Acetylation accumulates PFKFB3 in cytoplasm to promote glycolysis and protects cells from cisplatin-induced apoptosis

Nat Commun. 2018 Feb 6;9(1):508. doi: 10.1038/s41467-018-02950-5.

Abstract

Enhanced glycolysis in cancer cells has been linked to cell protection from DNA damaging signals, although the mechanism is largely unknown. The 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) catalyzes the generation of fructose-2,6-bisphosphate, a potent allosteric stimulator of glycolysis. Intriguingly, among the four members of PFKFB family, PFKFB3 is uniquely localized in the nucleus, although the reason remains unclear. Here we show that chemotherapeutic agent cisplatin promotes glycolysis, which is suppressed by PFKFB3 deletion. Mechanistically, cisplatin induces PFKFB3 acetylation at lysine 472 (K472), which impairs activity of the nuclear localization signal (NLS) and accumulates PFKFB3 in the cytoplasm. Cytoplasmic accumulation of PFKFB3 facilitates its phosphorylation by AMPK, leading to PFKFB3 activation and enhanced glycolysis. Inhibition of PFKFB3 sensitizes tumor to cisplatin treatment in a xenograft model. Our findings reveal a mechanism for cells to stimulate glycolysis to protect from DNA damage and potentially suggest a therapeutic strategy to sensitize tumor cells to genotoxic agents by targeting PFKFB3.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Acetylation / drug effects*
  • Adenylate Kinase / drug effects
  • Adenylate Kinase / metabolism
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Cell Line, Tumor
  • Cisplatin / pharmacology*
  • Cytoplasm / drug effects
  • Cytoplasm / metabolism
  • Glycolysis / drug effects*
  • HCT116 Cells
  • HeLa Cells
  • Humans
  • Nuclear Localization Signals / drug effects
  • Nuclear Localization Signals / metabolism
  • Phosphofructokinase-2 / drug effects*
  • Phosphofructokinase-2 / metabolism
  • Phosphorylation / drug effects

Substances

  • Antineoplastic Agents
  • Nuclear Localization Signals
  • PFKFB3 protein, human
  • Phosphofructokinase-2
  • Adenylate Kinase
  • Cisplatin