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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Exploiting Substrate Recognition for Selective Inhibition of Protein Kinases

Author(s): Avital Licht-Murava and Hagit Eldar-Finkelman

Volume 18, Issue 20, 2012

Page: [2914 - 2920] Pages: 7

DOI: 10.2174/138161212800672741

Price: $65


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).

Keywords: Protein kinase, GSK-3, substrate recognition, inhibitor design, substrate binding site, competitive inhibitors, selectivity, phosphorylation, Synthetic peptides, long-term treatment

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