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Control of HIV Through the Inhibition of HIV-1 Integrase: A Medicinal Chemistry Perspective

[ Vol. 3 , Issue. 2 ]


C. P. Gordon, R. Griffith and P. A. Keller   Pages 199 - 220 ( 22 )


This article reviews the current status of classes of HIV-1 integrase enzyme inhibitors. These classes include peptide-based inhibitors, natural products, polyhydroxylated aromatics, diketo acids, naphthyridines, and sulfonated compounds including sulfonic acids. Discussions of structure activity relationships are presented and include the current overview of the structure-based model, suitable for the further design and development. To date, the advances in the medicinal chemistry of HIV-1 integrase inhibitors have relied mostly on ligand-based designs leading to most displaying similar binding interactions within the active site or at the dimer interface. This paves the way for single enzyme mutations rendering entire compound classes inactive and thus, the requirement for second and third generation inhibitors with novel modes of binding is apparent. To facilitate future structure-based drug design efforts, a model of the biologically relevant structure of the HIV-1 integrase enzyme, a dimer of dimers has also been discussed.


HIV-1 Integrase, Inhibitor, Inhibitor classes, Structure-activity relationship


Department of Chemistry,University of Wollongong, Wollongong, NSW 2522, Australia.

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