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Title: Pachastrissamine (jaspine B) and its stereoisomers inhibit sphingosine kinases and atypical protein kinase C.
Authors: Yoshimitsu, Yuji
Oishi, Shinya  kyouindb  KAKEN_id
Miyagaki, Jun
Inuki, Shinsuke
Ohno, Hiroaki  kyouindb  KAKEN_id
Fujii, Nobutaka  KAKEN_id
Author's alias: 大石, 真也
Keywords: Jaspine B
Protein kinase C
Sphingosine kinase
Issue Date: 15-Sep-2011
Publisher: Elsevier Ltd.
Journal title: Bioorganic & medicinal chemistry
Volume: 19
Issue: 18
Start page: 5402
End page: 5408
Abstract: 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.
Rights: © 2011 Elsevier Ltd.
This is not the published version. Please cite only the published version. この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。
DOI(Published Version): 10.1016/j.bmc.2011.07.061
PubMed ID: 21868240
Appears in Collections:Journal Articles

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