期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 136, 期 7, 页码 2731-2734出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja4117395
关键词
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资金
- National Key Scientific Program of China [2011CB911000]
- Foundation for Innovative Research Groups of the NSFC [NSFC 21221003, NSFC 21327009]
- China National Instrumentation Program [2011YQ03012412]
- Scientific Research Foundation for the Returned Overseas Chinese Scholars, State Education Ministry
Aptamer-drug 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 aptamer 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.
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