Introduction of a Polar Functional Group to the Lipid Tail of 4-<i>epi</i>-Jaspine B Affects Sphingosine Kinase Isoform Selectivity

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  • Highlighted Paper selected by Editor-in-Chief : Introduction of a Polar Functional Group to the Lipid Tail of 4-epi-Jaspine B Affects Sphingosine Kinase Isoform Selectivity

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Abstract

<p>Sphingosine kinases (SphKs) are key enzymes that regulate sphingosine 1-phosphate production levels, and are involved in a range of cellular processes. Focusing on a hydrophilic residue in the hydrophobic binding pocket of SphKs, we designed and synthesized 4-epi-jaspine B derivatives containing a polar functional group in the lipid tail. A biological evaluation revealed that the introduction of ether groups to the lipid tail of 4-epi-jaspine B modulated its isoform selectivity toward SphKs.</p>

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