Author: Robert A. Goodnow, Jr. Publisher: John Wiley & Sons ISBN: 1118487680 Category : Science Languages : en Pages : 495
Book Description
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
Author: Joost N. H. Reek Publisher: John Wiley & Sons ISBN: 9783527629718 Category : Science Languages : en Pages : 211
Book Description
This long-awaited first book on this exciting new field in organic and supramolecular chemistry explains the fundamentals as well as possible applications of DCC. Authored by the "Who's Who" of DCC it spans the whole range of topics: catalysts, sensors, polymers, ligands, receptors, concluding with a look at future developments and perspectives. All set to become the standard text in the field, this one-stop reference contains everything organic, catalytic, polymer, physical and biochemists need to know.
Author: Lisa B. English Publisher: Springer Science & Business Media ISBN: 1592592856 Category : Science Languages : en Pages : 380
Book Description
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.
Author: Andreas Brunschweiger Publisher: Springer Nature ISBN: 303118629X Category : Science Languages : en Pages : 280
Book Description
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.
Author: Andrea Trabocchi Publisher: John Wiley & Sons ISBN: 1118618149 Category : Science Languages : en Pages : 550
Book Description
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.
Author: Paul Brennan Publisher: Royal Society of Chemistry ISBN: 1839160845 Category : Science Languages : en Pages : 272
Book Description
Numerous genetic methods can be utilised to link a phenotype to a single molecular target but annotated small molecule chemical probes and even entire chemogenomic libraries are increasingly being used as a complementary approach. This book will comprehensively cover the state of the art in chemical probes and best practice for use in target discovery, illustrated throughout with examples. Ideal for students and established biochemists, the book will also 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.
Author: Ali Tavassoli Publisher: Royal Society of Chemistry ISBN: 178801569X Category : Science Languages : en Pages : 357
Book Description
Protein-protein interactions (PPI) are at the heart of the majority of cellular processes, and are frequently dysregulated or usurped in disease. Given this central role, the inhibition of PPIs has been of significant interest as a means of treating a wide variety of diseases. However, there are inherent challenges in developing molecules capable of disrupting the relatively featureless and large interfacial areas involved. Despite this, there have been a number of successes in this field in recent years using both traditional drug discovery approaches and innovative, interdisciplinary strategies using novel chemical scaffolds. This book comprehensively covers the various aspects of PPI inhibition, encompassing small molecules, peptidomimetics, cyclic peptides, stapled peptides and macrocycles. Illustrated throughout with successful case studies, this book provides a holistic, cutting-edge view of the subject area and is ideal for chemical biologists and medicinal chemists interested in developing PPI inhibitors.
Author: Steven Howard Publisher: Royal Society of Chemistry ISBN: 1782625658 Category : Medical Languages : en Pages : 314
Book Description
Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique. This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.
Author: Daniel A. Erlanson Publisher: John Wiley & Sons ISBN: 352733775X Category : Medical Languages : en Pages : 524
Book Description
From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.
Author: David Israel Publisher: Springer Nature ISBN: 1071625454 Category : Science Languages : en Pages : 225
Book Description
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.
Author: Robert A. Goodnow, Jr.
Author: Joost N. H. Reek
Author: Lisa B. English
Author: Andreas Brunschweiger
Author: Andrea Trabocchi
Author: Paul Brennan
Author: Ali Tavassoli
Author: Steven Howard
Author: Daniel A. Erlanson
Author: David Israel