Polycomb repressive complex 2 and its core component EZH2: potential targeted therapeutic strategies for head and neck squamous cell carcinoma

• Published in: Clinical epigenetics Vol. 16; no. 1; p. 54
• Main Authors: Cheng, Yuxi, Song, Zhengzheng, Fang, Xiaodan, Tang, Zhangui
• Format: Journal Article
• Language: English
• Published: Germany BioMed Central Ltd 10.04.2024; BioMed Central; BMC
• Subjects: Brain cancer; Carcinogenesis; Cell division; Drug therapy; EMT; Epigenetic inheritance; Epigenetics; EZH2; Gene expression; Genes; Genetic aspects; Head & neck cancer; Head and neck carcinoma; Head and neck squamous cell carcinoma; Health aspects; Insects; Medical research; Metastases; Metastasis; Mutation; Oral carcinoma; Oral squamous cell carcinoma; Pluripotency; Polycomb group proteins; Polycomb repressive complex; PRC2; Prognosis; Proteins; Review; Squamous cell carcinoma; Stat3 protein; Stem cells; Transcription factors; Transcription regulation; Tumors; China; PRC2; Targeted therapy; Head and neck squamous cell carcinoma; Polycomb repressive complex; EMT; EZH2; Transcription regulation
• ISSN: 1868-7083; 1868-7075; 1868-7083; 1868-7075
• DOI: 10.1186/s13148-024-01666-2

The polycomb group (PcG) comprises a set of proteins that exert epigenetic regulatory effects and play crucial roles in diverse biological processes, ranging from pluripotency and development to carcinogenesis. Among these proteins, enhancer of zeste homolog 2 (EZH2) stands out as a catalytic component of polycomb repressive complex 2 (PRC2), which plays a role in regulating the expression of homologous (Hox) genes and initial stages of x chromosome inactivation. In numerous human cancers, including head and neck squamous cell carcinoma (HNSCC), EZH2 is frequently overexpressed or activated and has been identified as a negative prognostic factor. Notably, EZH2 emerges as a significant gene involved in regulating the STAT3/HOTAIR axis, influencing HNSCC proliferation, differentiation, and promoting metastasis by modulating related oncogenes in oral cancer. Currently, various small molecule compounds have been developed as inhibitors specifically targeting EZH2 and have gained approval for treating refractory tumors. In this review, we delve into the epigenetic regulation mediated by EZH2/PRC2 in HNSCC, with a specific focus on exploring the potential roles and mechanisms of EZH2, its crucial contribution to targeted drug therapy, and its association with cancer markers and epithelial-mesenchymal transition. Furthermore, we aim to unravel its potential as a therapeutic strategy for oral squamous cell carcinoma.