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Influence of Generation 2-5 of PAMAM Dendrimer on the Inhibition of Tat peptide/ TAR RNA Binding in HIV-1 Transcription

Influence of Generation 2-5 of PAMAM Dendrimer on the Inhibition of Tat peptide/ TAR RNA Binding in HIV-1 Transcription

Wei Wang, Zhenpeng Guo, Yi Chen, Tao Liu, Long Jiang

Chem Biol Drug Des. 2006 Dec;68(6):314-8.

PMID: 17177893

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP173612607	Thiophosphoryl-PMMH-12 dendrimer, generation 2.5		173612-60-7	Price

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