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Nat Rev Cancer. 2017 Aug;17(8):502-508. doi: 10.1038/nrc.2017.36. Epub 2017 Jun 23.

Drugging the 'undruggable' cancer targets.

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Abramson Cancer Center, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
Ludwig Institute for Cancer Research, New York, New York 10017, USA, and The Wistar Institute, Philadelphia, Pennsylvania 19104, USA.
Department of Oncological Sciences, Icahn School of Medicine at Mount Sinai, 1425 Madison Avenue, New York, New York 10029, USA.
Department of Cellular and Molecular Pharmacology, University of California, San Francisco &Howard Hughes Medical Institute, San Francisco, California 94158, USA.
Vall d'Hebron Institute of Oncology (VHIO), Cellex Centre, Barcelona 08035; Institució Catalana de Recerca i Estudis Avançats (ICREA), Barcelona 08010; and Department of Biochemistry and Molecular Biology, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain.


The term 'undruggable' was coined to describe proteins that could not be targeted pharmacologically. However, progress is being made to 'drug' many of these targets, and therefore more appropriate terms might be 'difficult to drug' or 'yet to be drugged'. Many desirable targets in cancer fall into this category, including the RAS and MYC oncogenes, and pharmacologically targeting these intractable proteins is now a key challenge in cancer research that requires innovation and the development of new technologies. In this Viewpoint article, we asked four scientists working in this field for their opinions on the most crucial advances, as well as the challenges and what the future holds for this important area of research.

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