Download or read book Serpins and Protein Kinase Inhibitors written by Bojidor Georgiev and published by . This book was released on 2010 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Serpins, a group of proteins with similar structures, were first identified as a set of proteins able to inhibit proteases. The first members of the serpin superfamily to be extensively studied were the human plasma proteins antithrombin and antitrypsin, which play key roles in controlling blood coagulation and inflammation. Today, over 1000 serpins have been identified, including 36 human proteins, as well as molecules in plants, fungi, bacteria, archaea and certain viruses. Serpins are thus the largest and most diverse family of protease inhibitors. In contrast, a protein kinase inhibitor is an enzyme that modifies other proteins by chemically adding phosphate groups to them (phosphorylation). Protein tyrosine kinases (PTKs) play a key role in the regulation of cell proliferation, differentiation, metabolism, migration and survival. Due to their involvement in various forms of cancer, PTKs have become prominent targets for therapy. This new book gathers the latest research from around the globe in this dynamic field.
Download or read book Serine Proteases and Their Serpin Inhibitors in the Nervous System written by Barry W. Festoff and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 359 pages. Available in PDF, EPUB and Kindle. Book excerpt: Proceedings of a NATO ARW held in Maratea, Italy, July 2-8, 1989
Download or read book Inhibitors of Protein Kinases and Protein Phosphates written by Lorenzo A. Pinna and published by Springer Science & Business Media. This book was released on 2006-03-30 with total page 456 pages. Available in PDF, EPUB and Kindle. Book excerpt: The aims of this volume are to highlight the tremendous pharmacological potential of protein kinase and protein phosphatase inhibitors, to provide a thorough overview of the most remarkable achievements in the field and to illustrate how beneficial these studies can be for the advancement of both basic knowledge on biological regulation and deregulation and for the clinical treatment of a wide spectrum of diseases. This goal is attained by contributions of leader investigators in the field, who address the issue from different angles.
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
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.
Download or read book Proteinkinase Inhibitors written by Stefan Laufer and published by Springer Nature. This book was released on 2021-03-23 with total page 256 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book reviews the principles of design and examples of successful implementation of proteinkinase inhibitors (PKI), and offers a comprehensive and authoritative overview of the history and latest developments in the field. Chapters written by experts from industry and academia cover the function, structure and topology of Proteinkinases, molecular modelling, disclose how to achieve high level of selectivity for kinase inhibitors, and exploit kinase inhibitors for cancer treatment. Particular attention is given to Inhibitors of c-Jun N-terminal kinase 3, and to covalent Janus Kinase 3 Inhibitors. A case study on Receptor Tyrosine Kinases EGFR, VEGFR, PDGFR is also presented in this book. Given its breath, this book will appeal to medicinal chemists, students, researchers and professionals alike.
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
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.
Download or read book Protein Kinases as Drug Targets written by Bert Klebl and published by John Wiley & Sons. This book was released on 2011-03-16 with total page 570 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Protein Kinases written by and published by BoD – Books on Demand. This book was released on 2021-12-08 with total page 164 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book A Closer Look at Kinase Inhibition written by Alex Tompson and published by . This book was released on 2020-04-14 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: The book opens with a discussion on the roles of various tyrosine kinases inhibitors and molecular mechanisms of acquired resistance to tyrosine kinase inhibitor drugs therapy in colon-rectal cancer. The authors summarise host cell and viral protein kinases, the progress in their use, and the repurposing of approved kinase inhibitors as broad-spectrum antivirals. The key kinases, namely CLK1, DYRK1A, CDK5, GSK3 and CK1, are analysed as data indicate that targeting these proteins may have therapeutic promise against Alzheimer's disease.
Download or read book Targeting Protein Kinases for Cancer Therapy written by David J. Matthews and published by John Wiley & Sons. This book was released on 2011-09-20 with total page 719 pages. Available in PDF, EPUB and Kindle. Book excerpt: An expert guide to targeting protein kinases in cancer therapy Research has shown that protein kinases can instigate the formation and spread of cancer when they transmit faulty signals inside cells. Because of this fact, pharmaceutical scientists have targeted kinases for intensive study, and have been working to develop medicinal roadblocks to sever their malignant means of communication. Complete with full-color presentations, Targeting Protein Kinases for Cancer Therapy defines the structural features of protein kinases and examines their cellular functions. Combining kinase biology with chemistry and pharmacology applications, this book enlists emerging data to drive the discovery of new cancer-fighting drugs. Valuable information includes: Comprehensive overviews of the major kinase families involved in oncology, integrating protein structure and function, and providing important tools to assist pharmaceutical researchers to understand and work in this dynamic area of cancer drug research Focus on small molecule inhibitors as well as other therapeutic modalities Discussion of kinase inhibitors that have entered clinical trials for the treatment of cancer, with an emphasis on molecules that have progressed to late stage clinical trials and, in a few cases, to market Providing a platform for further study, this important work reviews both the successes and challenges of kinase inhibitor therapy, and provides insight into future directions in the war against cancer.
Download or read book Kinase Inhibitor Drugs written by Rongshi Li and published by John Wiley & Sons. This book was released on 2011-09-20 with total page 463 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive resource on case studies of marketed kinase drugs and promising drug trials Since the discovery of protein kinase activity in 1954, the field of protein kinase drug discovery has advanced dramatically. With the ongoing clinical success of the Bcr-Abl kinase inhibitor Gleevec in the treatment of chronic myelogenous leukemia and seven additional marketed kinase inhibitor drugs, researchers have compelling evidence that kinase inhibitors can be highly efficacious in the treatment of diseases caused by aberrant activity of protein kinase. Currently more than 100 protein kinase inhibitors are in clinical development. In one comprehensive volume, the editors, Dr. Rongshi Li and Dr. Jeffrey Stafford, present timely and important case studies of marketed kinase drugs and several of the most advanced kinase inhibitors in clinical trials. Kinase Inhibitor Drugs includes: Case studies from leading investigators and experts in the field that provide firsthand accounts of kinase inhibitor discovery Current thinking on kinase structure, biochemistry, and signal transduction pathways Information on state-of-the-art technologies and tools such as structure-based and fragment-based drug discovery A lineup of clinical-phase growth factor receptor inhibitors Inhibitors of cell cycle kinases The discovery of allosteric inhibitors of MEK kinase Information on pharmacogenomics and its application to kinase inhibitor clinical development
Download or read book Protein Kinase Inhibitors in Research and Medicine Part B written by and published by Academic Press. This book was released on 2013-08-26 with total page 0 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 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
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 252 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
Download or read book Kinase Inhibitors written by and published by Springer. This book was released on 2011-10-01 with total page 270 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Kinase Targets and Inhibitors in Inflammation 2007 written by Khusru Asadullah and published by . This book was released on 2007-01-01 with total page 162 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
