New application of tiplaxtinin as an effective FtsZ-targeting chemotype for an antimicrobial study.
Basic Information
ID: ALA4261566
Journal: Medchemcomm
Title: New application of tiplaxtinin as an effective FtsZ-targeting chemotype for an antimicrobial study.
Authors: Sun N, Zheng YY, Du RL, Cai SY, Zhang K, So LY, Cheung KC, Zhuo C, Lu YJ, Wong KY.
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.
CiteXplore: 30108711
DOI: 10.1039/C7MD00387K
Patent ID: ┄