蛋白精氨酸甲基转移酶（PRMTs）是催化目标蛋白甲基化的酶，在维持正常生理平衡中发挥着重要作用。PRMTs异常表达和增强的催化活性与癌症、炎症、免疫、代谢和神经退行性疾病等病理状态密切相关。因此，针对PRMTs的抑制剂的开发引起了制药行业和学术界的极大关注。本综述主要关注2019年以来关于肿瘤治疗中针对PRMTs的小分子抑制剂专利。同时，还讨论了其最新的临床发展情况。近年来，小分子PRMT抑制剂的发现，特别是PRMT5抑制剂在癌症治疗中的应用已成为一个快速扩展的研究领域。虽然已经开发出许多具有不同化学支架的有效PRMT抑制剂，其中九个已经进入了临床试验，但它们的支架相对较少。应该考虑亚型选择性来指导药物发现，因为非选择性抑制PRMTs可能引起不良药理效应。因此，开发具有异构体特异性和肿瘤偏向分布的新型有效抑制剂仍然是进一步研究的重要领域。

Protein arginine methyltransferases (PRMTs), enzymes catalyzing the methylation of target proteins, play an essential role in maintaining functional homeostasis in normal physiology. Aberrant expressions and enhanced enzymatic activities of PRMTs have been closely associated with pathological states such as cancer, inflammatory, immune, metabolic, and neurodegenerative diseases. Therefore, the development of inhibitors targeting PRMTs has attracted a great deal of attention in both pharmaceutical industries and academic community. This review focuses on the small-molecule inhibitors targeting PRMTs in cancer therapy in the patents published since 2019. The recent clinical development is also discussed here. In recent years, the discovery of small-molecule PRMT inhibitors, especially PRMT5 inhibitors has become a rapidly expanding research area for cancer therapy. Although a number of potent PRMT inhibitors with different chemical scaffolds have been developed and nine of them have entered into clinical trials, their scaffolds are relatively less diverse. Sub-type selectivity should be considered in drug discovery as nonselective inhibition of PRMTs may cause undesirable pharmacological effects. Hence, the development of new effective inhibitors with isoform-specific and tumor-biased distributions remains an important area for further studies.