Author: Paul Shapiro
Publisher: Springer Nature
ISBN: 3030482839
Category : Medical
Languages : en
Pages : 224
Get Book Here
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:
Publisher: Academic Press
ISBN: 0128127384
Category : Medical
Languages : en
Pages : 294
Get Book Here
Book Description
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
Author: Giuseppe Tridente
Publisher: Academic Press
ISBN: 0128094451
Category : Medical
Languages : en
Pages : 738
Get Book Here
Book Description
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
Author: Doriano Fabbro
Publisher: Springer Science & Business Media
ISBN: 1592599621
Category : Science
Languages : en
Pages : 599
Get Book Here
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: Denis Alexander
Publisher: Handbook of Experimental Pharmacology
ISBN:
Category : Medical
Languages : en
Pages : 476
Get Book Here
Book Description
with contributions by numerous experts
Author: Richard A. Ward
Publisher: Royal Society of Chemistry
ISBN: 1849731748
Category : Medical
Languages : en
Pages : 333
Get Book Here
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: Richard A Ward
Publisher: Royal Society of Chemistry
ISBN: 1788015630
Category : Science
Languages : en
Pages : 430
Get Book Here
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: Ruben Vardanyan
Publisher: Academic Press
ISBN: 0124115241
Category : Medical
Languages : en
Pages : 870
Get Book Here
Book Description
Synthesis of Best-Seller Drugs is a key reference guide for all those involved with the design, development, and use of the best-selling drugs. Designed for ease of use, this book provides detailed information on the most popular drugs, using a practical layout arranged according to drug type. Each chapter reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and synthesis. Of high interest to all those who work in the captivating areas of biologically active compounds and medicinal drug synthesis, in particular medicinal chemists, biochemists, and pharmacologists, the book aims to support current research efforts, while also encouraging future developments in this important field. - Describes methods of synthesis, bioactivity and related drugs in key therapeutic areas - Reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and more - Presents a practical layout designed for use as a quick reference tool by those working in drug design, development and implementation
Author: Richard M. Steingart
Publisher: Springer Nature
ISBN: 3030709981
Category : Medical
Languages : en
Pages : 316
Get Book Here
Book Description
This atlas provides a practically applicable didatic case-based guide to the use of cardiac imaging in patient care during and after cancer therapy. It features detailed information on a variety of imaging modalities, including transesophageal echocardiography, magnetic resonance angiography and positron emission tomography. A range of actual patient presentations are included covering both diagnosis and management during curative and palliative surgery, as well as cancer pharmacotherapy with the use of drugs including Trastuzumab, Anthracycline, Cisplatin and Carboplatin. Topics relevant to survivorship are also described. Atlas of Imaging in Cardio-Oncology enables the reader to develop a deep understanding of how to utilise a variety of imaging modalities used in cardio-oncology in a range of scenarios. It provides a critical and timely resource for the trainee and experienced cardiologist, oncologist and radiologist.
Author: Jean-Paul Renaud
Publisher: John Wiley & Sons
ISBN: 1118900502
Category : Medical
Languages : en
Pages : 1437
Get Book Here
Book Description
With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
