Journal article
GSK-3 inhibition: Achieving moderate efficacy with high selectivity
Biochimica Et Biophysica Acta-Proteins And Proteomics, Vol.1834(7), pp.1410-1414
Jul/2013
Abstract
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). (C) 2013 Elsevier B.V. All rights reserved.
Details
- Title
- GSK-3 inhibition; Achieving moderate efficacy with high selectivity
- Creators
- Limor Avrahami (null)Avital Licht-Murava (null)Miriam Eisenstein (null) - 972WIS_INST___100Hagit Eldar-Finkelman (null)
- Resource Type
- Journal article; Review
- Publication Details
- Biochimica Et Biophysica Acta-Proteins And Proteomics, Vol.1834(7), pp.1410-1414; Jul/2013
- Number of pages
- 5
- Language
- English
- DOI
- https://doi.org/10.1016/j.bbapap.2013.01.016
- Record Identifier
- 993262901303596
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