Sphingosine kinase inhibitors and cancer: seeking the golden sword of Hercules

Susan Pyne, Robert Bittman, Nigel Pyne

Research output: Contribution to journalArticlepeer-review

80 Citations (Scopus)


There is considerable evidence that sphingosine kinases play a key role in cancer progression, which might involve positive selection of cancer cells that have been provided with a survival and growth advantage as a consequence of overexpression of the enzyme. Therefore, inhibitors of sphingosine kinase represent a novel class of compounds that have potential as anticancer agents. Poor inhibitor potency is a major issue that has precluded successful translation of these compounds into the clinic. However, recent discoveries have shown that sphingosine kinase 1 is an allosteric enzyme and that some inhibitors offer improved effectiveness by inducing proteasomal degradation of the enzyme or having nanomolar potency. Herein, we provide a perspective about these recent developments and highlight the importance of translating basic pharmacologic and biochemical findings on sphingosine kinase into new drug discovery programs for treatment of cancer.
Original languageEnglish
Pages (from-to)6576-6582
Number of pages7
JournalCancer Research
Issue number21
Early online date22 Sept 2011
Publication statusPublished - 2011


  • sphingosine kinase inhibitors
  • cancer
  • hercules
  • golden sword


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