WEE1 kinase is a therapeutic vulnerability in CIC-DUX4 undifferentiated sarcoma

JCI Insight. 2022 Mar 22;7(6):e152293. doi: 10.1172/jci.insight.152293.

Abstract

CIC-DUX4 rearrangements define an aggressive and chemotherapy-insensitive subset of undifferentiated sarcomas. The CIC-DUX4 fusion drives oncogenesis through direct transcriptional upregulation of cell cycle and DNA replication genes. Notably, CIC-DUX4-mediated CCNE1 upregulation compromises the G1/S transition to confer a dependence on the G2/M cell cycle checkpoint. Through an integrative transcriptional and kinase activity screen using patient-derived specimens, we now show that CIC-DUX4 sarcomas depend on the G2/M checkpoint regulator WEE1 as part of an adaptive survival mechanism. Specifically, CIC-DUX4 sarcomas depended on WEE1 activity to limit DNA damage and unscheduled mitotic entry. Consequently, genetic or pharmacologic WEE1 inhibition in vitro and in vivo led to rapid DNA damage-associated apoptotic induction of patient-derived CIC-DUX4 sarcomas. Thus, we identified WEE1 as a vulnerability targetable by therapeutic intervention in CIC-DUX4 sarcomas.

Keywords: Cancer; Oncology.

MeSH terms

  • Cell Cycle Proteins* / genetics
  • Gene Rearrangement
  • Humans
  • Oncogene Proteins, Fusion / genetics
  • Protein-Tyrosine Kinases* / genetics
  • Sarcoma, Small Cell* / genetics
  • Soft Tissue Neoplasms* / genetics

Substances

  • CIC-DUX4 fusion protein, human
  • Cell Cycle Proteins
  • Oncogene Proteins, Fusion
  • Protein-Tyrosine Kinases
  • WEE1 protein, human