Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase
文献类型：期刊论文
| 作者 | Wu, Yang; Yu, Kunqian ; Xu, Bin; Chen, Lili; Chen, Xianglong; Mao, Jialing; Danchin, Antoine; Shen, Xu; Qu, Di; Jiang, Hualiang
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| 刊名 | JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
 |
| 出版日期 | 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 |
| WOS记录号 | WOS:000249882200008 |
| 出版者 | OXFORD UNIV PRESS |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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