New application of tiplaxtinin as an effective FtsZ-targeting chemotype for an antimicrobial studyThe authors declare no competing interests.Electronic supplementary information (ESI) available: Supplementary materials and methods. See DOI: 10.1039/c7md00387k

The filamenting temperature-sensitive mutant Z (FtsZ) protein is generally recognized as a promising antimicrobial drug target. In the present study, a small organic molecule (tiplaxtinin) was identified for the first time as an excellent cell division inhibitor by using a cell-based screening appro...

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Main Authors: Sun, Ning, Zheng, Yuan-Yuan, Du, Ruo-Lan, Cai, Sen-Yuan, Zhang, Kun, So, Lok-Yan, Cheung, Kwan-Choi, Zhuo, Chao, Lu, Yu-Jing, Wong, Kwok-Yin
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Language:English
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Summary:The filamenting temperature-sensitive mutant Z (FtsZ) protein is generally recognized as a promising antimicrobial drug target. In the present study, a small organic molecule (tiplaxtinin) was identified for the first time as an excellent cell division inhibitor by using a cell-based screening approach from a library with 250 compounds. Tiplaxtinin possesses potent antibacterial activity against Gram-positive pathogens. Both in vitro and in vivo results reveal that the compound is able to disrupt dynamic assembly of FtsZ and Z-ring formation effectively through the mechanism of stimulating FtsZ polymerization and impairing GTPase activity. Tiplaxtinin exhibits an excellent cell division inhibitory effect with potent antibacterial activity through interacting with FtsZ.
ISSN:2040-2503
2040-2511
DOI:10.1039/c7md00387k