FTY720 induces non-canonical phosphatidylserine externalization and cell death in acute myeloid leukemia

Cell Death Dis. 2019 Nov 7;10(11):847. doi: 10.1038/s41419-019-2080-5.

Abstract

FTY720 (fingolimod) is a FDA-approved sphingosine analog that is phosphorylated in vivo to modulate sphingosine-1-phosphate receptor (S1PR) signaling for immunosuppression in patients with refractory multiple sclerosis. FTY720 also exhibits promising anticancer efficacy in several preclinical models. While FTY720-induced cytotoxicity is not due to S1PR signaling, the mechanism remains unclear and is reported to occur through various cell death pathways. Here, we performed a systematic, mechanistic study of FTY720-induced cell death in acute myeloid leukemia (AML). We found that FTY720 induced cell death in a panel of genetically diverse AML cell lines that was accompanied by rapid phosphatidylserine (PS) externalization. Importantly, FTY720-induced PS exposure was not due to any direct effects on plasma membrane integrity and was independent of canonical signaling by regulated cell death pathways known to activate lipid flip-flop, including caspase-dependent apoptosis/pyroptosis, necroptosis, ferroptosis, and reactive oxygen species-mediated cell death. Notably, PS exposure required cellular vacuolization induced by defects in endocytic trafficking and was suppressed by the inhibition of PP2A and shedding of Annexin V-positive subcellular particles. Collectively, our studies reveal a non-canonical pathway underlying PS externalization and cell death in AML to provide mechanistic insight into the antitumor properties of FTY720.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis*
  • Caspases / metabolism
  • Cell Membrane / metabolism*
  • Fingolimod Hydrochloride / pharmacology*
  • Humans
  • Leukemia, Myeloid, Acute / drug therapy*
  • Leukemia, Myeloid, Acute / metabolism
  • Leukemia, Myeloid, Acute / pathology
  • Necroptosis*
  • Phosphatidylserines / metabolism*
  • Receptors, Lysosphingolipid / metabolism
  • Signal Transduction
  • Sphingosine 1 Phosphate Receptor Modulators / pharmacology

Substances

  • Phosphatidylserines
  • Receptors, Lysosphingolipid
  • Sphingosine 1 Phosphate Receptor Modulators
  • Caspases
  • Fingolimod Hydrochloride