Exploiting substrate recognition for selective inhibition of protein kinases

Avital Licht-Murava, Hagit Eldar-Finkelman*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

Protein kinases are potential targets of drugs to treat many human diseases. Intensive efforts have been made to develop protein kinase inhibitors, but a major challenge is achieving specificity. Exploiting regulatory elements outside the ATP binding pocket, such as the substrate binding site, may provide an alternative that allows generation of competitive inhibitors with improved selectivity. Indepth understanding of substrate recognition by protein kinase is essential for design and refinement of competitive inhibitors. Here we described strategies for specifically targeting protein kinases and highlight our current progress in the development of substrate competitive inhibitors for glycogen synthase kinase-3 (GSK-3).

Original languageEnglish
Pages (from-to)2914-2920
Number of pages7
JournalCurrent Pharmaceutical Design
Volume18
Issue number20
DOIs
StatePublished - Jul 2012

Keywords

  • GSK-3
  • Inhibitor design
  • Protein kinase
  • Substrate recognition

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