School of Pharmaceutical Sciences, Sun Yat-sen University, 132 Waihuan East Road, Guangzhou University City, Guangzhou 510006, China.
Int J Mol Sci. 2022 Mar 31;23(7):3872. doi: 10.3390/ijms23073872.
I-motifs play key regulatory roles in biological processes, holding great potential as attractive therapeutic targets. In the present study, we developed a novel fluorescent probe with strong and selective binding to the gene promoter i-motif. had an i-motif-binding carbazole moiety conjugated with naphthalimide fluorescent groups. could differentiate the i-motif from other DNA structures through selective activation of its fluorescence, with its apparent visualization in solution. The smart probe showed excellent sensitivity, with a low fluorescent detection limit of 154 nM and effective stabilization to the i-motif. could serve as a rapid and sensitive probe for label-free screening of selective i-motif binding ligands under neutral crowding conditions. To the best of our knowledge, is the first fluorescent probe with high sensitivity for recognizing the i-motif structure and screening for selective binding ligands.
I 型结构在生物过程中发挥着关键的调控作用,具有成为有吸引力的治疗靶点的巨大潜力。在本研究中,我们开发了一种新型荧光探针 ,它能与 基因启动子的 I 型结构强烈且选择性地结合。 具有与萘酰亚胺荧光基团共轭的 I 型结构结合咔唑部分。 通过选择性激活其荧光, 可以将 I 型结构与其他 DNA 结构区分开来,在溶液中可以明显观察到。智能探针 表现出优异的灵敏度,荧光检测限低至 154 nM,并且可以有效地稳定 I 型结构。 可以作为一种快速灵敏的探针,用于在中性拥挤条件下无标记筛选选择性 I 型结构结合配体。据我们所知, 是第一个用于识别 I 型结构并筛选选择性结合配体的高灵敏度荧光探针。