Our Research

Our current research focuses on understanding the biological roles of epigenetic proteins, including readers, writers and erasers, in cancer using a combination of chemistry, medicinal chemistry, chemical biology, and biology approaches. 

Bromodomains are epigenetic readers that recognize acetyl-lysine mark on histone. We have developed small molecule inhibitors for the bromodomain and extra-terminal (BET) subfamily (BRD2, BRD3, BRD4 and BRDT).  With the chemical probe and chemical biology platform we have established, we are now further developing small molecule inhibitors for other bromodomain family members and studying their roles in different types of cancers.

Histone methylation contributes to the regulation of chromatin structure and function, thereby modulating gene expression. Histone methyltransferases are epigenetic writers that manage methylation on different locations.  We have been focusing on developing small molecule inhibitors for DOT1L that catalyzes the methylation of H3K79, as well as assay platform to further optimize current probes. We are now developing small molecule inhibitors and tool compounds to study other methyltransferases, including EZH2, PRMT5, and NSD2.

Histone methylation is tightly regulated by methyltransferases and demethylases that mediate the addition and removal of this modification.  We are developing small molecule inhibitors and tool compounds for histone lysine demethylases (KDMs) to validate the therapeutic potential of KDM inhibition.