Targeting EZH2 in Cancer: Mechanisms, Pathways, and Therapeutic Potential
Enhancer of zeste homolog 2 (EZH2) is a methyltransferase involved in cell cycle regulation, cell differentiation, and cell death and plays a role in modulating the immune response. Although it mainly functions by catalyzing the tri-methylation of H3 histone on K27 (H3K27), to inhibit the transcript...
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MDPI AG
2024-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/29/24/5817 |
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| author | Maria Saveria Gilardini Montani Rossella Benedetti Mara Cirone |
| author_facet | Maria Saveria Gilardini Montani Rossella Benedetti Mara Cirone |
| author_sort | Maria Saveria Gilardini Montani |
| collection | DOAJ |
| description | Enhancer of zeste homolog 2 (EZH2) is a methyltransferase involved in cell cycle regulation, cell differentiation, and cell death and plays a role in modulating the immune response. Although it mainly functions by catalyzing the tri-methylation of H3 histone on K27 (H3K27), to inhibit the transcription of target genes, EZH2 can directly methylate several transcription factors or form complexes with them, regulating their functions. EZH2 expression/activity is often dysregulated in cancer, contributing to carcinogenesis and immune escape, thereby representing an important target in anti-cancer therapy. This review summarizes some of the mechanisms through which EZH2 regulates the expression and function of tumor suppressor genes and oncogenic molecules such as STAT3, mutant p53, and c-Myc and how it modulates the anti-cancer immune response. The influence of posttranslational modifications on EZH2 activity and stability and the possible strategies leading to its inhibition are also reviewed. |
| format | Article |
| id | doaj-art-33ac5686d2044792ba5eff6802df12c2 |
| institution | DOAJ |
| issn | 1420-3049 |
| language | English |
| publishDate | 2024-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj-art-33ac5686d2044792ba5eff6802df12c22025-08-20T02:39:41ZengMDPI AGMolecules1420-30492024-12-012924581710.3390/molecules29245817Targeting EZH2 in Cancer: Mechanisms, Pathways, and Therapeutic PotentialMaria Saveria Gilardini Montani0Rossella Benedetti1Mara Cirone2Department of Experimental Medicine, Sapienza University of Rome, 00161 Rome, ItalyDepartment of Experimental Medicine, Sapienza University of Rome, 00161 Rome, ItalyDepartment of Experimental Medicine, Sapienza University of Rome, 00161 Rome, ItalyEnhancer of zeste homolog 2 (EZH2) is a methyltransferase involved in cell cycle regulation, cell differentiation, and cell death and plays a role in modulating the immune response. Although it mainly functions by catalyzing the tri-methylation of H3 histone on K27 (H3K27), to inhibit the transcription of target genes, EZH2 can directly methylate several transcription factors or form complexes with them, regulating their functions. EZH2 expression/activity is often dysregulated in cancer, contributing to carcinogenesis and immune escape, thereby representing an important target in anti-cancer therapy. This review summarizes some of the mechanisms through which EZH2 regulates the expression and function of tumor suppressor genes and oncogenic molecules such as STAT3, mutant p53, and c-Myc and how it modulates the anti-cancer immune response. The influence of posttranslational modifications on EZH2 activity and stability and the possible strategies leading to its inhibition are also reviewed.https://www.mdpi.com/1420-3049/29/24/5817EZH2methylationoncogenic pathwaysimmune escape and EZH2 inhibitors |
| spellingShingle | Maria Saveria Gilardini Montani Rossella Benedetti Mara Cirone Targeting EZH2 in Cancer: Mechanisms, Pathways, and Therapeutic Potential Molecules EZH2 methylation oncogenic pathways immune escape and EZH2 inhibitors |
| title | Targeting EZH2 in Cancer: Mechanisms, Pathways, and Therapeutic Potential |
| title_full | Targeting EZH2 in Cancer: Mechanisms, Pathways, and Therapeutic Potential |
| title_fullStr | Targeting EZH2 in Cancer: Mechanisms, Pathways, and Therapeutic Potential |
| title_full_unstemmed | Targeting EZH2 in Cancer: Mechanisms, Pathways, and Therapeutic Potential |
| title_short | Targeting EZH2 in Cancer: Mechanisms, Pathways, and Therapeutic Potential |
| title_sort | targeting ezh2 in cancer mechanisms pathways and therapeutic potential |
| topic | EZH2 methylation oncogenic pathways immune escape and EZH2 inhibitors |
| url | https://www.mdpi.com/1420-3049/29/24/5817 |
| work_keys_str_mv | AT mariasaveriagilardinimontani targetingezh2incancermechanismspathwaysandtherapeuticpotential AT rossellabenedetti targetingezh2incancermechanismspathwaysandtherapeuticpotential AT maracirone targetingezh2incancermechanismspathwaysandtherapeuticpotential |