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基于吗啉代的肽寡聚物:合成与 DNA 结合特性。

Morpholino-based peptide oligomers: Synthesis and DNA binding properties.

机构信息

Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Milano, Italy.

DeFENS - Dipartimento di Scienze per gli Alimenti, la Nutrizione e l'Ambiente, Università degli Studi di Milano, Milano, Italy.

出版信息

Biochem Biophys Res Commun. 2021 Apr 16;549:8-13. doi: 10.1016/j.bbrc.2021.02.087. Epub 2021 Feb 27.

Abstract

The chemical structure of oligonucleotide analogues dictates the conformation of oligonucleotide analogue oligomers, their ability to hybridize complementary DNA and RNA, their stability to degradation and their pharmacokinetic properties. In a study aimed at investigating new analogues featuring a neutral backbone, we explored the ability of oligomers containing a morpholino-peptide backbone to bind oligonucleotides. Circular Dichroism studies revealed the ability of our oligomers to interact with DNA, molecular modelling studies revealed the interaction responsible for complex stabilization.

摘要

寡核苷酸类似物的化学结构决定了寡核苷酸类似物寡聚物的构象、与互补 DNA 和 RNA 杂交的能力、对降解的稳定性和药代动力学性质。在一项旨在研究具有中性骨架的新类似物的研究中,我们探索了含有吗啉代肽骨架的寡聚物结合寡核苷酸的能力。圆二色性研究揭示了我们的寡聚物与 DNA 相互作用的能力,分子建模研究揭示了导致复合物稳定的相互作用。

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