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  • IN BRIEF

SUMO1 degrader extends mouse survival

  1. Sarah Crunkhorn
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Although sumoylation has been widely implicated in cancer, therapeutic blockade has been challenging due to a lack of safe and specific drug targets. Using a cancer cell-based screen, Bellail et al. have identified HB007, a small-molecule degrader of the SUMO1 protein. HB007 was found to bind to CAPRIN1 and induce its interaction with FBXO42, which led to recruitment of SUMO1 to the CAPRIN-CUL1-FBXO42 ubiquitin ligase complex, resulting in degradation of SUMO1 and growth inhibition in human cancer cells. In xenograft mouse models, HB007 selectively degraded SUMO1, inhibited cancer progression and increased survival.

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Nature Reviews Drug Discovery 20, 898 (2021)

doi: https://doi.org/10.1038/d41573-021-00182-9

References

  1. Bellail, A. C. et al. Ubiquitination and degradation of SUMO1 by small-molecule degraders extends survival of mice with patient-derived tumors. Sci. Transl Med. 13, eabh1486 (2021)

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