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

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.

SUBMITTER: Sun N

PROVIDER: S-EPMC6072346 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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

Sun Ning N Zheng Yuan-Yuan YY Du Ruo-Lan RL Cai Sen-Yuan SY Zhang Kun K So Lok-Yan LY Cheung Kwan-Choi KC Zhuo Chao C Lu Yu-Jing YJ Wong Kwok-Yin KY

MedChemComm 20170822 10

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 <i>in vitro</i> and <i>in vivo</i> results reveal that the compound is ...[more]

PMID: 30108711

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