Examples of Cyclic Peptides -- 5.4.1 Stapled Peptides Targeting p53:Mdm2/Mdm4 -- 5.4.2 Investigating the Biology of HIF-1 in Response to Hypoxia-Inhibiting Dimerization -- 5.4.3 Activation of the MET Receptor -- Induction of Dimerization -- 5.4.4 Macrocyclic Peptides as Co-crystallization Ligands -- 5.4.5 Substrate-competitive Selective KDM4A-C Inhibitor |
| Note |
5.4.6 Strategies for Improving Cellular Permeability of "Probes": Bicyclic Cell-permeable Peptides. |
| Summary |
Ideal for students and established biochemists, this book will cover new technologies for probe discovery, new probe modalities, the new field of probes for RNA targets and the mature field of kinase chemical probes. |
| Local Note |
eBooks on EBSCOhost EBSCO eBook Subscription Academic Collection - North America |
| Subject |
Molecular probes.
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Molecular probes. |
| Genre/Form |
Electronic books.
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Electronic books.
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| Added Author |
Brennan, Paul E.
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Rodriguez, Saleta Vazquez.
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| Other Form: |
Print version: Brennan, Paul The Discovery and Utility of Chemical Probes in Target Discovery Cambridge : Royal Society of Chemistry,c2020 9781788015899 |
| ISBN |
1839160845 |
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9781839160844 (electronic book) |
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9781839160745 (PDF ebook) |
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1839160748 |
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9781788015899 hardback |
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