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Single-molecule Manipulation of G-quadruplexes by Magnetic Tweezers
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Published on: September 19, 2017

Natural G-Quadruplex Stabilizers: A Targeted Strategy for Breast Cancer Therapy

Chengjian Cao1, Chaoxiang Lv2, Ali ElFar2

  • 1Zigong Academy of Medical Sciences, Zigong First People's Hospital, Zigong, Sichuan, People's Republic of China.

Drug Design, Development and Therapy
|June 1, 2026
PubMed

Insights

Natural compounds can stabilize G-quadruplexes (G4s), crucial in cancer gene regulation. This review explores natural G4 stabilizers for breast cancer (BC) therapy, highlighting their potential and research gaps.

Area of Science:

  • Genomics and Molecular Biology
  • Pharmacology and Drug Discovery
  • Oncology

Background:

  • G-quadruplexes (G4s) are non-canonical DNA structures vital for gene regulation, telomere maintenance, and implicated in cancer development.
  • Breast cancer (BC) exhibits G4 enrichment in oncogene promoters (e.g., c-MYC, HER2), presenting therapeutic targets.
  • While synthetic G4 stabilizers are studied, natural products offer a less explored avenue for selective, biocompatible, and multi-target ligands.

Purpose of the Study:

  • To systematically review and analyze natural compounds with G4-stabilizing effects, focusing on their potential application in breast cancer (BC).
  • To define the interactions between G4 ligands and map these compounds to BC-associated genomic regions.
  • To identify research gaps and propose a roadmap for natural G4 stabilizer drug discovery for BC.

Main Methods:

  • Systematic literature review and analysis of natural compounds (flavonoids, alkaloids, polyphenols, terpenoids, organosulfur compounds) exhibiting G4-stabilizing properties.
  • Landscape approach to define G4-ligand interactions, including stabilization mechanisms (π-π stacking, electrostatic interactions, groove binding).
  • Mapping of identified compounds to genomic regions associated with G4 formation in breast cancer.

Main Results:

  • Identified various natural compound classes with G4-stabilizing effects, showing potential for BC therapy.
  • Detailed interactions between G4 ligands and stabilization mechanisms were analyzed.
  • Key research gaps identified: limited in vivo validation, lack of subtype-specific efficacy data, and pharmacokinetic challenges.

Conclusions:

  • Natural G4 stabilizers demonstrate promise as multi-target, biocompatible agents for breast cancer (BC) therapy.
  • Current effectiveness is limited by insufficient in vivo studies and subtype-specific data.
  • A prospective roadmap involving in silico docking, mechanistic studies, and translational strategies is proposed for future drug discovery.
Keywords:
G-quadruplexesG4 stabilizersbreast cancerdrug discoveryfuture roadmapnatural products

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