Target Discovery and Validation
Target Discovery and Validation

Author: Alleyn T. Plowright

Publisher: John Wiley & Sons

Published: 2020-02-18

Total Pages: 396

ISBN-13: 3527345299

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The modern drug developers? guide for making informed choices among the diverse target identification methods Target Discovery and Validation: Methods and Strategies for Drug Discovery offers a hands-on review of the modern technologies for drug target identification and validation. With contributions from noted industry and academic experts, the book addresses the most recent chemical, biological, and computational methods. Additionally, the book highlights techologies that are applicable to ?difficult? targets and drugs directed at multiple targets, including chemoproteomics, activity-based protein profiling, pathway mapping, genome-wide association studies, and array-based profiling. Throughout, the authors highlight a range of diverse approaches, and target validation studies reveal how these methods can support academic and drug discovery scientists in their target discovery and validation research. This resource: -Offers a guide to identifying and validating targets, a key enabling technology without which no new drug development is possible -Presents the information needed for choosing the appropriate assay method from the ever-growing range of available options -Provides practical examples from recent drug development projects, e. g. in kinase inhibitor profiling Written for medicinal chemists, pharmaceutical professionals, biochemists, biotechnology professionals, and pharmaceutical chemists, Target Discovery and Validation explores the current methods for the identification and validation of drug targets in one comrpehensive volume. It also includes numerous practical examples.

Kinase Drug Discovery
Kinase Drug Discovery

Author: Richard A. Ward

Publisher: Royal Society of Chemistry

Published: 2012

Total Pages: 333

ISBN-13: 1849731748

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Kinase drug discovery remains an area of significant interest across academia and in the pharmaceutical industry. There are now around 13 FDA approved small molecule drugs which target kinases and many more compounds in various stages of clinical development. Although there have been a number of reviews/publications on kinase research, this book fills a gap in the literature by considering the current and future opportunities and challenges in targeting this important family of enzymes. The book is forward-looking and identifies a number of hot topics and key areas for kinase drug discovery over the coming years. It includes contributions from highly respected authors with a combined experience in the industry of well over 200 years, which has resulted in a book of great interest to the kinase field and across drug discovery more generally. Readers will gain a real insight into the huge challenges and opportunities which this target class has presented drug discovery scientists. The many chapters cover a wide breadth of topics, are well written and include high quality colour and black and white images. Topics covered include an outline of how medicinal chemistry has been able to specifically exploit this unique target class, along with reflections on the mechanisms of kinases inhibitors. Also covered is resistance to kinase inhibitors caused by amino acid mutations, case studies of kinase programs and reviews areas beyond protein kinases and beyond the human kinome. Also described are modern approaches to finding kinase leads and the book finishes with a reflection of how kinase drug discovery may progress over the coming years.

Chemical Proteomics
Chemical Proteomics

Author: Gerard Drewes

Publisher: Humana Press

Published: 2011-11-08

Total Pages: 0

ISBN-13: 9781617793639

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The multidisciplinary science of chemical proteomics studies how small molecules of synthetic or natural origin bind to proteins and modulate their function. In Chemical Proteomics: Methods and Protocols, expert researchers in the field provide key techniques to investigate chemical proteomics focusing on analytical strategies, how probes are generated, techniques for the discovery of small molecule targets and the probing of target function, and small molecule ligand and drug discovery. Written in the highly successful Methods in Molecular BiologyTM series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and key tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Chemical Proteomics : Methods and Protocols seeks to provide methodologies that will contribute to a wider application of chemical proteomics methods in biochemical and cell biological laboratories.

Mass Spectrometry-Based Chemical Proteomics
Mass Spectrometry-Based Chemical Proteomics

Author: W. Andy Tao

Publisher: John Wiley & Sons

Published: 2019-07-10

Total Pages: 449

ISBN-13: 1118970217

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PROVIDES STRATEGIES AND CONCEPTS FOR UNDERSTANDING CHEMICAL PROTEOMICS, AND ANALYZING PROTEIN FUNCTIONS, MODIFICATIONS, AND INTERACTIONS—EMPHASIZING MASS SPECTROMETRY THROUGHOUT Covering mass spectrometry for chemical proteomics, this book helps readers understand analytical strategies behind protein functions, their modifications and interactions, and applications in drug discovery. It provides a basic overview and presents concepts in chemical proteomics through three angles: Strategies, Technical Advances, and Applications. Chapters cover those many technical advances and applications in drug discovery, from target identification to validation and potential treatments. The first section of Mass Spectrometry-Based Chemical Proteomics starts by reviewing basic methods and recent advances in mass spectrometry for proteomics, including shotgun proteomics, quantitative proteomics, and data analyses. The next section covers a variety of techniques and strategies coupling chemical probes to MS-based proteomics to provide functional insights into the proteome. In the last section, it focuses on using chemical strategies to study protein post-translational modifications and high-order structures. Summarizes chemical proteomics, up-to-date concepts, analysis, and target validation Covers fundamentals and strategies, including the profiling of enzyme activities and protein-drug interactions Explains technical advances in the field and describes on shotgun proteomics, quantitative proteomics, and corresponding methods of software and database usage for proteomics Includes a wide variety of applications in drug discovery, from kinase inhibitors and intracellular drug targets to the chemoproteomics analysis of natural products Addresses an important tool in small molecule drug discovery, appealing to both academia and the pharmaceutical industry Mass Spectrometry-Based Chemical Proteomics is an excellent source of information for readers in both academia and industry in a variety of fields, including pharmaceutical sciences, drug discovery, molecular biology, bioinformatics, and analytical sciences.

