Sphingosine kinases as druggable targets

Susan Pyne, David R. Adams, Nigel J. Pyne

Research output: Chapter in Book/Report/Conference proceedingChapter

8 Citations (Scopus)


There is substantial evidence that the enzymes, sphingosine kinase 1 and 2, which catalyse the formation of the bioactive lipid, sphingosine 1-phosphate are involved in physiological and pathophysiological processes. In this chapter, we appraise the evidence that both enzymes are druggable and describe how isoform-specific inhibitors can be developed based on the plasticity of the sphingosine-binding site. This is contextualised with the effect of sphingosine kinase inhibitors in cancer, pulmonary hypertension, neurodegeneration, inflammation and sickling.
Original languageEnglish
Title of host publicationLipid Signaling in Human Diseases
Subtitle of host publicationHandbook of Experimental Pharmacology
EditorsJulian Gomez-Cambronero, Michael A. Frohman
Place of PublicationCham, Switzerland
Number of pages28
ISBN (Electronic)978-3-030-33668-4
Publication statusPublished - 25 Apr 2020


  • Sphingosine kinase
  • sphingosine 1-phosphate (SIP)
  • cancer
  • pulmonary hypertension
  • Inflammation
  • neurodegeneration
  • sickling


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