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Anticancer drugs

Redesigning kinase inhibitors

Nature Reviews Drug Discovery volume 7, pages 120–121 (2008)Cite this article

Protein kinases are prime targets for anticancer therapies, but their close structural similarities can make achieving specificity for a particular kinase challenging, potentially leading to unwanted side effects. With this in mind, the authors aimed to redesign imatinib, focusing its specificity on C-Kit (also known as KIT) kinase inhibition (the therapeutic target for GIST) while reducing its effect on the kinase BCR–ABL (the therapeutic target for CML), which has also been linked to the cardiovascular side effects of the drug. Furthermore, they aimed to promote inhibition of JNK1, as previous research has indicated that this could ameliorate the adverse effects of imatinib on heart cells.

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ORIGINAL RESEARCH PAPER

  1. Fernández, A. et al. An anticancer C-Kit kinase inhibitor is reengineered to make it more active and less cardiotoxic. J. Clin. Invest. 117, 4044–4054 (2007)

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  1. Sarah Crunkhorn
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Crunkhorn, S. Redesigning kinase inhibitors. Nat Rev Drug Discov 7, 120–121 (2008). https://doi.org/10.1038/nrd2524

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  • DOI: https://doi.org/10.1038/nrd2524

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