Ong Jun Xiang, Yap Jian Yu, Yap Siew Qi, Ang Wee Han
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore.
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.
J Inorg Biochem. 2015 Dec;153:272-278. doi: 10.1016/j.jinorgbio.2015.10.002. Epub 2015 Oct 22.
Fluorescence microscopy has emerged as an attractive technique for imaging intracellular Pt species arising from exposure to clinical anticancer drugs such as cisplatin. A rhodamine-B based fluorogenic probe termed Rho-DDTC can be activated selectively in the presence of Pt(II) compounds, and possesses the ability to discriminate Pt(II) species from Pt(IV) carboxylate prodrug complexes, thereby providing a unique platform to investigate the reduction of these Pt(IV) complexes after cell entry. In this report, we seek to establish the mechanism of activation of Rho-DDTC through a structure-activity relationship study on its structural analogues.
荧光显微镜已成为一种颇具吸引力的技术，可用于对细胞内由接触顺铂等临床抗癌药物产生的铂物种进行成像。一种名为Rho-DDTC的基于罗丹明B的荧光探针可在铂（II）化合物存在下被选择性激活，并具有区分铂（II）物种与铂（IV）羧酸盐前药复合物的能力，从而为研究这些铂（IV）复合物进入细胞后的还原过程提供了一个独特的平台。在本报告中，我们试图通过对其结构类似物的构效关系研究来确定Rho-DDTC的激活机制。
