Fluorescent indicator displacement assay of ligands targeting 10 microRNA precursors

Fluorescent indicator displacement assay of ligands targeting 10 microRNA precursors
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DOI:
10.1016/j.bmc.2013.09.007
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发表时间:
2013-11-15
影响因子:
3.5
通讯作者:
Nakatani, Kazuhiko
Nakatani, Kazuhiko
中科院分区:
医学3区
文献类型:
--
作者:
Murata, Asako;Harada, Yasue;Nakatani, Kazuhiko

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荧光指示剂置换法(FID)是一种快速方便的方法,用于鉴定与目标分子结合的新配体。在我们之前的研究中,我们已经证明了一系列2,7-二氨基烷氧基山酮和硫氧山酮衍生物可以作为检测RNA与配体相互作用的荧光指示剂。杂山酮和硫杂山酮荧光染料在与靶RNA结合后表现出高效的荧光猝灭。随后用与靶RNA结合更强的配体置换结合的荧光色素,通过从RNA中释放荧光色素来恢复荧光。在这里,我们报告了一个化学文库的试点筛选,该文库包含9600种结构不同的化合物,用于使用FID测定与特定miRNA前体结合的分子。(C) 2013 Elsevier Ltd.版权所有。
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. (C) 2013 Elsevier Ltd. All rights reserved.