文献类型：期刊文献

英文题名：Graphene Quantum Dots Downregulate Multiple Multidrug-Resistant Genes via Interacting with Their C-Rich Promoters

作者：Luo, Chao[1];Li, Yanfang[1];Guo, Lijuan[1];Zhang, Fangwei[2];Liu, Hui[1];Zhang, Jiali[2];Zheng, Jing[1];Zhang, Jingyan[1];Guo, Shouwu[2]

机构：[1]East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, State Key Lab Bioreactor Engn, 130 Meilong Rd, Shanghai 200237, Peoples R China;[2]Shanghai Jiao Tong Univ, Sch Elect Informat & Elect Engn, 800 Dongchuan Rd, Shanghai 200240, Peoples R China

年份：2017

卷号：6

期号：21

外文期刊名：ADVANCED HEALTHCARE MATERIALS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000417544400010)】；

基金：This research was carried out with financial support from the national 973 Program of China (Grant No. 2015CB931801), National Science Foundation of China (Grant No. 11374205), the State Key Laboratory of Bioreactor Engineering (Grant No. 2060204), and the Shanghai Committee of Science and Technology (Grant No. 11DZ2260600).

语种：英文

外文关键词：ABC transporters; gene regulation; graphene quantum dots; multidrug resistance

摘要：Multidrug resistance (MDR) is the major factor in the failure of many forms of chemotherapy, mostly due to the increased efflux of anticancer drugs that mediated by ATP-binding cassette (ABC) transporters. Therefore, inhibiting ABC transporters is one of effective methods of overcoming MDR. However, high enrichment of ABC transporters in cells and their broad substrate spectra made to circumvent MDR are almost insurmountable by a single specific ABC transporter inhibitor. Here, this study demonstrates that graphene quantum dots (GQDs) could downregulate the expressions of P-glycoprotein, multidrug resistance protein MRP1, and breast cancer resistance protein genes via interacting with C-rich regions of their promoters. This is the first example that a single reagent could suppress multiple MDR genes, suggesting that it will be possible to target multiple ABC transporters simultaneously with a single reagent. The inhibitory ability of the GQDs to these drug-resistant genes is validated further by reversing the doxorubicin resistance of MCF-7/ADR cells. Notably, GQDs have superb chemical and physical properties, unique structure, low toxicity, and high biocompatibility; hence, their capability of inhibiting multiple drug-resistant genes holds great potential in cancer therapy.