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首页> 外文期刊>Chemistry & biology >Synthesis and functional evaluation of DNA-assembled polyamidoamine dendrimer clusters for cancer cell-specific targeting
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Synthesis and functional evaluation of DNA-assembled polyamidoamine dendrimer clusters for cancer cell-specific targeting

机译：DNA组装的聚酰胺胺树枝状大分子簇的合成和功能评估癌细胞特异性靶向。

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We sought to produce dendrimers conjugated to different biofunctional moieties (fluorescein [FITC] and folic acid [FA]), and then link them together using complementary DNA oligonucleotides to produce clustered molecules that target cancer cells that overexpress the high-affinity folate receptor. Amine-terminated, generation 5 polyamidoamine (G5 PAMAM) dendrimers are first partially acetylated and then conjugated with FITC or FA, followed by the covalent attachment of complementary, 5'-phosphate-modified 34-base-long oligonucleotides. Hybridization of these oligonucleotide conjugates led to the self-assembly of the FITC-and FA-conjugated dendrimers. In vitro studies of the DNA-linked dendrimer clusters indicated specific binding to KB cells expressing the folate receptor. Confocal microscopy also showed the internalization of the dendrimer cluster. These results demonstrate the ability to design and produce supramolecular arrays of dendrimers using oligonucleotide bridges. This will also allow for further development of DNA-linked dendrimer clusters as imaging agents and therapeutics.
机译：我们试图生产与不同生物功能部分（荧光素[FITC]和叶酸[FA]）缀合的树状聚合物，然后使用互补的DNA寡核苷酸将它们连接在一起，以产生靶向于过表达高亲和力叶酸受体的癌细胞的簇状分子。首先将胺末端的第5代聚酰胺型胺（G5 PAMAM）树状聚合物部分乙酰化，然后与FITC或FA偶联，然后共价连接5'-磷酸修饰的34-碱基长的寡核苷酸。这些寡核苷酸缀合物的杂交导致FITC-和FA-缀合的树枝状聚合物的自组装。 DNA连接的树枝状大分子簇的体外研究表明与表达叶酸受体的KB细胞有特异性结合。共聚焦显微镜也显示了树枝状聚合物簇的内在化。这些结果证明了使用寡核苷酸桥设计和产生树状聚合物的超分子阵列的能力。这也将允许进一​​步开发DNA连接的树枝状大分子簇作为显像剂和治疗剂。

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