Studies on the binding affinity of aminoglycoside antibiotics to the HIV-1 Rev Responsive Element for designing potential antiviral agents

The Rev binding to Rev Responsive Element (RRE) of HIV-1 mRNA plays an important role in the HIV-1 viral replication cycle. The disruption of the Rev-RRE interaction has been studied extensively in order to develop a potential antiviral drug. In order to provide the basis for a more promising approach to develop a Rev-RRE binding inhibitor against HIV-1 infection, it is necessary to understand the binding modes of the aminoglycoside antibiotics to RRE. In the present study, the binding mode of a modified antibiotic, a neamine conjugated with pyrene and arginine (NCPA), to RRE has been studied by the methods of T_m measurement and spectroscopic analysis of RRE with or without antibiotics. The results confirmed that NCPA competes with Rev in binding to RRE.