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Updated: Aug 5, 2026

Dot Blot Assay for Detecting Global N6-Methyladenosine RNA Modification Levels
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Dot Blot Assay for Detecting Global N6-Methyladenosine RNA Modification Levels

Published on: February 6, 2026

m1A and m6A RNA Methylations as Druggable Targets in Cancer

Yasemin Gazaloğlu1, Buket Sağlam-Şen1, Bünyamin Akgül1

  • 1Noncoding RNA Laboratory, Department of Molecular Biology and Genetics, İzmir Institute of Technology, 35430 Izmir, Türkiye.

Pharmaceuticals (Basel, Switzerland)
|July 28, 2026
PubMed

Insights

Epitranscriptomic RNA modifications like N6-methyladenosine (m6A) and N1-methyladenosine (m1A) are key in cancer. Targeting these modifications, from small molecules to PROTACs, offers new therapeutic strategies for oncology.

Area of Science:

  • Molecular Biology
  • Cancer Research
  • Pharmacology

Background:

  • Epitranscriptomic modifications, especially RNA methylations, regulate gene expression and are implicated in cancer development and spread.
  • N6-methyladenosine (m6A) primarily affects mRNA turnover, while N1-methyladenosine (m1A) influences translation and cellular stress response in malignant cells.
  • These methylation marks exhibit crosstalk via shared regulatory proteins, complicating therapeutic targeting.

Purpose of the Study:

  • To review the therapeutic landscape of m6A and m1A modifications in cancer treatment.
  • To analyze current and emerging pharmacological strategies targeting the m6A and m1A regulatory machinery.
  • To discuss clinical progress and challenges in developing epitranscriptomic-based cancer therapies.

Main Methods:

  • Comprehensive analysis of existing literature on m6A and m1A targeting strategies.
  • Evaluation of small-molecule inhibitors and proteolysis-targeting chimeras (PROTACs) for m6A regulators (METTL3, FTO, ALKBH5).
  • Assessment of tRNA methyltransferase 6/61A (TRMT6/61A) and AlkB homolog 1-3 (ALKBH1-3) as potential m1A therapeutic targets.

Main Results:

  • Pharmacological targeting of m6A regulators has evolved from traditional inhibitors to innovative PROTACs.
  • The m1A machinery, including TRMT6/61A writers and ALKBH1-3 erasers, presents novel therapeutic opportunities.
  • Despite progress, challenges like off-target toxicity, pharmacokinetics, and resistance mechanisms need addressing.

Conclusions:

  • Targeting RNA methylation pathways offers promising avenues for cancer therapy.
  • Precision therapies and site-specific modulation are crucial for overcoming current translational obstacles.
  • The future of oncology may involve sophisticated epitranscriptomic-based treatments for enhanced efficacy.
Keywords:
RNA modificationsadenosine methylationsepitranscriptomicsproteolysis-targeting chimeras (PROTACs)small molecule inhibitorstargeted cancer therapytranslational reprogramming

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