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Small-Molecule Inhibitors Targeting RNA m6A Modifiers for Cancer Therapeutics: Latest Advances and Future

Hairong Tang1,2,3, Ruijia Zhang1,2, Ao Zhang1,2,4,5,6

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Small molecule inhibitors targeting oncogenic N6-methyladenosine (m6A) modifying proteins represent a promising cancer therapy. Recent advances and future directions in this RNA epigenetic drug discovery field are discussed.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • N6-methyladenosine (m6A) is a prevalent RNA modification crucial for RNA metabolism and protein expression.
  • Dysregulated m6A modifications and aberrant m6A modifiers are linked to cancer initiation, progression, metastasis, metabolism, and immune evasion.

Purpose of the Study:

  • To review the latest advances in small molecule inhibitors targeting oncogenic m6A modifying proteins.
  • To discuss limitations, challenges, and future prospects in RNA m6A epigenetic drug discovery for cancer therapy.

Main Methods:

  • This perspective synthesizes recent research findings on small molecule inhibitors of m6A modifying proteins.
  • It analyzes the therapeutic potential and challenges in developing these inhibitors for cancer treatment.

Main Results:

  • The development of small molecule inhibitors targeting m6A modifying proteins is an emerging and effective cancer therapeutic strategy.
  • The first-in-class METTL3 inhibitor STC-15 has entered clinical trials, demonstrating progress in this field.

Conclusions:

  • Pharmacological inhibition of dysregulated oncogenic m6A modifying proteins offers a novel therapeutic avenue for cancer.
  • Further research and development are needed to overcome challenges and optimize RNA m6A epigenetic drug discovery for cancer treatment.