Carrier-Free Delivery of Precise Drug-Chemogene Conjugates for Synergistic Treatment of Drug-Resistant Cancer.,Angewandte Chemie International Edition

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Carrier-Free Delivery of Precise Drug-Chemogene Conjugates for Synergistic Treatment of Drug-Resistant Cancer.
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2020-07-08 , DOI: 10.1002/anie.202006895
Lijuan Zhu _{1,

2} , Yuanyuan Guo ₂ , Qiuhui Qian ₂ , Deyue Yan _{1,

2} , Yuehua Li ₃ , Xinyuan Zhu ₂ , Chuan Zhang ₂

Affiliation

Combinatorial antitumor therapies using different combinations of drugs and genes are emerging as promising ways to overcome drug resistance, which is a major cause for the failure of cancer treatment. However, dramatic pharmacokinetic differences of drugs greatly impede their combined use in cancer therapy, raising the demand for drug delivery systems (DDSs) for tumor treatment. By employing fluorescent dithiomaleimide (DTM) as a linker, we conjugate two paclitaxel (PTX) molecules with a floxuridine (FdU)‐integrated antisense oligonucleotide (termed chemogene) to form a drug–chemogene conjugate. This PTX–chemogene conjugate can self‐assemble into a spherical nucleic acid (SNA)‐like micellular nanoparticle as a carrier‐free DDS, which knocks down the expression of P‐glycoprotein and subsequently releases FdU and PTX to exert a synergistic antitumor effect and greatly inhibit tumor growth.

中文翻译：

精确的药物-化学原缀合物的无载体递送可用于抗药性癌症的协同治疗。

使用药物和基因的不同组合的组合抗肿瘤疗法正在成为克服耐药性的有希望的方法，这是导致癌症治疗失败的主要原因。然而，药物的巨大药代动力学差异极大地阻碍了它们在癌症治疗中的联合使用，从而增加了用于肿瘤治疗的药物递送系统（DDS）的需求。通过使用荧光二硫马来酰亚胺（DTM）作为接头，我们将两个紫杉醇（PTX）分子与氟尿苷（FdU）整合的反义寡核苷酸（称为化学基因）结合，形成药物-化学结合物。这种PTX-化学原共轭物可以自组装成球形核酸（SNA）状的微细胞纳米粒子，作为无载体的DDS，

更新日期：2020-07-08

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