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  • Title: Identification of TB-E12 as a novel FtsZ inhibitor with anti-tuberculosis activity.
    Author: Lin Y, Zhang H, Zhu N, Wang X, Han Y, Chen M, Jiang J, Si S.
    Journal: Tuberculosis (Edinb); 2018 May; 110():79-85. PubMed ID: 29779778.
    Abstract:
    The global pandemic of multidrug-resistant (MDR) Mycobacterium tuberculosis (TB) drives for more effective anti-TB drugs with new drug target. Filamentous temperature sensitive protein Z (FtsZ), a GTP dependent prokaryotic cell division protein, forms a dynamic Z-ring in the center of the cell. Differences between bacterial FtsZ and eukaryotic tubulin make FtsZ a highly attractive drug target. In this study, we used phenotype screening of M. smegmatis and model screening targeting M. tuberculosis FtsZ (Mtb-FtsZ) to identify a hit compound TB-E12. TB-E12 was found to prevent the growth of M. smegmatis by inhibiting the GTPase activity of Mtb-FtsZ. Molecular docking and site-directed mutagenesis analyses identified Asn22 of Mtb-FtsZ as the key amino site. The higher MIC of TB-E12 for M. smegmatis strain overexpressing Mtb-FtsZ confirmed that Mtb-FtsZ is likely the target. Importantly, TB-E12 exhibits excellent anti-TB activity, but had no anti-bacterial activity to other strains. In vitro, the proliferation of Mycobacterium smegmatis was inhibited by TB-E12. All these results indicate TB-E12 is a promising lead compound against drug-resistant tuberculosis.
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