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甲萘醌生物合成抑制:新型抗生素作用机制的研究进展综述

Menaquinone biosynthesis inhibition: a review of advancements toward a new antibiotic mechanism.

作者信息

Boersch M, Rudrawar S, Grant G, Zunk M

机构信息

School of Pharmacy and Pharmacology, Griffith University Gold Coast Queensland 4222 Australia

Quality Use of Medicines Network, Griffith University Gold Coast Queensland 4222 Australia.

出版信息

RSC Adv. 2018 Jan 29;8(10):5099-5105. doi: 10.1039/c7ra12950e.

Abstract

Menaquinone is essential in electron transport and ATP generation in all Gram-positive, and anaerobically respiring Gram-negative bacteria. By inhibiting menaquinone production in target organisms, bactericidal action can be achieved irrespective of the organisms' growth phase. This pathway is absent in human cells, as menaquinone is obtained only through the diet. This paper provides a succinct review of major advancements, where present, at all enzymatic steps of the biosynthetic pathway of menaquinone. Structure-activity relationships are evaluated, as well as results translating these relationships to growth inhibition studies.

摘要

甲萘醌在所有革兰氏阳性菌以及进行厌氧呼吸的革兰氏阴性菌的电子传递和ATP生成过程中至关重要。通过抑制靶标生物中甲萘醌的产生,无论生物处于何种生长阶段,均可实现杀菌作用。由于甲萘醌仅通过饮食获取,因此该途径在人体细胞中不存在。本文简要综述了甲萘醌生物合成途径中所有酶促步骤(如存在)的主要进展。评估了结构-活性关系,以及将这些关系转化为生长抑制研究的结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/99e9/9078190/76df53c0ea84/c7ra12950e-f1.jpg

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