Kinase Inhibitors

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Next Generation Kinase Inhibitors

Author : Paul Shapiro
Publisher : Springer Nature
ISBN 13 : 3030482839
Total Pages : 224 pages
Book Rating : 4.0/5 (34 download)

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Book Synopsis Next Generation Kinase Inhibitors by : Paul Shapiro

Download or read book Next Generation Kinase Inhibitors written by Paul Shapiro and published by Springer Nature. This book was released on 2020-07-14 with total page 224 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein kinases are fascinating enzymes that maintain the proper function of nearly every task performed by the cells of the human body. By extracting a phosphate from the energy molecule ATP and linking it to another protein, protein kinases alter the structure and ultimate function of other proteins. In this way, protein kinases help monitor the extracellular environment and integrate signaling cues that, for the most part, are beneficial for human health and survival. However, protein kinases are often dysregulated and responsible for the initiation and progression of many types of cancers, inflammatory disorders, and other diseases. Thus, decades of research have revealed much about how protein kinases are regulated and approaches to inhibit these enzymes to treat disease. However, nearly 30 years since the identification of the first clinically beneficial small molecule protein kinase inhibitor, there are only a few examples where these drugs provide sustained and durable patient responses. The goal of this book is to provide biomedical scientists, graduate, and professional degree students insight into different approaches using small molecules to block specific protein kinase functions that promote disease.

Adverse Events and Oncotargeted Kinase Inhibitors

Author : Giuseppe Tridente
Publisher : Academic Press
ISBN 13 : 0128094451
Total Pages : 738 pages
Book Rating : 4.1/5 (28 download)

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Book Synopsis Adverse Events and Oncotargeted Kinase Inhibitors by : Giuseppe Tridente

Download or read book Adverse Events and Oncotargeted Kinase Inhibitors written by Giuseppe Tridente and published by Academic Press. This book was released on 2017-05-08 with total page 738 pages. Available in PDF, EPUB and Kindle. Book excerpt: Adverse Events and Oncotargeted Kinase Inhibitors gathers and evaluates data on adverse events associated with tyrosine kinase inhibitors (TKIs), a powerful anti-tumor drug class that has recently been introduced for human therapy. This book compiles a comprehensive safety profile of each TKI from experiences in official therapeutic indications, also exploring off-label exploratory investigations and postmarketing pharmaceutical surveillance databases. A brief history of each drug's development and submission is provided, along with a more detailed analysis of the mechanism(s) of action involved in therapeutic activity or related to the insurgence of specific adverse events. Early chapters focus on general characteristics of TKIs, typology, and classification of adverse events, while the final chapters analyze TKIs as AE inducers and classes of AEs by system or organ involvement. This comprehensive resource compiles and critically reviews all of the relevant safety data for this class of drugs, with the goal of improving the understanding of pathogenesis and facilitating the prevention, monitoring, and management of these adverse events. - Offers a unique and comprehensive publication on the adverse events associated with a new and fast-growing class of medicines - Provides a systematic analysis of adverse events aimed at better prevention through understanding and offering insights for the development of safer drugs - Uses practical guidelines to establish a leading reference on this class of drugs for educators, researchers, drug developers, clinicians, safety professionals, and more

Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy

Author :
Publisher : Academic Press
ISBN 13 : 0128127384
Total Pages : 294 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy by :

Download or read book Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy written by and published by Academic Press. This book was released on 2018-11-21 with total page 294 pages. Available in PDF, EPUB and Kindle. Book excerpt: Tyrosine Kinase Inhibitors as Sensitizing Agents for Chemotherapy, the fourth volume in the Cancer Sensitizing Agents for Chemotherapy Series, focuses on strategic combination therapies that involve a variety of tyrosine kinase inhibitors working together to overcome multi-drug resistance in cancer cells. The book discusses several tyrosine kinase inhibitors that have been used as sensitizing agents, such as EGFR, BCR-ABL, ALK and BRAF. In each chapter, readers will find comprehensive knowledge on the inhibitor and its action, including its biochemical, genetic, and molecular mechanisms' emphases. This book is a valuable source for oncologists, cancer researchers and those interested in applying new sensitizing agents to their research in clinical practice and in trials. - Summarizes the sensitizing role of some tyrosine kinase inhibitors in existing research - Brings recent findings in several cancer types, both experimental and clinically, with a particular emphases on underlying biochemical, genetic, and molecular mechanisms - Provides an updated and comprehensive knowledge regarding the field of combinational cancer treatment

