HIV-1 integrase (IN) is a crucial enzyme in the life cycle of HIV-1 and also a validated target for developing
anti-HIV inhibitors. Recent progress in drug design has significantly accelerated the development of anti-AIDS IN
inhibitors. A large amount of novel inhibitors that interact specifically with IN were developed along with the expanding
and application of methods to drug design. This article reviewed the anti-HIV IN inhibitors discovered by the rational
drug design approaches in the recent 5-year.
Keywords: de novo drug design, HIV, integrase inhibitors, ligand-based drug design, pharmacophore, receptor-based drug
design, virtual screening, Genetic Algorithms, DOCK
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