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FTY-P |
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FTY720 (generic name fingolimod; drug name Gilenya (Novartis)) is a synthetic sphingosine analog (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol) that can be phosphorylated by sphingosine kinases. The designation FTY-P is used for the phosphorylated compound. The phosphorylated compound acts as a ligand/agonist for the S1PR1 receptor (Brinkmann et al, 2002) and is very effective in downregulating S1PR1 expression (Matloubian et al, 2004; Kunisawa et al, 2008; Gräler and Goetzl, 2004).
FTY720 has been shown to be highly active at inducing the internalization, ubiquitylation and subsequent degradation of S1PR1. Rapid induction of lymphopenia through the sequestration of lymphocytes
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