多重耐药
细胞内
体内
体外
化学
药理学
癌症研究
抗药性
医学
生物
生物化学
微生物学
生物技术
作者
Yue Yuan,Lin Wang,Wei Du,Zhanling Ding,Jia Zhang,Tao Han,Linna An,Huafeng Zhang,Gaolin Liang
标识
DOI:10.1002/anie.201504329
摘要
Multidrug resistance (MDR) remains the biggest challenge in treating cancers. Herein we propose the intracellular self-assembly of nanodrugs as a new strategy for overcoming MDR. By employing a biocompatible condensation reaction, we rationally designed a taxol derivative Ac-Arg-Val-Arg-Arg-Cys(StBu)-Lys(taxol)-2-cyanobenzothiazole (CBT-Taxol) which could be subjected to furin-controlled condensation and self-assembly of taxol nanoparticles (Taxol-NPs). In vitro and in vivo studies indicated that, compared with taxol, CBT-Taxol showed a 4.5-fold or 1.5-fold increase in anti-MDR effects, respectively, on taxol-resistant HCT 116 cancer cells or tumors without being toxic to the cells or the mice. Our results demonstrate that structuring protease-susceptible agents and assembling them intracellularly into nanodrugs could be a new optimal strategy for overcoming MDR.
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