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Targeted therapies

Hippo effector YAP1 inhibition—towards a new therapeutic option to overcome drug resistance

Nature Reviews Clinical Oncology volume 12, page 190 (2015)Cite this article

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Targeted therapies using RAF and MEK inhibitors have been developed for the treatment of patients with BRAF/RAS-mutated tumours, and have demonstrated clinical efficacy in melanoma and non-small-cell lung cancer (NSCLC). However, responses are variable, incomplete and transient owing to development of drug resistance. Now, Trever Bivona and colleagues shed new light on the molecular events that limit response to these targeted therapies.

These results indicate a previously unappreciated role for the Hippo–YAP pathway in drug resistance with important clinical implications. “YAP levels could be used as a biomarker to identify patients likely to have a poor response to BRAF and MEK inhibition,” says Bivona. He concludes, “YAP is a new therapeutic target that when co-inhibited with RAF–MEK might enhance response in patients with RAS/BRAF-mutated cancer.”

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References

  1. Lin, L. et al. The Hippo effector YAP promotes resistance to RAF- and MEK-targeted cancer therapies. Nat. Genet. 10.1038/ng.3218

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Authors
  1. Alessia Errico
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Errico, A. Hippo effector YAP1 inhibition—towards a new therapeutic option to overcome drug resistance. Nat Rev Clin Oncol 12, 190 (2015). https://doi.org/10.1038/nrclinonc.2015.31

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  • DOI: https://doi.org/10.1038/nrclinonc.2015.31

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