Human MYC G-quadruplex: From discovery to a cancer therapeutic target

Area of Science:

• Oncology
• Molecular Biology
• Genetics

Background:

• MYC oncogene overexpression drives cancer initiation and progression.
• A G-quadruplex (G4) DNA structure in the MYC gene promoter is a potential therapeutic target.
• G4 structures are increasingly recognized as key regulators of gene expression.

Purpose of the Study:

• To review the MYC G4 structure, its formation, and its role in MYC gene regulation.
• To summarize proteins that interact with and modulate MYC G4 structures.
• To assess G4-binding molecules and their potential as anticancer therapeutics.

Main Methods:

• Literature review of studies on MYC G4 structure and function.
• Analysis of evidence for G4 formation in vitro and in cells.
• Summary of research on G4-interacting proteins and G4-binding molecules.

Main Results:

• The MYC gene contains a G4 structure in its promoter region (NHE III1).
• G4 structures play a functional role in regulating MYC transcription.
• Various proteins and small molecules interact with MYC G4, influencing its stability and function.

Conclusions:

• The MYC G4 structure is a validated target for cancer therapy.
• G4-stabilizing ligands, including small molecules and peptides, show anticancer activity.
• Targeting MYC G4 offers a promising strategy for novel cancer therapeutics.