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首页> 外文期刊>Chemistry: A European journal >Oncogenic MicroRNAs Biogenesis as a Drug Target: Structure-Activity Relationship Studies on New Aminoglycoside Conjugates
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Oncogenic MicroRNAs Biogenesis as a Drug Target: Structure-Activity Relationship Studies on New Aminoglycoside Conjugates

机译：致癌MicroRNAs生物发生作为药物靶标：新的氨基糖苷结合物的结构-活性关系研究

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摘要

MicroRNAs (miRNAs) are a recently discovered category of small RNA molecules that regulate gene expression at the post-transcriptional level. Accumulating evidence indicates that miRNAs are aberrantly expressed in a variety of human cancers and that the inhibition of these oncogenic miRNAs could find application in the therapy of different types of cancer. Herein, we describe the synthesis and biological evaluation of new small-molecule drugs that target oncogenic miRNAs production. In particular, we chose to target two miRNAs (i.e., miRNA-372 and -373) implicated in various types of cancer, such as gastric cancer. Their precursors (pre-miRNAs) are overexpressed in cancer cells and lead to mature miRNAs after cleavage of their stem-loop structure by the enzyme Dicer in the cytoplasm. Some of the newly synthesized conjugates can inhibit Dicer processing of the targeted pre-miRNAs in vitro with increased efficacy relative to our previous results (D.D. Vo etal., ACS Chem. Biol. 2014, 9, 711-721) and, more importantly, to inhibit proliferations of adenocarcinoma gastric cancer (AGS) cells overexpressing these miRNAs, thus representing promising leads for future drug development.
机译：MicroRNA（miRNA）是最近发现的在转录后水平上调节基因表达的小RNA分子类别。越来越多的证据表明，miRNA在多种人类癌症中异常表达，并且抑制这些致癌性miRNA可以用于治疗不同类型的癌症。在本文中，我们描述了靶向致癌性miRNA生产的新型小分子药物的合成和生物学评估。特别是，我们选择靶向与多种类型的癌症（例如胃癌）有关的两个miRNA（即miRNA-372和-373）。它们的前体（pre-miRNA）在癌细胞中过表达，并在细胞质中被切酶酶切开其茎环结构后导致成熟的miRNA。相对于我们先前的结果（DD Vo等人，ACS Chem。Biol。2014，9，711-721），一些新合成的结合物可以在体外抑制Dicer对靶标pre-miRNA的加工，并具有更高的功效，更重要的是，抑制过度表达这些miRNA的腺癌胃癌（AGS）细胞的增殖，从而代表了未来药物开发的有希望的线索。

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