一般描述
Sphingosine 1-phosphate (S1P) is a sphingolipid derived from ceramide by an enzymatic reaction in vivo.1 S1P acts as a signaling molecule by binding to G-protein coupled receptors (S1PR) (S1P1-5 receptors) which results in activation of small GTPases such as Ras, Rac Rho and further downstream intracellular effects such as PI-3-Kinase, Protein kinase C and Hippo signaling pathways. This generates an effect on cell migration, differentiation and survival and therefore effects variety of systems such as immune system, central nervous system and cardiovascular system.2 For instance, S1P was found to inhibit cell apoptosis and induce cell proliferation by binding S1P1 to promote activation of ERK pathway.3 In addition, S1P was found to support cancer cells by inducing angiogenesis and survival of proliferative cells in the tumor microenvironment.4 Due to the vast activities of S1P and the resulted S1PR irregular activation, large discovery efforts are made to identify therapy by S1PR antagonists.5
