Automated modular synthesis of aptamer-drug conjugates for targeted drug delivery.
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.
Molecular Sciences and Biomedicine Laboratory, State Key Laboratory for Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering and College of Biology, Collaborative Innovation Center for Chemistry and Molecular Medicine, Hunan University , Changsha 410082, China.
RuoWen
R
Wang
Guizhi
G
Zhu
Lei
L
Mei
Yan
Y
Xie
Haibin
H
Ma
Mao
M
Ye
Feng-Ling
FL
Qing
Weihong
W
Tan
D000577:Amides / Q000737:chemistry; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism; D052157:Aptamers, Nucleotide / Q000737:chemistry*; D001331:Automation; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry*; D045325:HCT116 Cells; D006801:Humans; D010756:Phosphoric Acids / Q000737:chemistry; D055668:Photochemical Processes; D060327:Solid-Phase Synthesis Techniques
D000577:Amides; D000970:Antineoplastic Agents; D052157:Aptamers, Nucleotide; D004337:Drug Carriers; D010756:Phosphoric Acids; C011067:phosphoramidic acid