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卤化酶用于活性药物合成:已迈出第一步,后续仍有许多工作要做。

Halogenating Enzymes for Active Agent Synthesis: First Steps Are Done and Many Have to Follow.

机构信息

Institute for Bio- and Geosciences I: Bioorganic Chemistry, Forschungszentrum Jülich GmbH, D-52426 Jülich, Germany.

Institute of Bioorganic Chemistry, Heinrich Heine University Düsseldorf, D-52426 Jülich, Germany.

出版信息

Molecules. 2019 Nov 5;24(21):4008. doi: 10.3390/molecules24214008.

DOI:10.3390/molecules24214008
PMID:31694313
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6864650/
Abstract

Halogens can be very important for active agents as vital parts of their binding mode, on the one hand, but are on the other hand instrumental in the synthesis of most active agents. However, the primary halogenating compound is molecular chlorine which has two major drawbacks, high energy consumption and hazardous handling. Nature bypassed molecular halogens and evolved at least six halogenating enzymes: Three kind of haloperoxidases, flavin-dependent halogenases as well as α-ketoglutarate and adenosylmethionine (SAM)-dependent halogenases. This review shows what is known today on these enzymes in terms of biocatalytic usage. The reader may understand this review as a plea for the usage of halogenating enzymes for fine chemical syntheses, but there are many steps to take until halogenating enzymes are reliable, flexible, and sustainable catalysts for halogenation.

摘要

卤素可以作为它们结合模式的重要组成部分,对于活性物质非常重要,但另一方面,卤素也是大多数活性物质合成的关键。然而,主要的卤化化合物是氯气,它有两个主要缺点,即高能耗和危险的处理。大自然避开了分子卤素,并进化出了至少六种卤化酶:三种过氧化物酶、黄素依赖性卤化酶以及α-酮戊二酸和腺苷甲硫氨酸(SAM)依赖性卤化酶。这篇综述展示了目前关于这些酶在生物催化应用方面的知识。读者可以将这篇综述理解为呼吁使用卤化酶进行精细化学品合成,但在卤化酶成为可靠、灵活和可持续的卤化催化剂之前,还有许多步骤需要走。

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