Michigan Nanotechnology Institute for Medicine and Biological Sciences, University of Michigan, 9220 MSRB III, Box 0648, Ann Arbor, MI 48109, USA.
Bioorg Med Chem Lett. 2012 May 1;22(9):3152-6. doi: 10.1016/j.bmcl.2012.03.052. Epub 2012 Mar 21.
The facile conjugation of three azido modified functionalities, namely a therapeutic drug (methotrexate), a targeting moiety (folic acid), and an imaging agent (fluorescein) with a G5 PAMAM dendrimer scaffold with cyclooctyne molecules at the surface through copper-free click chemistry is reported. Mono-, di-, and tri-functional PAMAM dendrimer conjugates can be obtained via combinatorial mixing of different azido modified functionalities simultaneously or sequentially with the dendrimer platform. Preliminary flow cytometry results indicate that the folic acid targeted nanoparticles are efficiently binding with KB cells.
本文报道了通过无铜点击化学，将三种叠氮修饰功能（治疗药物甲氨蝶呤、靶向部分叶酸和成像剂荧光素）与表面带有环辛炔分子的 G5 PAMAM 树枝状大分子支架轻易地连接在一起。通过同时或顺序地将不同的叠氮修饰功能与树枝状大分子平台组合混合，可以得到单功能、双功能和三功能的 PAMAM 树枝状大分子缀合物。初步的流式细胞术结果表明，靶向叶酸的纳米颗粒能够有效地与 KB 细胞结合。
