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http://hdl.handle.net/10397/76365
Title: | A thiazole orange derivative targeting the bacterial protein FtsZ shows potent antibacterial activity | Authors: | Sun, N Lu, YJ Chan, FY Du, RL Zheng, YY Zhang, K So, LY Abagyan, R Zhuo, C Leung, YC Wong, KY |
Issue Date: | 11-May-2017 | Source: | Frontiers in microbiology, 11 May 2017, v. 8, 855, p. 1-12 | Abstract: | The prevalence of multidrug resistance among clinically significant bacteria calls for the urgent development of new antibiotics with novel mechanisms of action. In this study, a new small molecule exhibiting excellent inhibition of bacterial cell division with potent antibacterial activity was discovered through cell-based screening. The compound exhibits a broad spectrum of bactericidal activity, including the methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and NDM-1 Escherichia coli. The in vitro and in vivo results suggested that this compound disrupts the dynamic assembly of FtsZ protein and Z-ring formation through stimulating FtsZ polymerization. Moreover, this compound exhibits no activity on mammalian tubulin polymerization and shows low cytotoxicity on mammalian cells. Taken together, these findings could provide a new chemotype for development of antibacterials with FtsZ as the target. | Keywords: | Bacterial resistance Antibacterial activity Cell division FtsZ inhibitor FtsZ polymerization |
Publisher: | Frontiers Research Foundation | Journal: | Frontiers in microbiology | ISSN: | 1664-302X | DOI: | 10.3389/fmicb.2017.00855 | Rights: | Copyright © 2017 Sun, Lu, Chan, Du, Zheng, Zhang, So, Abagyan, Zhuo, Leung and Wong. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY) (https://creativecommons.org/licenses/by/4.0/). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. The following publication Sun N, Lu Y-J, Chan F-Y, Du R-L, Zheng Y-y, Zhang K, So L-Y, Abagyan R, Zhuo C, Leung Y-C and Wong K-Y (2017) A Thiazole Orange Derivative Targeting the Bacterial Protein FtsZ Shows Potent Antibacterial Activity. Front. Microbiol. 8:855,1-12 is available at https://dx.doi.org/10.3389/fmicb.2017.00855 |
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