A Handbook for DNA-Encoded Chemistry
A Handbook for DNA-Encoded Chemistry

Author: Robert A. Goodnow, Jr.

Publisher: John Wiley & Sons

Published: 2014-04-28

Total Pages: 495

ISBN-13: 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

DNA-Encoded Chemical Libraries
DNA-Encoded Chemical Libraries

Author: David Israel

Publisher: Springer Nature

Published: 2022-09-09

Total Pages: 225

ISBN-13: 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
Platform Technologies in Drug Discovery and Validation

Author:

Publisher: Academic Press

Published: 2017-11-21

Total Pages: 692

ISBN-13: 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
Nucleic Acids in Medicinal Chemistry and Chemical Biology

Author: Lihe Zhang

Publisher: John Wiley & Sons

Published: 2023-01-05

Total Pages: 564

ISBN-13: 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.

Chemical Sciences in Early Drug Discovery
Chemical Sciences in Early Drug Discovery

Author: Pierfausto Seneci

Publisher: Elsevier

Published: 2018-06-05

Total Pages: 196

ISBN-13: 008099928X

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Chemical Sciences in Early Drug Discovery: Medicinal Chemistry 2.0 describes how new technologies and approaches can be used to improve the probability of success in fulfilling the perennial goal of finding and developing new drugs. Drawing on the author's extensive experience consulting and teaching in medicinal chemistry, the book outlines ways in which medicinal chemistry is widening its reach to meet modern demands, and how modern technologies and approaches are facilitating this growth into new fields. Supported by examples throughout, the book is a practical resource for organic-medicinal chemists, biological chemists and pharmacologists involved in drug discovery. - Reviews the key application of chemistry in drug discovery for both medicinal and non-medicinal chemists, clarifying and explaining the role of medicinal chemistry in supporting the modern drug discovery pipeline - Shows how a wider medicinal chemistry view is essential for anyone in an integrated drug discovery project looking to reduce costs and save time - Provides the critical success factors needed to successfully identify hits from both biological and chemical perspectives

Diversity-Oriented Synthesis
Diversity-Oriented Synthesis

Author: Andrea Trabocchi

Publisher: John Wiley & Sons

Published: 2013-06-17

Total Pages: 550

ISBN-13: 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.

Drug Discovery and Development, Third Edition
Drug Discovery and Development, Third Edition

Author: James J. O'Donnell

Publisher: CRC Press

Published: 2019-11-21

Total Pages: 697

ISBN-13: 1351625144

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Drug Discovery and Development, Third Edition presents up-to-date scientific information for maximizing the ability of a multidisciplinary research team to discover and bring new drugs to the marketplace. It explores many scientific advances in new drug discovery and development for areas such as screening technologies, biotechnology approaches, and evaluation of efficacy and safety of drug candidates through preclinical testing. This book also greatly expands the focus on the clinical pharmacology, regulatory, and business aspects of bringing new drugs to the market and offers coverage of essential topics for companies involved in drug development. Historical perspectives and predicted trends are also provided. Features: Highlights emerging scientific fields relevant to drug discovery such as the microbiome, nanotechnology, and cancer immunotherapy; and novel research tools such as CRISPR and DNA-encoded libraries Case study detailing the discovery of the anti-cancer drug, lorlatinib Venture capitalist commentary on trends and best practices in drug discovery and development Comprehensive review of regulations and their impact on drug development, highlighting special populations, orphan drugs, and pharmaceutical compounding Multidiscipline functioning of an Academic Research Enterprise, plus a chapter on Ethical Concerns in Research Contributions by 70+ experts from industry and academia specialists who developed and are practitioners of the science and business

DNA-Encoded Libraries
DNA-Encoded Libraries

Author: Andreas Brunschweiger

Publisher: Springer Nature

Published: 2022-11-25

Total Pages: 280

ISBN-13: 303118629X

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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.

Practical Medicinal Chemistry with Macrocycles
Practical Medicinal Chemistry with Macrocycles

Author: Eric Marsault

Publisher: John Wiley & Sons

Published: 2017-08-03

Total Pages: 653

ISBN-13: 1119092582

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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

Combinatorial Library
Combinatorial Library

Author: Lisa B. English

Publisher: Springer Science & Business Media

Published: 2008-02-04

Total Pages: 380

ISBN-13: 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.