Strategically targeting MYC in cancer

Valeriya Posternak1, Michael D Cole2

  • 1Department of Pharmacology and Toxicology, Geisel School of Medicine at Dartmouth, Norris Cotton Cancer Center, Lebanon, NH, USA.

F1000Research
|April 16, 2016
PubMed

Insights

Targeting MYC (Myc) oncoprotein is crucial for cancer therapy. Researchers are developing novel compounds that indirectly inhibit MYC transcription, showing promise for treating MYC-driven cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The MYC oncoprotein drives cancer progression by regulating genes involved in cell growth, proliferation, metabolism, and survival.
  • Targeting MYC is a key strategy in cancer therapy, with various compounds developed to inhibit its function or stability.
  • Direct MYC inhibitors targeting the MYC-MAX interaction have shown limitations in pharmacokinetic and pharmacodynamic properties for in vivo use.

Purpose of the Study:

  • To review the development of compounds that indirectly inhibit MYC.
  • To highlight the therapeutic potential of novel MYC-targeting agents in MYC-driven cancers.

Main Methods:

  • Review of recent studies on compounds inhibiting MYC transcription.
  • Analysis of indirect inhibition strategies targeting transcription factors.

Main Results:

  • Two compounds, JQ1 and THZ1, indirectly inhibit MYC by targeting unique transcription stages.
  • These compounds demonstrate therapeutic value in MYC-driven cancers, though some effects may be MYC-independent.
  • Current indirect inhibition approaches provide a basis for developing new anti-cancer drugs.

Conclusions:

  • Indirect inhibition of MYC through transcription targeting represents a promising therapeutic strategy.
  • Novel compounds targeting MYC transcription hold potential for treating various cancers.
  • Further research into MYC-targeting agents is essential for advancing cancer therapy.

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