Creating chemical diversity to target protein kinases

Comb Chem High Throughput Screen. 2004 Aug;7(5):453-72. doi: 10.2174/1386207043328580.


Protein kinases play crucial roles in regulating virtually every cellular process and are currently attracting tremendous interest as drug targets from the pharmaceutical industry. The major challenges facing the development of the potential kinase inhibitor drugs are: selectivity, physical properties (solubility, molecular weight), and pharmacological properties (bioavailability, half life, toxicity, etc.) This review focuses on how selective protein kinase inhibitors that target the ATP and allosteric binding sites are currently being identified and optimized.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Molecular Conformation
  • Protein Kinase Inhibitors*
  • Protein Kinases / chemistry
  • Structure-Activity Relationship


  • Enzyme Inhibitors
  • Protein Kinase Inhibitors
  • Protein Kinases