Jiangsu Key Laboratory of Drug Design and Optimization, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Jiangsu Key Laboratory of Drug Design and Optimization, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Eur J Med Chem. 2020 Jun 15;196:112325. doi: 10.1016/j.ejmech.2020.112325. Epub 2020 Apr 15.
N-methyladenosine (mA) is the most abundant internal post-transcriptional modification in eukaryotic mRNA. The development of emerging technologies such as mA-seq, has helped reveal the fundamental role of mA-RNA in regulation of the mammalian transcriptome. With the identification and advances in the understanding of mA modulators, the relationship between mA and human diseases is gradually being revealed. This review summarizes recent progress in the understanding of the role of mA modulators in human disease and their structural characteristics. We highlight the potential of small-molecule regulators targeting mA associated proteins as tool molecules and disease treatment options from the medicinal chemistry perspective.
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 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。本文综述了近年来人们对 m6A 调节剂在人类疾病中的作用及其结构特征的理解的最新进展。我们从药物化学的角度强调了针对 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。