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新型氨基糖苷-蒽醌化合物双重识别端粒 G-四链体。

Dual recognition of the human telomeric G-quadruplex by a neomycin-anthraquinone conjugate.

机构信息

Laboratory of Bioorganic and Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, USA.

出版信息

Chem Commun (Camb). 2013 Jun 28;49(51):5796-8. doi: 10.1039/c3cc42721h.

DOI:10.1039/c3cc42721h
PMID:23698792
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3977216/
Abstract

The authors report the recognition of a G-quadruplex formed by four repeat human telomeric DNA with aminosugar intercalator conjugates. The recognition of the G-quadruplex through dual binding mode ligands significantly increased the affinity of ligands for the G-quadruplex. One such example is a neomycin-anthraquinone conjugate (2) which exhibited nanomolar affinity for the quadruplex, and the affinity of (2) is nearly 1000 fold higher for the human telomeric G-quadruplex DNA than its constituent units, neomycin and anthraquinone.

摘要

作者报告了一种由四个重复的人类端粒 DNA 与氨基糖插合剂缀合物形成的 G-四链体的识别。通过双重结合模式配体识别 G-四链体,显著增加了配体对 G-四链体的亲和力。一个这样的例子是新霉素-蒽醌缀合物(2),它对四链体表现出纳摩尔亲和力,并且(2)对人端粒 G-四链体 DNA 的亲和力比其组成单元新霉素和蒽醌高近 1000 倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c970/3977216/e03a679eb3f0/nihms483749f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c970/3977216/aefb83a45c8e/nihms483749f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c970/3977216/e1b568c1a774/nihms483749f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c970/3977216/e03a679eb3f0/nihms483749f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c970/3977216/aefb83a45c8e/nihms483749f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c970/3977216/e1b568c1a774/nihms483749f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c970/3977216/e03a679eb3f0/nihms483749f3.jpg

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