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Current status and prospects of methylthioadenosine phosphorylase/protein arginine methyltransferase 5 target therapy

Jing Lin1, Huishan Zhang2, Hui Kang3

  • 1Department of Medical Oncology, Clinical Oncology School of Fujian Medical University, Fujian Cancer Hospital, Fuzhou, Fujian, 350000, China; Cancer Bio-Immunotherapy Center, Clinical Oncology School of Fujian Medical University, Fujian Cancer Hospital, Fuzhou, Fujian, 350000, China; Clinical Oncology School of Fujian Medical University, Fujian Cancer Hospital NHC Key Laboratory of Cancer Metabolism, China.

Biochemical Pharmacology
|November 28, 2025
PubMed

Insights

Methylthioadenosine phosphorylase (MTAP) and protein arginine methyltransferase 5 (PRMT5) are key cancer targets. MTAP-deficient tumors show synthetic lethality with PRMT5 inhibition, offering new therapeutic avenues.

Area of Science:

  • Oncology
  • Biochemistry
  • Molecular Biology

Background:

  • Methylthioadenosine phosphorylase (MTAP) and protein arginine methyltransferase 5 (PRMT5) are critical in cancer.
  • MTAP absence elevates methylthioadenosine (MTA), an endogenous PRMT5 inhibitor.
  • PRMT5 regulates cell cycle, differentiation, and DNA repair via arginine methylation.

Purpose of the Study:

  • To review the significance of MTAP/PRMT5 as cancer therapeutic targets.
  • To summarize the current research status of MTAP/PRMT5-targeted therapies.
  • To highlight challenges and future directions in MTAP/PRMT5-targeted cancer treatment.

Main Methods:

  • Literature review of MTAP/PRMT5 in cancer therapy.
  • Analysis of PRMT5 inhibitor efficacy in MTAP-null models.
  • Discussion of challenges including toxicity and heterogeneity.

Main Results:

  • PRMT5 inhibitors demonstrate anti-tumor activity in MTAP-null cancers.
  • MTAP-depleted tumors exhibit synthetic lethality with PRMT5 inhibition.
  • Therapies face challenges: off-target toxicity, normal tissue effects, and tumor heterogeneity.

Conclusions:

  • MTAP/PRMT5 targeting offers novel therapeutic strategies for refractory cancers.
  • Optimization of drug design, combination therapies, and biomarker identification are crucial.
  • Future research aims to achieve precision medicine for improved patient outcomes.
Keywords:
Methylthioadenosine phosphorylaseProtein arginine methyltransferase 5Synthetic lethalityTargeted therapyTumour

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