Genome-wide CRISPR screens reveal synthetic lethality of RNASEH2 deficiency and ATR inhibition

Oncogene. 2019 Apr;38(14):2451-2463. doi: 10.1038/s41388-018-0606-4. Epub 2018 Dec 7.

Abstract

Ataxia telangiectasia mutated and RAD3 related (ATR) protein kinase plays critical roles in ensuring DNA replication, DNA repair, and cell cycle control in response to replication stress, making ATR inhibition a promising therapeutic strategy for cancer treatment. To identify genes whose loss makes tumor cells hypersensitive to ATR inhibition, we performed CRISPR/Cas9-based whole-genome screens in 3 independent cell lines treated with a highly selective ATR inhibitor, AZD6738. These screens uncovered a comprehensive genome-wide profile of ATR inhibitor sensitivity. From the candidate genes, we demonstrated that RNASEH2 deficiency is synthetic lethal with ATR inhibition both in vitro and in vivo. RNASEH2-deficient cells exhibited elevated levels of DNA damage and, when treated with AZD6738, underwent apoptosis (short-time treated) or senescence (long-time treated). Notably, RNASEH2 deficiency is frequently found in prostate adenocarcinoma; we found decreased RNASEH2B protein levels in prostate adenocarcinoma patient-derived xenograft (PDX) samples. Our findings suggest that ATR inhibition may be beneficial for cancer patients with reduced levels of RNASEH2 and that RNASEH2 merits further exploration as a potential biomarker for ATR inhibitor-based therapy.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / drug therapy
  • Adenocarcinoma / genetics
  • Animals
  • Apoptosis / drug effects
  • Apoptosis / genetics
  • Ataxia Telangiectasia Mutated Proteins / genetics*
  • Cell Cycle Checkpoints / drug effects
  • Cell Cycle Checkpoints / genetics
  • Cell Cycle Proteins / genetics
  • Cell Line
  • Cell Line, Tumor
  • Clustered Regularly Interspaced Short Palindromic Repeats / drug effects
  • Clustered Regularly Interspaced Short Palindromic Repeats / genetics*
  • DNA Damage / drug effects
  • DNA Damage / genetics
  • DNA Repair / drug effects
  • DNA Repair / genetics
  • Genome-Wide Association Study / methods
  • HCT116 Cells
  • HEK293 Cells
  • HeLa Cells
  • Humans
  • Indoles
  • Male
  • Mice
  • Mice, Nude
  • Morpholines
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / genetics
  • Pyrimidines / pharmacology
  • Ribonuclease H / genetics*
  • Sulfonamides
  • Sulfoxides / pharmacology

Substances

  • Cell Cycle Proteins
  • Indoles
  • Morpholines
  • Pyrimidines
  • Sulfonamides
  • Sulfoxides
  • ceralasertib
  • ATR protein, human
  • Ataxia Telangiectasia Mutated Proteins
  • ribonuclease HII
  • Ribonuclease H