Designing HIV integrase inhibitors--shooting the last arrow.
The arsenal of drugs in the fight against AIDS is rapidly diminishing as the HIV becomes resistant to the available reverse transcriptase and protease inhibitors. After killing millions all over the world, the virus is still on the rampage and hence the pharmaceutical industry is resorting to the development of inhibitors of integrase. This seems to be the last arrow in the quiver of potential drug leads to combat the deadly infection. Several classes of HIV integrase inhibitors have been reported to date; however, none is clinically useful. This review details the existing knowledge of the biological functions of the HIV-1 integrase with the focus on its available inhibitors, their disadvantages, and the current trends in designing novel compounds as anti-integrase.
Makhija
Mahindra T
MT
West Australian Biomedical Research Institute, School of Biomedical Sciences, Curtin University of Technology, Kent Street, Bentley, WA 6102, Australia. mahindra.makhija@altanapharma.in
D020650:Combinatorial Chemistry Techniques; D016208:Databases, Factual; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D019427:HIV Integrase / Q000737:chemistry* / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011487:Protein Conformation; D017434:Protein Structure, Tertiary
D019428:HIV Integrase Inhibitors; D019427:HIV Integrase