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The formation of G-quadruplex in biologically relevant DNA sequences induced by alkaloid

机译:生物碱诱导的生物学相关DNA序列中的G-Quadruplem

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Many Guanine-rich DNA sequences are capable of forming G-quadruplex, such as the telomeric chromosomal terminals and the promoters of several genes including c-myc, c-kit and bcl-2 oncogenes. G-quadruplex structure have conspicuous biological significance and hence the ligands which can promote the formation and stabilize G-quadruplex have attracted much attention. In this paper, we have evaluated the abilities of Jatrorrhizine and Chelerythrine in inducing the formation of G-quadruplex employing Circular Dichroism spectroscopy. Our results indicate that Jatrorrhizine can induce Pu18 and c-kit87up to form mixed-type and parallel G-quadruplex respectively. Chelerythrine can induce Pu18 and c-kit87up to form parallel and antiparallel G-quadruplex respectively. Jatrorrhizine and Chelerythrine can induce the switch of Pu18 G-quadruplex in the presence of K+ from mixed-type to antiparallel and parallel respectively. However, Jatrorrhizine and Chelerythrine can not change the conformation of c-kit87up G-quadruplex in the presence of K+. From experimental results it is clear that Jatrorrhizine and Chelerythrine may have the potential to inhibit the growth of tumour cell and also can be useful guidelines for the design of anticancer agents.
机译:许多富鸟嘌呤-DNA序列能够形成G-四链体,如端粒染色体终端和几种基因包括c-myc和c-kit和BCL-2癌基因的启动子。 G-四结构具有明显的生物学意义,因此它可以促进形成和稳定G-四备受关注的配体。在本文中,我们在诱导采用圆二色谱法G-四联体的形成评估药根碱和白屈菜红的能力。我们的结果表明药根碱可诱导Pu18和c-kit87up以形成混合型和分别平行G-四链体。白屈菜红可以分别诱导Pu18和c-kit87up以形成平行和反平行G-四链体。药根碱和白屈菜红可诱导Pu18 G-四链的开关以K 的存在+ 从混合型反平行并分别平行。然而,药根碱和白屈菜红不能改变的c-kit87up G-四链的构象以K 的+ 的存在。从实验结果很清楚,药根碱和白屈菜红可以具有抑制肿瘤细胞生长的潜力,并且还可以是用于抗癌剂的设计有用的准则。

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