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
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
相关论文
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[11]  
WILL DW, 1992, TETRAHEDRON LETT, V38, P2729