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The (un)targeted cancer kinome

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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Correspondence to Stefan Knapp.

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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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