Development of a fluorescence-based HIV-1 integrase DNA binding assay for identification of novel HIV-1 integrase inhibitors
Han, Ying-Shan1; Xiao, Wei-Lie2; Quashie, Peter K.1; Mesplede, Thibault1; Xu, Hongtao1; Deprez, Eric3; Delelis, Olivier3; Pu, Jian-Xin2; Sun, Han-Dong2; Wainberg, Mark A.1
2013-06-01
发表期刊ANTIVIRAL RESEARCH
ISSN0166-3542
卷号98期号:3页码:441-448
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.
关键词Hiv-1 Integrase Inhibitors Integrase Dna Binding Fluorescent Assay
资助信息Canadian Institutes for Health Research (CIHR); BMS/CTN; CAHR/CIHR; CAS [KSCX2-EW-Q-10]; Natural Science Foundation of China [30830115]; Canadian Institutes for Health Research (CIHR); BMS/CTN; CAHR/CIHR; CAS(KSCX2-EW-Q-10); Natural Science Foundation of China(30830115)
学科领域Pharmacology & Pharmacy ; Virology
DOI10.1016/j.antiviral.2013.04.001
收录类别SCI
语种英语
WOS研究方向Pharmacology & Pharmacy ; Virology
WOS类目Pharmacology & Pharmacy ; Virology
WOS记录号WOS:000320296400012
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被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/16587
专题植物化学与西部植物资源持续利用国家重点实验室
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
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Han, Ying-Shan,Xiao, Wei-Lie,Quashie, Peter K.,et al. Development of a fluorescence-based HIV-1 integrase DNA binding assay for identification of novel HIV-1 integrase inhibitors[J]. ANTIVIRAL RESEARCH,2013,98(3):441-448.
APA Han, Ying-Shan.,Xiao, Wei-Lie.,Quashie, Peter K..,Mesplede, Thibault.,Xu, Hongtao.,...&Wainberg, Mark A..(2013).Development of a fluorescence-based HIV-1 integrase DNA binding assay for identification of novel HIV-1 integrase inhibitors.ANTIVIRAL RESEARCH,98(3),441-448.
MLA Han, Ying-Shan,et al."Development of a fluorescence-based HIV-1 integrase DNA binding assay for identification of novel HIV-1 integrase inhibitors".ANTIVIRAL RESEARCH 98.3(2013):441-448.
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