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Protein structure determination of soluble globular protein domains has developed into an efficient routine technology which can now be applied to generate and analyze structures of entire human protein families. In the kinase area, several kinase families still lack comprehensive structural analysis. Nevertheless, Structural Genomics (SG) efforts contributed more than 40 kinase catalytic domain structures during the past 4 years providing a rich resource of information for large scale comparisons of kinase active sites. Moreover, many of the released structures are inhibitor complexes that offer chemical starting points for development of selective and potent inhibitors. Here we discuss the currently available structural data and strategies that can be utilized for the development of highly selective inhibitors.

Original publication

DOI

10.1016/j.bbapap.2009.10.013

Type

Journal article

Journal

Biochim Biophys Acta

Publication Date

03/2010

Volume

1804

Pages

429 - 432

Keywords

Animals, Humans, Protein Kinase Inhibitors, Protein Kinases, Protein Structure, Tertiary, Structure-Activity Relationship