Enzyme-Responsive Procarriers Capable of Transporting Chloride Ions across Lipid and Cellular Membranes
Enzyme-Responsive Procarriers Capable of Transporting Chloride Ions across Lipid and Cellular Membranes
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DOI：
10.1021/jacs.6b10592
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发表时间：
2016-11-30
影响因子：
15
通讯作者：
Jeong, Kyu-Sung
中科院分区：
文献类型：
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作者：
Choi, Ye Rin;Lee, Bom;Jeong, Kyu-Sung
首次采用前载体的概念，我们证明了氯离子跨脂质和细胞膜的受控运输。含有高度亲水性附件的前载体最初是无活性的，这是由于它们不能分配到亲脂性膜中，但在特定酶的存在下被活化以转运氯离子，所述酶能够水解掉附件以在特定条件下产生活性载体。即，具有酯键连接的附件的前载体在pH = 7.4时被酯酶（PLE）活化最多，而具有糖基键连接的附件的前载体在微酸性条件（pH = 5.5-6）下仅被糖基化酶（AOG）活化。除了控制氯离子转运之外，亲水性附件大大增加了前载体的水溶性，这可以改善疏水活性载体进入质膜的递送能力。
Adopting the concept of procarrier for the first time, we demonstrated the controlled transport of chloride ions across lipid and cellular membranes. Procarriers containing highly hydrophilic appendages were initially inactive due to the lack of their partitioning into lipophilic membranes but were activated to transport chloride ions in the presence of specific enzymes that were able to hydrolyze off the appendages to generate an active carrier under specific conditions. Namely, the procarrier with an ester-bond-linked appendage was most activated by an esterase (PLE) at pH = 7.4, whereas the procarrier with a glycosyl-bond-linked appendage was activated only by a glycosylase (AOG) under slightly acidic conditions (pH = 5.5-6). In addition to controlling chloride transport, hydrophilic appendages greatly increase the water solubility of the procarrier, which may improve the deliverability of a hydrophobic active carrier into a plasma membrane.