It is widely appreciated that MYCN is a potent oncogene but efforts to inhibit it have been hampered by the lack of surfaces to which small molecules can bind. Now, Gustafson et al. have shown that targeting and destabilizing Aurora kinase A (AURKA), a binding partner of MYCN, is sufficient to inhibit MYCN activity in a variety of tumour types. This result highlights AURKA inhibitors as potential anticancer therapeutics in a variety of MYCN- and, possibly, MYC-driven tumours.
References
Gustafson, W. C. et al. Drugging MYCN through an allosteric transition in aurora kinase A. Cancer Cell 26, 414–427 (2014)
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Lokody, I. Disrupting an oncogenic relationship. Nat Rev Cancer 14, 649 (2014). https://doi.org/10.1038/nrc3833
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DOI: https://doi.org/10.1038/nrc3833