Influence of generation 2-5 of PAMAM dendrimer on the inhibition of Tat peptide/ TAR RNA binding in HIV-1 transcription.

The special binding of Tat protein to TAR RNA leads to the transcription of HIV-1 virus. In this study, the influence of 2-5 generation of PAMAM dendrimers on the inhibition of Tat protein/TAR RNA binding has been investigated. The absorption of PAMAM dendrimers on TAR RNA, fixed on a gold substrate through an avidin-biotion connection, was carried out by using a quartz crystal microbalance. Experimental result shows a Langmuir-type isotherm could be used to describe this kind of binding, implying a specific and monolayer adsorption existed. The combination coefficient (K(D)(-1))s can be calculated according to Langmuir Equation, having the order of G3 > G4 > G5 >Tat > G2, indicating that PAMAM G3, G4 and G5 having the possibility to be the inhibitors of HIV-1 transcription. The migration time (T(migra)) of capillary electrophoretic technique has the same sequence as (K(D)(-1))s. These two parameters could be used as simple and quantitative criteria for the selection of possible drugs from numerous candidates for HIV therapy in vitro.