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The roles of EZH2 in cancer and its inhibitors
1Beijing Key Laboratory of Gene Resource and Molecular Development, Beijing Normal University, Beijing, China.
Abstract:
The enhancer of zeste homolog 2 (EZH2) is encoded by the Enhancer of zeste 2 polycomb repressive complex 2 subunit gene. EZH2 is involved in the cell cycle, DNA damage repair, cell differentiation, autophagy, apoptosis, and immunological modulation. The main function of EZH2 is to catalyze the methylation of H3 histone of H3K27Me3, which inhibits the transcription of target genes, such as tumor suppressor genes. EZH2 also forms complexes with transcriptions factors or directly binds to the promoters of target genes, leading to regulate gene transcriptions. EZH2 has been as a prominent target for cancer therapy and a growing number of potential targeting medicines have been developed. This review summarized the mechanisms that EZH2 regulates gene transcription and the interactions between EZH2 and important intracellular signaling molecules (Wnt, Notch, MEK, Akt) and as well the clinical applications of EZH2-targeted drugs.
Insights
The enhancer of zeste homolog 2 (EZH2) protein regulates gene transcription and is crucial in cell processes. EZH2 inhibitors are emerging as a promising strategy for cancer therapy.
Area of Science:
- Molecular Biology
- Epigenetics
- Cancer Research
Background:
- The enhancer of zeste homolog 2 (EZH2) is a key epigenetic regulator encoded by the Enhancer of zeste 2 polycomb repressive complex 2 subunit gene.
- EZH2 plays critical roles in cell cycle, DNA repair, differentiation, autophagy, apoptosis, and immune modulation.
Purpose of the Study:
- To review the mechanisms by which EZH2 regulates gene transcription.
- To explore the interactions between EZH2 and key intracellular signaling pathways.
- To summarize the clinical applications of EZH2-targeted cancer therapies.
Main Methods:
- Literature review of EZH2 functions and therapeutic targeting.
- Analysis of EZH2's role in gene transcription regulation.
- Examination of EZH2 interactions with Wnt, Notch, MEK, and Akt signaling pathways.
Main Results:
- EZH2 catalyzes H3K27Me3 methylation, inhibiting tumor suppressor gene transcription.
- EZH2 forms complexes with transcription factors and binds gene promoters to regulate transcription.
- EZH2 is implicated in various cellular processes and is a significant target in cancer therapy.
Conclusions:
- EZH2's multifaceted roles in gene regulation and cellular functions highlight its importance.
- Understanding EZH2's interactions with signaling pathways is crucial for developing effective cancer treatments.
- Targeting EZH2 presents a promising therapeutic avenue for various cancers, with several drugs in development.
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