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Author: Hicham Zegzouti
Publisher:
ISBN: 9781493930739
Category : Life sciences
Languages : en
Pages : 223
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Book Description
This volume focuses on screening and profiling kinase inhibitors or activators. Chapters in this book cover several facets of the drug discovery processes starting with target identification, and assay development and screening chemical libraries for hit identification and lead optimization. The profiling portion of Kinase Screening and Profiling: Methods and Protocols discusses several strategies and techniques that are required to minimize off target hits and reduce cellular toxicities that are caused by liability kinases. 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. Timely and authoritative, Kinase Screening and Profiling: Methods and Protocols, will benefit scientists and researchers who are interested in exploring the role of kinases in academic, as well as pharmaceutical research.
Author: Hicham Zegzouti
Publisher:
ISBN: 9781493930739
Category : Life sciences
Languages : en
Pages : 223
Get Book Here
Book Description
This volume focuses on screening and profiling kinase inhibitors or activators. Chapters in this book cover several facets of the drug discovery processes starting with target identification, and assay development and screening chemical libraries for hit identification and lead optimization. The profiling portion of Kinase Screening and Profiling: Methods and Protocols discusses several strategies and techniques that are required to minimize off target hits and reduce cellular toxicities that are caused by liability kinases. 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. Timely and authoritative, Kinase Screening and Profiling: Methods and Protocols, will benefit scientists and researchers who are interested in exploring the role of kinases in academic, as well as pharmaceutical research.
Author: Gerard Drewes
Publisher: Humana Press
ISBN: 9781617793639
Category : Science
Languages : en
Pages : 0
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Book Description
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.
Author: Bert Klebl
Publisher: John Wiley & Sons
ISBN: 3527633499
Category : Science
Languages : en
Pages : 570
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Book Description
This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs. Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry.
Author: Alleyn T. Plowright
Publisher: John Wiley & Sons
ISBN: 3527345299
Category : Medical
Languages : en
Pages : 396
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Book Description
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.
Author: Richard A. Ward
Publisher: Royal Society of Chemistry
ISBN: 1849731748
Category : Medical
Languages : en
Pages : 333
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Book Description
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.
Author: Chi-yun Charles Kung
Publisher:
ISBN:
Category :
Languages : en
Pages : 336
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Book Description
Protein phosphorylation catalyzed by protein kinases is a major mechanism by which cells transmit signals within cells. Over the past decade, significant efforts have been devoted to identifying potent and highly selective inhibitors of kinases associated with disease. Specific kinase inhibitors would also serve as powerful chemical tools to probe cellular signaling in a temporal and spatially controlled manner.
Author:
Publisher: Academic Press
ISBN: 9780123984616
Category : Medical
Languages : en
Pages : 0
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Book Description
This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This is the second of two volumes covering protein kinase inhibitors in research and medicine, and includes chapters on such topics as fragment-based screening, broad kinome profiling of kinase inhibitors, and designing drug-resistant kinase alleles. Second of two volumes focusing on protein kinase inhibitors in research and medicine Part of the Methods in Enzymology serial with authors who are experts in their disciplines
Author: William P. Janzen
Publisher: Springer Science & Business Media
ISBN: 1592591809
Category : Medical
Languages : en
Pages : 269
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Book Description
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.
Author: W. Andy Tao
Publisher: John Wiley & Sons
ISBN: 1118970217
Category : Science
Languages : en
Pages : 448
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Book Description
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.
Author: Alexander Heifetz
Publisher: Humana
ISBN: 9781071617892
Category : Medical
Languages : en
Pages : 0
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Book Description
This volume looks at applications of artificial intelligence (AI), machine learning (ML), and deep learning (DL) in drug design. The chapters in this book describe how AI/ML/DL approaches can be applied to accelerate and revolutionize traditional drug design approaches such as: structure- and ligand-based, augmented and multi-objective de novo drug design, SAR and big data analysis, prediction of binding/activity, ADMET, pharmacokinetics and drug-target residence time, precision medicine and selection of favorable chemical synthetic routes. How broadly are these approaches applied and where do they maximally impact productivity today and potentially in the near future. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary software and tools, step-by-step, readily reproducible modeling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique, Artificial Intelligence in Drug Design is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists and drug designers.
