Abstract
Phosphorothioate oligonucleotides complementary to target mRNA are stable in biological milieu and are capable of decreasing levels of this mRNA and the protein encoded by this mRNA (antisense knockdown). The results of our study are compared with the data published in the literature on the efficacy of three antisense 18—21-mer oligonucleotides, which are targeted to the start codon or nearby sequences of α2A-adrenoceptor mRNA, on receptor expression, and functions regulated by these receptors. The highest biological efficacy was shown by the oligonucleotide, which is complementary to the mRNA region and contains the largest number of unpaired bases in the theoretically calculated conformation corresponding to the free energy minimum. Targeting of both ends of the antisense on unpaired bases of the target also leads to the enhancement of its biological efficacy.
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Dygalo, N.N., Kalinina, T.S. & Shishkina, G.T. Biological efficacy of antisense oligonucleotides complementary to overlapping regions of the mRNA target. Russian Chemical Bulletin 51, 1118–1121 (2002). https://doi.org/10.1023/A:1020941705927
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DOI: https://doi.org/10.1023/A:1020941705927