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Treating human cancer by targeting EZH2
Mengfei Xu1,2, Chunyan Xu1, Rui Wang1,2
1The Second Clinical Medical College, Guangzhou University of Chinese Medicine, Guangzhou, Guangdong 510120, China.
Abstract:
Enhancer of zeste homolog 2 (EZH2), an epigenetic regulator that primarily inhibits downstream gene expression by tri-methylating histone H3, which is usually overexpressed in tumors and participates in many processes such as tumor occurrence and development, invasion, migration, drug resistance, and anti-tumor immunity as an oncogene, making it an important biomarker in cancer therapy. Collectively, several transcription factors and RNAs cooperate to facilitate the elevated expression of EZH2 in cancer. Although the significance of blocking EZH2 in cancer for inhibiting cancer progression is widely recognized, the clinical application of EZH2 inhibitors continues to encounter numerous challenges. In this review, drawing upon our comprehensive understanding of the factual underpinnings of EZH2's role in cancer, we aim to clarify the crucial importance of targeting EZH2 in cancer treatment. Furthermore, we summarize the current research landscape surrounding targeted EZH2 inhibitors and offer insights into potential future applications of these inhibitors.
Insights
Enhancer of zeste homolog 2 (EZH2) is an oncogene overexpressed in tumors, driving cancer progression. Targeting EZH2 is crucial for cancer therapy, though clinical applications face challenges.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Enhancer of zeste homolog 2 (EZH2) is an epigenetic regulator overexpressed in various tumors.
- EZH2 acts as an oncogene, promoting tumor occurrence, development, invasion, migration, drug resistance, and impacting anti-tumor immunity.
- Elevated EZH2 expression in cancer is facilitated by cooperating transcription factors and RNAs.
Purpose of the Study:
- To clarify the critical importance of targeting EZH2 in cancer treatment.
- To summarize the current research landscape of targeted EZH2 inhibitors.
- To offer insights into potential future applications of EZH2 inhibitors in oncology.
Main Methods:
- This review synthesizes current research on EZH2's role in cancer.
- Literature review focusing on EZH2's function, overexpression mechanisms, and therapeutic targeting.
- Analysis of existing and potential EZH2 inhibitors and their clinical challenges.
Main Results:
- EZH2 plays a multifaceted role as an oncogene in cancer progression and metastasis.
- Several factors contribute to EZH2 overexpression in malignant tumors.
- Targeting EZH2 holds significant therapeutic potential despite current clinical hurdles.
Conclusions:
- Targeting EZH2 is a promising strategy for cancer therapy due to its oncogenic functions.
- Overcoming challenges in the clinical application of EZH2 inhibitors is essential for effective cancer treatment.
- Further research into EZH2 inhibitors may unlock new therapeutic avenues for various cancers.
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