SYNTHESIS AND PROPERTIES OF CHOLESTERYL-MODIFIED TRIPLE-HELIX FORMING OLIGONUCLEOTIDES CONTAINING A TRIGLYCYL LINKER

被引：22

作者：

VU, H

HILL, TS

JAYARAMAN, K

机构：

[1] Triplex Pharmaceutical Corporation, Texas 77380, 9391 Grogans Mill Road, The Woodlands

来源：

BIOCONJUGATE CHEMISTRY | 1994年 / 5卷 / 06期

关键词：

D O I：

10.1021/bc00030a024

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

In order to enhance the nuclear uptake of triple-helix forming oligonucleotides (TFOs), a triglycylcholesterol group was attached to the 3' end. The peptide unit was introduced as a ''labile'' linker with the aim of releasing the oligonucleotide from the endosomes by the action of peptidases after crossing the cell membrane. Cholesteryl-CPG (8) and -TentaGel (9) supports containing 2-[N(glycylglycylglycyl)amino]propane-1,3-diol (GAP-3) linker were prepared and used for automated oligonucleotide synthesis. The synthesis, characterization, and stability of these compounds are described.

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页码：666 / 668

页数：3

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