A Handbook for DNA-Encoded Chemistry

by Robert A. Goodnow, Jr.
A Handbook for DNA-Encoded Chemistry
Author: Robert A. Goodnow, Jr.
Publisher: John Wiley & Sons
Total Pages: 495
Release: 2014-04-28
Genre: Science
ISBN: 1118487680
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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

A Handbook for DNA-Encoded Chemistry

by Robert A. Goodnow, Jr.
A Handbook for DNA-Encoded Chemistry
Author: Robert A. Goodnow, Jr.
Publisher: John Wiley & Sons
Total Pages: 527
Release: 2014-04-10
Genre: Science
ISBN: 1118832671
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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

DNA-Encoded Chemical Libraries

by David Israel
DNA-Encoded Chemical Libraries
Author: David Israel
Publisher: Springer Nature
Total Pages: 225
Release: 2022-09-09
Genre: Science
ISBN: 1071625454
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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.

Platform Technologies in Drug Discovery and Validation

by
Platform Technologies in Drug Discovery and Validation
Author:
Publisher: Academic Press
Total Pages: 692
Release: 2017-11-21
Genre: Medical
ISBN: 0128130709
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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

by Lihe Zhang
Nucleic Acids in Medicinal Chemistry and Chemical Biology
Author: Lihe Zhang
Publisher: John Wiley & Sons
Total Pages: 564
Release: 2023-01-05
Genre: Science
ISBN: 1119692741
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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.

Diversity-Oriented Synthesis

by Andrea Trabocchi
Diversity-Oriented Synthesis
Author: Andrea Trabocchi
Publisher: John Wiley & Sons
Total Pages: 550
Release: 2013-06-17
Genre: Science
ISBN: 1118618149
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Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.

Small Molecule Medicinal Chemistry

by Werngard Czechtizky
Small Molecule Medicinal Chemistry
Author: Werngard Czechtizky
Publisher: John Wiley & Sons
Total Pages: 528
Release: 2015-09-21
Genre: Science
ISBN: 1118771575
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Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs. • Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives • Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches • Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques • Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting

Combinatorial Library

by Lisa B. English
Combinatorial Library
Author: Lisa B. English
Publisher: Springer Science & Business Media
Total Pages: 380
Release: 2008-02-04
Genre: Science
ISBN: 1592592856
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The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms—such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules—has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.

Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis

by E. Fernández
Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis
Author: E. Fernández
Publisher: Thieme
Total Pages: 582
Release: 2020-05-22
Genre: Science
ISBN: 3132429732
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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.