FTY720是ISP-1(myriocin)的衍生物,ISP-1是中草药苁蓉的真菌代谢产物,也是鞘氨醇的结构类似物。它是一种新型免疫调节剂,可通过抑制淋巴细胞从淋巴器官移出,延长多种模型的异体移植存活率。FTY720 会被鞘氨醇激酶磷酸化,然后成为四种鞘氨醇-1-磷酸(S1P)受体(S1P1、S1P3、S1P4 和 S1P5)的强效激动剂2。叠氮-FTY720 是一种高光反应性的 FTY720 类似物,可用于鉴定这种配体的受体结合位点。
azido-FTY720 参考文献
1 Brinkmann, V., Pinschewer, D.D., Feng, L., et al. FTY720: Altered lymphocyte traffic results in allograft protection. Transplantation 72 764-769 (2001). 2 Brinkmann, V., Davis, M.D., Heise, C.E., et al. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem 277(24) 21453-21457 (2002). 3 Matloubian, M., Lo, C.G., Cinamon, G., et al. Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature 427 355-360 (2004). 4 Sun, C., Bittman, R. A photoreactive analogue of the immunosuppressant FTY720. J Org Chem 71 2200-2202 (2006).