A hypoxia-responsive TRAF6-ATM-H2AX signalling axis promotes HIF1α activation, tumorigenesis and metastasis

Nat Cell Biol. 2017 Jan;19(1):38-51. doi: 10.1038/ncb3445. Epub 2016 Dec 5.

Abstract

The understanding of how hypoxia stabilizes and activates HIF1α in the nucleus with related oncogenic signals could revolutionize targeted therapy for cancers. Here, we find that histone H2AX displays oncogenic activity by serving as a crucial regulator of HIF1α signalling. H2AX interacts with HIF1α to prevent its degradation and nuclear export in order to allow successful VHL-independent HIF1α transcriptional activation. We show that mono-ubiquitylation and phosphorylation of H2AX, which are strictly mediated by hypoxia-induced E3 ligase activity of TRAF6 and ATM, critically regulate HIF1α-driven tumorigenesis. Importantly, TRAF6 and γH2AX are overexpressed in human breast cancer, correlate with activation of HIF1α signalling, and predict metastatic outcome. Thus, TRAF6 and H2AX overexpression and γH2AX-mediated HIF1α enrichment in the nucleus of cancer cells lead to overactivation of HIF1α-driven tumorigenesis, glycolysis and metastasis. Our findings suggest that TRAF6-mediated mono-ubiquitylation and subsequent phosphorylation of H2AX may serve as potential means for cancer diagnosis and therapy.

MeSH terms

  • Animals
  • Ataxia Telangiectasia Mutated Proteins / metabolism*
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Carcinogenesis / metabolism*
  • Carcinogenesis / pathology
  • Cell Hypoxia
  • Cell Line, Tumor
  • Cell Nucleus / metabolism
  • Cell Proliferation
  • Cellular Senescence
  • Female
  • Fibroblasts / metabolism
  • Gene Knockdown Techniques
  • Glycolysis
  • Histones / metabolism*
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / metabolism*
  • Immunohistochemistry
  • Mice
  • Neoplasm Metastasis
  • Protein Stability
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Signal Transduction*
  • TNF Receptor-Associated Factor 6 / metabolism*
  • Treatment Outcome
  • Ubiquitin / metabolism

Substances

  • H2AX protein, human
  • H2AX protein, mouse
  • Histones
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • RNA, Messenger
  • TNF Receptor-Associated Factor 6
  • Ubiquitin
  • Ataxia Telangiectasia Mutated Proteins