[HTML][HTML] Phosphorylation of the immunomodulatory drug FTY720 by sphingosine kinases
A Billich, F Bornancin, P Dévay… - Journal of Biological …, 2003 - ASBMB
The immunomodulatory drug FTY720 is phosphorylated in vivo, and the resulting FTY720
phosphate as a ligand for sphingosine-1-phosphate receptors is responsible for the unique
biological effects of the compound. So far, phosphorylation of FTY720 by murine
sphingosine kinase (SPHK) 1a had been documented. We found that, while FTY720 is also
phosphorylated by human SPHK1, the human type 2 isoform phosphorylates the drug 30-
fold more efficiently, because of a lower K m of FTY720 for SPHK2. Similarly, murine SPHK2 …
phosphate as a ligand for sphingosine-1-phosphate receptors is responsible for the unique
biological effects of the compound. So far, phosphorylation of FTY720 by murine
sphingosine kinase (SPHK) 1a had been documented. We found that, while FTY720 is also
phosphorylated by human SPHK1, the human type 2 isoform phosphorylates the drug 30-
fold more efficiently, because of a lower K m of FTY720 for SPHK2. Similarly, murine SPHK2 …