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Slight modification of a G-quadruplex-targeted quinoxaline may boost type-1 photodynamic therapy for triple-negative breast cancer
Sensors and Actuators B: Chemical ( IF 8.0 ) Pub Date : 2024-11-20 , DOI: 10.1016/j.snb.2024.136952
Xiao Zhang, Ming-Hao Hu

G-quadruplexes (G4s) are potential drug targets in cancer treatment. However, the G4-targeted ligands seem to be lack of enough selectivity between tumors and normal tissues, appealing for more precise therapeutic strategies. Type-1 photodynamic therapy (PDT) is a promising strategy possessing excellent spatiotemporal precision for solid tumors with hypoxic microenvironment. However, rational design of type-1 photosensitizers that target G4s are never reported. In this study, we designed a novel G4-targeted ligand (DQ4) by introducing an electron-donating piperazine unit into our previously reported quinoxaline scaffold. Such a slight modification significantly eliminated its intrinsic emission, which made DQ4 a promising “turn-on” fluorescent probe for detecting G4s. Moreover, this modification greatly boosted the production of type-1 ROS, enabling DQ4 to be an excellent photosensitizer potentially for treating hypoxic solid tumors.

中文翻译:


对 G 四链体靶向喹喔啉的轻微修改可能会促进三阴性乳腺癌的 1 型光动力疗法



G-四链体 (G4) 是癌症治疗中的潜在药物靶点。然而,G4 靶向配体在肿瘤和正常组织之间似乎缺乏足够的选择性,需要更精确的治疗策略。1 型光动力疗法 (PDT) 是一种很有前途的策略,对于低氧微环境的实体瘤具有出色的时空精度。然而,从未报道过针对 G4 的 1 型光敏剂的合理设计。在这项研究中,我们通过将电子供体哌嗪单元引入我们之前报道的喹喔啉支架中,设计了一种新的 G4 靶向配体 (DQ4)。如此轻微的修饰显着消除了其内禀发射,这使得 DQ4 成为一种很有前途的用于检测 G4 的“开启”荧光探针。此外,这种修饰极大地促进了 1 型 ROS 的产生,使 DQ4 成为一种可能用于治疗缺氧性实体瘤的优秀光敏剂。
更新日期:2024-11-20
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