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靶向MreB用于抗生素开发的现状。

Status of Targeting MreB for the Development of Antibiotics.

作者信息

Awuni Elvis

机构信息

Department of Biochemistry, School of Biological Sciences, CANS, University of Cape Coast, Cape Coast, Ghana.

出版信息

Front Chem. 2020 Jan 10;7:884. doi: 10.3389/fchem.2019.00884. eCollection 2019.

Abstract

Although many prospective antibiotic targets are known, bacterial infections and resistance to antibiotics remain a threat to public health partly because the druggable potentials of most of these targets have yet to be fully tapped for the development of a new generation of therapeutics. The prokaryotic actin homolog MreB is one of the important antibiotic targets that are yet to be significantly exploited. MreB is a bacterial cytoskeleton protein that has been widely studied and is associated with the determination of rod shape as well as important subcellular processes including cell division, chromosome segregation, cell wall morphogenesis, and cell polarity. Notwithstanding that MreB is vital and conserved in most rod-shaped bacteria, no approved antibiotics targeting it are presently available. Here, the status of targeting MreB for the development of antibiotics is concisely summarized. Expressly, the known therapeutic targets and inhibitors of MreB are presented, and the way forward in the search for a new generation of potent inhibitors of MreB briefly discussed.

摘要

尽管已知许多潜在的抗生素靶点,但细菌感染和对抗生素的耐药性仍然对公众健康构成威胁,部分原因在于这些靶点中的大多数在开发新一代治疗药物方面的可药用潜力尚未得到充分挖掘。原核肌动蛋白同源物MreB是尚未得到充分利用的重要抗生素靶点之一。MreB是一种细菌细胞骨架蛋白,已被广泛研究,它与杆状形态的确定以及包括细胞分裂、染色体分离、细胞壁形态发生和细胞极性在内的重要亚细胞过程有关。尽管MreB在大多数杆状细菌中至关重要且保守,但目前尚无针对它的获批抗生素。在此,简要总结了以MreB为靶点开发抗生素的现状。具体而言,介绍了已知的MreB治疗靶点和抑制剂,并简要讨论了寻找新一代强效MreB抑制剂的前进方向。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1217/6965359/1ea5f6512a21/fchem-07-00884-g0001.jpg

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