Histone-lysine N-methyltransferase SUV39H2 (SUV39H2)

SUV39H2 is a SET-domain-containing histone methyltransferase that preferentially catalyzes the di- and tri-methylation of lysine 9 on histone H3. This post-translational modification is a hallmark of heterochromatin, transcriptional repression, and epigenetic silencing. SUV39H2 also methylates non-histone substrates such as H2AX and LSD1, impacting DNA repair and protein stability. SUV39H2 expression is normally restricted to embryonic and testis tissues, but it is frequently upregulated and has oncogenic function in many human cancers. It interacts with androgen receptor and other factors to modulate gene transcription and is involved in chemoresistance, cell cycle regulation, senescence, and genome stability. Knockdown or knockout of SUV39H2 results in cell cycle arrest, apoptosis, and genomic instability. Despite its promise as a cancer therapeutic target, no specific inhibitors have reached clinical development.

Other names

Suppressor of variegation 3-9 homolog 2KMT1Blysine N-methyltransferase 2

Drugs or molecules that inhibit SUV39H2 would reduce H3K9 methylation, leading to de-repression of silenced genes, modulation of cell cycle, and induction of apoptosis in cancer cells. Restoration of normal gene expression through epigenetic reprogramming.