生体細胞における酸セラミダースの活動ベースのイメージング
Yadira F Ordóñez1, José Luís Abad1, Mazen Aseeri1
1Research Unit on Bioactive Molecules (RUBAM), Department of Biological Chemistry , Institute for Advanced Chemistry of Catalonia (IQAC-CSIC) , Jordi Girona, 18 , 08034 Barcelona , Spain.
Journal of the American Chemical Society
|April 30, 2019
まとめ
研究者は細胞内の活性酸セラミダース (AC) を検出するための新しい活動ベースのプローブを開発しました. ガンやアルツハイマー病の 診断と治療に不可欠なACを 視覚化できます
科学分野:
- 生物化学
- 分子生物学
- 化学生物学
背景:
- 酸セラミダース (AC) はセラミドを水分解する酵素である.
- 癌やアルツハイマー病に繋がっています
- ACの欠陥は 治らない遺伝的障害を引き起こす
研究 の 目的:
- 触媒的に活性なACの特定の視覚化のための活動ベースのプローブを開発します.
- ACに関連する疾患の診断と治療監視を可能にします.
主な方法:
- SABRACを基にした新しい酸セラミダース阻害剤の合成.
- AC検出のために光とクリック化学のアプローチを使用した.
- 細胞のないシステムと生きた細胞でテストした探査機.
主要な成果:
- 強力で不可逆的なAC阻害剤を 開発した. nMの2桁の強さ.
- 光SABRACアナログとクリック化学を用いたセルフリーシステムでの活性ACを特定した.
- アクティブACのラベルを 生体細胞で取得しました
結論:
- アクティビティベースの探知器は,活性酸セラミダースを検出するための新しい方法を提供します.
- これらの探査機は 癌やアルツハイマー病などの 病気の研究に役立つツールです
- 開発された探査機は,診断と治療戦略のフォローアップを容易にする.
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