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
Corresponding AuthorWainberg, MA (reprint author), McGill Univ, Jewish Gen Hosp, AIDS Ctr, Lady Davis Med Res, Montreal, PQ H3T 1E2, Canada. ; mark.wainberg@mcgill.ca
2013-06-01
Source PublicationANTIVIRAL RESEARCH
ISSN0166-3542
Volume98Issue:3Pages:441-448
AbstractHuman 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.
KeywordHiv-1 Integrase Inhibitors Integrase Dna Binding Fluorescent Assay
Subject AreaPharmacology & Pharmacy ; Virology
DOI10.1016/j.antiviral.2013.04.001
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy ; Virology
WOS SubjectPharmacology & Pharmacy ; Virology
WOS IDWOS:000320296400012
Citation statistics
Cited Times:7[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/16587
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.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
GB/T 7714
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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