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Updated: Jun 4, 2025

Quantitative Methods to Study Protein Arginine Methyltransferase 1-9 Activity in Cells
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Protein arginine methyltransferase 7 modulators in disease therapy: Current progress and emerged opportunity

Dongmin Yu1, Limei Zeng2, Yuqi Wang3

  • 1Department of Breast Disease Comprehensive Center, First Affiliated Hospital of Gannan Medical University, Ganzhou, 341000, China.

Bioorganic Chemistry
|December 29, 2024
PubMed

Insights

Protein arginine methyltransferase 7 (PRMT7) is crucial for cell function and implicated in cancer. This review details PRMT7 inhibitors and their potential for developing novel anti-tumor therapeutics.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Pharmacology

Background:

  • Protein arginine methyltransferase 7 (PRMT7) is a key epigenetic regulator in eukaryotes.
  • PRMT7 dysregulation is linked to various human diseases, especially cancer.
  • PRMT7 influences critical cellular processes like growth, migration, invasion, apoptosis, and drug resistance in cancers.

Purpose of the Study:

  • To provide a comprehensive overview of PRMT7 structure, function, and disease associations.
  • To summarize current PRMT7 inhibitors in clinical trials and their structural characteristics.
  • To highlight recent advancements in PRMT7 modulator design and development for cancer therapy.

Main Methods:

  • Literature review of PRMT7 research and drug development.
  • Analysis of PRMT7 inhibitor structures and clinical trial data.
  • Evaluation of rational design, pharmacodynamics, and pharmacokinetics of PRMT7 modulators.

Main Results:

  • Overview of PRMT7's biological roles and disease connections.
  • Summary of PRMT7 inhibitors, including those in clinical trials and co-crystal structures.
  • Discussion of novel PRMT7 modulators, encompassing isoform-selective, non-selective, and dual-target inhibitors.

Conclusions:

  • PRMT7 is a promising therapeutic target for anti-tumor drug discovery.
  • Recent progress shows potential in developing effective PRMT7-targeting agents.
  • Further research is needed to address challenges and advance PRMT7-based cancer therapies.
Keywords:
ChallengesInhibitorsModulatorsProtein arginine methyltransferase 7

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