Design and discovery of highly potent lysine 27 of histone H3 (H3K27) demethylase inhibitors for the treatment of inflammatory bowel disease.
Lysine specific demethylase 6A/B (KDM6A/B), histone lysine demethylases targeting H3K27me3, have emerged as key regulators of inflammatory gene expression and are increasingly implicated in the pathogenesis of inflammatory bowel disease (IBD). However, there remains a critical need for potent, selective, and cell-activ...