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S1P Receptor


The sphingosine-1-phosphate receptors are a class of G protein-coupled receptors that are targets of the lipid signalling molecule Sphingosine-1-phosphate (S1P). They are divided into five subtypes: S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5. The sphingosine-1-phosphate receptors regulate fundamental biological processes such as cell proliferation, angiogenesis, migration, cytoskeleton organization, endothelial cell chemotaxis, immune cell trafficking and mitogenesis. Sphingosine-1-phosphate receptors are also involved in immune-modulation and directly involved in suppression of innate immune responses from T cells.
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    Fingolimod (FTY720) HCl是一种1-磷酸-神经鞘氨醇S1P受体拮抗剂,IC50为0.33 nM。

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  • PF-543 EY1215

    PF-543柠檬酸盐是鞘氨醇竞争性的,且可渗透入细胞的SphK1选择性抑制剂,Ki为3.6 nM,对SphK2的抑制性较弱。

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  • SKI II EY0309

    SKI II是一种高度选择性的,非ATP竞争性的S1P receptor抑制剂,IC50为0.5 μM,对其他激酶,包括PI3K, PKCα和ERK2没有抑制作用。

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