書誌事項
- タイトル別名
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- Synthesis of novel vitamin K analogues with modification at ω-terminal position and evaluation of their transcriptional activity via steroid and xenobiotic receptor (SXR)
- ガワ クサリマッタンブ オ シュウショク シタ シンキ ビタミン K ユウドウタイ ノ ゴウセイ ト カク ナイ ジュヨウタイ SXR オ カイシタ テンシャ カッセイ ノ ケントウ
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抄録
Menaquinone-4 (vitamin K_2) is a ligand for a nuclear receptor, steroid and xenobiotic receptor (SXR), that induces the gene expressions of CYP3A4. We synthesized vitamin K_2 analogues with hydroxyl or phenyl groups at the ω-terminal of the side chain. The up-regulation 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. A new analogue that has phenyl group introduced to menaquinone-3 showed the most potent activity among our synthesized compounds. The analogue was approximately estimated twice as active as menaquinone-4, and almost same as the known SXR ligand rifampicin.
収録刊行物
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- ビタミン
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ビタミン 86 (9), 493-498, 2012
公益社団法人 日本ビタミン学会
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詳細情報 詳細情報について
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- CRID
- 1390282680676991104
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- NII論文ID
- 110009518112
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- NII書誌ID
- AN00207833
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- ISSN
- 2424080X
- 0006386X
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- NDL書誌ID
- 024010914
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- 本文言語コード
- ja
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- データソース種別
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- JaLC
- NDL
- CiNii Articles
- KAKEN
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- 抄録ライセンスフラグ
- 使用不可