DNA aptamers as potential anti-HIV agents

被引:64
作者
Chou, SH [1 ]
Chin, KH
Wang, AHJ
机构
[1] Natl Chung Hsing Univ, Inst Biochem, Taichung 40227, Taiwan
[2] Acad Sinica, Inst Biol Chem, Nankang, Taiwan
关键词
D O I
10.1016/j.tibs.2005.03.004
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Guanine (G)-rich DNA sequences can adopt stable G-quadruplex structures by G-tetrad hydrogen-bonding and hydrophobic stacking. Recently, it has been shown that a DNA sequence forms an aptamer (termed 93del) and adopts a novel dimeric quadruplex folding topology in K+ solution. This aptamer exhibits anti-HIV1 integrase activity in the nanomolar range in vitro. A docking-based model of the 93del-integrase complex positions the DNA aptamer within a channel of the tetrameric integrase. This mutual fitting blocks several catalytic amino acid residues that are essential for integrase function, and accounts for the anti-HIV1 activity of the 93del aptamer.
引用
收藏
页码:231 / 234
页数:4
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