ブテラゼ1による循環性バクテリオシンの総合成
Xinya Hemu1, Yibo Qiu1, Giang K T Nguyen1
1School of Biological Sciences, Nanyang Technological University , 60 Nanyang Drive, 637551 Singapore.
Journal of the American Chemical Society
|May 21, 2016
まとめ
研究者達は 乳酸細菌から 強力な抗菌剤である 大きな円形バクテリオシンを合成しました 彼らの化学酵素法では 薬剤耐性病原体に対する 活性化合物が得られます
科学分野:
- 生物化学
- 有機化学
- 微生物学
背景:
- 循環型バクテリオシン (Circular bacteriocins) は,乳酸バクテリアの大きな循環型ペプチドであり,他のバクテリアを抑制するために重要である.
- 循環構造は食品保存の安定性を高めますが,水害性のセグメントにより化学合成を複雑にします.
研究 の 目的:
- AS-48,ウベロリシン,ガービシンMLの3つの大きな円形のバクテリオシンを合成する.
- これらの複雑なペプチドによって引き起こされる合成の課題を克服する効率的な化学酵素戦略を開発する.
主な方法:
- 線形ペプチド前駆体を準備するために,マイクロ波段階的合成が採用された.
- 効率的なバックボーンリング閉鎖のために,Asn特異のブテラゼ媒介サイクライゼーションが利用されました.
- 抗菌作用は標準的な測定法で評価された.
主要な成果:
- AS-48,ウベロリシン,ガービシンMLの全合成が成功しました.
- AS-48の線形前駆体は100μMまで抗菌作用を示さなかった.
- マクロサイクリックAS-48は,微小分子MICで,病原性および薬剤耐性細菌に対する強力な抗菌作用を示した.
結論:
- 開発された化学酵素戦略は,大規模で複雑な循環型バクテリオシンを合成するのに効率的です.
- AS-48のようなバクテリオシンの強力な抗菌作用にはサイクル化が不可欠です.
- この作業は 価値ある抗菌剤を 生産するための 実行可能な経路を提供します
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