THE SYNTHESIS OF POLYAMIDE OLIGONUCLEOTIDE CONJUGATE MOLECULES
THE SYNTHESIS OF POLYAMIDE OLIGONUCLEOTIDE CONJUGATE MOLECULES
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DOI：
10.1093/nar/18.3.493
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发表时间：
1990-02-11
影响因子：
14.9
通讯作者：
TREGEAR, GW
中科院分区：
文献类型：
--
作者：
HARALAMBIDIS, J;DUNCAN, L;TREGEAR, GW
我们已经开发了合成肽-寡脱氧核糖核苷酸缀合物分子的方法，特别是合成聚酰胺-寡核苷酸缀合物的方法。合成通过固相程序进行，并且涉及在固体载体上组装聚酰胺，通过与α反应将末端氨基转化为受保护的伯脂族羟基。欧米加羟基羧酸衍生物，最后使用亚磷酰胺化学合成寡核苷酸。缀合物分子可用作DNA探针，其中聚酰胺组分携带一种或多种非放射性标记物。这些缀合物还具有用作基因表达的反义抑制剂的潜力，其中肽段充当靶向部分。
We have developed methods for the synthesis of peptide-oligodeoxyribonucleotide conjugate molecules in particular, and polyamide-oligonucleotide conjugates in general. Synthesis is carried out by a solid-phase procedure and involves the assembly of a polyamide on the solid support, conversion of the terminal amino group to a protected primary aliphatic hydroxy group by reaction with .alpha.,.omega.-hydroxycarboxylic acid derivatives, and finally oligonucleotide synthesis using phosphoramidite chemistry. The conjugate molecules can be used as DNA probes, with the polyamide component carrying one or more non-radioactive markers. These conjugates also have the potential to be used as anti-sense inhibitors of gene expression, with the peptide segment acting as a targeting moiety.