Protein Tyrosine Kinases

1. Front Matter

   Pages i-xiii

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2. Protein Tyrosine Kinases as Targets for Cancer and Other Indications

   • Mark Pearson, Carlos García-Echeverría, Doriano Fabbro

   Pages 1-29

3. Inhibitors of Signaling Interfaces

   • Carlos García-Echeverría

   Pages 31-52

4. PI3-Kinase Inhibition

   • Peter M. Finan, Stephen G. Ward

   Pages 53-69

5. Src as a Target for Pharmaceutical Intervention

   • Mira Šuša, Martin Missbach, Rainer Gamse, Michaela Kneissel, Thomas Buhl, Jürg A. Gasser et al.

   Pages 71-92

6. Activated FLT3 Receptor Tyrosine Kinase as a Therapeutic Target In Leukemia

   • Blanca Scheijen, James D. Griffin

   Pages 93-113

7. JAK Kinases in Leukemias, Lymphomas, and Multiple Myeloma

   • Renate Burger, Martin Gramatzki

   Pages 115-144

8. Glivec® (Gleevec®, Imatinib, STI571)

   • Elisabeth Buchdunger, Renaud Capdeville

   Pages 145-160

9. Platelet-Derived Growth Factor

   • Tobias Sjöblom, Kristian Pietras, Arne östman, Carl-Henrik Heldin

   Pages 161-186

10. Structural Biology of Protein Tyrosine Kinases

    • Sandra W. Cowan-Jacob, Paul Ramage, Wilhelm Stark, Gabriele Fendrich, Wolfgang Jahnke

    Pages 187-230

11. Testing of Signal Transduction Inhibitors in Animal Models of Cancer

    • Terence O’Reilly, Robert Cozens

    Pages 231-264

12. Phosphoproteomics in Drug Discovery and Development

    • Michael F. Moran, Jarrod A. Marto, Cynthia J. Brame, Olga Ornatsky, Mark M. Ross, Leticia M. Toledo-Sherman et al.

    Pages 265-278

13. Back Matter

    Pages 279-290

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Leading researchers, from the Novartis group that pioneered Gleevec/Glivec™ 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.

• Proteomics
• biology
• cancer
• drug design
• drug discovery
• protein
• receptor
• structural biology

• Novartis Institutes for BioMedical Research Basel, Novartis Pharma AG, Basel, Switzerland

  Doriano Fabbro

• UCSF Comprehensive Cancer Center, University of California, San Francisco, San Francisco

  Frank McCormick

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