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Kuznetsova S. A., Sumbatyan N. V., Malvy C., Bertrand J. -R., Harel-Bellan A., Korshunova G. A., Svinarchuk F. P.

Synthesis of Oligonucleotide– Peptide Conjugates: The Use of N-Hydroxybenzotriazole Esters

Abstract

Conjugates of oligodeoxynucleotides with peptides that are potential inhibitors and activators of gene expression were synthesized. The easy and effective method including a condensation of 3’- or 5’-N-hydroxybenzotriazole ester of an oligonucleotide phosphate with terminal amino group of peptide was used for preparing covalent conjugates of two types. The conjugates of the first type were constructed of the antisense oligonucleotide, 5’-GAACACGCCATGTCGp-3’, complementary to the env AUG codon region of the Friend murine leukemia virus mRNA, and the following peptides: [Leu5]-enkephaline, [DAla2, Ual5]-enkephaline and nucleopeptides on the base of d-ornithine, in which a-amino function has been modified with pyrimidyl-1- and purinyl-9-acetic acids or pyrimidyl-1- and purinyl-9-alanines. The second type conjugates have contained two or three minimal transcriptional activation domains derived from protein VP16, H-GGG(PADALDDFDLDML)n-OH (n=2 and 3), linked to the 3’- or 5’-end of the oligonucleotide, 5’-GGAGGAGGAGGAGGGGGAGG-3’, forming stable triplexes with a promoter region of the HIV-2 virus vpx gene.
Moscow University Chemistry Bulletin.
2001, Vol. 42, No. 4, P. 281
   

Copyright (C) Chemistry Dept., Moscow State University, 2002
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