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| j.bmc.2011.07.061.pdf | 643.77 kB | Adobe PDF | 見る/開く |
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| DCフィールド | 値 | 言語 |
|---|---|---|
| dc.contributor.author | Yoshimitsu, Yuji | en |
| dc.contributor.author | Oishi, Shinya | en |
| dc.contributor.author | Miyagaki, Jun | en |
| dc.contributor.author | Inuki, Shinsuke | en |
| dc.contributor.author | Ohno, Hiroaki | en |
| dc.contributor.author | Fujii, Nobutaka | en |
| dc.contributor.alternative | 大石, 真也 | ja |
| dc.date.accessioned | 2011-10-06T07:41:37Z | - |
| dc.date.available | 2011-10-06T07:41:37Z | - |
| dc.date.issued | 2011-09-15 | - |
| dc.identifier.issn | 0968-0896 | - |
| dc.identifier.uri | http://hdl.handle.net/2433/147238 | - |
| dc.description.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. | en |
| dc.format.mimetype | application/pdf | - |
| dc.language.iso | eng | - |
| dc.publisher | Elsevier BV | en |
| dc.rights | © 2011 Elsevier Ltd. | en |
| dc.rights | 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。 | ja |
| dc.rights | This is not the published version. Please cite only the published version. | en |
| dc.subject | Jaspine B | en |
| dc.subject | Pachastrissamine | en |
| dc.subject | Protein kinase C | en |
| dc.subject | Sphingosine kinase | en |
| dc.subject | Sphingolipid | en |
| dc.title | Pachastrissamine (jaspine B) and its stereoisomers inhibit sphingosine kinases and atypical protein kinase C. | en |
| dc.type | journal article | - |
| dc.type.niitype | Journal Article | - |
| dc.identifier.ncid | AA10938083 | - |
| dc.identifier.jtitle | Bioorganic & medicinal chemistry | en |
| dc.identifier.volume | 19 | - |
| dc.identifier.issue | 18 | - |
| dc.identifier.spage | 5402 | - |
| dc.identifier.epage | 5408 | - |
| dc.relation.doi | 10.1016/j.bmc.2011.07.061 | - |
| dc.textversion | author | - |
| dc.identifier.pmid | 21868240 | - |
| dcterms.accessRights | open access | - |
| dc.identifier.pissn | 0968-0896 | - |
| 出現コレクション: | 学術雑誌掲載論文等 | |
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