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Updated: Nov 12, 2025

Exploring the Arginine Methylome by Nuclear Magnetic Resonance Spectroscopy
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Exploring the Arginine Methylome by Nuclear Magnetic Resonance Spectroscopy

Published on: December 16, 2021

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Protein arginine methylation: from enigmatic functions to therapeutic targeting

Qin Wu1,2,3,4, Matthieu Schapira2,5, Cheryl H Arrowsmith2,3,4

  • 1School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China.

Nature Reviews. Drug Discovery
|March 20, 2021
PubMed

Insights

Protein arginine methyltransferases (PRMTs) are key targets for cancer therapy. Research explores how PRMTs fuel cancer cells, leading to new inhibitor development and potential combination treatments.

Area of Science:

  • Biochemistry and Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • Protein arginine methyltransferases (PRMTs) play critical roles in fundamental cellular processes including transcription, splicing, RNA biology, DNA damage response, and metabolism.
  • Dysregulation of these processes is implicated in various diseases, particularly cancer, making PRMTs attractive therapeutic targets.

Purpose of the Study:

  • To elucidate the mechanistic roles of PRMTs in cancer cell metabolism and identify them as therapeutic targets in oncology.
  • To review ongoing inhibitor development and clinical programs for PRMTs, focusing on PRMT1 and PRMT5.
  • To explore the potential of PRMTs in regulating immune cells, cardiovascular function, and neuronal function for synergistic combination therapies.

Main Methods:

  • Utilizing structural biology to facilitate inhibitor development for PRMTs.
  • Employing genetic and chemical tools for in-depth mechanistic investigations.
  • Analyzing the roles of PRMTs in various cellular and physiological contexts.

Main Results:

  • Development of tool compounds for most PRMTs, with clinical programs advanced for PRMT1 and PRMT5.
  • Delineation of PRMT roles in cancer cell metabolism, immune cell regulation, and cardiovascular/neuronal function.
  • Identification of potential synergistic targets involving PRMT pathways for cancer combination therapies.

Conclusions:

  • Targeting PRMTs offers a promising strategy for cancer therapy, supported by ongoing inhibitor development and mechanistic studies.
  • Further research into arginine methylation functions will guide future clinical development and may uncover new therapeutic indications.
  • Understanding PRMTs' roles in diverse biological systems can lead to novel combination treatment strategies.

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