Protein Tyrosine Kinases

Author : Doriano Fabbro
Publisher : Springer Science & Business Media
ISBN 13 : 1592599621
Total Pages : 599 pages
Book Rating : 4.5/5 (925 download)

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Book Synopsis Protein Tyrosine Kinases by : Doriano Fabbro

Download or read book Protein Tyrosine Kinases written by Doriano Fabbro and published by Springer Science & Business Media. This book was released on 2007-11-13 with total page 599 pages. Available in PDF, EPUB and Kindle. Book excerpt: Leading researchers, from the Novartis group that pioneered Gleevec/GlivecTM and around the world, comprehensively survey the state of the art in the drug discovery processes (bio- and chemoinformatics, structural biology, profiling, generation of resistance, etc.) aimed at generating PTK inhibitors for the treatment of various diseases, including cancer. Highlights include a discussion of the rationale and the progress made towards generating "selective" low molecular-weight kinase inhibitors; an analysis of the normal function, role in disease, and application of platelet-derived growth factor antagonists; and a summary of the factors involved in successful structure-based drug design. Additional chapters address the advantages and disadvantages of in vivo preclinical models for testing protein kinase inhibitors with antitumor activity and the utility of different methods in the drug discovery and development process for determining "on-target" vs "off-target" effects of kinase inhibitors.

Inhibitors of Protein Kinases and Protein Phosphates

Author : Denis Alexander
Publisher : Handbook of Experimental Pharmacology
ISBN 13 :
Total Pages : 476 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Inhibitors of Protein Kinases and Protein Phosphates by : Denis Alexander

Download or read book Inhibitors of Protein Kinases and Protein Phosphates written by Denis Alexander and published by Handbook of Experimental Pharmacology. This book was released on 2004-10-04 with total page 476 pages. Available in PDF, EPUB and Kindle. Book excerpt: with contributions by numerous experts

Kinase Drug Discovery

Author : Richard A. Ward
Publisher : Royal Society of Chemistry
ISBN 13 : 1849731748
Total Pages : 333 pages
Book Rating : 4.8/5 (497 download)

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Book Synopsis Kinase Drug Discovery by : Richard A. Ward

Download or read book Kinase Drug Discovery written by Richard A. Ward and published by Royal Society of Chemistry. This book was released on 2012 with total page 333 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Synthesis of Best-Seller Drugs

Author : Ruben Vardanyan
Publisher : Academic Press
ISBN 13 : 0124115241
Total Pages : 870 pages
Book Rating : 4.1/5 (241 download)

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Book Synopsis Synthesis of Best-Seller Drugs by : Ruben Vardanyan

Download or read book Synthesis of Best-Seller Drugs written by Ruben Vardanyan and published by Academic Press. This book was released on 2016-01-07 with total page 870 pages. Available in PDF, EPUB and Kindle. Book excerpt: Synthesis of Best-Seller Drugs is a key reference guide for all those involved with the design, development, and use of the best-selling drugs. Designed for ease of use, this book provides detailed information on the most popular drugs, using a practical layout arranged according to drug type. Each chapter reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and synthesis. Of high interest to all those who work in the captivating areas of biologically active compounds and medicinal drug synthesis, in particular medicinal chemists, biochemists, and pharmacologists, the book aims to support current research efforts, while also encouraging future developments in this important field. - Describes methods of synthesis, bioactivity and related drugs in key therapeutic areas - Reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and more - Presents a practical layout designed for use as a quick reference tool by those working in drug design, development and implementation

Kinase Drug Discovery

Author : Richard A Ward
Publisher : Royal Society of Chemistry
ISBN 13 : 1788015630
Total Pages : 430 pages
Book Rating : 4.7/5 (88 download)

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Book Synopsis Kinase Drug Discovery by : Richard A Ward

Download or read book Kinase Drug Discovery written by Richard A Ward and published by Royal Society of Chemistry. This book was released on 2018-10-31 with total page 430 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Protein Kinase Inhibitors

Author : Md. Imtaiyaz Hassan
Publisher : Academic Press
ISBN 13 : 0323913490
Total Pages : 832 pages
Book Rating : 4.3/5 (239 download)

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Book Synopsis Protein Kinase Inhibitors by : Md. Imtaiyaz Hassan

