EZH1

Oncogene
Histone-lysine N-methyltransferase EZH1 UniProt accession Q92800

Polycomb group (PcG) protein. Catalytic subunit of the PRC2/EED-EZH1 complex, which methylates 'Lys-27' of histone H3, leading to transcriptional repression of the affected target gene. Able to mono-, di- and trimethylate 'Lys-27' of histone H3 to form H3K27me1, H3K27me2 and H3K27me3, respectively.

Required for embryonic stem cell derivation and self-renewal, suggesting that it is involved in safeguarding embryonic stem cell identity. Compared to EZH2-containing complexes, it is less abundant in embryonic stem cells, has weak methyltransferase activity and plays a less critical role in forming H3K27me3, which is required for embryonic stem cell identity and proper differentiation

Source: UniProt

Component of the PRC2/EED-EZH1 complex, which includes EED, EZH1, SUZ12, RBBP4 and AEBP2 (PubMed:19026781). The PRC2/EED-EZH1 is less abundant than the PRC2/EED-EZH2 complex, has weak methyltransferase activity and compacts chromatin in the absence of the methyltransferase cofactor S-adenosyl-L-methionine (SAM) (PubMed:19026781). Interacts with EZHIP; the interaction blocks EZH1 methyltransferase activity (PubMed:31451685)

Source: UniProt
Nucleus
Source: UniProt

Synthetic Lethal Network

Genes with an experimentally identified or computationally predicted synthetic-lethal relationship to EZH1, aggregated across our SSL data sources. Click any partner node to view that gene’s page.

Nodes and edges are coloured by the SSL data source. Partners appearing in more than one source are shown in grey.

BioGRID SLOrth SynLethDB MexDrugs Multi-source
Sources: BioGRID, SLOrth, SynLethDB, MexDrugs

Clinical Trials

Total Trials Found: 16

NCT ID Condition Brief Title Phase Status
NCT03460977 Metastatic Castration Resistant Prostate Cancer (mCRPC), Small Cell Lung Cancer (SCLC), Follicular Lymphoma (FL) A Study of Mevrometostat for Treatment of Relapsed/Refractory SCLC, Castration Resistant Prostate Cancer, and Follicular Lymphoma PHASE1 RECRUITING
NCT07190300 Metastatic Hormone-Sensitive Prostate Cancer (mHSPC) TulmiSTAR-02: A Phase I/II Open-label Study of Tulmimetostat in Combination With Darolutamide vs. Darolutamide, and Tulmimetostat With Abiraterone in Patients With Metastatic Hormone-sensitive Prostate Cancer (mHSPC) PHASE1, PHASE2 RECRUITING
NCT06392230 Healthy Participants A Study to Learn How the Medicine Called [14C] PF-06821497 is Taken up Into and Removed From the Body. PHASE1 COMPLETED
NCT04703192 Relapsed/Refractory Peripheral T-Cell Lymphoma, Adult T Cell Leukemia/Lymphoma Valemetostat Tosylate (DS-3201b), an Enhancer of Zeste Homolog (EZH) 1/2 Dual Inhibitor, for Relapsed/Refractory Peripheral T-Cell Lymphoma (VALENTINE-PTCL01) PHASE2 ACTIVE_NOT_RECRUITING
NCT03303950 Anemia, ASXL1 Gene Mutation, EZH2 Gene Mutation, IDH1 Gene Mutation, IDH2 Gene Mutation, Plasma Cell Myeloma, Primary Myelofibrosis, Recurrent Plasma Cell Myeloma, Secondary Myelofibrosis, Thrombocytopenia Allogeneic Stem Cell Transplantation for Multiple Myeloma and Myelofibrosis PHASE2 TERMINATED
NCT03456726 Relapsed or Refractory B-cell Non-Hodgkin's Lymphoma Study of Tazemetostat in Participants With Relapsed or Refractory B-cell Non-Hodgkin's Lymphoma With EZH2 Gene Mutation PHASE2 COMPLETED
NCT07303387 Solid Tumor Malignancies, Clear Cell Endometrial Carcinoma, Ovarian Cancer Efficacy and Safety of the Valemetostat in Patients With Selected Solid Tumors. PHASE2 RECRUITING
NCT05633979 Breast Cancer Phase 1b Study of EZH1/2 Inhibitor Valemetostat in Combination With Trastuzumab Deruxtecan in Subjects With HER2 Low/Ultra-low/Null Metastatic Breast Cancer PHASE1 ACTIVE_NOT_RECRUITING
NCT06909877 Relapsed/Refractory Peripheral T-Cell Lymphoma (R/R PTCL) Study to Evaluate Efficacy and Safety of HH2853 in Relapsed/Refractory Peripheral T-cell Lymphoma PHASE1, PHASE2 RECRUITING
NCT05228158 Lymphoma, Follicular A Study of Tazemetostat on Safety in Participants With Relapsed or Refractory Follicular Lymphoma With Enhancer of Zeste Homolog 2 (EZH2) Gene Mutation in Japan N/A ACTIVE_NOT_RECRUITING