SELECTIVE INHIBITORS OF HISTONE METHYLTRANSFERASE DOT1L

摘要

Structure and mechanism based design was used to design potent ribose containing inhibitors of DOT1L with IC50 values as low as 38 nM. These ribose containing inhibitors exhibit only weak or no activities against four other representative histone lysine and arginine methyltransferases, G9a, SUV39H1, PRMT1 and CARM1.