Histone modifications across cancers: mechanisms, therapy and clinical translation - PubMed
5 hours ago
- #epigenetic therapy
- #cancer epigenetics
- #histone modifications
- Histone modifications (e.g., acetylation, methylation, phosphorylation) are key epigenetic changes involved in cancer development, heterogeneity, and drug resistance.
- Dysregulation of histone-modifying enzymes (writers, erasers, readers) contributes to oncogenic states in both solid tumors and hematological malignancies.
- Crosstalk exists between histone modifications, DNA methylation, non-coding RNAs, and metabolic reprogramming, forming complex epigenetic networks in cancer.
- Epigenetic therapies, including HDAC inhibitors, EZH2 inhibitors, and BET inhibitors, show promise, with emerging approaches like PROTACs and dual inhibitors.
- Combining epigenetic therapy with chemotherapy or immunotherapy represents a new therapeutic avenue for cancer treatment.
- Histone modifications such as H3K27me3 and H2BK120ub have context-dependent roles, and enzymes like EZH2 and BRD4 are potential therapeutic targets.
- Expression changes in histone-modifying enzymes underpin oncogenic transcriptional states across all cancer types.