FTY720 (S)-Phosphate is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs. Phosphorylated by sphingosine kinases in vivo, FTY720 then acts as a potent agonist at EDG-1, EDG-3, EDG-4 and EDG-5 (Endothelial differential gene). FTY720 (S)-phosphate is the single stereoisomer formed by phosphorylation of FTY720 in vivo, as determined in rats and humans. It exhibits Ki values of 2.1, 5.9, 23, and 2.2 nM for EDG-1,-3,-4 and -5, respectively, whereas the R enantiomer binds with 5-130-fold lower affinity. FTY720 (S)-phosphate causes internalization of S1P1 on lymphocytes, abrogating S1P-dependent egress of lymphocytes from lymphoid organs. It also enhances endothelial barrier function, stimulates the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc16 and inhibits cytosolic phospholipase A2 activity.
1. Brinkmann, V., et al. 2001. Transplantation. 72: 764-769. PMID: 11571432
2. Brinkmann, V., et al. 2002. J. Biol. Chem. 277: 21453-21457. PMID: 11967257
3. Albert, R., et al. 2005. J. Med Chem. 48: 5373-5377. PMID: 16078855
4. Kiuchi, M., et al. 2005. Bioorg. Med. Chem. 13: 425-432. PMID: 15598563
5. Brinkmann, V. 2004. Yonsei Med. J. 45: 991-997. PMID: 15627289
6. Honig, S.M., et al. 2003. J. Clin. Invest. 111: 627-637. PMID: 12618517
7. Payne, S.G., et al. Blood. 109: 1077-1085. PMID: 17008548
See how others have used FTY720 (S)-Phosphate. Click on the entry to view the PubMed entry .
PMID: # 26216939 Skrzeczyńska-Moncznik, J. et al. 2015. J. Leukoc. Biol. 98: 591-9.
PMID: # 16549044 Chiba, K. et al. 2006. Cell. Mol. Immunol. 3: 11-19.
PMID: # 15808561 Chiba, K. et al. 2005 Jan-Feb. Transplant. Proc. 37: 102-106.
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