Bacterial Cell Growth Inhibitors Targeting Undecaprenyl Diphosphate Synthase and Undecaprenyl Diphosphate Phosphatase

CORC > 天津工业生物技术研究所 > 结构生物学与蛋白酶学实验室郭瑞庭 > 期刊论文

	Bacterial Cell Growth Inhibitors Targeting Undecaprenyl Diphosphate Synthase and Undecaprenyl Diphosphate Phosphatase
	Wang, Yang 1; Desai, Janish 2; Zhang, Yonghui 1; Malwal, Satish R.1; Shin, Christopher J.1; Feng, Xinxin 1; Sun, Hong 3; Liu, Guizhi 3; Guo, Rey-Ting 3; Oldfield, Eric 1,2
刊名	CHEMMEDCHEM
	2016-10-19
卷号	11 期号:20 页码:2311-2319
关键词	benzoic acids cell-wall biosynthesis drug discovery membrane proteins Staphylococcus aureus
英文摘要	We synthesized a series of benzoic acids and phenylphosphonic acids and investigated their effects on the growth of Staphylococcus aureus and Bacillus subtilis. One of the most active compounds, 5-fluoro-2-(3-(octyloxy) benzamido) benzoic acid (7, ED50 similar to 0.15 mu g mL(-1)) acted synergistically with seven antibiotics known to target bacterial cell-wall biosynthesis (a fractional inhibitory concentration index (FICI) of similar to 0.35, on average) but had indifferent effects in combinations with six non-cell-wall biosynthesis inhibitors (average FICI similar to 1.45). The most active compounds were found to inhibit two enzymes involved in isoprenoid/bacterial cell-wall biosynthesis: undecaprenyl diphosphate synthase (UPPS) and undecaprenyl diphosphate phosphatase (UPPP), but not farnesyl diphosphate synthase, and there were good correlations between bacterial cell growth inhibition, UPPS inhibition, and UPPP inhibition.
WOS标题词	Science & Technology ; Life Sciences & Biomedicine
类目[WOS]	Chemistry, Medicinal ; Pharmacology & Pharmacy
研究领域[WOS]	Pharmacology & Pharmacy
收录类别	SCI
语种	英语
WOS记录号	WOS:000387392800007
内容类型	期刊论文
源URL	[http://124.16.173.210/handle/834782/2299]
专题	天津工业生物技术研究所_结构生物学与蛋白酶学实验室郭瑞庭_期刊论文
作者单位	1.Univ Illinois, Dept Chem, 600 South Mathews Ave, Urbana, IL 61801 USA 2.Univ Illinois, Ctr Biophys & Quantitat Biol, 1110 West Green St, Urbana, IL 61801 USA 3.Chinese Acad Sci, Tianjin Inst Ind Biotechnol, Ind Enzymes Natl Engn Lab, Tianjin 300308, Peoples R China
推荐引用方式 GB/T 7714	Wang, Yang,Desai, Janish,Zhang, Yonghui,et al. Bacterial Cell Growth Inhibitors Targeting Undecaprenyl Diphosphate Synthase and Undecaprenyl Diphosphate Phosphatase[J]. CHEMMEDCHEM,2016,11(20):2311-2319.
APA	Wang, Yang.,Desai, Janish.,Zhang, Yonghui.,Malwal, Satish R..,Shin, Christopher J..,...&Oldfield, Eric.(2016).Bacterial Cell Growth Inhibitors Targeting Undecaprenyl Diphosphate Synthase and Undecaprenyl Diphosphate Phosphatase.CHEMMEDCHEM,11(20),2311-2319.
MLA	Wang, Yang,et al."Bacterial Cell Growth Inhibitors Targeting Undecaprenyl Diphosphate Synthase and Undecaprenyl Diphosphate Phosphatase".CHEMMEDCHEM 11.20(2016):2311-2319.