Understanding and exploiting substrate recognition by protein kinases

Curr Opin Chem Biol. 2008 Feb;12(1):4-10. doi: 10.1016/j.cbpa.2008.01.018. Epub 2008 Mar 7.


Protein kinases play a virtually universal role in cellular regulation and are emerging as an important class of new drug targets, yet the cellular functions of most human kinases largely remain obscure. Aspects of substrate recognition common to all kinases in the ATP nucleotide binding site have been exploited in the generation of analog-specific mutants for exploring kinase function and discovering novel protein substrates. Likewise, understanding interactions with the protein substrate, which differ substantially between kinases, can also help to identify substrates and to produce tools for studying kinase pathways, including fluorescent biosensors. Principles of kinase substrate recognition are particularly valuable in guiding bioinformatics and phosphoproteomics approaches that impact our understanding of signaling pathways and networks on a global scale.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Amino Acid Motifs
  • Animals
  • Binding Sites
  • Biosensing Techniques
  • Humans
  • Protein Binding
  • Protein Kinases / chemistry*
  • Protein Kinases / metabolism*
  • Substrate Specificity


  • Protein Kinases