EZH2

EZH2 or Enhancer of Zeste Homolog 2 is a human gene that encodes a member of the Polycomb-group (PcG) family. The protein encoded by this gene forms one of the essential components of a non-DNA-binding Polycomb Repressive Complex 2 (PRC2) that functions in the methylation of histone H3.

Function

EZH2 is a histone-lysine N-methyltransferase enzyme, which participates in histone methylation and gene silencing. It has been identified to have a central role in the process of histone H3 lysine 27 trimethylation (H3K27me3). This process is recognized as a crucial mechanism for the regulation of gene expression.

Clinical Significance

EZH2 is often found to be overexpressed in a wide variety of cancer types, including prostate cancer, breast cancer, and melanoma. Overexpression of EZH2 can lead to the proliferation of cancer cells and is associated with advanced and metastatic disease stages.

Role in Cancer

In cancer, EZH2 functions as an oncogene. It promotes cell proliferation and cell cycle progression by silencing genes that regulate these processes. EZH2 overexpression has been linked to poor prognosis in several types of cancers, including breast cancer, prostate cancer, and ovarian cancer.

Inhibitors

Several EZH2 inhibitors are currently in clinical trials for the treatment of various cancers. These inhibitors work by blocking the enzymatic activity of EZH2, thereby preventing the methylation of histone H3 and the subsequent silencing of tumor suppressor genes.

See Also

• Polycomb-group (PcG)
• Polycomb Repressive Complex 2 (PRC2)
• Histone H3 lysine 27 trimethylation (H3K27me3)