简介
Summary:
Publisher Summary 1
Protein tyrosine kinases (PTKs) function as components of signal transduction pathways and play a central role in the control of cell growth, metabolism, differentiation and apoptosis. Currently 20 different PTKs are being considered as potential therapeutic targets in oncology. In this collection of 11 articles, contributors describe their work in PTKs in such areas as using PTKs as targets for cancer and other indications, targeting Src homology 2 domains in drug discovery, using P12-kinase inhibition as a target for therapeutic intervention, using an activated FLT3 receptor tyrosine kinase as a therapeutic target in leukemia and JAK kinases in leukemia, lymphomas and multiple myeloma, applying platelet-derived growth factor, using a targeted therapy for myelogenous leukemia, testing signal transduction inhibitors in animal models of cancer, and using phosphoproteomics in drug discovery and development. Annotation 漏2005 Book News, Inc., Portland, OR (booknews.com)
Publisher Summary 2
Leading researchers, from the Novartis group that pioneered Gleevec/Glivec鈩?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.
目录
Preface p. v
Contributors p. xi
1 Protein Tyrosine Kinases as Targets for Cancer and Other Indications Mark Pearson and Carlos Garc铆a-Echeverria and Doriano Fabbro p. 1
2 Inhibitors of Signaling Interfaces: Targeting Src Homology 2Domains in Drug Discovery Carlos Garcia-Echeverr铆a p. 31
3 PI3-Kinase Inhibition: A Target for Therapeutic Intervention Peter M. Finan and Stephen G. Ward p. 53
4 Src as a Target for Pharmaceutical Intervention: Potential and Limitations Mira Susa and Martin Missbach and Rainer Gamse and Michaela Kneissel and Thomas Buhl and Jurg A. Gasser and Markus Glatt and Terence O'Reilly and Anna Teti and Jonathan Green
5 Activated FLT3 Receptor Tyrosine Kinase as a Therapeutic Target in Leukemia Blanca Scheijen and James D. Griffin p. 93
6 JAK Kinases in Leukemias, Lymphomas, and Multiple Myeloma Renate Burger and Martin Gramatzki p. 115
7 Glivec(r) (Gleevec(r), Imatinib, STI571): A Targeted Therapy for Chronic Myelogenous Leukemia Elisabeth Buchdunger and Renaud Capedeville p. 145
8 Platelet-Derived Growth Factor: Normal Function, Role in Disease, and Application of PDGF Antagonists Tobias Sj枚blom and Kristian Pietras and Arne 脰stman and Carl-Henrik Heldin p. 161
9 Structural Biology of Protein Tyrosine Kinases Sandra W. Cowan-Jacob and Paul Ramage and Wilhelm Stark and Gabriele Fendrich and Wolfgang Jahnke p. 187
10 Testing of Signal Transduction Inhibitors in Animal Models of Cancer Terence O'Reilly and Robert Cozens p. 231
11 Phosphoproteomics in Drug Discovery and Development Michel F. Moran and Jarrod A. Marto and Cynthia J. Brame and Olga Ornatsky and Mark M. Ross and Leticia M. Toledo-Sherman and Alfredo C. Castro and Brett Larsen and Henry Duewel and Christopher Hosfield and Christopher Orsi and Thodoros Topaloglou and Daniel Figeys and Jennifer A. Caldwell-Busby and David R. Stover
Index p. 279
Contributors p. xi
1 Protein Tyrosine Kinases as Targets for Cancer and Other Indications Mark Pearson and Carlos Garc铆a-Echeverria and Doriano Fabbro p. 1
2 Inhibitors of Signaling Interfaces: Targeting Src Homology 2Domains in Drug Discovery Carlos Garcia-Echeverr铆a p. 31
3 PI3-Kinase Inhibition: A Target for Therapeutic Intervention Peter M. Finan and Stephen G. Ward p. 53
4 Src as a Target for Pharmaceutical Intervention: Potential and Limitations Mira Susa and Martin Missbach and Rainer Gamse and Michaela Kneissel and Thomas Buhl and Jurg A. Gasser and Markus Glatt and Terence O'Reilly and Anna Teti and Jonathan Green
5 Activated FLT3 Receptor Tyrosine Kinase as a Therapeutic Target in Leukemia Blanca Scheijen and James D. Griffin p. 93
6 JAK Kinases in Leukemias, Lymphomas, and Multiple Myeloma Renate Burger and Martin Gramatzki p. 115
7 Glivec(r) (Gleevec(r), Imatinib, STI571): A Targeted Therapy for Chronic Myelogenous Leukemia Elisabeth Buchdunger and Renaud Capedeville p. 145
8 Platelet-Derived Growth Factor: Normal Function, Role in Disease, and Application of PDGF Antagonists Tobias Sj枚blom and Kristian Pietras and Arne 脰stman and Carl-Henrik Heldin p. 161
9 Structural Biology of Protein Tyrosine Kinases Sandra W. Cowan-Jacob and Paul Ramage and Wilhelm Stark and Gabriele Fendrich and Wolfgang Jahnke p. 187
10 Testing of Signal Transduction Inhibitors in Animal Models of Cancer Terence O'Reilly and Robert Cozens p. 231
11 Phosphoproteomics in Drug Discovery and Development Michel F. Moran and Jarrod A. Marto and Cynthia J. Brame and Olga Ornatsky and Mark M. Ross and Leticia M. Toledo-Sherman and Alfredo C. Castro and Brett Larsen and Henry Duewel and Christopher Hosfield and Christopher Orsi and Thodoros Topaloglou and Daniel Figeys and Jennifer A. Caldwell-Busby and David R. Stover
Index p. 279
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