Small DNA circles as bacterial topoisomerase I inhibitors

被引:6
作者
Li, Dawei [1 ,3 ]
Wang, Qiang [1 ]
Zhou, Bing [1 ]
Zhuge, Qiang [1 ]
Lv, Bei [2 ]
机构
[1] Nanjing Forestry Univ, Coll Biol & Environm, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China
[2] Jiangsu Second Normal Univ, Coll Life Sci & Chem, Jiangsu Key Lab Biofunct Mol, Nanjing 210013, Jiangsu, Peoples R China
[3] Nanjing Forestry Univ, Southern Modern Forestry Collaborat Innovat Ctr, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China
关键词
Drug therapy;
D O I
10.1039/c9ra02398d
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Bacterial topoisomerase I is a potential target during the course of antibacterial drug therapy. In our studies, specifically designed small DNA circles with high bending stress were synthesized. It is demonstrated that small DNA circles showed high inhibitory effect on the activity of bacterial topoisomerase I and the single-stranded regions associated with bending deformation in DNA circles are believed to be the crucial factor for trapping the enzymes and decreasing the effective concentration of the topoisomerases in the reaction solution. In addition, the DNA circles showed high thermal stability and excellent nuclease resistance. In consideration of the low cytotoxicity of DNA-based biopharmaceuticals, our results may provide a new idea for the future design and optimization of DNA-based therapeutic agents for antibacterial therapy.
引用
收藏
页码:18415 / 18419
页数:5
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