Sphingosine and FTY720 directly bind pro-survival 14-3-3 proteins to regulate their function

Cell Signal. 2010 Sep;22(9):1291-9. doi: 10.1016/j.cellsig.2010.04.004. Epub 2010 Apr 18.

Abstract

The dimeric 14-3-3 protein family protects cells from apoptosis by regulating pro-apoptotic molecules. Conversely, the cationic lipid sphingosine is associated with physiological apoptosis and induces apoptosis in its own right by a largely undefined mechanism. We show here that sphingosine and 14-3-3 interact directly in the control of cell death. The binding of sphingosine to 14-3-3 proteins renders them phosphorylatable at the dimer interface, an event that abolishes the pro-survival signalling of 14-3-3. Sphingosine kinase 1 reduces availability of sphingosine for interaction with 14-3-3, thus inhibiting cell death and providing a new mechanistic insight into the role of this enzyme in cell survival and oncogenesis. Importantly, FTY720, a sphingosine analogue with apoptotic activity that is currently in phase III clinical trials for multiple sclerosis, acts in a similar manner to sphingosine in potentiating 14-3-3 phosphorylation. The biological significance of 14-3-3 phosphorylation was demonstrated with a non-phosphorylatable 14-3-3zeta mutant which retarded apoptosis induced by sphingosine and FTY720. These results demonstrate that direct association of sphingosine with 14-3-3 is required for 14-3-3 phosphorylation, and that this axis can control cell fate. Furthermore, these results suggest a new therapeutic activity for FTY720 as an anti-cancer agent based on this mechanism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 14-3-3 Proteins / metabolism*
  • Animals
  • Apoptosis
  • COS Cells
  • Caspases / metabolism
  • Cell Survival
  • Chlorocebus aethiops
  • Fingolimod Hydrochloride
  • Humans
  • Jurkat Cells
  • Phosphorylation
  • Phosphotransferases (Alcohol Group Acceptor) / metabolism
  • Propylene Glycols / metabolism
  • Propylene Glycols / pharmacology
  • Protein Isoforms / metabolism
  • Protein Kinase C-delta / metabolism
  • Sphingosine / analogs & derivatives
  • Sphingosine / metabolism*
  • Sphingosine / pharmacology

Substances

  • 14-3-3 Proteins
  • Propylene Glycols
  • Protein Isoforms
  • Phosphotransferases (Alcohol Group Acceptor)
  • sphingosine kinase
  • Protein Kinase C-delta
  • Caspases
  • Fingolimod Hydrochloride
  • N,N-dimethylsphingosine
  • Sphingosine