Download or read book Protein Kinase Inhibitors written by Md. Imtaiyaz Hassan and published by Academic Press. This book was released on 2022-05-19 with total page 832 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein Kinase Inhibitors: From Discovery to Therapeutics offers a foundational, pragmatic overview of protein kinases inhibitors and their potential role in disease modulation and treatment. Here, international experts in the field offer an integrated discussion of kinase inhibitor biology, biomarker discovery, and methods for drug design and development. After a brief overview of kinases and kinase inhibitors, subsequent chapters discuss individual kinases that are representative of the wider kinases and kinase families, including their roles in disease pathogenesis, underlying mechanisms, potential inhibitors and their modes of action for therapeutic modulation. Several potential drugs under different stages of clinical trials are discussed, including their relevance to cancer, diabetes, obesity, cardiovascular, neurological, and auto-immune and inflammatory disease, among other disorders. The book also addresses the challenges and opportunities for future kinase inhibitor development. - Provides a thorough overview of kinase inhibitor biology and its role in disease progression and modulation - Examines protein kinase inhibitor drugs in various stages of clinical trials and development - Offers methods and protocols for protein kinase inhibitor research studies and drug design and development - Includes chapter contributions from international leaders in the field

Drug Selectivity

Author : Norbert Handler
Publisher : John Wiley & Sons
ISBN 13 : 3527335382
Total Pages : 538 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Drug Selectivity by : Norbert Handler

Download or read book Drug Selectivity written by Norbert Handler and published by John Wiley & Sons. This book was released on 2018-02-27 with total page 538 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book "Drug Selectivity - An Evolving Concept in Medicinal Chemistry" provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process. The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist.

Methods of Therapeutic Drug Monitoring Including Pharmacogenetics

Author : Georg Hempel
Publisher : Elsevier
ISBN 13 : 0444640673
Total Pages : 382 pages
Book Rating : 4.4/5 (446 download)

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Book Synopsis Methods of Therapeutic Drug Monitoring Including Pharmacogenetics by : Georg Hempel

Download or read book Methods of Therapeutic Drug Monitoring Including Pharmacogenetics written by Georg Hempel and published by Elsevier. This book was released on 2019-10-17 with total page 382 pages. Available in PDF, EPUB and Kindle. Book excerpt: Methods of Therapeutic Drug Monitoring Including Pharmacogenetics, Second Edition, Volume Seven in the Handbook of Analytical Separations series, covers all aspects of drug monitoring, including laboratory work, pharmacokinetic analysis and clinical aspects, thus enabling readers from different fields to understand the whole process of therapeutic drug monitoring and how to avoid common pitfalls. The book contains analytical techniques for the quantification of drugs, along with pharmacogenetic and pharmacogenomic methods. Also included are updates on sample preparation, including dried blood spot technology and microextraction methods. In addition, the book includes new drugs, such as tyrosine kinase inhibitors and the monitoring of immunosuppressant drugs. - Presents a unique, interdisciplinary approach that appeals to a wide range of users - Written by authors from international labs, providing a global perspective that can be applied in various regulatory environments - Features additional therapeutic drugs to reflect the rising number of immunocompromised patients - Includes a new mass spectroscopic methods chapter to capture the frequent use in TDM and the improved availability of LC-MS across laboratories

Structural Biology in Drug Discovery

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1437 pages
Book Rating : 4.1/5 (189 download)

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Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1437 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Atlas of Imaging in Cardio-Oncology

Author : Richard M. Steingart
Publisher : Springer Nature
ISBN 13 : 3030709981
Total Pages : 316 pages
Book Rating : 4.0/5 (37 download)

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Book Synopsis Atlas of Imaging in Cardio-Oncology by : Richard M. Steingart

Download or read book Atlas of Imaging in Cardio-Oncology written by Richard M. Steingart and published by Springer Nature. This book was released on 2021-08-03 with total page 316 pages. Available in PDF, EPUB and Kindle. Book excerpt: This atlas provides a practically applicable didatic case-based guide to the use of cardiac imaging in patient care during and after cancer therapy. It features detailed information on a variety of imaging modalities, including transesophageal echocardiography, magnetic resonance angiography and positron emission tomography. A range of actual patient presentations are included covering both diagnosis and management during curative and palliative surgery, as well as cancer pharmacotherapy with the use of drugs including Trastuzumab, Anthracycline, Cisplatin and Carboplatin. Topics relevant to survivorship are also described. Atlas of Imaging in Cardio-Oncology enables the reader to develop a deep understanding of how to utilise a variety of imaging modalities used in cardio-oncology in a range of scenarios. It provides a critical and timely resource for the trainee and experienced cardiologist, oncologist and radiologist.

