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The (un)targeted cancer kinome

Nature Chemical Biology volume 6, pages 166–169 (2010)Cite this article

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The complexity of cancer signaling and the resulting difficulties in target selection have strongly biased kinase drug discovery towards clinically validated targets. Recently, novel kinase targets that are uncharacterized have emerged from genome sequencing and RNAi studies. Chemical probes are urgently needed to functionally annotate these kinases and to stimulate new drug discovery efforts.

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Figure 1: Kinase targets in clinical trials and the currently targeted kinome.
Figure 2: Kinase structure and inhibitor design.

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Authors and Affiliations

  1. Susanne Müller and Stefan Knapp are in the Nuffield Department of Clinical Medicine, Oleg Fedorov, Structural Genomics Consortium, University of Oxford, Oxford, UK.,

    Oleg Fedorov, Susanne Müller & Stefan Knapp

  2. Stefan Knapp is also in the Department of Clinical Pharmacology, University of Oxford, Oxford, UK.,

    Stefan Knapp

Authors
  1. Oleg Fedorov
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  2. Susanne Müller
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  3. Stefan Knapp
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Correspondence to Stefan Knapp.

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The authors declare no competing financial interests.

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Fedorov, O., Müller, S. & Knapp, S. The (un)targeted cancer kinome. Nat Chem Biol 6, 166–169 (2010). https://doi.org/10.1038/nchembio.297

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