Despite intense research efforts, our pharmaceutical repertoire against high-grade brain tumours has not been able to increase patient survival for a decade and life expectancy remains at less than 16 months after diagnosis, on average. Inhibitors of protein arginine methyltransferases (PRMTs) have been developed and investigated over the past 15 years and have now entered oncology clinical trials, including for brain tumours. This review collates recent advances in the understanding of the role of PRMTs and arginine methylation in brain tumours. We provide an up-to-date literature review on the mechanisms for PRMT regulation. These include endogenous modulators such as alternative splicing, miRNA, post-translational modifications and PRMT–protein interactions, and synthetic inhibitors. We discuss the relevance of PRMTs in brain tumours with a particular focus on PRMT1, -2, -5 and -8. Finally, we include a future perspective where we discuss possible routes for further research on arginine methylation and on the use of PRMT inhibitors in the context of brain tumours.

尽管进行了大量的研究工作，我们针对高级别脑肿瘤的药物组合在十年内仍无法提高患者的生存率，诊断后的平均预期寿命仍不足 16 个月。蛋白质精氨酸甲基转移酶 (PRMT) 抑制剂在过去 15 年中得到了开发和研究，现已进入肿瘤学临床试验，包括脑肿瘤的临床试验。这篇综述整理了在理解 PRMT 和精氨酸甲基化在脑肿瘤中的作用方面的最新进展。我们提供有关 PRMT 监管机制的最新文献综述。其中包括内源性调节剂，如选择性剪接、miRNA、翻译后修饰和 PRMT-蛋白质相互作用，以及合成抑制剂。我们讨论 PRMT 在脑肿瘤中的相关性，特别关注 PRMT1、-2、-5 和 -8。最后，我们展望了未来的前景，讨论了进一步研究精氨酸甲基化以及在脑肿瘤中使用 PRMT 抑制剂的可能途径。