|
" A Thiazole Orange Derivative Targeting the Bacterial Protein FtsZ Shows Potent Antibacterial Activity. "
Sun, NingLu, Yu-JingChan, Fung-YiDu, Ruo-LanZheng, Yuan-YuanZhang, KunSo, Lok-YanAbagyan, RubenZhuo, ChaoLeung, Yun-ChungWong, Kwok-Yin
| Document Type
|
:
|
AL
|
| Record Number
|
:
|
901758
|
| Doc. No
|
:
|
LA0sb575tr
|
| Title & Author
|
:
|
A Thiazole Orange Derivative Targeting the Bacterial Protein FtsZ Shows Potent Antibacterial Activity. [Article]\ Sun, NingLu, Yu-JingChan, Fung-YiDu, Ruo-LanZheng, Yuan-YuanZhang, KunSo, Lok-YanAbagyan, RubenZhuo, ChaoLeung, Yun-ChungWong, Kwok-Yin
|
| Date
|
:
|
2017
|
| Title of Periodical
|
:
|
UC San Diego
|
| Abstract
|
:
|
The prevalence of multidrug resistance among clinically significant bacteria calls for the urgent development of new antibiotics with novel mechanisms of action. In this study, a new small molecule exhibiting excellent inhibition of bacterial cell division with potent antibacterial activity was discovered through cell-based screening. The compound exhibits a broad spectrum of bactericidal activity, including the methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and NDM-1 Escherichia coli. The in vitro and in vivo results suggested that this compound disrupts the dynamic assembly of FtsZ protein and Z-ring formation through stimulating FtsZ polymerization. Moreover, this compound exhibits no activity on mammalian tubulin polymerization and shows low cytotoxicity on mammalian cells. Taken together, these findings could provide a new chemotype for development of antibacterials with FtsZ as the target.
|
| |