Introduction of a Polar Functional Group to the Lipid Tail of 4-<i>epi</i>-Jaspine B Affects Sphingosine Kinase Isoform Selectivity
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- Inuki Shinsuke
- Graduate School of Pharmaceutical Sciences, Kyoto University
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- Miyagawa Takashi
- Graduate School of Pharmaceutical Sciences, Kyoto University
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- Oishi Shinya
- Graduate School of Pharmaceutical Sciences, Kyoto University
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- Ohno Hiroaki
- Graduate School of Pharmaceutical Sciences, Kyoto University
Bibliographic Information
- Other Title
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- Highlighted Paper selected by Editor-in-Chief : Introduction of a Polar Functional Group to the Lipid Tail of 4-epi-Jaspine B Affects Sphingosine Kinase Isoform Selectivity
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Abstract
<p>Sphingosine kinases (SphKs) are key enzymes that regulate sphingosine 1-phosphate production levels, and are involved in a range of cellular processes. Focusing on a hydrophilic residue in the hydrophobic binding pocket of SphKs, we designed and synthesized 4-epi-jaspine B derivatives containing a polar functional group in the lipid tail. A biological evaluation revealed that the introduction of ether groups to the lipid tail of 4-epi-jaspine B modulated its isoform selectivity toward SphKs.</p>
Journal
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 66 (9), 866-872, 2018-09-01
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390845712995171072
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- NII Article ID
- 130007479591
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- NII Book ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL BIB ID
- 029184653
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- PubMed
- 30175743
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
- KAKEN
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- Abstract License Flag
- Disallowed