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GC选择性配体光辉霉素会改变其结合位点侧翼(AT)n序列的结构。

The GC-selective ligand mithramycin alters the structure of (AT)n sequences flanking its binding sites.

作者信息

Cons B M, Fox K R

机构信息

Dept. Physiology & Pharmacology, University of Southampton, UK.

出版信息

FEBS Lett. 1990 May 7;264(1):100-4. doi: 10.1016/0014-5793(90)80775-e.

DOI:10.1016/0014-5793(90)80775-e
PMID:2140099
Abstract

DNA fragments containing (AT)n inserts cloned adjacent to putative mithramycin binding sites have been examined by footprinting experiments using a variety of nucleases in the presence of the drug. The results demonstrate that mithramycin induces a DNA structural change which renders adjacent (AT)n sequences sensitive to attack by DNase II. Significant changes are also revealed with DNase I and micrococcal nuclease. The results are consistent with a model in which mithramycin opens the DNA minor groove changing it to a structure which is locally more like A-DNA.

摘要

通过在药物存在的情况下使用多种核酸酶进行足迹实验,对含有克隆于假定光神霉素结合位点附近的(AT)n插入片段的DNA片段进行了检测。结果表明,光神霉素诱导了一种DNA结构变化,使相邻的(AT)n序列对DNase II的攻击敏感。DNase I和微球菌核酸酶也显示出显著变化。这些结果与一个模型一致,即光神霉素打开DNA小沟,将其改变为局部更类似于A-DNA的结构。

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FEBS Lett. 1990 May 7;264(1):100-4. doi: 10.1016/0014-5793(90)80775-e.
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光神霉素通过与Fe(II)螯合形成稳定的二聚体复合物:与DNA相互作用的特性、细胞渗透和细胞毒性。
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