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Techniques and methods employed in the preparation and application of DNA-Encoded Libraries.
DNA Encoded Libraries (DELs) have transformed the way we explore chemical space, accelerating drug discovery and innovation. This volume contains a collection of articles, bringing together many of the leaders in the field, from both industry and academia, to explore the cutting-edge techniques, strategies, and applications that are reshaping the landscape of chemical synthesis.
The volume covers many aspects of this rapidly expanding field, from DNA-compatible organic reactions to innovative encoding methods and setup strategies, selection procedures, and advanced chemoinformatic techniques.
Whilst background information is provided, the focus of the articles is on the techniques and methods: experts in the field present selected procedures, showing the state of the art in each area covered.
This volume is an indispensable resource for chemists, researchers, and professionals seeking to stay at the forefront of chemical synthesis and drug discovery.
List of contents
1 Introduction
2 DNA-Compatible Organic Reactions
2.1 Amide-Bond-Forming Reactions
2.2 Metal-Promoted DEL-Compatible C C Bond Forming Reactions
2.3 Metal-Free DEL-Compatible C C Bond Forming Reactions
2.4 On-DNA C X (X = N, O, P, S, Se) Bond Forming Reactions
2.5 On-DNA C H Transformations
2.6 On-DNA Photoredox-Catalyzed Reactions
2.7 On-DNA Cyclization Reactions
2.8 DNA-Encoded Isocyanide Multicomponent Reactions
2.9 On-DNA Functional-Group Transformations
2.10 Reversible Immobilization of DNA for Chemical Modification
2.11 Covalent Attachment on a Solid Support
2.12 Micelle-Mediated Synthesis
3 DEL Encoding and Setup Strategies
3.1 DNA-Templated Synthesis
3.2 DNA-Recorded Synthesis
3.2.1 Single Pharmacophore Libraries
3.2.1.1 Encoding Using Double-Stranded DNA: A Headpiece-Based DNA Ligation Strategy
3.2.1.2 Encoding Using Single-Stranded DNA (Iterative Splint-Ligation Procedures)
3.2.1.3 Chemical Ligation/Encoding
3.2.2 Dual-Pharmacophore Libraries
3.2.2.1 Encoded Self-Assembling (Dynamic) Chemical Libraries
3.2.2.2 Peptide Nucleic Acid (PNA) Encoded Libraries
3.2.2.3 DNA-Encoded Dynamic Combinatorial Chemical Libraries
3.2.3 Special Libraries
3.2.3.1 Macrocyclic DELs
3.2.3.2 Natural-Product-Enriched DELs
4 Library Selection Procedures
4.1 Selections by Affinity Capture on Solid Support
4.2 DEL Selection Using DNA-Programmed Affinity Labelling (DPAL)
4.3 Selections of DNA-Encoded Libraries to Protein Targets on Living Cells
4.4 Selections of DNA-Encoded Libraries to Protein Targets within Living Cells
5 Evaluation/Cheminformatic Methods
5.1 Informatic Tools, Processing, and Evaluation of DEL Selection Data
5.2 On-DNA Resynthesis and Affinity Selection Mass Spectrometry (ASMS)
