Chu Yu-Hsuan, Sibrian-Vazquez Martha, Escobedo Jorge O, Phillips Amanda R, Dickey D Thomas, Wang Qi, Ralle Martina, Steyger Peter S, Strongin Robert M
Department of Chemistry, Portland State University , Portland, Oregon 97201, United States.
Mol Pharm. 2016 Aug 1;13(8):2677-82. doi: 10.1021/acs.molpharmaceut.6b00240. Epub 2016 Jun 24.
Cisplatin is widely used to treat a variety of cancers. However, ototoxicity and nephrotoxicity remain serious side effects of cisplatin-based chemotherapy. In order to inform the study of cisplatin's off-target effects, a new drug-fluorophore conjugate was synthesized that exhibited utility as a tracer to determine the cellular uptake and in vivo distribution of cisplatin. This probe will serve as a useful tool to facilitate investigations into the kinetics and biodistribution of cisplatin and its associated side effects in preclinical models after systemic administration.
顺铂被广泛用于治疗多种癌症。然而,耳毒性和肾毒性仍然是基于顺铂化疗的严重副作用。为了为顺铂脱靶效应的研究提供信息,合成了一种新的药物-荧光团共轭物,该共轭物可作为示踪剂来确定顺铂的细胞摄取和体内分布。该探针将作为一种有用的工具,有助于在临床前模型中全身给药后研究顺铂的动力学、生物分布及其相关副作用。