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IDrugs. 2010 Jul;13(7):457-66.

The 'retro-design' concept for novel kinase inhibitors.

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Proteros Fragments GmbH, Fraunhoferstrasse 20, 82152 Martinsried, Germany.


Protein kinases are among the most attractive therapeutic targets for a broad range of diseases. This feature review highlights and classifies the main design principles employed to generate active and selective kinase inhibitors. In particular, emphasis is focused on a fragment-based lead-generation approach, which constitutes a novel design method for developing type II kinase inhibitors with distinct binding kinetic attributes. This 'retro-design' strategy relies on a customized fragment library, and contrasts the traditional approach used in the design of type II inhibitors.

[Indexed for MEDLINE]

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