Hydroxamic acids are metal-chelating compounds that show important biological activity including anti-tumor effects. We have recently engineered the transketolase from Geobacillus stearothermopilus (TK_gst) to convert benzaldehyde as a non-natural acceptor substrate. Realizing the structural and electronic similarity to nitrosobenzene, we studied the TK-catalyzed conversion of nitrosoarenes to yield N-arylated hydroxamic acids. Here we demonstrate that wild-type and variants of this versatile TK_gst enzyme indeed induce the rapid biocatalytic conversion of variously p-, m- and o-substituted nitrosoarenes to produce a variety of corresponding N-aryl hydroxamic acids via creation of a carbon-nitrogen instead of a carbon-carbon bond. Further structural modifications can be introduced by varying the donor component, such as hydroxypyruvate or pyruvate.

中文翻译：

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转酮酶催化合成N-芳基羟肟酸

异羟肟酸是一种金属螯合化合物，具有重要的生物活性，包括抗肿瘤作用。我们最近设计了来自Geobacillus stearothermopilus (TK _gst ) 的转酮醇酶，以将苯甲醛转化为非天然受体底物。认识到与亚硝基苯的结构和电子相似性，我们研究了 TK 催化的亚硝基芳烃转化为N-芳基化异羟肟酸。_{在这里，我们证明了这种多功能 TK gst}酶的野生型和变体确实诱导各种p-、m-和o-取代的亚硝基芳烃的快速生物催化转化，以产生各种相应的N-芳基异羟肟酸通过产生碳-氮而不是碳-碳键。通过改变供体组分，例如羟基丙酮酸或丙酮酸，可以引入进一步的结构修饰。