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

The filamenting temperature-sensitive mutant Z (FtsZ) protein is widely regarded as a potential target for antimicrobial drug development. In this study, a small organic molecule, tiplaxtinin, was identified for the first time as an effective inhibitor of cell division through a cell-based screening approach using a library of 250 compounds. Tiplaxtinin demonstrates strong antibacterial activity against Gram-positive pathogens. Both in vitro and in vivo findings show that the compound disrupts the dynamic assembly of FtsZ and the formation of the Z-ring by promoting FtsZ polymerization and inhibiting its GTPase activity.