A self-immolative dendritic glucuronide prodrug of doxorubicin

被引：37
|
作者：
Grinda, Marion [1 ]
Clarhaut, Jonathan [2 ,3 ]
Renoux, Brigitte [1 ]
Tranoy-Opalinski, Isabelle [1 ]
Papot, Sebastien [1 ]
机构：
[1] Univ Poitiers, CNRS, UMR 6514, F-86022 Poitiers, France
[2] Univ Poitiers, CNRS, UMR 6187, F-86022 Poitiers, France
[3] CHU Poitiers, INSERM, CIC 0802, F-86021 Poitiers, France
来源：
MEDCHEMCOMM | 2012年 / 3卷 / 01期
关键词：
DRUG-RELEASE; DENDRIMERS; ELIMINATION; ACTIVATION; THERAPY; MUSTARD;
D O I：
10.1039/c1md00193k
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The first self-immolative dendritic glucuronide prodrug of doxorubicin was studied with the aim to target beta-glucuronidase overexpressed in the microenvironment of numerous tumors. This compound includes a chemical amplifier programmed to release two molecules of doxorubicin after a single enzymatic activation step. Upon beta-glucuronidase activation, the dendritic prodrug was twice more toxic than its monomeric counterpart against H661 lung cancer cells.
引用
收藏
页码：68 / 70
页数：3
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