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Killing two kinase families with one stone

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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