Surgical Neurology Branch, National Institute of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, MD 20892, USA.
Cells. 2021 Jan 11;10(1):124. doi: 10.3390/cells10010124.
Protein arginine methylation is a common post-translational modification that plays a pivotal role in cellular regulation. Protein arginine methyltransferases (PRMTs) catalyze the modification of target proteins by adding methyl groups to the guanidino nitrogen atoms of arginine residues. Protein arginine methylation takes part in epigenetic and cellular regulation and has been linked to neurodegenerative diseases, metabolic diseases, and tumor progression. Aberrant expression of PRMTs is associated with the development of brain tumors such as glioblastoma and medulloblastoma. Identifying PRMTs as plausible contributors to tumorigenesis has led to preclinical and clinical investigations of PRMT inhibitors for glioblastoma and medulloblastoma therapy. In this review, we discuss the role of arginine methylation in cancer biology and provide an update on the use of small molecule inhibitors of PRMTs to treat glioblastoma, medulloblastoma, and other cancers.
蛋白质精氨酸甲基化是一种常见的翻译后修饰，在细胞调节中起着关键作用。蛋白质精氨酸甲基转移酶（PRMTs）通过向精氨酸残基的胍氮原子添加甲基基团来催化靶蛋白的修饰。蛋白质精氨酸甲基化参与表观遗传和细胞调节，与神经退行性疾病、代谢疾病和肿瘤进展有关。PRMTs 的异常表达与脑肿瘤的发展有关，如神经胶质瘤和髓母细胞瘤。将 PRMTs 鉴定为肿瘤发生的合理贡献者，导致了针对神经胶质瘤和髓母细胞瘤治疗的 PRMT 抑制剂的临床前和临床研究。在这篇综述中，我们讨论了精氨酸甲基化在癌症生物学中的作用，并介绍了 PRMTs 的小分子抑制剂治疗神经胶质瘤、髓母细胞瘤和其他癌症的最新进展。
