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Related Experiment Videos

Drugging the "undruggable" microRNAs.

Dejun Liu1, Xinqiang Wan2, Xiangxiang Shan3

  • 1The Yancheng Clinical College of Xuzhou Medical University, Yancheng, 224001, China.

Cellular and Molecular Life Sciences : CMLS
|October 14, 2020
PubMed
Summary

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Small molecules can now target microRNAs (miRNAs), previously considered undruggable gene regulators. This review covers small-molecule inhibitors (SMIs) and degraders (SMDs) for novel miRNA-targeted therapeutics and cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • MicroRNAs (miRNAs) are crucial gene regulators with therapeutic potential.
  • RNAs, including miRNAs, were historically considered undruggable targets.
  • Previous therapeutic strategies focused on synthetic oligonucleotides for miRNA regulation.

Purpose of the Study:

  • To review emerging small-molecule inhibitors (SMIs) and small-molecule degraders (SMDs) for targeting miRNAs.
  • To summarize strategies for discovering SMIs and developing SMDs.
  • To introduce applications of SMIs and SMDs in miRNA inhibition and cancer therapy.

Main Methods:

  • Literature review of recent findings on small molecules targeting miRNAs.
  • Summary of methodologies for SMI discovery and SMD development.
Keywords:
Cancer therapyDrug developmentMicroRNASmall-molecule degraderSmall-molecule inhibitor

Related Experiment Videos

  • Analysis of reported applications in miRNA inhibition and oncology.

    • Main Results:

    • Small molecules, including SMIs and SMDs, can directly target and modulate miRNA activity.
    • SMIs inhibit miRNA biogenesis by direct binding.
    • SMDs induce miRNA degradation through a bifunctional mechanism.

    Conclusions:

    • SMIs and SMDs offer potent and specific inhibition of miRNAs.
    • These small molecules represent a novel therapeutic avenue for previously undruggable miRNA targets.
    • The development of SMIs and SMDs holds promise for future miRNA-based therapeutics, particularly in cancer treatment.