Retro-1 Analogues Differentially Affect Oligonucleotide Delivery and Toxin Trafficking.
Retro-1 Analogues Differentially Affect Oligonucleotide Delivery and Toxin Trafficking.
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Retro-1 类似物对寡核苷酸递送和毒素贩运有不同的影响。
DOI：
10.1002/cmdc.201600463
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发表时间：
2016
期刊：
影响因子：
3.4
通讯作者：
Juliano,Rudy
中科院分区：
文献类型：
--
作者：
Yang,Bing;Ming,Xin;Abdelkafi,Hajer;Pons,Valerie;Michau,Aurelien;Gillet,Daniel;Cintrat,Jean-Christophe;Barbier,Julien;Juliano,Rudy
Retro‐1是一种小分子，具有两种重要的生物活性：首先，它通过改变细胞内运输来阻断某些毒素的作用。第二，它通过将寡核苷酸从内体中的包埋释放而增强寡核苷酸的活性。这就提出了一个问题，即这两种作用是否涉及相同的细胞靶点。在本文中，我们报告了几种Retro-1类似物对毒素和寡核苷酸的影响。我们发现类似物影响毒素，但不影响寡核苷酸，反之亦然，而Retro-1是唯一影响两者的化合物。这表明参与这两个过程的分子靶标是不同的。
Retro‐1 is a small molecule that displays two important biological activities: First, it blocks the actions of certain toxins by altering their intracellular trafficking. Second, it enhances the activity of oligonucleotides by releasing them from entrapment in endosomes. This raises the question of whether the two actions involve the same cellular target. Herein we report the effects of several Retro‐1 analogues on both toxins and oligonucleotides. We found analogues that affect toxins but not oligonucleotides and vice‐versa, while Retro‐1 is the only compound that affects both. This indicates that the molecular target(s) involved in the two processes are distinct.