Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase

doi:10.1093/jac/dkm229

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 新药研究国家重点实验室

	Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase
	Wu, Yang ; Yu, Kunqian; Xu, Bin; Chen, Lili; Chen, Xianglong ; Mao, Jialing ; Danchin, Antoine ; Shen, Xu; Qu, Di ; Jiang, Hualiang
刊名	JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
	2007-09
卷号	60 期号:3 页码:502-509
关键词	WRS virtual screening S. epidermidis antibacterials
ISSN号	0305-7453
DOI	10.1093/jac/dkm229
文献子类	Article
英文摘要	Objectives: The skin commensal and opportunistic pathogen Staphylococcus epidermidis is one of the leading causes of nosocomial and biofilm-associated infections, which urgently requires discovery of new antibiotics. We decided to find new leads that target the S. epidermidis tryptophanyl-tRNA synthetase (SeWRS), which is essential for translation. Methods: We applied an approach combining structure-based discovery in silico with biochemical and biological experiments in vitro to screen SeWRS inhibitors. Results: Three compounds have an inhibitory effect on enzymatic activities of SeWRS, of which two show low inhibition of the human tryptophanyl-tRNA synthetase. Binding of these compounds to bacterially expressed SeWRS was demonstrated by surface plasmon resonance technology. These three compounds can also obviously inhibit growth of S. epidermidis in vitro and displayed low cytotoxicity to mammalian cells. Conclusions: These compounds are good leads to develop new antibiotics.
WOS关键词	COAGULASE-NEGATIVE STAPHYLOCOCCI ; DISCOVERY ; ANALOGS ; ANGIOGENESIS ; RECOGNITION ; INFECTIONS ; STRATEGIES ; RESISTANCE ; PATHOGENS ; VIRULENCE
WOS研究方向	Infectious Diseases ; Microbiology ; Pharmacology & Pharmacy
语种	英语
出版者	OXFORD UNIV PRESS
WOS记录号	WOS:000249882200008
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/273160]
专题	新药研究国家重点实验室中科院受体结构与功能重点实验室
通讯作者	Qu, Di
作者单位	1.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol, State Key Lab Mol Biol, Shanghai 200031, Peoples R China 2.Fudan Univ, Shanghai Med Sch, Inst Med Microbiol, Key Lab Med Mol Virol Minist Educ & Hlth, Shanghai 200032, Peoples R China 3.Fudan Univ, Shanghai Med Sch, Inst Biomed Sci, Shanghai 200032, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res,Drug Discovery & Design Ct, Shanghai 201203, Peoples R China 5.Inst Pasteur, CNRS, URA 2171, Genet Bacterial Genomes, F-75724 Paris 15, France
推荐引用方式 GB/T 7714	Wu, Yang,Yu, Kunqian,Xu, Bin,et al. Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase[J]. JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY,2007,60(3):502-509.
APA	Wu, Yang.,Yu, Kunqian.,Xu, Bin.,Chen, Lili.,Chen, Xianglong.,...&Jiang, Hualiang.(2007).Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase.JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY,60(3),502-509.
MLA	Wu, Yang,et al."Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase".JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY 60.3(2007):502-509.