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细菌乙酰羟酸合酶及其抑制剂:结构、生物活性及研究现状综述。

Bacterial acetohydroxyacid synthase and its inhibitors--a summary of their structure, biological activity and current status.

机构信息

Department of Chemistry, Institute of Natural Sciences, Hanyang University, Seoul, Korea.

出版信息

FEBS J. 2012 Mar;279(6):946-63. doi: 10.1111/j.1742-4658.2012.08505.x. Epub 2012 Feb 27.

Abstract

Acetohydroxyacid synthase (anabolic AHAS; EC 2.2.1.6) is a thiamin diphosphate-dependent enzyme that catalyzes the first step in the branched-chain amino acid (BCAA) biosynthesis pathway. BCAAs are synthesized by plants, algae, fungi and bacteria, although not by animals. Thus, the enzymes of the BCAA biosynthetic pathway are potential targets in the development of herbicides, fungicides and antimicrobial compounds. Plant AHASs are well studied in this regard because specific plant AHAS inhibitors are considered to comprise the most potent herbicides. These inhibitors are also effective against bacterial AHASs, inhibit the growth of several bacterial strains and have little to no toxicity in mammals. This review provides an overview of bacterial AHASs with an update of the current status of AHAS inhibitors.

摘要

乙酰羟酸合酶(合成型 AHAS;EC 2.2.1.6)是一种依赖于硫胺素焦磷酸的酶,催化支链氨基酸(BCAA)生物合成途径的第一步。BCAAs 由植物、藻类、真菌和细菌合成,但动物不能合成。因此,BCAA 生物合成途径的酶是除草剂、杀真菌剂和抗菌化合物开发的潜在靶点。在这方面,植物 AHAS 研究得比较透彻,因为特定的植物 AHAS 抑制剂被认为是最有效的除草剂。这些抑制剂对细菌 AHAS 也有效,能抑制几种细菌菌株的生长,对哺乳动物的毒性很小或几乎没有。本文综述了细菌 AHAS,并更新了 AHAS 抑制剂的最新研究进展。

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