Department of Chemistry, BK School of Molecular Science, Pohang University of Science and Technology, Pohang, 790-784 Korea.
Org Biomol Chem. 2011 Jan 7;9(1):291-6. doi: 10.1039/c0ob00580k. Epub 2010 Nov 17.
We synthesized five novel uridine-based cationic nucleolipids, introducing basic amino acid residues at the 5' position of uridine, through 1,3-dipolar cycloaddition, and hydrophobic alkyl moieties at the 2' and 3' positions, through carbamate linkages. Their lipoplexes delivered siRNAs efficiently to cells, in vitro, without any severe toxicity.
我们通过 1,3-偶极环加成反应，在尿嘧啶的 5'位引入碱性氨基酸残基，通过氨基甲酸酯键在 2'和 3'位引入疏水烷基部分，合成了五种新型的尿嘧啶基阳离子核苷脂质体。它们的脂质体复合物在体外有效地将 siRNA 递送到细胞中，没有任何严重的毒性。
