Kinamycin-mediated DNA cleavage under biomimetic conditions

Kinamycin-mediated DNA cleavage under biomimetic conditions
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DOI:
10.1016/j.tetlet.2008.03.019
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发表时间:
2008-05-05
影响因子:
1.8
通讯作者:
Melander, Christian
Melander, Christian
中科院分区:
化学4区
文献类型:
--
作者:
Ballard, T. Eric;Melander, Christian

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运动霉素是具有生物活性的次级代谢产物,其特征在于不常见的重氮苯并[b]芴骨架。 Kinamycin D 已被证明可以在温和的仿生条件下有效切割 DNA。使用浓度为 570 μM 的内源丰富还原剂谷胱甘肽、运动霉素 D 可以以浓度、温度和时间依赖性方式有效切割 DNA。二硫苏糖醇在低浓度下也被证明是有效的,而其他还原剂未能诱导 DNA 裂解。描述了 DNA 切割结果的机械后果。 (C) 2008 Elsevier Ltd. 保留所有权利。
The kinamycins are biologically active secondary metabolites characterized by an uncommon diazobenzo[b]fluorene skeleton. Kinamycin D has been shown to potently cleave DNA under mild biomimetic conditions. Use of the endogenously abundant reductant glutathione at 570 mu M, kinamycin D effectively cleaved DNA in a concentration, temperature, and time-dependent fashion. Dithiothreitol also proved effective at low concentration while other reductants failed to induce DNA cleavage. Mechanistic consequences of the DNA cleavage results are described. (C) 2008 Elsevier Ltd. All rights reserved.