( R)-FTY720 methyl ether is a specific sphingosine kinase 2 inhibitor: Effect on sphingosine kinase 2 expression in HEK 293 cells and actin rearrangement and survival of MCF-7 breast cancer cells

Sphingosine kinase 2 (SK2) catalyses the conversion of sphingosine to the bioactive lipid sphingosine 1-phosphate (S1P). We report here, the stereospecific synthesis of an analogue of FTY720 called ( R)-FTY720-OMe, which we show is a competitive inhibitor of SK2. ( R)-FTY720-OMe failed to inhibit sp...

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Bibliographic Details
Published in:Cellular signalling 2011-10, Vol.23 (10), p.1590-1595
Main Authors: Lim, Keng Gat, Sun, Chaode, Bittman, Robert, Pyne, Nigel J., Pyne, Susan
Format: Article
Language:English
Subjects:
actin
Actins - drug effects
Actins - metabolism
Antineoplastic Agents - pharmacology
Apoptosis
bioactive properties
Blotting, Western
Breast cancer
breast neoplasms
Cell Line, Tumor
Cell Membrane - metabolism
DNA
Enzyme Assays - methods
Female
Fingolimod Hydrochloride
FTY720 analogues
HEK293 Cells
Humans
Kinetics
Lysophospholipids - metabolism
Microscopy, Fluorescence
neoplasm cells
Phosphorylation
Phosphotransferases (Alcohol Group Acceptor) - antagonists & inhibitors
Phosphotransferases (Alcohol Group Acceptor) - metabolism
Propylene Glycols - chemical synthesis
Propylene Glycols - pharmacology
pseudopodia
Pseudopodia - metabolism
sphingosine
Sphingosine - analogs & derivatives
Sphingosine - chemical synthesis
Sphingosine - metabolism
Sphingosine - pharmacology
Sphingosine kinase 2
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