Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase
文献类型：期刊论文
| 作者 | Wu, Y; Yu, KQ; Xu, B; Chen, LL; Chen, XL; Mao, JL; Danchin, A; Shen, X; Qu, D; Jiang, HL |
| 刊名 | JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
 |
| 出版日期 | 2007 |
| 卷号 | 60期号:3页码:502-509 |
| 关键词 | WRS virtual screening S. epidermidis antibacterials |
| 通讯作者 | Qu, D (reprint author), Fudan Univ, Shanghai Med Sch, Inst Med Microbiol, Key Lab Med Mol Virol Minist Educ & Hlth, Shanghai 200032, Peoples R China.,dqu@shmu.edu.cn |
| 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. |
| 学科主题 | Infectious Diseases; Microbiology; Pharmacology & Pharmacy |
| 类目[WOS] | Infectious Diseases ; Microbiology ; Pharmacology & Pharmacy |
| 关键词[WOS] | COAGULASE-NEGATIVE STAPHYLOCOCCI ; DISCOVERY ; ANALOGS ; ANGIOGENESIS ; RECOGNITION ; INFECTIONS ; STRATEGIES ; RESISTANCE ; PATHOGENS ; VIRULENCE |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000249882200008 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/1537]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 推荐引用方式 GB/T 7714 | Wu, Y,Yu, KQ,Xu, B,et al. Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase[J]. JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY,2007,60(3):502-509. |
| APA | Wu, Y.,Yu, KQ.,Xu, B.,Chen, LL.,Chen, XL.,...&Jiang, HL.(2007).Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase.JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY,60(3),502-509. |
| MLA | Wu, Y,et al."Potent and selective inhibitors of Staphylococcus epidermidis tryptophanyl-tRNA synthetase".JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY 60.3(2007):502-509. |
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