GSK-3 inhibition: Achieving moderate efficacy with high selectivity

Limor Avrahami, Avital Licht-Murava, Miriam Eisenstein, Hagit Eldar-Finkelman*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review


Inhibiting glycogen synthase kinase-3 (GSK-3) activity has become an attractive approach for treatment of neurodegenerative and psychiatric disorders. Diverse GSK-3 inhibitors have been reported and used in cellular and in vivo models. A major challenge, however, is achieving selectivity. In addition, it is increasingly recognized that a moderate inhibition of a cellular target, particularly for long-term treatment, provides more favorable outcome than complete inhibition. Substrate competitive inhibitors can fulfill the requirement for selectivity and allow fine tuning of the degree of inhibition. Here we describe the therapeutic potential of GSK-3 inhibitors and highlight our progress in the development of substrate competitive inhibitors. This article is part of a Special Issue entitled: Inhibitors of Protein Kinases (2012).

Original languageEnglish
Pages (from-to)1410-1414
Number of pages5
JournalBiochimica et Biophysica Acta - Proteins and Proteomics
Issue number7
StatePublished - 2013


  • Alzheimer's disease
  • CNS disorders
  • Drug design
  • GSK-3 inhibitors
  • L803-mts


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