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小分子靶向 RNA G-四链体用于药物发现的最新进展。

Recent advances in the development of small molecules targeting RNA G-quadruplexes for drug discovery.

机构信息

State Key Laboratory of Agricultural Microbiology, Huazhong Agricultural University, Wuhan 430070, China; National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, College of Veterinary Medicine, Huazhong Agricultural University, Wuhan 430070, China.

State Key Laboratory of Agricultural Microbiology, Huazhong Agricultural University, Wuhan 430070, China; Department of Chemistry, College of Science, Huazhong Agricultural University, Wuhan 430070, China.

出版信息

Bioorg Chem. 2021 May;110:104804. doi: 10.1016/j.bioorg.2021.104804. Epub 2021 Mar 6.

DOI:10.1016/j.bioorg.2021.104804
PMID:33740677
Abstract

Extensive evidence indicates that RNA G-quadruplexes have associated with some important cellular events. Investigation of RNA G-quadruplexes is thus vital to revealing their biofunctions. Several small molecules have been developed to target RNA G-quadruplexes to date. Some of the small molecules showed significantly light-up fluorescence signals upon binding to RNA G-quadruplexes, while some of them regulated the biofunctions of RNA G-quadruplexes. In this mini-review, the small molecules divided into four kinds are expounded which focused mainly on their structural features and biological activities. Moreover, we raised the current challenges and promising prospects. This mini-review might contribute to exploiting more sophisticated small molecules targeting RNA G-quadruplexes with high specificity based on the reported chemical structural features.

摘要

大量证据表明,RNA 四链体与一些重要的细胞事件有关。因此,研究 RNA 四链体对于揭示其生物功能至关重要。迄今为止,已经开发出几种小分子来靶向 RNA 四链体。一些小分子在与 RNA 四链体结合时显示出明显的荧光信号增强,而另一些小分子则调节 RNA 四链体的生物功能。在这篇迷你综述中,我们主要阐述了分为四类的小分子,重点介绍了它们的结构特征和生物活性。此外,我们还提出了当前的挑战和有前途的前景。本综述可能有助于根据报道的化学结构特征,开发出更多针对 RNA 四链体的具有高特异性的复杂小分子。

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