CHK it out! Blocking WEE kinase routs TP53 mutant cancer

Clin Cancer Res. 2014 Aug 15;20(16):4173-5. doi: 10.1158/1078-0432.CCR-14-0720.

Abstract

Mutations in TP53, encoding the master tumor suppressor p53, have posed a developmental therapeutic dilemma due to inability to target loss of function. Inhibition of WEE1 or CHK1 kinase, negative regulators of the G2-M checkpoint, selectively sensitizes p53-deficient cells to exogenous DNA damage, abrogating G2 arrest and precipitating mitotic catastrophe.

Publication types

  • Research Support, N.I.H., Extramural
  • Comment

MeSH terms

  • Animals
  • Carcinoma, Squamous Cell / metabolism*
  • Cell Cycle Proteins / antagonists & inhibitors*
  • Head and Neck Neoplasms / metabolism*
  • Humans
  • Nuclear Proteins / antagonists & inhibitors*
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinases / chemistry*
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • RNA, Small Interfering / genetics*
  • Tumor Suppressor Protein p53 / metabolism*

Substances

  • Cell Cycle Proteins
  • Nuclear Proteins
  • Protein Kinase Inhibitors
  • RNA, Small Interfering
  • Tumor Suppressor Protein p53
  • Protein Kinases
  • Protein-Tyrosine Kinases