Bisaryldiketene derivatives: A new class of selective ligands for c-myc G-quadruplex DNA
Bisaryldiketene derivatives: A new class of selective ligands for c-myc G-quadruplex DNA
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双芳基双烯酮衍生物：c-myc G-四链体 DNA 的新型选择性配体
DOI：
10.1016/j.bmc.2010.10.021
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发表时间：
2010-12-01
影响因子：
3.5
通讯作者：
Huang, Zhi-Shu
中科院分区：
文献类型：
--
作者：
Peng, Dan;Tan, Jia-Heng;Huang, Zhi-Shu
设计合成了一系列双芳基二烯酮衍生物，作为一类新型的g -四复体配体。通过FRET， ITC和PCR停止试验进一步评估配体与四重体的相互作用。与迄今为止报道的大多数g -四重体配体不同，这些化合物既不是多环也不是大环，而是在两个喹啉基团之间有一个非芳香族的相对灵活的连接体，从而使化合物的构象具有灵活性。我们的研究结果表明，这些双芳基二烯衍生物可以选择性地识别g -四重体DNA，而不是与双双体DNA结合。此外，它们还显示出不同g -四重体DNA之间有希望的区别。配体M2对c-myc g -四重体DNA的初级结合亲和力是端粒g -四重体DNA的200倍以上。(C) 2010 Elsevier Ltd.版权所有。
A series of bisaryldiketene derivatives were designed and synthesized as a new class of specific G-quadruplex ligands. The ligand-quadruplex interactions were further evaluated by FRET, ITC, and PCR stop assay. In contrast to most of the G-quadruplex ligands reported so far, which comprise an extended aromatic ring, these compounds are neither polycyclic nor macrocyclic, but have a non-aromatic and relative flexible linker between two quinoline moieties enabling the conformation of compounds to be flexible. Our results showed that these bisaryldiketene derivatives could selectively recognize G-quadruplex DNA rather than binding to duplex DNA. Moreover, they showed promising discrimination between different G-quadruplex DNA. The primary binding affinity of ligand M2 for c-myc G-quadruplex DNA was over 200 times larger than that for telomere G-quadruplex DNA. (C) 2010 Elsevier Ltd. All rights reserved.