A Handbook For Dna Encoded Chemistry

This book comprehensively describes the development and practice of DNA-encoded library synthesis technology. Together, the chapters detail an approach to drug discovery that offers an attractive addition to the portfolio of existing hit generation technologies such as high-throughput screening, structure-based drug discovery and fragment-based screening. The book: Provides a valuable guide for understanding and applying DNA-encoded combinatorial chemistry Helps chemists generate and screen novel chemical libraries of large size and quality Bridges interdisciplinary areas of DNA-encoded combinatorial chemistry – synthetic and analytical chemistry, molecular biology, informatics, and biochemistry Shows medicinal and pharmaceutical chemists how to efficiently broaden available “chemical space” for drug discovery Provides expert and up-to-date summary of reported literature for DNA-encoded and DNA-directed chemistry technology and methods

This book deals with the recent advances in DNA-Encoded Library (DEL) technology that has emerged as an alternative to high throughput screening (HTS) over the last decade and has been heralded as a "disruptive" technology for drug discovery. The book aims to provide a comprehensive overview of all of the major components of the DEL process from conception to bench execution and clinical investigations. The contributions from experts in the field combine different perspectives from academia and industry. The book will be of interest to researchers in the drug discovery field as well as to graduate students and scholars who are interested in this rapidly improving technology.

This volume discusses protocols that cover synthesis, screening by selection, and analysis of DNA-encoded chemical libraries (DEL). Chapters in this book focus on methods used to practice DEL technology and include solution phase library synthesis using a variety of chemistries; DNA encoding of chemical structure; design, preparation and analysis of target proteins and tool compounds; screening of soluble protein targets by affinity selection; DEL qPCR, preparative PCR and DNA sequence analysis; computational methods used to analyze selections and choose compounds for resynthesis; and analysis of hit compounds. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and comprehensive, DNA-Encoded Chemical Libraries: Methods and Protocols is a valuable resource for scientists interested in DEL technology for drug discovery, and will contribute to the continued advancement in this important field.

This book comprehensively describes the development and practice of DNA-encoded library synthesis technology. Together, the chapters detail an approach to drug discovery that offers an attractive addition to the portfolio of existing hit generation technologies such as high-throughput screening, structure-based drug discovery and fragment-based screening. The book: Provides a valuable guide for understanding and applying DNA-encoded combinatorial chemistry Helps chemists generate and screen novel chemical libraries of large size and quality Bridges interdisciplinary areas of DNA-encoded combinatorial chemistry – synthetic and analytical chemistry, molecular biology, informatics, and biochemistry Shows medicinal and pharmaceutical chemists how to efficiently broaden available "chemical space" for drug discovery Provides expert and up-to-date summary of reported literature for DNA-encoded and DNA-directed chemistry technology and methods

The widespread use of organoboron compounds justifies the efforts devoted to their synthesis, as well as toward developing an understanding of their reactivity. The nature of the mono- or diboron species is of paramount importance in determining the reversible covalent binding properties of the boron atom with both nucleophiles and electrophiles. By wedding the rich chemical potential of organoboron compounds to the ubiquity of organic scaffolds, advanced borylation reactions have the potential to open unprecedented synthetic alternatives, and new knowledge in the field should encourage chemists to use organoboron compounds. In this volume, the main objective is to provide a collection of the most useful, practical, and reliable methods, reported mainly within the last decade, for boron activation and boron reactivity. The volume covers the main concepts of organoboron compounds and includes experimental procedures, enabling newcomers to the field the instant and reliable application of the new tools in synthesis. Rather than aiming for a comprehensive coverage, the most advanced solutions for challenging transformations are introduced. To this end, a team of pioneers and leaders in the field have been assembled who discuss both the practical and conceptual aspects of this rapidly growing field.

Platform Technologies in Drug Discovery and Validation, Volume 50, the latest release in the Annual Reports in Medicinal Chemistry series, provides timely and critical reviews of important topics in medicinal chemistry, with an emphasis on emerging topics in the biological sciences. Topics covered in this new volume include DELT, Oligos: ASO, siRNA, CRISPR, Micro-fluidic chemistry, High throughput screening, Kinase-centric computational drug development, Virtual Screening, Phenotypic screening, PROTACS, Chemical Biology, Fragment-based lead generation, Antibody-Drug Conjugates, Antibody-recruiting small molecules, Deuteration, and Peptides. Unique for its treatment of platform technologies for medicinal chemistry and target validation Provides a single, rich volume that summaries a broad spectrum of expertise relevant to the field Presents state-of-the-art summaries of platform technologies

Nucleic Acids in Medicinal Chemistry and Chemical Biology An up-to-date and comprehensive exploration of nucleic acid medicinal chemistry and its applications In Nucleic Acids in Medicinal Chemistry and Chemical Biology: Drug Development and Clinical Applications, a team of distinguished researchers delivers a comprehensive overview of the chemistry and biology of nucleic acids and their therapeutic applications. The book emphasizes the latest research in the field, including new technologies like CRISPR that create novel possibilities to edit mutated genes at the genomic DNA level and to treat inherited diseases and cancers. The authors explore the application of modified nucleosides and nucleotides in medicinal chemistry, a variety of current topics on nucleic acid chemistry and biology, nucleic acid drugs used to treat disease, and more. They also probe new domains of pharmaceutical research, offering the reader a wealth of new drug discovery opportunities emerging in this dynamic field. Readers will also find: A thorough introduction to the basic terminology and knowledge of the field of nucleic acid medicinal chemistry Comprehensive explorations of the methods used to determine the development of nucleic acid drugs Practical discussions of new technologies, like CRISPR, nanotechnology-based delivery systems, synthetic biology, and DNA-encoded chemical libraries In-depth examinations of the latest, cutting-edge developments in nucleic acid medicinal chemistry Perfect for medicinal and nucleic acid chemists, Nucleic Acids in Medicinal Chemistry and Chemical Biology will also earn a place in the libraries of biochemists, chemical biologists, and pharmaceutical researchers.

Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations