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首页> 外文期刊>Chemistry: A European journal >Synthesis, Structural Characterisation and Quadruplex DNA Binding Studies of a New GoldACHTUNGTRENUNG(III) Pyrazolylpyridine Complex
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Synthesis, Structural Characterisation and Quadruplex DNA Binding Studies of a New GoldACHTUNGTRENUNG(III) Pyrazolylpyridine Complex

机译：新型金ACHTUNGTRENUNG（III）吡唑基吡啶复合物的合成，结构表征和四链体DNA结合研究

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摘要

Guanine-rich sequences of DNA can assemble into quadruply stranded structures known as quadruplexes.[1] These structures arise thanks to the formation of guanine tetrads through hydrogen-bonding interactions between the Watson–Crick edge of one guanine and the Hoogsteen edge of its neighbour.[2] Quadruplex DNA structures have attracted recent interest since they have been identified as potential anticancer drug targets.[3] Bioinformatic studies have identified over 350 000 sequences in the human genome with the potential to form quadruplex structures.[4] Many of these sequences are found in the promoter regions of genes and hence it has been proposed that they might play important roles in regulating gene expression, for example, of certain oncogenes such as c-myc and c-kit.[5] On the other hand, formation of quadruplex DNA structures in the human telomere (HTelo) has been shown to inhibit telomerase.[6] The latter is an enzyme over-expressed in approximately 85% of cancer cells and plays an important role in cancer cell immortalisation.[ 6a,b] Therefore, molecules that template the formation or stabilise the structure of quadruplex DNA could pave the way for the development of new anticancer drugs.[3] While the majority of quadruplex DNA binders reported to date are based on planar organic heteroaromatic systems,[7] recently, several metal complexes have been shown to be excellent quadruplex DNA binders.[8] Herein we report the synthesis, structural characterisation and DNA binding studies of a new goldACHTUNGTRENUNG(III) complex. This is the first example of a quadruplex DNA binder based on a gold complex.
机译：富含鸟嘌呤的DNA序列可以组装成四链结构，称为四链体。[1]这些结构的产生归因于一个鸟嘌呤的沃森-克里克边缘与其邻域的Hoogsteen边缘之间通过氢键相互作用形成的鸟嘌呤四联体。[2]自从四链DNA结构被确定为潜在的抗癌药物靶标以来，它们就引起了人们的关注。[3]生物信息学研究已经鉴定出人类基因组中超过35万个序列，具有形成四链体结构的潜力。[4]这些序列中有许多是在基因的启动子区域发现的，因此有人提出它们可能在调节基因表达中起重要作用，例如某些癌基因，例如c-myc和c-kit。[5]另一方面，已证明在人端粒（HTelo）中形成四链DNA结构可抑制端粒酶。[6]后者是一种酶，在大约85％的癌细胞中过表达，并且在癌细胞永生化中起着重要作用。[6a，b]因此，以模板为模板或稳定四链DNA的结构的分子可以为开发新的抗癌药物。[3]尽管迄今为止报道的大多数四链体DNA结合物都是基于平面有机杂芳族体系，[7]最近，几种金属配合物已被证明是出色的四链体DNA结合物。[8]在这里，我们报告了新的金ACHTUNGTRENUNG（III）配合物的合成，结构表征和DNA结合研究。这是基于金络合物的四链DNA结合物的第一个例子。

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