Protein arginine methyltransferase 5: a potential cancer therapeutic target



PRMT5 is a type II protein arginine methyltransferase that methylates histone or non-histone proteins. Arginine methylation by PRMT5 has been implicated in gene transcription, ribosome biogenesis, RNA transport, pre-mRNA splicing and signal transduction. High expression of PRMT5 has been observed in various cancers and PRMT5 overexpression has been reported to improve cancer cell survival, proliferation, migration and metabolism and to inhibit cancer cell apoptosis. In addition, PRMT5 has been found to be required for cancer stem cell survival, self-renewal and differentiation. Several microRNAs have been shown to regulate PRMT5 expression. As PRMT5 has oncogene-like properties, several PRMT5 inhibitors have been used to explore their efficacy as potential drugs for different types of cancer, and three of them are now being tested in clinical trials.


In this review, we summarize current knowledge on the role of PRMT5 in cancer development and progression, including its functions and underlying mechanisms. In addition, we highlight the rapid development of PRMT5 inhibitors and summarize ongoing clinical trials for cancer therapy. By affecting both tumor cells and the tumor microenvironment, PRMT5 inhibitors may serve as effective anti-cancer agents, especially when combined with immune therapies.

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This study was supported by grants from the National Key R&D Program of China (2019YFA0111000), the Shanghai Science and Technology Committee (20ZR1448900), the Shanghai Healthy Committee (202040121), the National Natural Science Foundation of China (No. 81671590) and the Innovative research team of high-level local universities in Shanghai.

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YY wrote the manuscript. HN provided direction and reviewed and revised the manuscript. Both authors read and approved the final version of the manuscript.

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Yuan, Y., Nie, H. Protein arginine methyltransferase 5: a potential cancer therapeutic target. Cell Oncol. 44, 33–44 (2021).

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  • PRMT5
  • Cancer
  • Arginine methylation
  • Regulation
  • Inhibitor therapy