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  • RESEARCH HIGHLIGHT

Small-molecule PI3Kα binder with selective anticancer activity

By
  1. Katie Kingwell
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Mutations in the gene encoding PI3Kα are associated with several types of cancer, but selectively targeting oncogenic signalling while leaving physiological PI3Kα activity intact has proved challenging. A new study in Science reports the design of an oral small molecule, BBO-10203, that disrupts a cancer-associated RAS–PI3Kα interaction but preserves other PI3Kα functions including regulation of insulin signalling.

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Nature Reviews Drug Discovery 24, 664 (2025)

doi: https://doi.org/10.1038/d41573-025-00136-5

References

  1. Simanshu, D. K. et al. BBO-10203 inhibits tumor growth without inducing hyperglycemia by blocking RAS-PI3Kα interaction. Science 389, 409–415 (2025)

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