Abstract |
Three integrase (IN) inhibitors have been approved by FDA for clinical treatment of Human Immunodeficiency Virus ( HIV) infection. This stimulates more researchers to focus their studies on this target for anti-HIV drug development. Three steps regarding of IN activity have been validated for inhibitor discovery: strand transfer, 3'-terminal processing, and IN- lens epithelium-derived growth factor ( LEDGF)/p75 interaction. Among them, IN- LEDGF/p75 interaction is a new target validated in recent years. Emergence of drug-resistant virus strains makes this target appealing to pharmacologists. Compared with the traditional screening methods such as AlphaScreen and cell-based screening developed for IN inhibitor discovery, virtual screening is a powerful technique in modern drug discovery. Here we summarized the recent advances of virtual-screening targeting IN-LEDFG/p75 interaction. The combined application of virtual screening and experiments in drug discovery against IN-LEDFG/p75 interaction sheds light on anti-HIV research and drug discovery.
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Authors | Wan-Gang Gu, Bai-Nan Liu, Jun-Fa Yuan |
Journal | Journal of drug targeting
(J Drug Target)
Vol. 23
Issue 2
Pg. 134-9
(Feb 2015)
ISSN: 1029-2330 [Electronic] England |
PMID | 25230778
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
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Chemical References |
- HIV Integrase Inhibitors
- Intercellular Signaling Peptides and Proteins
- Ligands
- lens epithelium-derived growth factor
- HIV Integrase
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Topics |
- Computational Biology
- Drug Discovery
(methods)
- HIV Integrase
(chemistry, metabolism)
- HIV Integrase Inhibitors
(pharmacology)
- HIV-1
(drug effects, enzymology)
- High-Throughput Screening Assays
- Humans
- Intercellular Signaling Peptides and Proteins
(chemistry, metabolism)
- Ligands
- Protein Binding
- Protein Conformation
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