BRD4 amplification facilitates an oncogenic gene expression program in high-grade serous ovarian cancer and confers sensitivity to BET inhibitors

PLoS One. 2018 Jul 23;13(7):e0200826. doi: 10.1371/journal.pone.0200826. eCollection 2018.

Abstract

BRD4 is a transcriptional co-activator functioning to recruit regulatory complexes to acetylated chromatin. A subset of High-grade Serous Ovarian Cancer (HGSOC) patients are typified by focal, recurrent BRD4 gene amplifications. Despite previously described cancer dependencies, it is unclear whether BRD4 amplification events are oncogenic in HGSOC. We find that physiologically relevant levels of expression of BRD4 isoforms in non-transformed ovarian cells result in cellular transformation. Transcriptional profiling of BRD4-transformed ovarian cells, and BRD4-amplified HGSOC patient samples revealed shared expression patterns, including enriched MYC, and E2F1 gene signatures. Furthermore, we demonstrate that a novel BET inhibitor, AZD5153, is highly active in BRD4-amplified patient derived xenografts and uncover Neuregulin-1 as a novel BRD4 effector. Experiments involving Neuregulin-1 inhibition and exogenous addition, demonstrate Neuregulin-1 as necessary and sufficient for BRD4-mediated transformation. This study demonstrates the oncogenic potential of BRD4 amplification in cancer and establishes BRD4-amplified HGSOC as a potential patient population that could benefit from BET inhibitors.

Publication types

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

MeSH terms

  • Algorithms
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Carcinogenesis / genetics
  • Cell Cycle Proteins
  • Cell Line, Tumor
  • Cell Proliferation
  • Cystadenocarcinoma, Serous / genetics
  • Female
  • Gene Expression
  • Gene Expression Profiling
  • Gene Expression Regulation, Neoplastic*
  • Heterocyclic Compounds, 2-Ring / pharmacology*
  • Humans
  • Mice
  • Neoplasm Transplantation
  • Neuregulin-1 / metabolism
  • Nuclear Proteins / genetics*
  • Nuclear Proteins / metabolism
  • Ovarian Neoplasms / drug therapy
  • Ovarian Neoplasms / genetics*
  • Ovarian Neoplasms / metabolism
  • Piperazines / pharmacology*
  • Proteins / genetics
  • Proteins / metabolism
  • Pyrazoles
  • Pyridazines
  • Signal Transduction
  • Transcription Factors / genetics*
  • Transcription Factors / metabolism
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • BRD4 protein, human
  • Cell Cycle Proteins
  • Heterocyclic Compounds, 2-Ring
  • Neuregulin-1
  • Nuclear Proteins
  • Piperazines
  • Proteins
  • Pyrazoles
  • Pyridazines
  • Transcription Factors
  • bromodomain and extra-terminal domain protein, human
  • AZD5153