非那嗪卤化单组分卤化酶的发现与表征。

IF 5 1区化学 Q1 CHEMISTRY, ORGANIC

Organic Letters Pub Date : 2025-09-07 DOI:10.1021/acs.orglett.5c03444

Zhenshan Chen, He Duan, Mengqi Zhao, Fei Xiao and Wenli Li*,

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引用次数: 0

摘要

卤代苯那嗪作为抗菌和抗生物膜剂有很大的前景，但主要是通过化学合成获得的。在这里，我们报道了一种新的单组分黄素依赖卤化酶（FDH） PezW，它可以卤化吩那嗪支架，特别是可以酶合成生物活性的2-溴-1-羟基吩那嗪（2d）和2,4-溴-1-羟基吩那嗪（2f）。结构建模和诱变揭示了底物结合和催化的关键残基。这些发现突出了PezW作为合成具有药学意义的卤化非那嗪类生物催化剂的潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Discovery and Characterization of a Single-Component Halogenase for Phenazine Halogenation

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Discovery and Characterization of a Single-Component Halogenase for Phenazine Halogenation

Halogenated phenazines hold promise as antimicrobial and antibiofilm agents, yet are mainly accessed via chemical synthesis. Herein, we report PezW, a novel single-component flavin-dependent halogenase (FDH) that halogenates phenazine scaffolds, notably enabling enzymatic synthesis of bioactive 2-bromo-1-hydroxyphenazine (2d) and 2,4-bromo-1-hydroxyphenazine (2f). Structural modeling and mutagenesis revealed key residues critical for substrate binding and catalysis. These findings highlight PezW’s potential as a biocatalyst for the synthesis of halogenated phenazines with pharmaceutical relevance.

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来源期刊

Organic Letters 化学-有机化学

CiteScore

9.30

自引率

11.50%

发文量

1607

审稿时长

1.5 months

期刊介绍： Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.