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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.
Receptor Tyrosine Kinase: Structure, Functions and Role in Human Disease, for the first time, systematically covers the shared structural and functional features of the RTK family. Receptor Tyrosine Kinases (RTKs) play critical roles in embryogenesis, normal physiology and several diseases. And over the last decade they have become the Number 1 targets of cancer drugs. To be able to conduct fundamental research or to attempt to develop pharmacological agents able to enhance or intercept them, it is essential first to understand the evolutionary origin of the 58 RTKs and their roles in invertebrates and in humans, as well as downstream signaling pathways. The assembly of chapters is written by experts and underscores commonalities between and among the RTKs. It is an ideal companion volume to The Receptor Tyrosine Kinase: Families and Subfamilies, which proceeds, family by family through all of the specific subfamilies of RTKs, along with their unique landmarks.
This book devotes a chapter to each RTK family and the multiple receptors within each family, thoroughly covering all of the RTKs. The chapters all follow the same structure, presenting this essential information in an accessible and user-friendly format. Each chapter covers one specific family of receptors and begins with a general introduction to that family and a comprehensive discussion of that receptor’s family in development and human disease. Following are in-depth analyses of each family’s receptors with discussions on the gene, protein, ligands, activation, and signaling pathways along with discussion of receptor processing and signal attenuation. Further, cross talk with other receptors systems, post-translational modification and specific unique characteristics to each RTK are discussed. Because it isolates and explains each family, this book is an essential companion volume to Receptor Tyrosine Kinases: Structure, Functions and Role in Human Disease, by the same authors, which talks about RTKs more generally and without the family-by-family detail.
Receptor tyrosine kinases are cell-surface receptors that respond to numerous hormones and growth factors, including insulin, insulin-like growth factors, epidermal growth factor, and nerve growth factor. They activate highly conserved intracellular signaling pathways that regulate cell proliferation, differentiation, and metabolism, playing essential roles in developing and adult animals. This book examines the nature of these receptors and their ligands, the molecular mechanisms that they regulate within cells, and the roles of the receptors in normal physiology and control of embryogenesis. It also discusses how dysfunction of these mechanisms can contribute to cancer and other diseases.
Volume 1: How do you keep track of basic information on the proteins you work with? Where do you find details of their physicochemical properties, amino acid sequences, gene organization? Are you tired of scanning review articles, primary papers and databases to locate that elusive fact? The Academic Press FactsBook series will satisfy scientists and clinical researchers suffering from information overload. Each volume provides a catalogue of the essential properties of families of molecules. Gene organization, amino acid sequences, physicochemical properties, and biological activity are presented using a common, easy to follow format. Taken together they compile everything you wanted to know about proteins but were too busy to look for. The Protein Kinase FactsBook: Protein - Tyrosine Kinases contains over 65 entries on members of the family from vertebrates, Drosophila, slime moulds and other organisms. Entries provide information on: * Subunit structure and isoforms * Genetics * Sequence database accession numbers * Domain structures * Amino acid sequences * Homologues in other species * Patterns of expression * Physiological substrates and specificity determinants * Assays * Enzyme activators and inhibitors * References Volume 2: How do you keep track of basic information on the proteins you work with? Where do you find details of their physicochemical properties, amino acid sequences, gene organization? Are you tired of scanning review articles, primary papers and databases to locate that elusive fact? The Academic Press FactsBook series will satisfy scientists and clinical researchers suffering from information overload. Each volume provides a catalogue of the essential properties of families of molecules. Gene organization, amino acid sequences, physicochemical properties, and biological activity are presented using a common, easy to follow format. Taken together they compile everything you wanted to know about proteins but were too busy to look for. The Protein Kinase FactsBook: Protein - Tyrosine Kinases contains over 130 entries on members of the family from vertebrates, Drosophila, higher plants, yeasts, nematodes, slime moulds and other organisms. Entries provide information on: * Subunit structure and isoforms * Genetics * Sequence database accession numbers * Domain structures * Amino acid sequences * Homologues in other species * Patterns of expression * Physiological substrates and specificity determinants * Assays * Enzyme activators and inhibitors * References
Protein-Tyrosine Kinases: Advances in Research and Application: 2011 Edition is a ScholarlyEditions™ eBook that delivers timely, authoritative, and comprehensive information about Protein-Tyrosine Kinases. The editors have built Protein-Tyrosine Kinases: Advances in Research and Application: 2011 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about Protein-Tyrosine Kinases in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Protein-Tyrosine Kinases: Advances in Research and Application: 2011 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.
Receptor Protein-Tyrosine Kinases: Advances in Research and Application: 2011 Edition is a ScholarlyEditions™ eBook that delivers timely, authoritative, and comprehensive information about Receptor Protein-Tyrosine Kinases. The editors have built Receptor Protein-Tyrosine Kinases: Advances in Research and Application: 2011 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about Receptor Protein-Tyrosine Kinases in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Receptor Protein-Tyrosine Kinases: Advances in Research and Application: 2011 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.
Protein-Tyrosine Kinases—Advances in Research and Application: 2012 Edition is a ScholarlyEditions™ eBook that delivers timely, authoritative, and comprehensive information about Protein-Tyrosine Kinases. The editors have built Protein-Tyrosine Kinases—Advances in Research and Application: 2012 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about Protein-Tyrosine Kinases in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Protein-Tyrosine Kinases—Advances in Research and Application: 2012 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.