State Key Laboratory of Digital Medical Engineering, School of Biological Science and Medical Engineering, Southeast University, Nanjing 211189, China.
School of Chemistry and Chemical Engineering, Yangzhou University, Yangzhou 225002, China.
J Am Chem Soc. 2024 Sep 18;146(37):25462-25466. doi: 10.1021/jacs.4c10606. Epub 2024 Sep 6.
Near-infrared (NIR) aggregation-induced emission luminogens (AIEgens) are excellent probes for tumor imaging, but there still is space to improve their imaging specificity and sensitivity. In this work, a strategy of tandem targeting and dual aggregation of an AIEgen is proposed to achieve these two purposes. An AIEgen, β-tBu-Ala-Cys(StBu)-Lys(Biotin)-Pra(QMT)-CBT (), is designed to tandem target the biotin receptor and leucine aminopeptidase of a cancer cell and thereafter undergo CBT-Cys click reaction-mediated dual aggregations in the cell. Experimental results show that renders 4.8-fold and 7.9-fold higher NIR fluorescence signals over those in the "biotin + LAP inhibitor"-treated control groups in living HepG2 cells and HepG2 tumor-bearing mice, respectively. We anticipate that , which has the tandem targeting and dual aggregation property to simultaneously achieve enhanced tumor enrichment and fluorescence onset, could be applied for accurate cancer diagnosis in the clinic in the future.
近红外（NIR）聚集诱导发射发光体（AIEgens）是肿瘤成像的优秀探针，但仍有空间提高其成像特异性和灵敏度。在这项工作中，提出了一种串联靶向和双重聚集 AIEgen 的策略，以实现这两个目的。设计了一种 AIEgen，β-tBu-Ala-Cys（StBu）-Lys（生物素）-Pra（QMT）-CBT（），以串联靶向癌细胞的生物素受体和亮氨酸氨肽酶，然后在细胞内进行 CBT-Cys 点击反应介导的双重聚集。实验结果表明，在活 HepG2 细胞和 HepG2 荷瘤小鼠中，与“生物素+LAP 抑制剂”处理的对照组相比，分别产生了 4.8 倍和 7.9 倍的更高 NIR 荧光信号。我们预计，具有串联靶向和双重聚集特性，可同时实现增强的肿瘤富集和荧光起始，将来可用于临床的精确癌症诊断。
Zotero 插件