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特定吖啶低聚物的合成及其与G-四链体的结合特性

Synthesis and g-quadruplex-binding properties of defined acridine oligomers.

作者信息

Ferreira Rubén, Aviñó Anna, Pérez-Tomás Ricardo, Gargallo Raimundo, Eritja Ramon

机构信息

Institute for Research in Biomedicine, IQAC-CSIC, CIBER-BBN Networking Centre on Bioengineering, Biomaterials and Nanomedicine, Edifici Helix, Baldiri Reixac 15, 08028 Barcelona, Spain.

出版信息

J Nucleic Acids. 2010 Jun 13;2010:489060. doi: 10.4061/2010/489060.

DOI:10.4061/2010/489060
PMID:20725626
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2915818/
Abstract

The synthesis of oligomers containing two or three acridine units linked through 2-aminoethylglycine using solid-phase methodology is described. Subsequent studies on cell viability showed that these compounds are not cytotoxic. Binding to several DNA structures was studied by competitive dialysis, which showed a clear affinity for DNA sequences that form G-quadruplexes and parallel triplexes. The fluorescence spectra of acridine oligomers were affected strongly upon binding to DNA. These spectral changes were used to calculate the binding constants (K). Log K were found to be in the order of 4-6.

摘要

描述了使用固相方法合成通过2-氨基乙基甘氨酸连接的含有两个或三个吖啶单元的低聚物。随后对细胞活力的研究表明，这些化合物没有细胞毒性。通过竞争性透析研究了与几种DNA结构的结合，结果表明其对形成G-四链体和平行三链体的DNA序列具有明显的亲和力。吖啶低聚物与DNA结合后，其荧光光谱受到强烈影响。利用这些光谱变化计算结合常数（K）。发现log K约为4-6。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/219db13337c3/JNA2010-489060.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/02c84bb3d216/JNA2010-489060.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/742148effa53/JNA2010-489060.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/c60592c9ece7/JNA2010-489060.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/219db13337c3/JNA2010-489060.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/02c84bb3d216/JNA2010-489060.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/742148effa53/JNA2010-489060.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/c60592c9ece7/JNA2010-489060.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e2/2915818/219db13337c3/JNA2010-489060.004.jpg

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