Exploiting substrate recognition for selective inhibition of protein kinases.

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. In-depth 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).

journal_name

Curr Pharm Des

authors

Licht-Murava A,Eldar-Finkelman H

doi

10.2174/138161212800672741

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

2914-20

issue

20

eissn

1381-6128

issn

1873-4286

pii

CPD-EPUB-20120504-007

journal_volume

18

pub_type

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