Perspectives on Developing Small Molecule Inhibitors Targeting HIV-1 Integrase

J.      J. Tan; C.      Liu; X.      H. Sun; X.      J. Cong; L.      M. Hu; C.      X. Wang; X.      J. Liang

Abstract

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