EZH2 (RBT-EZH2), RMab

Summary and Explanation

Enhancer of zeste homolog 2 (EZH2) is an enzymatic catalytic subunit of polycomb repressive complex 2 (PRC2) which is involved in trimethylation of Lys 27 on Histone 3 and GATA4. Histone methylation and chromatin regulation are affected by EZH2 dysregulation and can lead to increased cell survival and cancer development as downstream genes are not properly silenced. EZH2 expression in naïve T cells promotes survival, proliferation, and function of effector T cells. EZH2 plays a key role for the function of tumor-specific effector T cells, while tumor microenvironments reduce EZH2 expression of T cells via glucose restriction and in turn, mediates T cell dysfunction. EZH2 may inhibit apoptosis in ectopic Breast Cancer, overexpression is correlated with poor clinical outcome in Prostate and Gastric Cancer. EZH2 overexpression is positively correlated with epithelial-mesenchymal transition, tumor size, lymphatic invasion and TNM stage, and poor disease-free survival and overall survival of patients. EZH2 regulates ADAR1 expression, and EZH2 and BET inhibitors show synergistic inhibition in pancreatic cancer. EZH2 expression is significantly higher in BAP1-mutant renal clear cell carcinoma patients with progressed stage, grade, nodal invasion, and metastasis.