Structure-Activity Relationship of Novel Vitamin K Analogues as Steroid and Xenobiotic Receptor (SXR) Agonists
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- Suhara Yoshitomo
- Yokohama College of Pharmacy
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- Motoyoshi Sayaka
- Department of Chemistry, Rikkyo University
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- Hirota Yoshihisa
- Kobe Pharmaceutical University
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- Sawada Natsumi
- Kobe Pharmaceutical University
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- Nakagawa Kimie
- Kobe Pharmaceutical University
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- Tokiwa Hiroaki
- Department of Chemistry, Rikkyo University
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- Okano Toshio
- Kobe Pharmaceutical University
Bibliographic Information
- Other Title
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- 核内受容体SXR (Steroid and Xenobiotic Receptor) のアゴニスト活性を持つ新規ビタミンK誘導体の合成と構造活性相関の検討
- カク ナイ ジュヨウタイ SXR(Steroid and Xenobiotic Receptor)ノ アゴニスト カッセイ オ モツ シンキ ビタミン K ユウドウタイ ノ ゴウセイ ト コウゾウ カッセイ ソウカン ノ ケントウ
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Description
Vitamin K2 is a ligand for a nuclear receptor, steroid and xenobiotic receptor (SXR), that induces the gene expressions of CYP3A4. We synthesized new vitamin K analogues with the same isoprene side chains symmetrically introduced at the 2 and 3 positions of 1,4-naphthoquinone and vitamin K2 analogues with hydroxyl or phenyl groups at the ω-terminal of the side chain. The upregulation of SXR-mediated transcription of the target gene by the analogues was dependent on the length of the side chain and the hydrophobicity of the ω-terminal residues. Phenyl analogue menaquinone-3 was as active as the known SXR ligand rifampicin.<br>
Journal
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- YAKUGAKU ZASSHI
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YAKUGAKU ZASSHI 132 (8), 881-886, 2012-08-01
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390282681104217344
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- NII Article ID
- 130001888705
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- NII Book ID
- AN00284903
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- COI
- 1:STN:280:DC%2BC38flsFOltw%3D%3D
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- ISSN
- 13475231
- 00316903
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- NDL BIB ID
- 023915640
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- PubMed
- 22864345
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- Text Lang
- ja
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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