DNA Trojan Horses: Self‐Assembled Floxuridine‐Containing DNA Polyhedra for Cancer Therapy

Based on their structural similarity to natural nucleobases, nucleoside analogue therapeutics were integrated into DNA strands through conventional solid‐phase synthesis. By elaborately designing their sequences, floxuridine‐integrated DNA strands were synthesized and self‐assembled into well‐define...

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Bibliographic Details
Published inAngewandte Chemie Vol. 129; no. 41; pp. 12702 - 12706
Main Authors Mou, Quanbing, Ma, Yuan, Pan, Gaifang, Xue, Bai, Yan, Deyue, Zhang, Chuan, Zhu, Xinyuan
Format Journal Article
LanguageEnglish
Published Weinheim Wiley Subscription Services, Inc 02.10.2017
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Summary:Based on their structural similarity to natural nucleobases, nucleoside analogue therapeutics were integrated into DNA strands through conventional solid‐phase synthesis. By elaborately designing their sequences, floxuridine‐integrated DNA strands were synthesized and self‐assembled into well‐defined DNA polyhedra with definite drug‐loading ratios as well as tunable size and morphology. As a novel drug delivery system, these drug‐containing DNA polyhedra could ideally mimic the Trojan Horse to deliver chemotherapeutics into tumor cells and fight against cancer. Both in vitro and in vivo results demonstrate that the DNA Trojan horse with buckyball architecture exhibits superior anticancer capability over the free drug and other formulations. With precise control over the drug‐loading ratio and structure of the nanocarriers, the DNA Trojan horse may play an important role in anticancer treatment and exhibit great potential in translational nanomedicine. Wie zu Homers Zeiten: Ein tumorbekämpfendes Nukleosidanalogon (Floxuridin) kann durch Festphasensynthese in DNA‐Stränge eingefügt werden. Diese Floxuridin‐haltigen DNA‐Oligomere mit exakt einstellbarer Wirkstoffbeladung bilden DNA‐Polyeder, die bei der In‐vitro‐ und In‐vivo‐Bekämpfung von Krebs wie nanoskopische Trojanische Pferde wirken.
Bibliography:These authors contributed equally to this work.
ISSN:0044-8249
1521-3757
DOI:10.1002/ange.201706301