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Recent developments of small molecules targeting RNA m6A modulators.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-04-15 , DOI: 10.1016/j.ejmech.2020.112325
Jing Gu 1 , Jun Xu 1 , Qidong You 1 , Xiaoke Guo 1
Affiliation  

N6-methyladenosine (m6A) is the most abundant internal post-transcriptional modification in eukaryotic mRNA. The development of emerging technologies such as m6A-seq, has helped reveal the fundamental role of m6A-RNA in regulation of the mammalian transcriptome. With the identification and advances in the understanding of m6A modulators, the relationship between m6A and human diseases is gradually being revealed. This review summarizes recent progress in the understanding of the role of m6A modulators in human disease and their structural characteristics. We highlight the potential of small-molecule regulators targeting m6A associated proteins as tool molecules and disease treatment options from the medicinal chemistry perspective.

中文翻译:

靶向RNA m6A调节剂的小分子的最新发展。

N6-甲基腺苷(m6A)是真核mRNA中最丰富的内部转录后修饰。m6A-seq等新兴技术的发展有助于揭示m6A-RNA在调节哺乳动物转录组中的基本作用。随着对m6A调节剂的鉴定和理解的进步,m6A与人类疾病之间的关系逐渐被揭示。这篇综述总结了在理解m6A调节剂在人类疾病中的作用及其结构特征方面的最新进展。我们从药物化学的角度强调了靶向m6A相关蛋白的小分子调节剂作为工具分子和疾病治疗选择的潜力。
更新日期:2020-04-21
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