Targeting EZH2 for cancer therapy: progress and perspective

Area of Science:

• Biochemistry
• Molecular Biology
• Oncology

Background:

• Enhancer of Zeste Homolog 2 (EZH2) is a key component of the Polycomb Repressive Complex 2 (PRC2).
• EZH2 catalyzes histone H3 lysine 27 di/trimethylation, regulating gene expression.
• Dysregulation of EZH2 is implicated in various cancers, highlighting its oncogenic role.

Purpose of the Study:

• To review current strategies for targeting EZH2 in cancer treatment.
• To evaluate existing compounds and agents that inhibit EZH2 function.
• To provide insights into future research directions for EZH2-targeted cancer therapies.

Main Methods:

• Comprehensive literature review of EZH2 structure, function, and PRC2 assembly.
• Analysis of molecular mechanisms for EZH2 recruitment to genomic regions.
• Discussion of EZH2 post-translational modifications.
• Evaluation of current EZH2 inhibitors and therapeutic strategies.

Main Results:

• EZH2 plays critical roles in development and its aberrant activity drives oncogenesis.
• Targeting EZH2 presents significant therapeutic potential in diverse cancer types.
• Current strategies focus on disrupting EZH2 enzymatic activity and protein interactions.

Conclusions:

• Understanding EZH2's structure, function, and regulation is crucial for developing effective cancer therapies.
• Novel strategies are needed to abolish EZH2-driven oncogenic effects.
• Further research into EZH2 pathways and inhibitors will advance cancer treatment options.