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靶向 10 个 microRNA 前体的配体的荧光指示剂置换分析。

Fluorescent indicator displacement assay of ligands targeting 10 microRNA precursors.

机构信息

Department of Regulatory Bioorganic Chemistry, The Institute of Scientific and Industrial Research, Osaka University, 8-1 Mihogaoka, Ibaraki 567-0047, Japan.

出版信息

Bioorg Med Chem. 2013 Nov 15;21(22):7101-6. doi: 10.1016/j.bmc.2013.09.007. Epub 2013 Sep 14.

Abstract

Fluorescent indicator displacement (FID) assay is a rapid and convenient assay for identifying new ligands that bind to the target molecules. In our previous studies, we have shown that a series of 2,7-diaminoalkoxy xanthone and thioxanthone derivatives can be used as fluorescent indicators for detecting the interaction between RNA and a ligand. The xanthone and thioxanthone fluorochromes showed efficient fluorescence quenching upon binding to target RNA. Subsequent displacement of the bound-fluorochrome with a ligand that binds more strongly to the target RNA led to the recovery of the fluorescence by releasing the fluorochrome from RNA. Here we report a pilot screening of a chemical library that contains 9600 structurally diverse compounds for molecules that bind to a specific miRNA precursor using the FID assay.

摘要

荧光指示剂位移(FID)分析是一种快速便捷的分析方法,可用于鉴定与靶分子结合的新配体。在我们之前的研究中,我们已经表明,一系列 2,7-二氨基烷氧基蒽酮和硫代蒽酮衍生物可用作荧光指示剂,用于检测 RNA 与配体之间的相互作用。当与靶 RNA 结合时,蒽酮和硫代蒽酮荧光团显示出有效的荧光猝灭,随后用与靶 RNA 结合更强的配体置换结合的荧光团,通过从 RNA 上释放荧光团来恢复荧光。在这里,我们报告了使用 FID 分析对包含 9600 种结构多样的化合物的化学文库进行的先导筛选,以寻找与特定 miRNA 前体结合的分子。

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