Nature Communications (Feb 2021)

Mutant-selective degradation by BRAF-targeting PROTACs

  • Shanique Alabi,
  • Saul Jaime-Figueroa,
  • Zhan Yao,
  • Yijun Gao,
  • John Hines,
  • Kusal T. G. Samarasinghe,
  • Lea Vogt,
  • Neal Rosen,
  • Craig M. Crews

DOI
https://doi.org/10.1038/s41467-021-21159-7
Journal volume & issue
Vol. 12, no. 1
pp. 1 – 11

Abstract

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Hundreds of BRAF mutations have been identified in patients with cancer but currently approved drugs only target BRAF V600 mutants. Here, the authors develop a vemurafenib-based PROTAC that induces degradation of all classes of BRAF mutants without affecting wild-type RAF proteins.