Enhancer of zeste homolog 2 (EZH2) mRNA (EZH2 mRNA)

Enhancer of zeste homolog 2 (EZH2) mRNA is the transcript that encodes the catalytic subunit of the Polycomb Repressive Complex 2 (PRC2), a key epigenetic regulator (Source: UniProt). This mRNA serves as the template for the synthesis of the EZH2 protein, which functions as a histone methyltransferase that tri-methylates histone H3 at lysine 27 (H3K27me3), leading to the transcriptional silencing of genes involved in cell differentiation and tumor suppression (Source: PubMed). Overexpression of EZH2 mRNA is frequently observed in various cancers, including B-cell lymphomas and solid tumors like prostate and breast cancer, where it drives oncogenesis by repressing tumor suppressor genes (Source: NIH). While small-molecule inhibitors typically target the EZH2 protein's catalytic site, targeting the EZH2 mRNA with antisense oligonucleotides (ASOs) or RNA interference (RNAi) allows for the depletion of the entire protein pool, including its non-catalytic scaffolding functions (Source: PubMed). Drugs such as IONIS-EZH2-Rx (also known as AZD6094) are designed to bind specifically to the EZH2 mRNA, triggering its degradation via RNase H and subsequently lowering EZH2 protein levels to restore normal gene expression (Source: ClinicalTrials.gov, Ionis Pharmaceuticals). This therapeutic approach is particularly valuable in cancers where EZH2 protein levels are high or where the protein exerts oncogenic effects independent of its methyltransferase activity (Source: PubMed).

Other names

KMT6 mRNAENX-1 mRNAEZH2 transcriptEnhancer of zeste 2 polycomb repressive complex 2 subunit mRNA

Antisense oligonucleotide-mediated RNase H-dependent degradation of mRNA