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A Pseudocatenane Structure Formed Between Dna And A Cyclic Bisintercalator

机译:Dna与环状双嵌入剂之间形成的伪联烷结构

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Targeting double-stranded DNA with small molecules remains an active area of basic research. Herein is described a cyclic DNA bisintercalator that is based on two naphthalene diimide (NDI) intercalating units tethered by one linking element specific for binding in the minor groove and the other linking element specific for binding in the major groove. DNase I footprinting revealed a strong preference for binding the sequence 5'-GGTACC-3'. NMR structural studies of the complex with d(CGGTACCG)_2 verified a pseudocatenane structure in which the NDI units reside four base pairs apart, with one linker segment located in the minor groove and the other in the major groove consistent with the linker designs. To the best of our knowledge, this is the first structurally well-characterized pseudocatenane complex between a sequence specific cyclic bisintercalator and intact DNA.
机译:用小分子靶向双链DNA仍然是基础研究的活跃领域。本文描述了一种环状DNA双嵌入剂,其基于两个萘二酰亚胺(NDI)嵌入单元,该嵌入单元由一个特定于在小沟中结合的连接元件和另一个特定于在主沟中结合的连接元件所束缚。 DNase I足迹显示出强烈倾向于结合序列5'-GGTACC-3'。带有d(CGGTACCG)_2的配合物的NMR结构研究证实了伪联烷结构,其中NDI单元相距4个碱基对,其中一个连接片段位于次要凹槽中,另一个位于主要凹槽中,与该连接物的设计一致。据我们所知,这是序列特异性环状双嵌入剂与完整DNA之间的第一个结构良好表征的假联烷复合物。

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