Stetsenko Dmitry A, Malakhov Andrey D, Gait Michael J
Medical Research Council, Laboratory of Molecular Biology, Cambridge CB2 2QH, UK.
Org Lett. 2002 Sep 19;4(19):3259-62. doi: 10.1021/ol026502u.
[structure: see text] An efficient total stepwise solid-phase synthesis of oligonucleotide-(3'-->N)-peptide conjugates is described that makes use of either a controlled pore glass support or macroporous polystyrene beads. Extending our previous homoserine linker approach, we prepared a range of conjugates containing one of four different cell or nuclear penetration peptides together with oligonucleotides containing 2'-deoxynucleoside or 2'-O-methylribonucleoside phosphodiesters, or gapmers containing 2'-deoxyphosphorothioates. The route also allows incorporation of a fluorescent label within the conjugate for cell uptake studies.
[结构：见原文] 本文描述了一种高效的寡核苷酸-(3'→N)-肽缀合物的全逐步固相合成方法，该方法使用可控孔玻璃载体或大孔聚苯乙烯珠。扩展我们之前的高丝氨酸连接子方法，我们制备了一系列缀合物，其中包含四种不同的细胞穿透肽或核穿透肽之一，以及含有2'-脱氧核苷或2'-O-甲基核糖核苷磷酸二酯的寡核苷酸，或含有2'-脱氧硫代磷酸酯的缺口嵌合体。该路线还允许在缀合物中掺入荧光标记用于细胞摄取研究。
