Protein Drugs Handbook from C.H.I.P.S.

Kinase Inhibitor Drugs
edited by Rongshi Li

A comprehensive resource on case studies of marketed kinase drugs and promising drug trials.

Kinase Inhibitor Drugs presents timely and important case studies of marketed kinase drugs and several of the most advanced kinase inhibitors in clinical trials.

Kinase Inhibitor Drugs includes:

  • Case studies from leading investigators and experts in the field that provide firsthand accounts of kinase inhibitor discovery
  • Current thinking on kinase structure, biochemistry, and signal transduction pathways
  • Information on state-of-the-art technologies and tools such as structure-based and fragment-based drug discovery
  • A lineup of clinical-phase growth factor receptor inhibitors
  • Inhibitors of cell cycle kinases
  • The discovery of allosteric inhibitors of MEK kinase
  • Information on pharmacogenomics and its application to kinase inhibitor clinical development


Part I: Growth Factor Inhibitors: VEGFR2, ERBB2, and Other Kinase

  1. Discovery and Development of Sunitinib (SU11248): A Multitarget Tyrosine Kinase Inhibitor of Tumor Growth, Survival, and Angiogenesis
  2. Tykerb Discovery: A Dual EGFR and ERBB2 Tyrosine Kinase Inhibitor
  3. Discovery of Pazopanib: A Pan Vascular Endothelial Growth Factor Kinase Inhibitor
  4. Road to ABT-869: A Multitargeted Receptor Tyrosine Kinase Inhibitor
  5. Discovery of Motesanib
  6. Discovery of Brivanib Alaninate: A Dual Vascular Endothelial Growth Factor and Fibroblast Growth Factor Receptor Inhibitor
  7. S tructure-Based Design and Characterization of Axitinib

Part II: Growth Factor Inhibitors: MEK Inhibitors

  1. Road to PD0325901 and Beyond: The MEK Inhibitor Quest
  2. Discovery of Allosteric MEK Inhibitors

Part III: Cell Cycle Kinase Inhibitors: Aurora Kinase and PLK Inhibitors

  1. Discovery of MK-0457 (VX-680)
  2. Discovery of PHA-739358
  3. Discovery of AZD1152: A Selective Inhibitor of Aurora-B Kinase with Potent Antitumor Activity
  4. Case Study of Aurora-A Inhibitor MLN8054
  5. Discovery of GSK461364: A Polo-like Kinase 1 Inhibitor for the Treatment of Cancer

Part IV: Related Special Topics

  1. Pharmacogenomics of Dasatinib (Sprycel)
  2. Practical Use of Computational Chemistry in Kinase Drug Discovery
  3. Approaches to Kinase Homology Modeling: Successes and Considerations for the Structural Kinome
  4. Fragment-Based Drug Discovery of Kinase Inhibitors
  5. Protein Kinase Structural Biology: Methods and Strategies for Targeted Drug Discovery


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Kinase Inhibitor Drugs
edited by Rongshi Li
2010 (available now) 510 pages $114.95 + shipping
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