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Killing two kinase families with one stone

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Multitargeted protein kinase inhibitors have shown great promise in cancer therapy, but the selectivity profiles of these compounds have largely relied on serendipity or 'off-target' activities rather than rational drug design. Purposefully designed compounds with activity against multiple target kinases bring us a step closer to personalized medicine.

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Figure 1: Size and shape selectivity of dual PI3K and tyrosine kinase inhibitors.

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B.V. is an advisor to Intellikine, and N.T. is a paid employee of Piramed Pharma.

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Bilanges, B., Torbett, N. & Vanhaesebroeck, B. Killing two kinase families with one stone. Nat Chem Biol 4, 648–649 (2008). https://doi.org/10.1038/nchembio1108-648

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