Light induced drug release from a folic acid-drug conjugate.
Light induced drug release from a folic acid-drug conjugate.
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光诱导的药物从叶酸 - 毒剂结合物中释放。
DOI：
10.1016/j.bmcl.2016.12.036
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发表时间：
2017-02-01
影响因子：
2.7
通讯作者：
Hartman MC
中科院分区：
文献类型：
--
作者：
Dcona MM;Sheldon JE;Mitra D;Hartman MC
癌症研究的一个主要领域是通过设计靶向肿瘤细胞上过表达受体的药物递送载体来提高治疗药物的特异性。最常用的方法之一是使用叶酸偶联到含有药物的大分子货物靶向叶酸受体。一旦通过内吞作用内化，药物必须从这些结构体中释放出来，以避免被困在核内体中。在这里，我们描述了一种小分子共轭物的合成，它通过光可切割的连接剂将叶酸偶联到阿霉素上。高效液相色谱法表明，阿霉素可以快速、高效地光释放。与大分子系统相比，该方法具有简单、高效的优点。
A major area of cancer research focuses on improving the specificity of therapeutic agents by engineering drug-delivery vehicles that target overexpressed receptors on tumor cells. One of the most commonly used approaches involves targeting of folate receptors using folic acid conjugated to a drug-containing macromolecular cargo. Once internalized via endocytosis, the drugs must be released from these constructs in order to avoid being trapped in the endosomes. Here, we describe the synthesis of a small-molecule conjugate that couples folic acid to doxorubicin via a photocleavable linker. Using HPLC we show that the doxorubicin can be released with light rapidly and with high efficiency. This approach has advantages over macromolecular systems due to its simplicity and efficiency.