Synthesis and evaluation of sphingoid analogs as inhibitors of sphingosine kinases

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概要

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• Sphingosine 1-phosphate (S1P), a product of sphingosine kinases (SphK), mediates diverse biological processes such as cell differentiation, proliferation, motility, and apoptosis. In an effort to search and identify specific inhibitors of human SphK, the inhibitory effects of synthetic sphingoid analogs on kinase activity were examined. Among the analogs tested, we found two, SG12 and SG14, that have specific inhibitory effects on hSphK2. N,N-Dimethylsphingosine (DMS), a well-known SphK inhibitor, displayed inhibitory effects for both SphK1 and SphK2, as well as protein kinase C. In contrast, SG12 and SG14 exhibited selective inhibitory effects on hSphK2. Furthermore, SG14 did not affect PKC. In isolated platelets, SG14 blocked the conversion of sphingosine into sphingosine 1-phosphate significantly. This is the first report on the identification of a hSphK2-specific inhibitor, which may provide a useful tool for studying the biological functions of hSphK2.

• Elsevier Ltdの論文
• 2005-05-16

著者

• Park Chang-seo

  Department Of Chemical And Biochemical Engineering Dongguk University

• Igarashi Yasuyuki

  北海道大学 大学院生命科学院生体機能化学研究室

• Mitsutake Susumu

  北海道大学 大学院生命科学院生体機能化学研究室

• Inagaki Yuichi

  Laboratory Of Biomembrane And Biofunctional Chemistry Faculty Of Pharmaceutical Science And Faculty

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