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具有结构限制的合成五聚体戊胺立体异构体中 I 组核酶活性的独特调节。

Distinct modulation of group I ribozyme activity among stereoisomers of a synthetic pentamine with structural constraints.

机构信息

Department of Chemistry, Graduate School of Science and Engineering, University of Toyama, Gofuku 3190, Toyama, 930-8555, Japan; Graduate School of Innovative Life Science, University of Toyama, Gofuku 3190, Toyama, 930-8555, Japan.

Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, 467-8603, Japan.

出版信息

Biochem Biophys Res Commun. 2018 Oct 12;504(4):698-703. doi: 10.1016/j.bbrc.2018.09.015. Epub 2018 Sep 10.

Abstract

Among cationic molecules that can modulate ribozyme activities, polyamines act as both activator and inhibitor of ribozyme reactions partly due to their structural flexibility. Restriction of structural flexibility of polyamines may allow them to emphasize particular modulation effects. We examined eight stereoisomers of a synthetic pentamine bearing three cyclopentane rings. In the reaction of a structurally unstable group I ribozyme, three stereoisomers exhibited distinct effects as inhibitor, an additive with a neutral effect, and also as an activator.

摘要

在能够调节核酶活性的阳离子分子中,多胺由于其结构的灵活性,既可以作为核酶反应的激活剂,也可以作为抑制剂。限制多胺结构的灵活性可能会使它们能够强调特定的调节作用。我们研究了带有三个环戊烷环的合成五胺的八个立体异构体。在结构不稳定的 I 类核酶的反应中,有三种立体异构体表现出不同的抑制作用,一种是具有中性效应的添加剂,另一种是激活剂。

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