Protein Kinase Inhibitors

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Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy

Author : Anonim
Publisher : Academic Press
Page : 292 pages
File Size : 54,6 Mb
Release : 2018-11-21
Category : Medical
ISBN : 9780128127384

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Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy by Anonim Pdf

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

Next Generation Kinase Inhibitors

Author : Paul Shapiro
Publisher : Springer Nature
Page : 224 pages
File Size : 55,9 Mb
Release : 2020-07-14
Category : Medical
ISBN : 9783030482831

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Next Generation Kinase Inhibitors by Paul Shapiro Pdf

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.

Protein Tyrosine Kinases

Author : Doriano Fabbro,Frank McCormick
Publisher : Springer Science & Business Media
Page : 599 pages
File Size : 42,7 Mb
Release : 2007-11-13
Category : Science
ISBN : 9781592599622

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Protein Tyrosine Kinases by Doriano Fabbro,Frank McCormick Pdf

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.

Protein Kinase Inhibitors

Author : Md. Imtaiyaz Hassan,Saba Noor
Publisher : Academic Press
Page : 832 pages
File Size : 47,7 Mb
Release : 2022-05-19
Category : Science
ISBN : 9780323913492

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Protein Kinase Inhibitors by Md. Imtaiyaz Hassan,Saba Noor Pdf

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

Targeting Protein Kinases for Cancer Therapy

Author : David J. Matthews,Mary E. Gerritsen
Publisher : John Wiley & Sons
Page : 719 pages
File Size : 41,7 Mb
Release : 2011-09-20
Category : Medical
ISBN : 9781118210772

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Targeting Protein Kinases for Cancer Therapy by David J. Matthews,Mary E. Gerritsen Pdf

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.

Protein Kinases as Drug Targets

Author : Bert Klebl,Gerhard Müller,Michael Hamacher
Publisher : John Wiley & Sons
Page : 570 pages
File Size : 47,7 Mb
Release : 2011-03-16
Category : Science
ISBN : 9783527633494

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Protein Kinases as Drug Targets by Bert Klebl,Gerhard Müller,Michael Hamacher Pdf

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.

Kinase Inhibitor Drugs

Author : Rongshi Li,Jeffrey A. Stafford
Publisher : John Wiley & Sons
Page : 463 pages
File Size : 43,7 Mb
Release : 2011-09-20
Category : Medical
ISBN : 9781118210901

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Kinase Inhibitor Drugs by Rongshi Li,Jeffrey A. Stafford Pdf

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

Protein Kinase Inhibitors in Research and Medicine

Author : Anonim
Publisher : Academic Press
Page : 252 pages
File Size : 47,8 Mb
Release : 2013-07-01
Category : Science
ISBN : 9780123984623

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Protein Kinase Inhibitors in Research and Medicine by Anonim Pdf

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

Inhibitors of Protein Kinases and Protein Phosphates

Author : Lorenzo A. Pinna,Patricia T.W. Cohen
Publisher : Springer Science & Business Media
Page : 458 pages
File Size : 53,6 Mb
Release : 2006-03-30
Category : Medical
ISBN : 9783540266709

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Inhibitors of Protein Kinases and Protein Phosphates by Lorenzo A. Pinna,Patricia T.W. Cohen Pdf

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.

Kinase Drug Discovery

Author : Richard A. Ward,Frederick Goldberg
Publisher : Royal Society of Chemistry
Page : 333 pages
File Size : 47,8 Mb
Release : 2012
Category : Medical
ISBN : 9781849731744

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Kinase Drug Discovery by Richard A. Ward,Frederick Goldberg Pdf

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.

Protein Kinases

Author : Anonim
Publisher : BoD – Books on Demand
Page : 164 pages
File Size : 44,9 Mb
Release : 2021-12-08
Category : Medical
ISBN : 9781838809065

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Protein Kinases by Anonim Pdf

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 Kinase-mediated Decisions Between Life and Death

Author : Ayse Basak Engin,Atilla Engin
Publisher : Springer Nature
Page : 415 pages
File Size : 50,5 Mb
Release : 2021-02-04
Category : Medical
ISBN : 9783030498443

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Protein Kinase-mediated Decisions Between Life and Death by Ayse Basak Engin,Atilla Engin Pdf

Protein phosphorylation via protein kinases is an inevitable process that alters physiological and pathological functions of the cells. Thus, protein kinases play key roles in the regulation of cell life or death decisions. Protein kinases are frequently a driving factor in a variety of human diseases including aging and cellular senescence, immune system and endothelial dysfunctions, cancers, insulin resistance, cholestasis and neurodegenerative diseases, as well as bacterial resistance in persistent infections. Recent developments in quantitative proteomics provide important opinions on kinase inhibitor selectivity and their modes of action in the biological context. Protein Kinase-mediated Decisions Between Life and Death aims to have the reader catch insights about up-to-date opinions on “Protein Kinases” related pathways that threaten human health and life. As “Protein Kinases” are related to many health problems, clinicians, basic science researchers and students need this information. Chapter “Signal Transduction in Immune Cells and Protein Kinases” is available open access under a Creative Commons Attribution 4.0 International License via link.springer.com.

Kinase Drug Discovery

Author : Richard A. Ward,Frederick W. Goldberg
Publisher : Royal Society of Chemistry
Page : 430 pages
File Size : 41,5 Mb
Release : 2018-11-06
Category : Medical
ISBN : 9781788010832

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Kinase Drug Discovery by Richard A. Ward,Frederick W. Goldberg Pdf

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.

Proteinkinase Inhibitors

Author : Stefan Laufer
Publisher : Springer Nature
Page : 256 pages
File Size : 52,7 Mb
Release : 2021-03-23
Category : Science
ISBN : 9783030681807

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Proteinkinase Inhibitors by Stefan Laufer Pdf

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.

Serpins and Protein Kinase Inhibitors

Author : Bojidor Georgiev,Sava Markovski
Publisher : Unknown
Page : 0 pages
File Size : 40,9 Mb
Release : 2010
Category : Protein Kinases
ISBN : 1607411873

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Serpins and Protein Kinase Inhibitors by Bojidor Georgiev,Sava Markovski Pdf

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.