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Author: Bert Klebl Publisher: John Wiley & Sons ISBN: 3527633499 Category : Science Languages : en Pages : 570
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: Bert Klebl Publisher: John Wiley & Sons ISBN: 3527633499 Category : Science Languages : en Pages : 570
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: Paul Shapiro Publisher: Springer Nature ISBN: 3030482839 Category : Medical Languages : en Pages : 224
Book Description
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.
Author: Doriano Fabbro Publisher: Springer Science & Business Media ISBN: 1592599621 Category : Science Languages : en Pages : 599
Book Description
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.
Author: Publisher: BoD – Books on Demand ISBN: 1838809066 Category : Medical Languages : en Pages : 164
Book Description
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.
Author: Richard A. Ward Publisher: Royal Society of Chemistry ISBN: 1849731748 Category : Medical Languages : en Pages : 333
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: Rossen Donev Publisher: Academic Press ISBN: 0323853145 Category : Science Languages : en Pages : 350
Book Description
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
Author: Richard A. Ward Publisher: Royal Society of Chemistry ISBN: 1788010833 Category : Medical Languages : en Pages : 430
Book Description
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.
Author: Khusru Asadullah Publisher: ISBN: 9788178952574 Category : Anti-inflammatory agents Languages : en Pages : 162
Book Description
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.
Author: Kazuwa Nakao Publisher: Springer ISBN: 4431556516 Category : Science Languages : en Pages : 330
Book Description
This book is devoted to innovative medicine, comprising the proceedings of the Uehara Memorial Foundation Symposium 2014. It remains extremely rare for the findings of basic research to be developed into clinical applications, and it takes a long time for the process to be achieved. The task of advancing the development of basic research into clinical reality lies with translational science, yet the field seems to struggle to find a way to move forward. To create innovative medical technology, many steps need to be taken: development and analysis of optimal animal models of human diseases, elucidation of genomic and epidemiological data, and establishment of “proof of concept”. There is also considerable demand for progress in drug research, new surgical procedures, and new clinical devices and equipment. While the original research target may be rare diseases, it is also important to apply those findings more broadly to common diseases. The book covers a wide range of topics and is organized into three complementary parts. The first part is basic research for innovative medicine, the second is translational research for innovative medicine, and the third is new technology for innovative medicine. This book helps to understand innovative medicine and to make progress in its realization.
Author: Gerard Drewes Publisher: Humana Press ISBN: 9781617793639 Category : Science Languages : en Pages : 0
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
Author: Bert Klebl
Author: Paul Shapiro
Author: Doriano Fabbro
Author: 
Author: Richard A. Ward
Author: Rossen Donev
Author: Richard A. Ward
Author: Khusru Asadullah
Author: Kazuwa Nakao
Author: Gerard Drewes