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  • 标题:Introduction of a Polar Functional Group to the Lipid Tail of 4-epi-Jaspine B Affects Sphingosine Kinase Isoform Selectivity
  • 作者:Shinsuke Inuki ; Takashi Miyagawa ; Shinya Oishi
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2018
  • 卷号:66
  • 期号:9
  • 页码:866-872
  • DOI:10.1248/cpb.c18-00366
  • 语种:English
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要: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.
  • 关键词:sphingosine kinase;inhibitor;lipid;jaspine B;structure–activity relationship
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