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 publicationJournal articleAcademic researchpeer-review

12 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 languageEnglish
Pages (from-to)1909-1913
Number of pages5
JournalMedChemComm
Volume8
Issue number10
DOIs
Publication statusPublished - 1 Jan 2017

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

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