Kinase Drug Discovery
Kinase Drug Discovery

Author: Richard A Ward

Publisher: Royal Society of Chemistry

Published: 2018-10-31

Total Pages: 430

ISBN-13: 1788015630

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Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years and builds on the first volume. This includes topics such as screening approaches to target kinases along with different modes of inhibition such as allosteric and covalent. Novel approaches such as macrocyclisation are considered along with how the properties of kinase inhibitors have evolved, including the potential for brain penetration. Recent areas of great importance also covered include cutting edge molecular modelling approaches and the importance of kinase mutations. The evolving biology of kinases has also resulted in increased interest in the immuno-oncology area and also pseudokinases as a target family. As with the first volume the book finishes with a forward looking view of how research against this fascinating target class may evolve.

Laboratory Screening and Diagnostic Evaluation
Laboratory Screening and Diagnostic Evaluation

Author: Kelly Small Casler, DNP, APRN, FNP-BC, CHSE

Publisher: Springer Publishing Company

Published: 2022-04-25

Total Pages: 1111

ISBN-13: 0826140939

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"[the authors] did a masterful job of creating and editing this gold standard book that should be used by all clinicians and incorporated into all nursing and health sciences curriculums." -Bernadette Mazurek Melnyk, PhD, APRN-CNP, FNAP, FAANP, FAAN Vice President for Health Promotion University Chief Wellness Officer Dean and Helene Fuld Health Trust Professor of Evidence-Based Practice, College of Nursing Professor of Pediatrics & Psychiatry, College of Medicine Executive Director, the Helene Fuld Health Trust National Institute for EBP The Ohio State University This is the only book to explicitly guide clinicians through an evidence-based approach to ordering and interpreting laboratory tests. With over 160 commonly ordered tests, this book is designed to foster more accurate clinical decision-making to attain the highest level of patient care. This book summarizes more than 3000 pieces of evidence and incorporates clinical expertise and decision-making on the ordering and interpretation of tests. To promote ease of use, a convenient table maps labs and their corresponding chapter numbers to the relevant body system to promote ease of use. Each laboratory test is presented in a consistent format with information on physiology, indications (screening, diagnosis, and monitoring), algorithms, test interpretation and follow-up testing, patient education, and related diagnoses. Additional valuable features include clinical pearls that highlight common pitfalls and gaps in reasoning, and a cost-benefit analysis. This book also includes CPT and ICD-10 codes, charts and tables for clarification, and references for further study. Key Features: Delivers a strong, evidence-based approach to ordering and interpreting over 160 laboratory tests Promotes accurate clinical decision-making toward achieving the Triple Aim Includes abundant clinical pearls highlighting common pitfalls and gaps in reasoning Provides cost-benefit analysis and discussion of laboratory testing within a high-value healthcare culture Includes 175 supplemental case examples and 200 self-assessment questions to facilitate instruction and learning Includes more than 3000 pieces of evidence from interprofessional resources

High Throughput Screening
High Throughput Screening

Author: William P. Janzen

Publisher: Humana Press

Published: 2002-04-18

Total Pages: 265

ISBN-13: 9780896038899

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In High Throughput Screening, leading scientists and researchers expert in molecular discovery explain the diverse technologies and key techniques used in HTS and demonstrate how they can be applied generically. Writing to create precisely the introductory guidebook they wish had been available when they started in HTS, these expert seasoned authors illuminate the HTS process with richly detailed tutorials on the biological techniques involved, the management of compound libraries, and the automation and engineering approaches needed. Extensive discussions provide readers with all those key elements of pharmacology, molecular biology, enzymology, and biochemistry that will ensure the identification of suitable targets and screens, and detail the technology necessary to mine millions of data points for meaningful knowledge.

Kinase Drug Discovery
Kinase Drug Discovery

Author: Richard A. Ward

Publisher: Royal Society of Chemistry

Published: 2019

Total Pages: 430

ISBN-13: 1788010833

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Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years and builds on the first volume. This includes topics such as screening approaches to target kinases along with different modes of inhibition such as allosteric and covalent. Novel approaches such as macrocyclisation are considered along with how the properties of kinase inhibitors have evolved, including the potential for brain penetration. Recent areas of great importance also covered include cutting edge molecular modelling approaches and the importance of kinase mutations. The evolving biology of kinases has also resulted in increased interest in the immuno-oncology area and also pseudokinases as a target family. As with the first volume the book finishes with a forward looking view of how research against this fascinating target class may evolve.

Chemical Genomics
Chemical Genomics

Author: Haian Fu

Publisher: Cambridge University Press

Published: 2012-02-13

Total Pages: 359

ISBN-13: 1107377587

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Advances in chemistry, biology and genomics coupled with laboratory automation and computational technologies have led to the rapid emergence of the multidisciplinary field of chemical genomics. This edited text, with contributions from experts in the field, discusses the new techniques and applications that help further the study of chemical genomics. The beginning chapters provide an overview of the basic principles of chemical biology and chemical genomics. This is followed by a technical section that describes the sources of small-molecule chemicals; the basics of high-throughput screening technologies; and various bioassays for biochemical-, cellular- and organism-based screens. The final chapters connect the chemical genomics field with personalized medicine and the druggable genome for future discovery of new therapeutics. This book will be valuable to researchers, professionals and graduate students in many fields, including biology, biomedicine and chemistry.