Strategies for identification of HIV-1 integrase inhibitors

被引:4
作者
Ramcharan, Joseph [1 ]
Skalka, Anna Marie [1 ]
机构
[1] Fox Chase Canc Ctr, Inst Canc Res, Philadelphia, PA 19111 USA
关键词
antiretroviral therapy; concerted integration; diketo acids; high-throughput screening; host protein targets; integrase tetramer models; joining reaction; preintegration complex; processing reaction; Tn5 surrogate target;
D O I
10.2217/17460794.1.6.717
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
HIV-1 integrase, which catalyzes the joining of viral DNA to the host cell DNA, has attracted considerable attention as a target for the design and screening of novel anti-HIV drugs as it is essential for virus replication and the establishment of persistent infection. Progress in the identification of different classes of compounds that block integrase activity has been summarized recently in several excellent reviews. Here, we present a brief overview of integrase inhibition, highlighting some of the unusual properties of this protein and important considerations in searching for potential new inhibitors and their evaluation.
引用
收藏
页码:717 / 731
页数:15
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