一种钌铂金属配合物，能与 Sarcin-Ricin 环 RNA 结合并降低 mRNA 表达。
A ruthenium-platinum metal complex that binds to sarcin ricin loop RNA and lowers mRNA expression.
机构信息
Department of Chemistry, Bard College, 30 Campus Road, Annandale-on-Hudson, New York 12504, USA.
出版信息
Chem Commun (Camb). 2018 Aug 21;54(65):8987-8990. doi: 10.1039/c8cc02131g. Epub 2018 Jun 28.
IT127 is a dinuclear transition metal complex that contains a Pt(ii) and a Ru(iii) metal center. We have shown that IT127 is significantly more effective in binding the 29-base sarcin ricin loop (SRL) RNA in comparison to Cisplatin, a hallmark anticancer agent. Binding site analysis shows that IT127 prefers purine bases and the GAGA tetraloop region of SRL RNA. Our results with a dihydrofolate reductase (DHFR) model system reveal that IT127 binding to mRNA reduces translation of DHFR enzyme and that the Ru(iii) and Pt(ii) centers in IT127 appear to work in a synergistic manner.
IT127 是一个双核过渡金属配合物，包含一个 Pt(ii) 和一个 Ru(iii) 金属中心。我们已经表明，与标志性的抗癌药物顺铂相比，IT127 更有效地结合 29 个碱基的 Sarcin Ricin 环（SRL）RNA。结合位点分析表明，IT127 更喜欢嘌呤碱基和 SRL RNA 的 GAGA 四链环区域。我们在二氢叶酸还原酶（DHFR）模型系统中的研究结果表明，IT127 与 mRNA 的结合降低了 DHFR 酶的翻译，并且 IT127 中的 Ru(iii) 和 Pt(ii) 中心似乎以协同方式发挥作用。
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