ABSTRACT
This review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 infection.
Subject(s)
Humans , Drug Resistance, Viral/genetics , HIV Infections/virology , HIV Integrase Inhibitors/pharmacology , HIV Integrase/genetics , HIV-1 , Virus Integration/drug effects , HIV Integrase/drug effects , HIV-1ABSTRACT
This review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 infection.
Subject(s)
Drug Resistance, Viral/genetics , HIV Infections/virology , HIV Integrase Inhibitors/pharmacology , HIV Integrase/genetics , HIV-1/enzymology , Virus Integration/drug effects , HIV Integrase/drug effects , HIV-1/drug effects , HumansABSTRACT
Virtual screening docking-based approach has been employed in order to select novel HIV-1 integrase (IN) potential inhibitors in large databases. Toxicity, metabolism and drug-like properties have been analyzed for the most promising compounds, using computational chemistry techniques. Results were compared and discussed with that obtained for a known HIV-1 (IN) inhibitor reported in the literature.