Enzymatic hydrolysis and biological activity of oligonucleotides containing 5-substituted pyrimidine bases.

L Otvös, J Sági, G Sági, A Szemzõ, F D Tóth, A Jeney
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引用次数: 6

Abstract

Two series of alternating ODNs containing 5-n.alkyl-, alkenyl- and alkynyl-dU and -dC units have been prepared in order to study the kinetics of their hydrolysis by SV PDE and human serum, respectively. Both in (r5dUpdA)10 and (r5dCpdG)6 series the rate of hydrolysis decreased with increasing length of side-chain. Replacement of thymidines by 5-hexynyl-dU in different antisense oligomers resulted in considerably higher biological activity relative to that of the thymidine-containing counterparts.

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含5-取代嘧啶基寡核苷酸的酶解和生物活性。
包含5-n的两个交替odn系列。制备了烷基-、烯基-、烷基- du和- dc单元,分别研究了它们在SV PDE和人血清中的水解动力学。在(r5dUpdA)10和(r5dCpdG)6系列中,水解速率随侧链长度的增加而降低。在不同的反义寡聚物中,5-己基- du取代胸腺嘧啶导致相对于含有胸腺嘧啶的对应物具有更高的生物活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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