Pachastrissamine (jaspine B) and its stereoisomers inhibit sphingosine kinases and atypical protein kinase C.

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抄録

Sphingosine kinases (SphKs) are oncogenic enzymes that regulate the critical balance between ceramide and sphingosine-1-phosphate. Much effort has been dedicated to develop inhibitors against these enzymes. Naturally occurring pachastrissamine (jaspine B) and all its stereoisomers were prepared and evaluated for their inhibitory effects against SphKs. All eight stereoisomers exhibited moderate to potent inhibitory activity against SphK1 and SphK2. Inhibitory effects were profiled against protein kinase C (PKC) isoforms by in vitro experiments. Atypical PKCs (PKCζ and PKCι) were inhibited by several pachastrissamine stereoisomers. The improved activity over N, N-dimethylsphingosine suggests that the cyclic scaffold in pachastrissamines facilitates potential favorable interactions with SphKs and PKCs.

収録刊行物

  • Bioorganic & medicinal chemistry

    Bioorganic & medicinal chemistry 19(18), 5402-5408, 2011-09-15

    Elsevier Ltd.

各種コード

  • NII論文ID(NAID)
    120003386631
  • NII書誌ID(NCID)
    AA10938083
  • 本文言語コード
    ENG
  • 資料種別
    journal article
  • ISSN
    0968-0896
  • データ提供元
    IR 
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