High-throughput screening using pseudotyped lentiviral particles: A strategy for the identification of HIV-1 inhibitors in a cell-based assay

doi:10.1016/j.antiviral.2008.12.004

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 国家新药筛选中心

	High-throughput screening using pseudotyped lentiviral particles: A strategy for the identification of HIV-1 inhibitors in a cell-based assay
	Garcia, Jean-Michel 1; Gao, Anhui 4; He, Pei-Lan 4; Choi, Joyce 1; Tang, Wei4 ; Bruzzone, Roberto 1; Schwartz, Olivier 3; Naya, Hugo 2; Nan, Fa Jun 4; Li, Jia4
刊名	ANTIVIRAL RESEARCH
	2009-03
卷号	81 期号:3 页码:239-247
关键词	HIV Pseudotyped lentiviral particles High-throughput screening HTS Cocktail library NNRTI
ISSN号	0166-3542
DOI	10.1016/j.antiviral.2008.12.004
文献子类	Article
英文摘要	Two decades after its discovery the human immunodeficiency virus (HIV) is still spreading worldwide and killing millions. There are 25 drugs formally approved for HIV currently on the market, but side effects as well as the emergence of HIV strains showing single or multiple resistances to current drug-therapy are causes for concern. Furthermore, these drugs target only 4 steps of the viral cycle, hence the urgent need for new drugs and also new targets. In order to tackle this problem, we have devised a cell-based assay using lentiviral particles to look for post-entry inhibitors of HIV-1. We report here the assay development, validation as well as confirmation of the hits using both wild-type and drug-resistant HIV-1 viruses. The screening was performed on an original library, rich in natural compounds and pure molecules from Traditional Chinese Medicine pharmacopoeia, which had never been screened for anti-HIV activity. The identified hits belong to four chemical sub-families that appear to be all non-nucleoside reverse transcriptase inhibitors (NNRTIs). Secondary tests with live viruses showed that there was good agreement with pseudotyped particles, confirming the validity of this approach for high-throughput drug screens. This assay will be a useful tool that can be easily adapted to screen for inhibitors of viral entry. (c) 2008 Elsevier B.V. All rights reserved.
资助项目	HKU[00000000] ; Li Ka Shing Foundation[00000000] ; Institut Pasteur[00000000] ; ANRS[00000000] ; Sidaction[00000000] ; EU[00000000]
WOS关键词	IMMUNODEFICIENCY-VIRUS TYPE-1 ; REVERSE-TRANSCRIPTASE ; RETROVIRAL VECTORS ; ENTRY INHIBITORS ; AIDS RESEARCH ; INFECTION ; REPLICATION ; NUCLEAR ; RESISTANCE ; INTEGRASE
WOS研究方向	Pharmacology & Pharmacy ; Virology
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000264278400007
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279297]
专题	国家新药筛选中心药理学第一研究室药物安全性评价中心
通讯作者	Garcia, Jean-Michel
作者单位	1.Univ Hong Kong, Pasteur Res Ctr Ltd, Dexter HC Man Bldg,8 Sassoon Rd, Hong Kong, Hong Kong, Peoples R China; 2.Inst Pasteur Montevideo, Montevideo, Uruguay 3.Inst Pasteur, Virus & Immun Unit, Paris, France; 4.Shanghai Inst Mat Med, Shanghai, Peoples R China;
推荐引用方式 GB/T 7714	Garcia, Jean-Michel,Gao, Anhui,He, Pei-Lan,et al. High-throughput screening using pseudotyped lentiviral particles: A strategy for the identification of HIV-1 inhibitors in a cell-based assay[J]. ANTIVIRAL RESEARCH,2009,81(3):239-247.
APA	Garcia, Jean-Michel.,Gao, Anhui.,He, Pei-Lan.,Choi, Joyce.,Tang, Wei.,...&Zuo, Jian-Ping.(2009).High-throughput screening using pseudotyped lentiviral particles: A strategy for the identification of HIV-1 inhibitors in a cell-based assay.ANTIVIRAL RESEARCH,81(3),239-247.
MLA	Garcia, Jean-Michel,et al."High-throughput screening using pseudotyped lentiviral particles: A strategy for the identification of HIV-1 inhibitors in a cell-based assay".ANTIVIRAL RESEARCH 81.3(2009):239-247.