G-quadruplex has been an emerging target for drug design due to its physiologically important roles in oncology. A number of quadruplex-interactive ligands have been developed by synthetic and medicinal chemists over the past decades. However, the great challenge still remains that the method for detecting the specific targeting of these ligands to the G-quadruplex structures in cells is still lacking. Herein, a detection system for directly identifying the specific targeting of a ligand to DNA G-quadruplexes in cells was constructed by using a small-molecular fluorescent probe (IMT) as a fluorescent indicator. Four typical ligands have been successfully evaluated, demonstrating the promising application of this detection system in the screening and evaluation of quadruplex-specific therapeutic agents.

中文翻译：

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用小分子荧光探针评估活细胞中 G-四链体配体的选择性

由于 G-四链体在肿瘤学中的重要生理作用，它已成为药物设计的新兴靶点。在过去的几十年中，合成和药物化学家开发了许多四链体相互作用配体。然而，仍然缺乏检测这些配体特异性靶向细胞中 G-四链体结构的方法的巨大挑战。在此，以小分子荧光探针（IMT）为荧光指示剂，构建了一种直接识别配体特异性靶向细胞内DNA G-四链体的检测系统。已成功评估了四种典型配体，证明了该检测系统在筛选和评估四联体特异性治疗剂中的有前景的应用。