Antibacterial Drug Leads: DNA and Enzyme Multitargeting
文献类型：期刊论文
| 作者 | Zhu, Wei1; Wang, Yang1; Li, Kai1; Gao, Jian2; Huang, Chun-Hsiang2; Chen, Chun-Chi2; Ko, Tzu-Ping3; Zhang, Yonghui1; Guo, Rey-Ting2; Oldfield, Eric1 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-02-12 |
| 卷号 | 58期号:3页码:1215-1227 |
| 英文摘要 | We report the results of an investigation of the activity of a series of amidine and bisamidine compounds against Staphylococcus aureus and Escherichia coli. The most active compounds bound to an AT-rich DNA dodecamer (CGCGAATTCGCG)(2) and using DSC were found to increase the melting transition by up to 24 degrees C. Several compounds also inhibited undecaprenyl diphosphate synthase (UPPS) with IC50 values of 100-500 nM, and we found good correlations (R-2 = 0.89, S. aureus; R-2 = 0.79, E. coli) between experimental and predicted cell growth inhibition by using DNA Delta(Tm) and UPPS IC50 experimental results together with one computed descriptor. We also solved the structures of three bisamidines binding to DNA as well as three UPPS structures. Overall, the results are of general interest in the context of the development of resistance-resistant antibiotics that involve multitargeting. |
| WOS标题词 | Science & Technology ; Life Sciences & Biomedicine |
| 类目[WOS] | Chemistry, Medicinal |
| 研究领域[WOS] | Pharmacology & Pharmacy |
| 关键词[WOS] | FARNESYL DIPHOSPHATE SYNTHASE ; ISOPRENOID BIOSYNTHESIS ; BISPHOSPHONATE INHIBITION ; CRYSTAL-STRUCTURE ; TARGET ; D(CGCGAATTCGCG) ; DISCOVERY ; DESIGN |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000349573800015 |
| 源URL | [http://124.16.173.210/handle/834782/1428]  |
| 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, Urbana, IL 61801 USA 2.Chinese Acad Sci, Tianjin Inst Ind Biotechnol, Ind Enzymes Natl Engn Lab, Tianjin 300308, Peoples R China 3.Acad Sinica, Inst Biol Chem, Taipei 11529, Taiwan |
| 推荐引用方式 GB/T 7714 | Zhu, Wei,Wang, Yang,Li, Kai,et al. Antibacterial Drug Leads: DNA and Enzyme Multitargeting[J]. JOURNAL OF MEDICINAL CHEMISTRY,2015,58(3):1215-1227. |
| APA | Zhu, Wei.,Wang, Yang.,Li, Kai.,Gao, Jian.,Huang, Chun-Hsiang.,...&Oldfield, Eric.(2015).Antibacterial Drug Leads: DNA and Enzyme Multitargeting.JOURNAL OF MEDICINAL CHEMISTRY,58(3),1215-1227. |
| MLA | Zhu, Wei,et al."Antibacterial Drug Leads: DNA and Enzyme Multitargeting".JOURNAL OF MEDICINAL CHEMISTRY 58.3(2015):1215-1227. |
入库方式： OAI收割
来源：天津工业生物技术研究所
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