Medicinal Chemistry of Anticancer Drugs

Author : Carmen Avendaño
Publisher : Elsevier
ISBN 13 : 0444626670
Total Pages : 767 pages
Book Rating : 4.4/5 (446 download)

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Book Synopsis Medicinal Chemistry of Anticancer Drugs by : Carmen Avendaño

Download or read book Medicinal Chemistry of Anticancer Drugs written by Carmen Avendaño and published by Elsevier. This book was released on 2015-06-11 with total page 767 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design. - Presents information in a clear and concise way using a large number of figures - Historical background provides insights on how the process of drug discovery in the anticancer field has evolved - Extensive references to primary literature

Chemical Proteomics

Author : Gerard Drewes
Publisher : Humana Press
ISBN 13 : 9781617793639
Total Pages : 0 pages
Book Rating : 4.7/5 (936 download)

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Book Synopsis Chemical Proteomics by : Gerard Drewes

Download or read book Chemical Proteomics written by Gerard Drewes and published by Humana Press. This book was released on 2011-11-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Multi-targeted Tyrosine Kinase Inhibitors in the Treatment of Cancer and Neurodegenerative Disorders

Author : Halilibrahim Ciftci
Publisher : Frontiers Media SA
ISBN 13 : 2832552951
Total Pages : 124 pages
Book Rating : 4.8/5 (325 download)

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Book Synopsis Multi-targeted Tyrosine Kinase Inhibitors in the Treatment of Cancer and Neurodegenerative Disorders by : Halilibrahim Ciftci

Download or read book Multi-targeted Tyrosine Kinase Inhibitors in the Treatment of Cancer and Neurodegenerative Disorders written by Halilibrahim Ciftci and published by Frontiers Media SA. This book was released on 2024-08-07 with total page 124 pages. Available in PDF, EPUB and Kindle. Book excerpt: Tyrosine kinases, which catalyze the transfer of a phosphate from ATP to a hydroxyl group of a tyrosine residue, play a plethora of roles in the regulation of diverse functions in normal cells including cell growth, motility, differentiation, and metabolism. Moreover, they are also associated with oncogenesis. Tyrosine kinases are mainly classified as receptor tyrosine kinases and non-receptor tyrosine kinases, including crucial members. Epidermal growth factor receptor (EGFR) belongs to the ERBB family of receptor tyrosine kinases along with three other closely related receptors, namely HER-2, HER-3 and HER-4. EGFR and HER-2, lead to autophosphorylation of the intracellular domain through tyrosine kinase activity and subsequent stimulation of downstream cascade that may result in proliferation, suppression of apoptosis, metastasis and angiogenesis. On the other hand, c-Abl (Abl-1) is a non-receptor tyrosine kinase, which is also essential in the regulation of several antiapoptotic and proliferative signal transduction pathways. They have mainly been identified as important targets for several types of cancer such as EGFR for non-small-cell lung cancer, glioma and colorectal cancer, HER-2 for breast and colorectal cancers and Abl for chronic myeloid leukemia. One of the major platforms that they have participated in is neurodegenerative disorders such as Parkinson’s disease, Alzheimer’s disease and amyotrophic lateral sclerosis. Aberrant activity of tyrosine kinases, in particular EGFR and Abl, have been reported to induce apoptosis and cell cycle arrest in response to a wide range of stimuli resulting in neurodegeneration and neuroinflammation. The main goal of this Research Topic is to identify new and potent effective tyrosine kinase inhibitors to be effective in cancer and neurodegenerative disorders.

Protein Kinase Inhibitors in Research and Medicine

Author :
Publisher : Academic Press
ISBN 13 : 0123984629
Total Pages : 296 pages
Book Rating : 4.1/5 (239 download)

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Book Synopsis Protein Kinase Inhibitors in Research and Medicine by :

Download or read book Protein Kinase Inhibitors in Research and Medicine written by and published by Academic Press. This book was released on 2013-07-01 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers 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. - Continues the legacy of this premier serial with quality chapters authored by leaders in the field - Covers research methods in biomineralization science - Contains sections focusing on protein kinase inhibitors in research and medicine