Table 1.
target PMT | most advanced example compound | chemical structure | binding modality | references |
---|---|---|---|---|
DOTI L | pinometostat (EPZ-5676) | SAM-competitive | [15] | |
EZH2 | tazemetostat (EPZ-6438) | SAM-competitive | [32] | |
EZH2/1 | 899145 | SAM-competitive | [33] | |
PRC2 complex | SAH-EZH2 (stable peptide) | disruption of subunit interactions | [34] | |
PRC2 complex | A-395 | disruption of subunit interactions | [35] | |
MLL complex | MI-503 | disruption of subunit interactions | [36] | |
EHMT1/EHMT2 | UNC0642 | peptide competitive | [37] | |
SUV420H1/2 | A-196 | peptide competitive | [38] | |
SMYD2 | EPZ033294 | peptide competitive | [39] | |
SMYD3 | EPZ031686 | peptide competitive | [40] | |
SETD7 | (R)PFI-2 | peptide competitive | [41] | |
SETD8 | UNC0379 | peptide competitive | [42] | |
pan-type 1 PRMT | MS023 | peptide competitive | [43] | |
PRMT3 | SGC707 | allosteric inhibitor | [44] | |
CARM1 (PRMT4) | SGC2085 | peptide competitive | [45] | |
PRMT5 | EPZ015666 | peptide competitive | [46] | |
PRMT6 | EPZ020411 | peptide competitive | [47] |