Innovative small molecules as inhibitors of ribonuclease H function of the HIV-1 reverse transcriptase enzyme
The goal of project is the development of compounds with selective inhibiting activity against RNase H domain of HIV-1 RT enzyme.
This group has already identified: i) a class of diketo acids that inhibits both HIV-1 RNase H and IN activities; ii) compounds binding to a novel RT site that are able to selectively inhibit RT-associated RNase H, iii) amino acid residues within the catalytic core of RNase H interacting with the inhibitors. This is a strong base for rational drug design of specific Rnase H inhibitors.The innovative aspect of this strategy is that targeted activity is the relatively unexplored reverse transcriptase (RT)-associated ribonuclease H (RNase H) function, which selectively degrades the RNA of the RNA-DNA hybrid produced by the retrotranscription
process.