Related Experiment Video
Updated: May 22, 2026
08:11
Quantitative Methods to Study Protein Arginine Methyltransferase 1-9 Activity in Cells
Published on: August 7, 2021
Update on the Development of Targeting Arginine Methyltransferase PRMT5 in Cancer Research
Hongyu Zeng1, Yiyu Long1, Yangrui Peng2
1School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products and Yunnan College of Modern Biomedical Industry, Kunming Medical University, Kunming 650500, China.
Current Topics in Medicinal Chemistry
|May 21, 2026
Summary
Protein Arginine Methyltransferase 5 (PRMT5) drives cancer by affecting gene expression and cell growth. New PROTACs offer a novel strategy to degrade PRMT5, potentially overcoming resistance to existing inhibitors.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Protein Arginine Methyltransferase 5 (PRMT5) is a key regulator of cellular processes, and its overexpression is linked to various cancers.
- PRMT5 promotes tumorigenesis through gene silencing, oncogenic pathway activation, and immune evasion.
- Methylthioadenosine Phosphorylase (MTAP)-deficient tumors present a synthetic lethal vulnerability due to PRMT5 inhibitor accumulation.
Purpose of the Study:
- To review current understanding of PRMT5 in tumorigenesis and tumor immunology.
- To analyze structure-activity relationships of PRMT5 inhibitors.
- To chart clinical progress of different PRMT5-targeting modalities.
Main Methods:
- Literature review synthesizing insights into PRMT5-driven cancer.
- Analysis of PRMT5 inhibitors including SAM-competitive, substrate-competitive, MTA-cooperative, and PROTAC-based drugs.
- Discussion of clinical trial progress and therapeutic strategies.
Main Results:
- PRMT5 overexpression is a validated oncogenic driver across multiple malignancies.
- Despite numerous clinical trials, no PRMT5 inhibitors have gained regulatory approval.
- Proteolysis-Targeting Chimeras (PROTACs) represent a promising next-generation strategy for PRMT5 degradation.
Conclusions:
- Targeting PRMT5 is crucial for cancer therapy, but challenges remain with current inhibitors.
- Novel strategies like PROTACs offer a distinct approach to overcome resistance.
- Precision medicine and combination therapies are essential to maximize PRMT5 targeting efficacy.
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