The SIRT1/HIF2α axis drives reductive glutamine metabolism under chronic acidosis and alters tumor response to therapy

Cancer Res. 2014 Oct 1;74(19):5507-19. doi: 10.1158/0008-5472.CAN-14-0705. Epub 2014 Aug 1.

Abstract

Extracellular tumor acidosis largely results from an exacerbated glycolytic flux in cancer and cancer-associated cells. Conversely, little is known about how tumor cells adapt their metabolism to acidosis. Here, we demonstrate that long-term exposure of cancer cells to acidic pH leads to a metabolic reprogramming toward glutamine metabolism. This switch is triggered by the need to reduce the production of protons from glycolysis and further maintained by the NAD(+)-dependent increase in SIRT1 deacetylase activity to ensure intracellular pH homeostasis. A consecutive increase in HIF2α activity promotes the expression of various transporters and enzymes supporting the reductive and oxidative glutamine metabolism, whereas a reduction in functional HIF1α expression consolidates the inhibition of glycolysis. Finally, in vitro and in vivo experiments document that acidosis accounts for a net increase in tumor sensitivity to inhibitors of SIRT1 and glutaminase GLS1. These findings highlight the influence that tumor acidosis and metabolism exert on each other.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acidosis / metabolism*
  • Basic Helix-Loop-Helix Transcription Factors / physiology*
  • Cell Line, Tumor
  • Chronic Disease
  • Glucose / metabolism
  • Glutamine / metabolism*
  • Glycolysis
  • Humans
  • Neoplasms / metabolism
  • Neoplasms / therapy*
  • Sirtuin 1 / physiology*

Substances

  • Basic Helix-Loop-Helix Transcription Factors
  • Glutamine
  • endothelial PAS domain-containing protein 1
  • SIRT1 protein, human
  • Sirtuin 1
  • Glucose