Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore, 117543, Singapore.
NUS Graduate School for Integrative Sciences and Engineering, National University of Singapore, 28 Medical Drive, Singapore, 117456, Singapore.
Chem Asian J. 2020 May 4;15(9):1449-1455. doi: 10.1002/asia.202000157. Epub 2020 Mar 30.
Fluorescence microscopy has emerged as an attractive technique to probe the intracellular processing of Pt-based anticancer compounds. Herein, we reported the first through-bond energy transfer (TBET) fluorescent probe NPR1 designed for sensitive detection and quantitation of Pt complexes. The novel TBET probe was successfully applied for ratiometric fluorescence imaging of anticancer Pt complexes such as cisplatin and JM118 in cells. Capitalizing on the ability of the probe to discriminate between Pt complexes and their Pt derivatives, the probe was further applied to study the activation of Pt prodrug complexes that are known to release active Pt species after intracellular reduction.
荧光显微镜已成为一种有吸引力的技术，可以探测基于铂的抗癌化合物的细胞内处理。本文报道了第一个用于敏感检测和定量铂配合物的基于键的能量转移（TBET）荧光探针 NPR1。新型 TBET 探针成功地应用于顺铂和 JM118 等抗癌铂配合物在细胞中的比率荧光成像。利用探针区分铂配合物与其铂衍生物的能力，进一步将探针应用于研究铂前药配合物的激活，已知这些配合物在细胞内还原后会释放活性铂物种。
