Chou Shan-Ho, Chin Ko-Hsin, Wang Andrew H-J
Institute of Biochemistry, National Chung-Hsing University, Taichung, Taiwan, Republic of China.
Trends Biochem Sci. 2005 May;30(5):231-4. doi: 10.1016/j.tibs.2005.03.004.
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.
富含鸟嘌呤（G）的DNA序列可通过G-四联体氢键和疏水堆积形成稳定的G-四链体结构。最近研究表明，一个DNA序列形成了一种适体（称为93del），并在钾离子溶液中采用了一种新型的二聚体四链体折叠拓扑结构。这种适体在体外纳摩尔浓度范围内表现出抗HIV-1整合酶活性。基于对接的93del-整合酶复合物模型将DNA适体定位在四聚体整合酶的一个通道内。这种相互契合阻断了整合酶功能所必需的几个催化氨基酸残基，这就解释了93del适体的抗HIV-1活性。
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