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 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 292 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
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
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 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 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 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 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 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 Kinase Drug Discovery written by Richard A. Ward and published by Royal Society of Chemistry. This book was released on 2018-11-06 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.
Download or read book Therapeutic Kinase Inhibitors written by Ingo K. Mellinghoff and published by Springer Science & Business Media. This book was released on 2012-11-27 with total page 237 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cancer drug development is currently undergoing a profound shift. Drugs targeting fundamental cellular processes such DNA-replication and microtubule function, often referred to as “chemotherapy” and still the backbone of most cancer treatment regimens, are increasingly being complemented by or replaced with kinase inhibitors. This new class of drugs targets enzymes which provide growth and survival signals to cancer cells by transferring phosphate groups from Adenosine-5'-triphosphate (ATP) to other proteins, lipids, nucleotides, and carbohydrates. This book summarizes the current state of kinase inhibitor therapy for cancer. Successful drug development relies on the expertise and dedication of many experts. To reflect this team approach to finding new kinase inhibitors and defining their optimal use for cancer treatment, the editors invited experts in academia and pharmaceutical industry to share their insights into various aspects of this process, ranging from the first chemical screens, to preclinical testing and disease-focused clinical drug development. The editors and authors hope these lessons will be instructive for the novice as well as the expert.
Download or read book Resistance to Tyrosine Kinase Inhibitors written by Daniele Focosi and published by Springer. This book was released on 2016-11-07 with total page 194 pages. Available in PDF, EPUB and Kindle. Book excerpt: The volume will serve as a primer on tyrosine kinase signaling and its importance in cancer. The volume will first introduce the common denominators of small-molecule and antibody-derived inhibitors, as well as the general phenomenon of resistance. The volume will then detail resistance to the most commonly used classes of tyrosine kinase inhibitors, and will focus specific chapters on resistance to BCR-ABL1, FLT3, angiokinase family members, and ALK inhibitors.
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.
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 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 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 Inhibitors written by Bernhard Kuster and published by Humana Press. This book was released on 2011-10-06 with total page 256 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein and lipid kinases are often the master regulators of cell signaling in eukaryotic systems. The human genome codes for more than 500 of these enzymes and their misregulation has been shown to be involved in the onset and progression of many diseases including cancer and inflammation. Therefore, small molecule kinase inhibitors have become important research tools for the elucidation of the many biological roles of kinases and their mechanisms of action. Kinase inhibitors thus also contribute significantly to the drug pipelines of the pharmaceutical and biotechnology industries and to the growing need to treat cancer and inflammation. In Kinase Inhibitors: Methods and Protocols, experts in kinase biology, drug discovery, and clinical research present a series of exemplary methods that can be used to address the many challenges facing scientists in the discovery and development of kinase inhibitors both for research and clinical use. Written in the highly successful Methods in Molecular BiologyTM series format, chapters contain introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and accessible, Kinase Inhibitors: Methods and Protocols aims to provide scientists with modern and relevant methods to accelerate or strengthen their research and drug discovery programs through the utilization of these vital regulators.