Targeting AURKA-CDC25C axis to induce synthetic lethality in ARID1A-deficient colorectal cancer cells

Nat Commun. 2018 Aug 10;9(1):3212. doi: 10.1038/s41467-018-05694-4.

Abstract

ARID1A, a component of the SWI/SNF chromatin remodeling complex, is a tumor suppressor with a high frequency of inactivating mutations in many cancers. Therefore, ARID1A deficiency has been exploited therapeutically for treating cancer. Here we show that ARID1A has a synthetic lethal interaction with aurora kinase A (AURKA) in colorectal cancer (CRC) cells. Pharmacological and genetic perturbations of AURKA selectively inhibit the growth of ARID1A-deficient CRC cells. Mechanistically, ARID1A occupies the AURKA gene promoter and negatively regulates its transcription. Cells lacking ARID1A show enhanced AURKA transcription, which leads to the persistent activation of CDC25C, a key protein for G2/M transition and mitotic entry. Inhibiting AURKA activity in ARID1A-deficient cells significantly increases G2/M arrest and induces cellular multinucleation and apoptosis. This study shows a novel synthetic lethality interaction between ARID1A and AURKA and indicates that pharmacologically inhibiting the AURKA-CDC25C axis represents a novel strategy for treating CRC with ARID1A loss-of-function mutations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis
  • Aurora Kinase A / antagonists & inhibitors
  • Aurora Kinase A / genetics
  • Aurora Kinase A / metabolism*
  • Colorectal Neoplasms / genetics*
  • Colorectal Neoplasms / pathology
  • DNA-Binding Proteins
  • Drug Evaluation, Preclinical
  • Female
  • G2 Phase
  • Gene Knockout Techniques
  • Humans
  • Mice, Inbred BALB C
  • Mice, Nude
  • Mitosis
  • Nuclear Proteins / deficiency*
  • Nuclear Proteins / metabolism
  • Signal Transduction*
  • Synthetic Lethal Mutations / genetics*
  • Transcription Factors / deficiency*
  • Transcription Factors / metabolism
  • Transcription, Genetic
  • cdc25 Phosphatases / metabolism*

Substances

  • ARID1A protein, human
  • DNA-Binding Proteins
  • Nuclear Proteins
  • Transcription Factors
  • AURKA protein, human
  • Aurora Kinase A
  • CDC25C protein, human
  • cdc25 Phosphatases