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Cancer

Drug for an 'undruggable' protein

Nature volume 497, pages 577–578 (2013)Cite this article

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Scientists have long aimed to develop drugs against the cancer-associated protein KRAS, but without success. An approach that targets the oncoprotein's cellular localization reignites lost enthusiasm. See Letter p.638

Human RAS genes have two claims to notoriety. First, they make up the most frequently mutated oncogene family in human cancer, having a prevalence of one in every three cases1. Second, despite more than three decades of intensive effort, no effective pharmacological inhibitor of the RAS oncoprotein has reached the clinic. So it is exciting that, on page 638 of this issue, Zimmermann et al.2 reportFootnote 1 the identification and characterization of a small-molecule inhibitor that interferes with the localization of KRAS — the RAS isoform most commonly mutated in human cancers — to the plasma membrane surrounding cells3.

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Notes

  1. *This article and the paper under discussion2 were published online on 22 May 2013.

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Authors and Affiliations

  1. Department of Pharmacology, Nicole M. Baker and Channing J. Der are in the Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599-7295, USA.,

    Nicole M. Baker & Channing J. Der

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  1. Nicole M. Baker
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  2. Channing J. Der
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Correspondence to Channing J. Der.

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Competing interests

C.J.D. has received honoraria from Bristol-Myers Squibb, Eli Lilly and Merck, and has a research contract with GlaxoSmithKline.

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Baker, N., Der, C. Drug for an 'undruggable' protein. Nature 497, 577–578 (2013). https://doi.org/10.1038/nature12248

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