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.
Wang
Wei
W
Center for Molecular Science, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100080, China.
Guo
Zhenpeng
Z
Chen
Yi
Y
Liu
Tao
T
Jiang
Long
L
D000595:Amino Acid Sequence; D019380:Anti-HIV Agents / Q000494:pharmacology*; D050091:Dendrimers; D019075:Electrophoresis, Capillary; D015696:Gene Products, tat / Q000037:antagonists & inhibitors*; D016325:HIV Long Terminal Repeat / Q000187:drug effects*; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D008969:Molecular Sequence Data; D011073:Polyamines / Q000494:pharmacology*; D012367:RNA, Viral / Q000037:antagonists & inhibitors; D014158:Transcription, Genetic / Q000187:drug effects; D054322:tat Gene Products, Human Immunodeficiency Virus
D019380:Anti-HIV Agents; D050091:Dendrimers; D015696:Gene Products, tat; C104700:PAMAM Starburst; D011073:Polyamines; D012367:RNA, Viral; D054322:tat Gene Products, Human Immunodeficiency Virus