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Therapy

GTPase Ral—a new tumour target

Nature Reviews Urology volume 11, page 658 (2014)Cite this article

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Novel small molecules can inhibit the activity of the Ras-like GTPases RalA and RalB and suppress tumour xenograft growth in mice, new research demonstrates.

Ras mutations are implicated in the development of many human tumours, but drugs that target Ras or its downstream signalling pathways have poor clinical efficacy. In a novel approach, reported in Nature, Dan Theodorescu and colleagues investigated inhibitors of Ral proteins, which are part of another Ras signalling pathway and have a role in proliferation and metastasis in many cancers, including prostate and bladder tumours. “The starting point was a hypothesis—inactive Ral has a cavity that collapses on activation and, as Ral cycles between inactive and active states, blocking Ral in the inactive form should be therapeutically viable,” explains Theodorescu.

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References

  1. Yan, C. et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature 10.1038/nature13713

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Authors
  1. Clemens Thoma
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Thoma, C. GTPase Ral—a new tumour target. Nat Rev Urol 11, 658 (2014). https://doi.org/10.1038/nrurol.2014.276

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  • DOI: https://doi.org/10.1038/nrurol.2014.276

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