Protein Tyrosine Kinases

From Inhibitors to Useful Drugs

  • Doriano Fabbro
  • Frank McCormick

Part of the Cancer Drug Discovery and Development book series (CDD&D)

Table of contents

  1. Front Matter
    Pages i-xiii
  2. Mark Pearson, Carlos García-Echeverría, Doriano Fabbro
    Pages 1-29
  3. Carlos García-Echeverría
    Pages 31-52
  4. Peter M. Finan, Stephen G. Ward
    Pages 53-69
  5. Mira Šuša, Martin Missbach, Rainer Gamse, Michaela Kneissel, Thomas Buhl, Jürg A. Gasser et al.
    Pages 71-92
  6. Renate Burger, Martin Gramatzki
    Pages 115-144
  7. Elisabeth Buchdunger, Renaud Capdeville
    Pages 145-160
  8. Tobias Sjöblom, Kristian Pietras, Arne östman, Carl-Henrik Heldin
    Pages 161-186
  9. Sandra W. Cowan-Jacob, Paul Ramage, Wilhelm Stark, Gabriele Fendrich, Wolfgang Jahnke
    Pages 187-230
  10. Terence O’Reilly, Robert Cozens
    Pages 231-264
  11. Michael F. Moran, Jarrod A. Marto, Cynthia J. Brame, Olga Ornatsky, Mark M. Ross, Leticia M. Toledo-Sherman et al.
    Pages 265-278
  12. Back Matter
    Pages 279-290

About this book


Protein kinases function as components of signal transduction pathways, playing a central role in the control of cell growth, metabolism, differentiation, and apoptosis. The development of selective protein tyrosine kinase (PTK) inhibitors that can block or modulate diseases, such as cancer, with abnormalities in these signaling pathways is considered a promising approach for drug development. Currently, more than 20 different PTKs are being considered as potential therapeutic targets in oncology. In Protein Tyrosine Kinases: From Inhibitors to Useful Drugs, leading researchers from the Novartis group that pioneered Gleevec/Glivec™ and from 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 toward 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 PTK 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.
Authoritative and state-of-the-art, Protein Tyrosine Kinases: From Inhibitors to Useful Drugs details the key stages in the design of PTK inhibitors and their development into useful drugs.


Proteomics biology cancer drug design drug discovery protein receptor structural biology

Editors and affiliations

  • Doriano Fabbro
    • 1
  • Frank McCormick
    • 2
  1. 1.Novartis Institutes for BioMedical Research BaselNovartis Pharma AGBaselSwitzerland
  2. 2.UCSF Comprehensive Cancer CenterUniversity of California, San FranciscoSan Francisco

Bibliographic information