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新型核肽的合成、光谱学研究及其对莫洛尼鼠白血病病毒逆转录酶的抑制活性。

Synthesis, spectroscopic studies and biological activity of a novel nucleopeptide with Moloney murine leukemia virus reverse transcriptase inhibitory activity.

机构信息

Istituto di Biostrutture e Bioimmagini, CNR, via Mezzocannone 16, 80134, Naples, Italy.

出版信息

Amino Acids. 2010 May;38(5):1489-96. doi: 10.1007/s00726-009-0361-5. Epub 2009 Oct 8.

Abstract

In this work, we report the synthesis of an alternate nucleo-alpha,epsilon-peptide based on L: -lysine moieties, an in vitro study of its biological activity, and spectroscopical binding studies between the novel nucleopeptide and Moloney murine leukemia virus reverse transcriptase as well as RNA. An alternate homothymine hexamer was synthesized by a straightforward solid phase route starting from commercial materials, purified by RP-HPLC and characterized by ESI-MS. The efficiency of the novel nucleo-alpha,epsilon-peptide in interfering with the reverse transcription of eukaryotic mRNA and the noteworthy enzymatic resistance demonstrated by specific assays are in favor of the employment of this nucleopeptide in novel biomedical strategies.

摘要

在这项工作中,我们报告了一种基于 L: -赖氨酸部分的替代核-α,ε-肽的合成,对其生物活性的体外研究,以及新型核肽与 Moloney 鼠白血病病毒逆转录酶和 RNA 之间的光谱结合研究。一种替代的同胸腺嘧啶六聚体通过从商业材料开始的直接固相路线合成,通过 RP-HPLC 纯化,并通过 ESI-MS 进行表征。新型核-α,ε-肽在干扰真核 mRNA 逆转录方面的效率以及通过特定测定显示出的显著酶抗性有利于将这种核肽用于新型生物医学策略。

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