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An enolase inhibitor for the targeted treatment of ENO1-deleted cancers

Yu-Hsi Lin1, Nikunj Satani1,2, Naima Hammoudi1

  • 1Department of Cancer Systems Imaging, University of Texas MD Anderson Cancer Center, Houston, TX, USA.

Nature Metabolism
|November 24, 2020
PubMed

Insights

Targeting cancer glycolysis is a key goal. A new drug, POMHEX, selectively kills cancer cells lacking enolase 1 (ENO1) by inhibiting enolase 2 (ENO2), demonstrating collateral lethality in preclinical models.

Area of Science:

  • Biochemistry
  • Oncology
  • Pharmacology

Background:

  • Glycolysis inhibition is a promising cancer treatment strategy.
  • Cancers with homozygous deletion of enolase 1 (ENO1) show sensitivity to ENO2 inhibition via collateral lethality.

Purpose of the Study:

  • To evaluate a small-molecule enolase inhibitor, POMHEX, for its efficacy against ENO1-deleted cancers.
  • To demonstrate the therapeutic potential of collateral lethality in precision oncology.

Main Methods:

  • Treatment of ENO1-deleted glioma cells with POMHEX.
  • In vivo studies using intracranial orthotopic ENO1-deleted tumor models in mice.
  • Toxicity assessment of POMHEX in non-human primates.

Main Results:

  • POMHEX selectively killed ENO1-deleted glioma cells at low nanomolar concentrations.
  • POMHEX eradicated intracranial ENO1-deleted tumors in mice.
  • POMHEX was well-tolerated in non-human primates.

Conclusions:

  • POMHEX is a potent inhibitor of glycolysis with selective activity against ENO1-deleted cancers.
  • Collateral lethality is a viable therapeutic strategy in precision oncology.
  • POMHEX shows promise for cancer treatment across various settings.

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