Division of Chemistry, Department of Medical Sciences, Faculty of Medicine, University of Miyazaki, 5200 Kihara, Kiyotake, Miyazaki 889-1692, Japan.
Analyst. 2017 Oct 23;142(21):4083-4088. doi: 10.1039/c7an00941k.
In the present study, we developed a multi-functional guanine derivative, G, as a G-quadruplex stabilizer, a fluorescent probe for the detection of G-quadruplex formation, and a F sensor for the observation of the G-quadruplex. We demonstrate that the functional nucleoside bearing a 3,5-bis(trifluoromethyl)benzene group at the 8-position of guanine stabilizes the DNA G-quadruplex structure and fluoresces following the G-quadruplex formation. Furthermore, we show that the functional sensor can be used to directly observe DNA G-quadruplexes by F-NMR in living cells. To our knowledge, this is the first study showing that the nucleoside derivative simultaneously allows for three kinds of functions at a single G-quadruplex DNA. Our results suggest that the multi-functional nucleoside derivative can be broadly used for studying the G-quadruplex structure and serves as a powerful tool for examining the molecular basis of G-quadruplex formation in vitro and in living cells.
在本研究中，我们开发了一种多功能鸟嘌呤衍生物 G，作为 G-四链体稳定剂、用于检测 G-四链体形成的荧光探针以及用于观察 G-四链体的 F 传感器。我们证明，在鸟嘌呤的 8-位带有 3,5-双（三氟甲基）苯基团的功能核苷稳定了 DNA G-四链体结构，并在 G-四链体形成后发出荧光。此外，我们表明，该功能传感器可通过 F-NMR 在活细胞中直接观察 DNA G-四链体。据我们所知，这是第一项表明核苷衍生物可在单个 G-四链体 DNA 上同时实现三种功能的研究。我们的结果表明，多功能核苷衍生物可广泛用于研究 G-四链体结构，并可作为研究 G-四链体体外和活细胞中形成的分子基础的有力工具。
