Protein Kinases As Drug Targets


Protein Kinases As Drug Targets
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Protein Kinases As Drug Targets


Protein Kinases As Drug Targets
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Author : Bert Klebl
language : en
Publisher: John Wiley & Sons
Release Date : 2011-03-16

Protein Kinases As Drug Targets written by Bert Klebl and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2011-03-16 with Science categories.


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.



Protein Kinases


Protein Kinases
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Author :
language : en
Publisher: BoD – Books on Demand
Release Date : 2021-12-08

Protein Kinases written by and has been published by BoD – Books on Demand this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021-12-08 with Medical categories.


For the past two decades, the protein kinase family has been an intense area of research for developing anticancer drugs. Despite tremendous advancements in kinase drug expansion, many kinases are still unexplored. As such, this book includes research and review articles from experts that focus on protein kinase signalling pathways as a molecular drug target. Chapters include illustrations and cover such topics as the mechanism of action and anticancer activity of protein kinase inhibitors on various cancer types. They also discuss new opportunities, challenges, and future perspectives in the field.



Protein Kinases In Drug Discovery


Protein Kinases In Drug Discovery
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Author : Rossen Donev
language : en
Publisher: Academic Press
Release Date : 2021-02-22

Protein Kinases In Drug Discovery written by Rossen Donev and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021-02-22 with Science categories.


Protein Kinases in Drug Discovery, Volume 124 discusses the latest information on protein kinases and how they modify other proteins by chemically adding phosphate groups to them. New chapters in this release include Transport Proteins and AMPs: Implications in Human Disease, Protein kinase CK2 inhibition as a pharmacological strategy, Emerging role of Protein kinase in diabetes mellitus: From Mechanism to therapy, Dual Roles of ATP-binding site in Protein Kinases: Orthosteric inhibition and Allosteric Regulation, Pseudokinases in drug discovery and development: progress, challenges and future prospects, Comparison of knowledge-based vs. combinatorial peptide library approaches for the identification of protein kinase substrates, and more. Contains timely chapters written by well-renown authorities in their field Includes a number of high-quality illustrations, figures and tables, and targets a very wide audience of specialists, researchers and students Integrates experimental and computational methods for studying the role of protein kinases in different diseases, along with sections on the design of suitable protein kinase inhibitors for use in the treatment of patients



Protein Tyrosine Kinases


Protein Tyrosine Kinases
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Author : Doriano Fabbro
language : en
Publisher: Springer Science & Business Media
Release Date : 2007-11-13

Protein Tyrosine Kinases written by Doriano Fabbro and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-11-13 with Science categories.


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.



Kinase Drug Discovery


Kinase Drug Discovery
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Author : Richard A. Ward
language : en
Publisher: Royal Society of Chemistry
Release Date : 2012

Kinase Drug Discovery written by Richard A. Ward and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012 with Medical categories.


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.



Kinase Drug Discovery


Kinase Drug Discovery
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Author : Richard A. Ward
language : en
Publisher: Royal Society of Chemistry
Release Date : 2018-11-06

Kinase Drug Discovery written by Richard A. Ward and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2018-11-06 with Medical categories.


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 Protein Interactions As New Drug Targets


Protein Protein Interactions As New Drug Targets
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Author : Enno Klussmann
language : en
Publisher: Springer Science & Business Media
Release Date : 2008-05-20

Protein Protein Interactions As New Drug Targets written by Enno Klussmann and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008-05-20 with Medical categories.


Disease-relevant intracellular protein-protein interactions occurring at defined cellular sites possess great potential as drug targets. They permit highly specific pharmacological interference with defined cellular functions. Drugs targeting such interactions are likely to act with fewer side effects than conventional medication influencing whole cell functions. This book discusses therapeutically relevant protein-protein interactions with a major focus on scaffolding proteins tethering signal transduction processes to defined cellular compartments by direct protein-protein interactions. Recent advances in the development of pharmacological agents interfering with protein-protein interactions are highlighted.



Kinase Targets And Inhibitors In Inflammation 2007


Kinase Targets And Inhibitors In Inflammation 2007
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Author : Khusru Asadullah
language : en
Publisher:
Release Date : 2007-01-01

Kinase Targets And Inhibitors In Inflammation 2007 written by Khusru Asadullah and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-01-01 with Anti-inflammatory agents categories.


Whereas G protein-coupled and nuclear receptors have been in the focus of the pharmaceutical industry since decades, protein kinases became interesting drug targets more recently. Several protein kinase inhibitors are well established for the treatment of tumors in the meantime, many more are in clinical development. Inside into the biology of protein kinases and progress in technologies to target these molecules, however, fostered the discovery and development of protein kinase inhibitors for the treatment of inflammation, too. They are particular promising since they are key factors in signal transduction with major impact for initiating, propagation and regulation of immunological responses. In addition, they are well drugable by small molecular weight inhibitors, opening the chance to discover oral bioavailable drugs. When considering kinases as targets in inflammation, however, there are several issues too. These are mainly the selectivity of both the target and the inhibitor and the associated side effect profile of corresponding drugs. In contrast to application in oncology where efficacy is more or less the most important criteria, a high safety profile is key for the chronic treatment of usual non-life treating inflammatory and autoimmune diseases. Having said this, however, clearly better drugs with a favorable therapeutic index (effect / side effect ratio) are needed for these indications, too. Thus, to be considered as a really promising drug target the protein kinase of interest should be significantly involved in the inflammatory process - otherwise insufficient efficacy and potency would have to be expected - without being involved in other physiological processes of essential biological importance or a very selective expression pattern. The same is true with the specifity of the inhibitors itself. So a compound hitting just one other kinase a little may not be acceptable, depending on the function of these off target molecule. Consequently, a solid target identification and validation is needed before lead identification and optimization with the goal of achieving high specifity is started. Despite all these challenges major progress has been made and the first promising kinase inhibitors are moving into the clinic for anti-inflammatory therapy. There are many more on the horizon and it s pretty likely that protein kinase inhibitors will enrich the spectrum of therapy for chronic inflammatory and autoimmune diseases. Within this issue an overview is given on recent progress in the field of protein kinase inhibitors for the treatment of inflammation addressing the opportunities and chances on one hand and the issues and hurdles on the other hand. We are very pleased that we were able to convince real experts to contribute to this hot topic issue. Starting with some general points the recent findings are issued and should enabled the reader to keep up with this fast developing field that is of substantial interest for basic and clinical orientated scientists on one hand and academia as well as pharmaceutical industry on the other hand. All chapters in this book have been published before as articles in a hot topic issue of Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Volume 6, Number 1, February 2007 and are reprinted here with permission by Bentham Science Publishers Ltd.



Sparking Signals


Sparking Signals
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Author : Gottfried Baier
language : en
Publisher: Springer Science & Business Media
Release Date : 2008-03-19

Sparking Signals written by Gottfried Baier and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008-03-19 with Medical categories.


The importance of the protein kinase family is underscored by numerous disease states that arise due to dysregulation of kinase activity. Recent progress in understanding the molecular regulation of kinases has led to the development of new therapeutics based on the inhibition of kinase activity. In this book, well known experts present their most recent findings on the fast developing kinase field. It will be of interest to basic researchers and the pharmaceutical industry.



Protein Kinase Inhibitors


Protein Kinase Inhibitors
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Author : Md. Imtaiyaz Hassan
language : en
Publisher: Academic Press
Release Date : 2022-05-19

Protein Kinase Inhibitors written by Md. Imtaiyaz Hassan and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2022-05-19 with Science categories.


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