Synthetic essentiality of chromatin remodelling factor CHD1 in PTEN-deficient cancer

Nature. 2017 Feb 23;542(7642):484-488. doi: 10.1038/nature21357. Epub 2017 Feb 6.

Abstract

Synthetic lethality and collateral lethality are two well-validated conceptual strategies for identifying therapeutic targets in cancers with tumour-suppressor gene deletions. Here, we explore an approach to identify potential synthetic-lethal interactions by screening mutually exclusive deletion patterns in cancer genomes. We sought to identify 'synthetic-essential' genes: those that are occasionally deleted in some cancers but are almost always retained in the context of a specific tumour-suppressor deficiency. We also posited that such synthetic-essential genes would be therapeutic targets in cancers that harbour specific tumour-suppressor deficiencies. In addition to known synthetic-lethal interactions, this approach uncovered the chromatin helicase DNA-binding factor CHD1 as a putative synthetic-essential gene in PTEN-deficient cancers. In PTEN-deficient prostate and breast cancers, CHD1 depletion profoundly and specifically suppressed cell proliferation, cell survival and tumorigenic potential. Mechanistically, functional PTEN stimulates the GSK3β-mediated phosphorylation of CHD1 degron domains, which promotes CHD1 degradation via the β-TrCP-mediated ubiquitination-proteasome pathway. Conversely, PTEN deficiency results in stabilization of CHD1, which in turn engages the trimethyl lysine-4 histone H3 modification to activate transcription of the pro-tumorigenic TNF-NF-κB gene network. This study identifies a novel PTEN pathway in cancer and provides a framework for the discovery of 'trackable' targets in cancers that harbour specific tumour-suppressor deficiencies.

Publication types

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

MeSH terms

  • Breast Neoplasms / genetics
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Chromatin Assembly and Disassembly* / genetics
  • DNA Helicases / chemistry
  • DNA Helicases / deficiency
  • DNA Helicases / genetics
  • DNA Helicases / metabolism*
  • DNA-Binding Proteins / chemistry
  • DNA-Binding Proteins / deficiency
  • DNA-Binding Proteins / genetics
  • DNA-Binding Proteins / metabolism*
  • Female
  • Gene Expression Regulation, Neoplastic
  • Genes, Essential / genetics*
  • Glycogen Synthase Kinase 3 beta / metabolism
  • Histones / metabolism
  • Humans
  • Lysine / metabolism
  • Male
  • Methylation
  • Molecular Targeted Therapy
  • NF-kappa B / metabolism
  • Neoplasms / genetics
  • Neoplasms / metabolism*
  • Neoplasms / pathology*
  • PTEN Phosphohydrolase / deficiency*
  • PTEN Phosphohydrolase / genetics
  • PTEN Phosphohydrolase / metabolism
  • Phosphorylation
  • Prostatic Neoplasms / genetics
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / pathology
  • Proteasome Endopeptidase Complex / metabolism
  • Protein Stability
  • Proteolysis
  • Tumor Necrosis Factor-alpha / metabolism
  • Ubiquitination
  • beta-Transducin Repeat-Containing Proteins / metabolism

Substances

  • BTRC protein, human
  • DNA-Binding Proteins
  • Histones
  • NF-kappa B
  • Tumor Necrosis Factor-alpha
  • beta-Transducin Repeat-Containing Proteins
  • Glycogen Synthase Kinase 3 beta
  • PTEN Phosphohydrolase
  • PTEN protein, human
  • Proteasome Endopeptidase Complex
  • DNA Helicases
  • CHD1 protein, human
  • Lysine