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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >BINDING STUDIES OF CATIONIC THYMIDYL DEOXYRIBONUCLEIC GUANIDINE TO RNA HOMOPOLYNUCLEOTIDES
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BINDING STUDIES OF CATIONIC THYMIDYL DEOXYRIBONUCLEIC GUANIDINE TO RNA HOMOPOLYNUCLEOTIDES

机译：阳离子嘧啶脱氧核糖核酸胍与RNA同源核苷酸的结合研究。

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摘要

Deoxyribonucleic guanidine is a potential antisense agent that is generated via the replacement of the negative phosphodiester linkages of DNA [-O-(PO2-)-O-] with positively-charged guanidinium (g) linkages [-NH-C(=NH2+)-NH-]. A pentameric thymidyl deoxyribonucleic guanidine molecule [d(Tg)(4)T-azido] has been shown to base pair specifically to poly(rA) with an unprecedented affinity. Both double and triple strands consisting of one and two equivalents of d(Tg)(4)T-azido paired with one equivalent of poly(rA) are indicated by thermal denaturation experiments. At an ionic strength of 0.22, the five bases of d(Tg)(4)T-azido are estimated to dissociate from a double helix with poly(rA) at > 100 degrees C! The effect of ionic strength on thermal denaturation is very pronounced, with stability greatest at low ionic strengths. The method of continuous variation indicates that there is an equilibrium complex with a molar ratio of d(Tg) to r(Ap) or d(Ap) of 2:1. Based on this evidence, models of the structures of d(Tg)(9)T-azido bound to r(Ap)(9)A are proposed. [References: 20]
机译：脱氧核糖核酸胍是一种潜在的反义剂，它是通过将DNA [-O-（PO2-）-O-]的负磷酸二酯键替换为带正电荷的胍盐（g）键[-NH-C（= NH2 +）而产生的-NH-]。五聚的胸苷基脱氧核糖核酸胍分子[d（Tg）（4）T-叠氮基]已经显示出与空前的亲和力与poly（rA）特异性碱基配对。通过热变性实验表明由一当量的d（Tg）（4）T-叠氮基与一当量的poly（rA）组成的双链和三链。在0.22的离子强度下，估计d（Tg）（4）T-叠氮基的5个碱基在大于100摄氏度时会从带有poly（rA）的双螺旋上解离！离子强度对热变性的影响非常明显，在低离子强度下稳定性最大。连续变化法表明存在一个平衡络合物，其d（Tg）与r（Ap）或d（Ap）的摩尔比为2：1。基于这一证据，提出了与r（Ap）（9）A结合的d（Tg）（9）T-叠氮基结构模型。 [参考：20]

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