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CDP-choline accumulation in breast and colorectal cancer cells treated with a GSK-3-targeting inhibitor

Su Myat Phyu1, Chih-Chung Tseng1, Tim Andrew Davies Smith2

  • 1Biomedical Physics Building, School of Medicine, Medical Sciences and Nutrition, University of Aberdeen, Foresterhill, Aberdeen, AB25 2ZD, UK.

Magma (New York, N.Y.)
|November 18, 2018
PubMed
Abstract

Insights

Glycogen synthase kinase 3 (GSK3) inhibition with SB216763 profoundly reduces phospholipid synthesis in cancer cells. This metabolic shift, marked by CDP-choline accumulation, offers potential biomarkers for targeted cancer therapies.

Area of Science:

  • Biochemistry
  • Cancer Biology
  • Metabolic Research

Background:

  • Glycogen synthase kinase 3 (GSK3) is a critical regulator of cellular processes, including cell-cycle progression.
  • Emerging research highlights GSK3 as a promising anticancer target.
  • GSK3 inhibition impacts glucose metabolism, potentially influencing lipid synthesis and providing molecular response markers.

Purpose of the Study:

  • To investigate the effects of GSK3 inhibition on lipid synthesis in cancer cells.
  • To determine if metabolic changes associated with GSK3 inhibition can serve as response markers.

Main Methods:

  • Treatment of SKBr3 breast and HCT8 colorectal cancer cells with the GSK3 inhibitor SB216763.
  • Quantification of [14C (U)] glucose and [3H] choline incorporation into lipids.
  • Analysis of cell extracts using 31P NMR spectroscopy.

Main Results:

  • SB216763 treatment significantly decreased choline incorporation into lipids.
  • An accumulation of CDP-choline was observed in treated cells.
  • The conversion of glucose into lipid components was reduced.

Conclusions:

  • SB216763 profoundly inhibits phospholipid synthesis in cancer cells.
  • Accumulation of CDP-choline, detectable by 31P NMR spectroscopy, is a key metabolic consequence.
  • Altered lipid metabolism presents potential response markers for drugs targeting GSK3.
Keywords:
31P nuclear magnetic resonance spectroscopyCDP-cholineCholineGlucoseGlycogen synthase kinase 3Lipid

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