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题名: Development of a fluorescence-based HIV-1 integrase DNA binding assay for identification of novel HIV-1 integrase inhibitors
作者: Han, Ying-Shan1; Xiao, Wei-Lie2; Quashie, Peter K.1; Mesplede, Thibault1; Xu, Hongtao1; Deprez, Eric3; Delelis, Olivier3; Pu, Jian-Xin2; null(孙汉董)2; Wainberg, Mark A.1
刊名: ANTIVIRAL RESEARCH
关键词: HIV-1 integrase inhibitors ; Integrase DNA binding ; Fluorescent assay
英文摘要: Human immunodeficiency virus integrase (HIV-1 IN) inhibitors that are currently approved or are in advanced clinical trials specifically target the strand transfer step of integration. However, considerable cross-resistance exists among some members of this class of IN inhibitors. Intriguingly, though, HIV-1 IN possesses multiple sites, distinct from those involved in the strand transfer step, that could be targeted to develop new HIV-1 IN inhibitors. We have developed a fluorescent HIV-1 IN DNA binding assay that can identify small molecules termed IN binding inhibitors (INBIs) that inhibit IN binding to viral DNA. This assay has been optimized with respect to concentrations of each protein, long terminal repeat (LTR) DNA substrate, salt, and time, and has been used successfully to measure the HIV-1 IN DNA binding activity of a well-characterized INBI termed FZ41. In addition, we have used the assay to screen a small library of natural products, resulting in the identification of nigranoic acid as a new INBI. The proposed fluorescence assay is easy and inexpensive, and provides a high-throughput detection method for determination of HIV-1 IN DNA binding activity, monitoring of enzyme kinetics, and high-throughput screening for the identification of new INBIs. (C) 2013 Elsevier B.V. All rights reserved.
出版日期: 2013-06-01
卷号: 98, 期号:3, 页码:441-448
DOI标识: 10.1016/j.antiviral.2013.04.001
语种: 英语
ISSN号: 0166-3542
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/16587
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.McGill Univ, Jewish Gen Hosp, AIDS Ctr, Lady Davis Med Res, Montreal, PQ H3T 1E2, Canada
2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resource West Chi, Kunming 650204, Peoples R China
3.ENS Cachan, CNRS, LBPA, Cachan, France

Recommended Citation:
Han, Ying-Shan; Xiao, Wei-Lie; Quashie, Peter K.; Mesplede, Thibault; Xu, Hongtao; Deprez, Eric; Delelis, Olivier; Pu, Jian-Xin; Sun, Han-Dong; Wainberg, Mark A..Development of a fluorescence-based HIV-1 integrase DNA binding assay for identification of novel HIV-1 integrase inhibitors,ANTIVIRAL RESEARCH,2013,98(3):441-448
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