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.