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Synthesis and evaluation of sphingoid analogs as inhibitors of sphingosine kinases

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Title: Synthesis and evaluation of sphingoid analogs as inhibitors of sphingosine kinases
Authors: Kim, Jin-Wook Browse this author
Kim, Yong-Woo Browse this author
Inagaki, Yuichi Browse this author
Hwang, You-A Browse this author
Mitsutake, Susumu5 Browse this author →KAKEN DB
Ryu, Yeon-Woo Browse this author
Lee, Won Koo Browse this author
Ha, Hyun-Joon Browse this author
Park, Chang-Seo Browse this author
Igarashi, Yasuyuki Browse this author →KAKEN DB
Authors(alt): 光武, 進5
Issue Date: 16-May-2005
Publisher: Elsevier Ltd
Journal Title: Bioorganic & Medicinal Chemistry
Volume: 13
Issue: 10
Start Page: 3475
End Page: 3485
Publisher DOI: 10.1016/j.bmc.2005.02.053
Abstract: 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.
Type: article (author version)
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 光武 進

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