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Nat Rev Drug Discov. 2013 Sep;12(9):688-702. doi: 10.1038/nrd4099. Epub 2013 Aug 19.

Targeting the sphingosine-1-phosphate axis in cancer, inflammation and beyond.

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1] Department of Biochemistry and Molecular Biology, Massey Cancer Center, Virginia Commonwealth University School of Medicine, 1101 E. Marshall Street, 2-017 Sanger Hall, Richmond, Virginia 23298, USA. [2].


The bioactive lipid sphingosine-1-phosphate (S1P) is involved in multiple cellular signalling systems and has a pivotal role in the control of immune cell trafficking. As such, S1P has been implicated in disorders such as cancer and inflammatory diseases. This Review discusses the ways in which S1P might be therapeutically targeted - for example, via the development of chemical inhibitors that target the generation, transport and degradation of S1P and via the development of specific S1P receptor agonists. We also highlight recent conflicting results observed in preclinical studies targeting S1P and discuss ongoing clinical trials in this field.

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