Abstract

Inhibitors for SMYD3, an epigenetic drug target

Joma Joy, Group Leader, Experimental Therapeutics Centre (ETC)

The SMYD (SET and MYND domain-containing protein) family of protein lysine methyltransferases have emerged as attractive targets for drug discovery due to their role in epigenetic regulation and association with many human cancers. Among them, SMYD3 is overexpressed in several cancers including liver, breast and rectal carcinomas. To identify inhibitors of SMYD3, our compound collection was screened using a high throughput biochemical assay. Hit validation was performed by biophysical and co-crystallization studies. These studies will enable us to advance the structure-based design of novel inhibitors.