Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), and Departamento de Química Orgánica, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
Angew Chem Int Ed Engl. 2016 Dec 12;55(50):15615-15618. doi: 10.1002/anie.201607965. Epub 2016 Nov 17.
Guanine quadruplexes (GQs) are compact four-stranded DNA structures that play a key role in the control of a variety of biological processes, including gene transcription. Bulky ruthenium complexes featuring a bipyridine, a terpyridine, and one exchangeable ligand ([Ru(terpy)(bpy)X] ) are able to metalate exposed guanines present in the GQ of the c-MYC promoter region that are not involved in quadruplex base pairing. qRT-PCR and western-blot experiments indicated that the complexes promote a remarkable increase in the expression of this oncogene. We also show that exchangeable thioether ligands (X=RSR', Met) allow regulation of the metalating activity of the complex with visible light.
鸟嘌呤四链体（GQs）是一种紧凑的四链 DNA 结构，在多种生物过程的控制中发挥着关键作用，包括基因转录。具有联吡啶、三吡啶和一个可交换配体([Ru(terpy)(bpy)X])的大体积钌配合物能够使 c-MYC 启动子区域 GQ 中不参与四链碱基配对的暴露鸟嘌呤金属化。qRT-PCR 和 western-blot 实验表明，这些配合物显著促进了这种致癌基因的表达。我们还表明，可交换的硫醚配体（X=RSR'，Met）允许用可见光调节配合物的金属化活性。
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