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Targeting Histone Demethylases in MYC-Driven Neuroblastomas with Ciclopirox

Jun Yang1, Sandra Milasta2, Dongli Hu3

  • 1Department of Surgery, St. Jude Children's Research Hospital, Memphis, Tennessee. Jun.Yang2@stjude.org.

Cancer Research
|July 8, 2017
PubMed

Insights

The antifungal drug ciclopirox inhibits histone demethylases, crucial for neuroblastoma cell survival and MYC oncogene activity. This discovery offers a new strategy for targeting cancer by indirectly inhibiting MYC signaling.

Area of Science:

  • Epigenetics
  • Molecular Oncology
  • Drug Discovery

Background:

  • Histone lysine demethylases regulate oncogenic transcription factors like MYC.
  • MYC is frequently overexpressed in neuroblastoma, contributing to poor prognosis.
  • Targeting epigenetic modifiers offers a potential therapeutic strategy for MYC-driven cancers.

Purpose of the Study:

  • To investigate the role of histone demethylases in neuroblastoma.
  • To identify novel inhibitors of histone demethylases.
  • To explore the therapeutic potential of targeting histone demethylases in neuroblastoma.

Main Methods:

  • Assessed the impact of histone demethylases on neuroblastoma cell viability and prognosis.
  • Screened for small-molecule inhibitors of histone demethylases.
  • Investigated the mechanism of action of identified inhibitors on MYC signaling and cellular metabolism.

Main Results:

  • Multiple histone demethylases were found to influence neuroblastoma cell viability and prognosis.
  • Ciclopirox, an antifungal agent, was identified as a novel pan-histone demethylase inhibitor.
  • Ciclopirox inhibited MYC signaling, mitochondrial oxidative phosphorylation, and suppressed neuroblastoma tumor growth, inducing differentiation.

Conclusions:

  • Histone demethylases are critical regulators of MYC function in neuroblastoma.
  • Ciclopirox represents a promising therapeutic agent for neuroblastoma by indirectly targeting MYC.
  • Targeting histone demethylases offers a novel indirect approach for MYC-targeting cancer therapy.

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