N<sup>6</sup>-甲基腺嘌呤去甲基化酶抑制剂研究进展

N⁶-甲基腺嘌呤去甲基化酶抑制剂研究进展

摘要: N⁶-甲基腺嘌呤（N⁶-methyladenine，m⁶A）修饰作为信使RNA中广泛存在的一种甲基化修饰，它的动态变化在生命活动和疾病的发生发展中发挥着重要的作用。近年来研究发现，通过改变靶基因的m⁶A修饰水平可以调控肿瘤的进展，因此，通过小分子靶向干预m⁶A去甲基化酶可作为抗肿瘤的新策略。本文重点讨论了m⁶A去甲基化酶，包括脂肪含量与肥胖相关蛋白（fat mass and obesity-associated protein，FTO）和AlkB同源蛋白5（AlkB homlog5，ALKBH5）的作用方式以及它们在肿瘤中发挥的生物学功能，并总结了m⁶A去甲基化酶小分子抑制剂的研究进展。

Abstract: N⁶-methyladenine (m⁶A) modification, the most abundant and dynamic chemical modification on messenger RNA, plays an essential role in physiological and pathological progress.Recent studies have found that tumor progression can be affected by altering the m⁶A modification level of target genes. Therefore, small molecule targeted m⁶A demethylase can be used as a new anti-tumor strategy.This review focuses on the regulatory mechanism of m⁶A demethylases, including fat mass and obesity-associated protein (FTO) and AlkB homlog 5 (ALKBH5), as well as their biological functions in tumors, and summarizes the research progress of their small molecule inhibitors.