脂質と細胞膜を通過する塩素イオンを輸送できる酵素反応性プロキャリア
Ye Rin Choi1, Bom Lee1, Jinhong Park2
1Department of Chemistry, Yonsei University , Seoul 120-749, Korea.
Journal of the American Chemical Society
|December 10, 2016
まとめ
研究者らは,膜を横断するクロライドイオン輸送を制御する酵素活性化プロカリアを開発した. これらのプロカリアは,溶解性を改善し,標的の活性化を可能にすることで,薬剤の投与を強化します.
科学分野:
- 膜輸送
- 生物化学
- 薬物投与システム
背景:
- 塩素イオン輸送は 細胞機能に不可欠です
- 水害を避ける分子の標的型配送システムを開発することは,依然として課題です.
- プロキャリア戦略は,制御された活性化と配送の可能性を提供します.
研究 の 目的:
- 制御された塩化イオン輸送のためのプロカリアーコンセプトを導入し,検証する.
- 特定の条件下でプロカリアの酵素媒介活性化を調査する.
- プロカリアの溶解性と膜分割に対する水性付属体の影響を評価する.
主な方法:
- エステル結合とグリコシル結合を伴うプロカリアの合成
- エステラーゼ (PLE) とグリコシラーゼ (AOG) を用いた付属体の酵素水解
- 脂質二層と細胞膜を通過する塩化イオン輸送測定法
- pHに依存した活性化試験
主要な成果:
- プロキャリアは当初はリポフィル膜に無活性であったが,特定の酵素によって活性化された.
- エステル結合プロカリアは,PLEによってpH7. 4で活性化されました.
- グリコシル結合プロカリアーはpH5. 5~6でAOGによって活性化されました.
- 水性付属体は,産卵体を水に溶けやすくし,産卵を助長した.
結論:
- プロカリア戦略は,塩化イオン輸送の制御された,酵素特有の活性化を可能にします.
- 条件付きのアクティベーションは,膜を横断して標的の輸送を可能にします.
- このアプローチは 防水薬の投与を改善する見込みです
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