Abstract: Methyltransferases (MTs) are increasingly recognized as promising drug targets in precision medicine due to their essential role in regulating diverse biological processes. Our research is centered on discovering cell-potent and isoform-selective inhibitors for epigenetic targets, including MTs, through innovative strategies.
In this talk, I will discuss our recent progress in developing selective and potent inhibitors for protein N-terminal methyltransferase 1 (NTMT1), which show significant potential in promoting muscle regeneration. Additionally, I will present our advancements in creating inhibitors for nicotinamide N-methyltransferase (NNMT) and protein arginine methyltransferase 4 (PRMT4), which are being actively investigated for their therapeutic efficacy in cancer treatment.