Drug pipeline
Full profile accessExplore the programs pursuing this target and their development progress.
- Drug candidates
- Developers
- Development stage
Target intelligence / Profile preview
Histone-lysine N-methyltransferase EZH1 and Histone-lysine N-methyltransferase EZH2 (EZH1/EZH2)
- Target
- EZH1/EZH2
- Molecular classification
- Enzyme, methyltransferase, histone methyltransferase, Polycomb group protein, Epigenetic regulator, PRC2 catalytic subunit
01
Overview
Histone-lysine N-methyltransferase EZH1 and EZH2 are the catalytic subunits of the polycomb repressive complex 2 (PRC2), which catalyze methylation of lysine 27 of histone H3 (H3K27). This modification leads to transcriptional repression and chromatin compaction, regulating stem cell identity, tissue homeostasis, and cellular differentiation. EZH2 is associated with proliferating tissues and is implicated in tumorigenesis, while EZH1 is expressed ubiquitously and complements EZH2, especially in differentiated and quiescent cells. Genetic and functional studies implicate these proteins in a range of cancers and developmental disorders, and they are active drug targets for oncology and regenerative medicine.
- Other names
- EZH1EZH2Histone-lysine N-methyltransferase EZH1/EZH2Polycomb repressive complex 2 subunit EZH1/EZH2Polycombeotic (pco)
02
Mechanism of action
Competitive inhibition of SAM (S-adenosyl methionine) binding site in the SET domain, blocking methyltransferase activity Reducing H3K27me3 marks to reverse epigenetic silencing and reactivate tumor suppressor genes
03
Biological functions
Histone H3 lysine 27 (H3K27) methylationTranscriptional repressionChromatin compactionStem cell identity maintenance and pluripotencyTissue homeostasis (e.g., hepatocyte and hair follicle homeostasis)Regulation of cell proliferation
04
Disease associations
Cancer (e.g., mixed-lineage leukemia (MLL), autonomous thyroid adenomas, other human cancers)Neurodevelopmental disorders (linked via mutations)Other developmental disordersWound repair deficits
05
Safety considerations
Off-target toxicity due to broad epigenetic regulationPotential impact on normal tissue homeostasis (hair follicles, wound repair, stem cell functions)Developmental effects in pediatric or prenatal contexts (since methyltransferases are essential in growth and differentiation)
06
Interacting drugs
EZH2 inhibitors (UNC1999 and other pyridone-based inhibitors)
1 more in the full profile.
07
Biomarkers
H3K27me3 level in tissuesEZH1 or EZH2 mutations (e.g., Q571R in EZH1 in thyroid adenomas; A678G in EZH1 in neurodevelopmental disorders)
Beyond the preview
Go deeper on Histone-lysine N-methyltransferase EZH1 and Histone-lysine N-methyltransferase EZH2 (EZH1/EZH2).
Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.
Clinical trials
Full profile accessFollow the clinical studies evaluating therapies directed at this target.
- Trial design
- Status
- Readouts
Competitive landscape
Full profile accessCompare approaches across drug candidates, modalities, and indications.
- Programs
- Modalities
- Indications
Literature & evidence
Full profile accessInvestigate the research and source evidence behind target biology and development.
- Publications
- Sources
- Analysis
Patents
Full profile accessExplore patent activity around therapies and technologies addressing this target.
- Patents
- Assignees
- Technologies
Research & analysis
Full profile accessConnect target biology, drug development, and emerging evidence in your research.
- Biology
- Development news
- Analysis
Bring the full picture into focus.
See how Gosset can support your research on Histone-lysine N-methyltransferase EZH1 and Histone-lysine N-methyltransferase EZH2 (EZH1/EZH2).