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Biological efficacy of antisense oligonucleotides complementary to overlapping regions of the mRNA target

机译:与mRNA靶标重叠区域互补的反义寡核苷酸的生物学功效

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摘要

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 knockodown). 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 alpha_2A-adrenoceptor mRNA, on recetor 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.
机译:与靶mRNA互补的硫代磷酸酯寡核苷酸在生物学环境中是稳定的,并且能够降低该mRNA和该mRNA编码的蛋白质的水平(反义敲低)。我们的研究结果与文献中发表的有关三种反义18-21-mer寡核苷酸功效的数据进行了比较,这三种寡核苷酸针对受体上的alpha_2A-肾上腺素受体mRNA的起始密码子或附近序列,并且数量最多在理论上计算的构象中,对应于自由能最小值的未配对碱基的数目。反义的两个末端靶向靶的未配对碱基也导致其生物学功效的增强。

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