A biochemical lysine methyltransferase assay to support oncology drug discovery

At Domainex, our assay biologists have developed a biochemical assay to measure lysine methyltransferase activity to support drug discovery in the field of oncology.  

laboratory assay

Lysine methyltransferases (KMTs) are enzymes that epigenetically regulate gene expression. Literature suggests KMTs have a role in carcinogenesis mechanisms, making them attractive targets in the field of oncology drug discovery. Domainex developed an assay to measure the activity of the KMT EZH2. Using this assay, Domainex investigated small molecule inhibitors of EZH2 and performed mechanism of action studies on selected compounds confirming that they blocked the KMT substrate binding site.

 

determination and inhibition curve graphs