Site-specific modification of the 5"-terminal fragment of PGY1/MDR1 gene mRNA by reactive conjugates of antisense oligonucleotides

作者: R. N. Kulikov , E. V. Kostenko , M. A. Kuznetsova , D. S. Novopashina , A. A. Chernonosov

DOI: 10.1023/A:1022437524278

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摘要: The site-specific modification of the 5"-terminal fragment PGY1/MDR1 mRNA by oligodeoxyribonucleotide conjugates bearing residues bleomycin A5 (Blm), cobalt(ii) tetracarboxyphthalocyanine (Phcn), 4-[N-(2-chloroethyl)-N-methylamino]benzylamine (RCl), or perfluoroarylazide (Az) was studied. Conjugates oligonucleotides complementary to RNA sequences 123—138 and 155—166 selectively modify in vicinity these regions. highest efficacy (up 50%) achieved reactions with alkylating oligonucleotides. 2"-O-modified are much more efficient than analogous oligodeoxyribonucleotides (extents 40—50% 20%, respectively).

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