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 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.
CITATION STYLE
Pyne, S., Adams, D. R., & Pyne, N. J. (2020). Sphingosine kinases as druggable targets. In Handbook of Experimental Pharmacology (Vol. 259, pp. 49–76). Springer Science and Business Media Deutschland GmbH. https://doi.org/10.1007/164_2018_96
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