New application of tiplaxtinin as an effective FtsZ-targeting chemotype for an antimicrobial study

Ning Sun; Yuan Yuan Zheng; Ruo Lan Du; Sen Yuan Cai; Kun Zhang; Lok Yan So; Kwan Choi Cheung; Chao Zhuo; Yu Jing Lu; Kwok Yin Wong

doi:10.1039/c7md00387k

New application of tiplaxtinin as an effective FtsZ-targeting chemotype for an antimicrobial study

Ning Sun, Yuan Yuan Zheng, Ruo Lan Du, Sen Yuan Cai, Kun Zhang, Lok Yan So, Kwan Choi Cheung, Chao Zhuo, Yu Jing Lu, Kwok Yin Wong

Research output: Journal article publication › Journal article › Academic research › peer-review

18 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	1909-1913
Number of pages	5
Journal	MedChemComm
Volume	8
Issue number	10
DOIs	https://doi.org/10.1039/c7md00387k
Publication status	Published - 1 Jan 2017

ASJC Scopus subject areas

Biochemistry
Pharmaceutical Science

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10.1039/c7md00387k

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abstract = "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.",

author = "Ning Sun and Zheng, {Yuan Yuan} and Du, {Ruo Lan} and Cai, {Sen Yuan} and Kun Zhang and So, {Lok Yan} and Cheung, {Kwan Choi} and Chao Zhuo and Lu, {Yu Jing} and Wong, {Kwok Yin}",

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AU - Sun, Ning

AU - Zheng, Yuan Yuan

AU - Du, Ruo Lan

AU - Cai, Sen Yuan

AU - Zhang, Kun

AU - So, Lok Yan

AU - Cheung, Kwan Choi

AU - Zhuo, Chao

AU - Lu, Yu Jing

AU - Wong, Kwok Yin

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AB - 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.

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DO - 10.1039/c7md00387k

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JF - MedChemComm

IS - 10

ER -

New application of tiplaxtinin as an effective FtsZ-targeting chemotype for an antimicrobial study

Abstract

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