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

• Inuki Shinsuke

  Graduate School of Pharmaceutical Sciences, Kyoto University

• Miyagawa Takashi

  Graduate School of Pharmaceutical Sciences, Kyoto University

• Oishi Shinya

  Graduate School of Pharmaceutical Sciences, Kyoto University

• Ohno Hiroaki

  Graduate School of Pharmaceutical Sciences, Kyoto University

書誌事項

タイトル別名

• Introduction of a Polar Functional Group to the Lipid Tail of 4-<i>epi</i>-Jaspine B Affects Sphingosine Kinase Isoform Selectivity

抄録

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.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 66 (9), 866-872, 2018-09-01

  公益社団法人 日本薬学会

キーワード

• sphingosine kinase
• inhibitor
• lipid
• jaspine B
• structure–activity relationship

詳細情報

• CRID: 1390845712995171072
• NII論文ID: 130007479591
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.c18-00366
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 029184653
• PubMed: 30175743
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I029184653
• Web Site: https://www.jstage.jst.go.jp/article/cpb/66/9/66_c18-00366/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2019133189
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
  • KAKEN
• 抄録ライセンスフラグ: 使用不可