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Structural biology contributions to tyrosine kinase drug discovery

Jacob, Sandra, Moebitz, Henrik and Fabbro, Doriano (2009) Structural biology contributions to tyrosine kinase drug discovery. Current Opinion in Cell Biology, 21 (2). pp. 280-287. ISSN 1879-0410


Successful kinase inhibitor drug discovery relies heavily on the structural knowledge of the interaction of inhibitors with the target. Structural biology of kinases and in particular of tyrosine kinases has given detailed insights into the intrinsic flexibility of the catalytic domain and has provided a rational basis for obtaining selective inhibitors. Important progress has been made recently, both in academia and in the pharmaceutical industry, with respect to solving structures of inactive, multidomain or protein-protein complexes of kinases, which helps our understanding of the dynamics of regulation of kinase activity. This leads to a better understanding of how mutations lead to activation of kinases and resistance, in addition to providing opportunities for novel modes of targeting kinases.

Item Type: Article
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Additional Information: Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
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Date Deposited: 22 Feb 2010 11:49
Last Modified: 31 Jan 2013 00:49


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