Novel selective inhibitors of ribonuclease H function of the HIV-1 reverse transcriptase enzyme
| Componente | Categoria |
|---|---|
| Arianna Granese | Componenti il gruppo di ricerca / Participants in the research project |
| Simonetta Masieri | Componenti il gruppo di ricerca / Participants in the research project |
| Martina Bortolami | Dottorando/Assegnista/Specializzando componente il gruppo di ricerca / PhD/Assegnista/Specializzando member of the research group |
| Roberto Di Santo | Componenti il gruppo di ricerca / Participants in the research project |
| Luigi Scipione | Componenti il gruppo di ricerca / Participants in the research project |
The primary objective of this project is to develop innovative small-molecules useful as therapeutic tool for the treatment and prevention of HIV/AIDS.
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.
The primary objective will be reached through 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 inhibitos. This is a strong base for rational drug design of specific Rnase H inhibitors.