Automated Modular Synthesis of Aptamer–Drug Conjugates for Targeted Drug Delivery

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• 作者：RuoWen Wang ; Guizhi Zhu ; Lei Mei ; Yan Xie ; Haibin Ma ; Mao Ye ; Feng-Ling Qing ; Weihong Tan
• 刊名：Journal of the American Chemical Society
• 出版年：2014
• 出版时间：February 19, 2014
• 年：2014
• 卷：136
• 期：7
• 页码：2731-2734
• 全文大小：248K
• ISSN：1520-5126

文摘

Aptamer鈥揹rug conjugates (ApDCs) are promising targeted drug delivery systems for reducing toxicity while increasing the efficacy of chemotherapy. However, current ApDC technologies suffer from problems caused by the complicated preparation and low controllability of drug鈥揳ptamer conjugation. To solve such problems, we have designed and synthesized a therapeutic module for solid phase synthesis, which is a phosphoramdite containing an anticancer drug moiety and a photocleavable linker. Using this module, we have realized automated and modular synthesis of ApDCs, and multiple drugs were efficiently incorporated into ApDCs at predesigned positions. The ApDCs not only recognize target cancer cells specifically, but also release drugs in a photocontrollable manner. We demonstrated the potential of automated and modular ApDC technology for applications in targeted cancer therapy.