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Sigma-1 Receptor Modulation by Ligands Coordinates Cancer Cell Energy Metabolism

Furkan E Oflaz1, Zhanat Koshenov1, Martin Hirtl1

  • 1Molecular Biology and Biochemistry, Gottfried Schatz Research Center, Medical University of Graz, 8010 Graz, Austria.

Biomolecules
|June 24, 2022
PubMed

Insights

Sigma-1 receptor (S1R) activation boosts cancer cell mitochondrial energy production and reduces glycolysis. S1R ligands may offer new ways to target cancer metabolism.

Area of Science:

  • Biochemistry
  • Cell Biology
  • Oncology

Background:

  • The sigma-1 receptor (S1R) is a key endoplasmic reticulum chaperone involved in cellular functions.
  • S1R's role in cancer energy metabolism, particularly under different activation states, requires further elucidation.

Purpose of the Study:

  • To investigate the involvement of S1R in cancer cell energy metabolism.
  • To determine how S1R activation and inactivation influence mitochondrial bioenergetics and glycolysis.

Main Methods:

  • Utilized two cancer cell lines with differential S1R expression.
  • Administered S1R agonist ((+)-SKF10047) and antagonist (BD1047).
  • Analyzed real-time ion and metabolite fluxes using single-cell fluorescence microscopy.

Main Results:

  • S1R activation by agonist enhanced mitochondrial bioenergetics in cancer cells.
  • S1R activation decreased cancer cell reliance on aerobic glycolysis.
  • S1R antagonist showed minimal impact on mitochondrial bioenergetics but increased aerobic glycolysis in S1R-expressing cells.

Conclusions:

  • S1R significantly influences cancer cell energy metabolism.
  • S1R ligands can be employed as tools to modulate cancer metabolism, offering potential therapeutic avenues.
Keywords:
A549MCF7cancer metabolismmitochondrial bioenergeticssigma-1 receptor

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