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.

中文翻译：

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Tiplaxtinin作为一种有效的针对FtsZ的化学型用于抗菌研究的新应用

丝状温度敏感突变体Z（FtsZ）蛋白通常被认为是一种有前途的抗菌药物靶标。在本研究中，通过使用具有250种化合物的文库中基于细胞的筛选方法，首次将小分子有机分子（tiplaxtinin）鉴定为优异的细胞分裂抑制剂。Tiplaxtinin对革兰氏阳性病原体具有强大的抗菌活性。二者在体外和体内结果表明，所述化合物能够有效地通过刺激FtsZ的聚合和损害GTP酶活性的机制破坏动态组件的FtsZ的和Z的环的形成。