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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
Author(s) -
Wang Wei,
Guo Zhenpeng,
Chen Yi,
Liu Tao,
Jiang Long
Publication year - 2006
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2006.00454.x
Subject(s) - dendrimer , rna , chemistry , transcription (linguistics) , monolayer , electrophoretic mobility shift assay , quartz crystal microbalance , biophysics , peptide , in vitro , adsorption , transcription factor , microbiology and biotechnology , biochemistry , biology , organic chemistry , philosophy , linguistics , gene
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 () 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 () 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 .