Exclusive platination of loop adenines in the human telomeric G-quadruplex
Exclusive platination of loop adenines in the human telomeric G-quadruplex
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DOI：
10.1039/b904599f
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发表时间：
2009-01-01
影响因子：
3.2
通讯作者：
Teulade-Fichou, Marie-Paule
中科院分区：
文献类型：
--
作者：
Bertrand, Helene;Bombard, Sophie;Teulade-Fichou, Marie-Paule
本文报道了三种铂三联吡啶配合物对人端粒G-四链体的铂化作用。它示出的三联吡啶部分周围的铂原子的芳香族表面的延伸影响的结合亲和力和铂化活性。值得注意的是，最强烈的结合复杂的Pt-ttpy坐标专门的腺嘌呤核碱基存在于环的G-四链体。这种独特的单位点铂化反应了化合物与G-四联体和环残基的相互作用。此外，在使用目前临床使用的顺铂衍生物的平行研究中，Pt-ttpy在一组癌细胞系上显示出有希望的抗增殖活性。
The present article reports on the platination of the human telomeric G-quadruplex by three Pt-terpyridine complexes. It is shown that extension of the aromatic surface of the terpyridine moiety surrounding the platinum atom influences both the binding affinity and the platination activity. Remarkably, the most strongly bound complex Pt-ttpy coordinates exclusively the adenine nucleobases present in the loop of the G-quadruplex. This exclusive single-site platination reflects the interaction of the compound with both the G-tetrad and the loop residues. In addition Pt-ttpy showed promising antiproliferative activity on a panel of cancer cell lines in a parallel study using cisplatin derivatives currently in clinical use.