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. 2018 Apr 23;373(1748):20170080. doi: 10.1098/rstb.2017.0080

Table 1.

Examples of PMT inhibitors. Examples used here are the most advanced compounds presented in the literature, to date, for which the chemical structures have been revealed.

target PMT most advanced example compound chemical structure binding modality references
DOTI L pinometostat (EPZ-5676) graphic file with name rstb20170080-i1.jpg SAM-competitive [15]
EZH2 tazemetostat (EPZ-6438) graphic file with name rstb20170080-i2.jpg SAM-competitive [32]
EZH2/1 899145 graphic file with name rstb20170080-i3.jpg SAM-competitive [33]
PRC2 complex SAH-EZH2 (stable peptide) graphic file with name rstb20170080-i4.jpg disruption of subunit interactions [34]
PRC2 complex A-395 graphic file with name rstb20170080-i5.jpg disruption of subunit interactions [35]
MLL complex MI-503 graphic file with name rstb20170080-i6.jpg disruption of subunit interactions [36]
EHMT1/EHMT2 UNC0642 graphic file with name rstb20170080-i7.jpg peptide competitive [37]
SUV420H1/2 A-196 graphic file with name rstb20170080-i8.jpg peptide competitive [38]
SMYD2 EPZ033294 graphic file with name rstb20170080-i9.jpg peptide competitive [39]
SMYD3 EPZ031686 graphic file with name rstb20170080-i10.jpg peptide competitive [40]
SETD7 (R)PFI-2 graphic file with name rstb20170080-i11.jpg peptide competitive [41]
SETD8 UNC0379 graphic file with name rstb20170080-i12.jpg peptide competitive [42]
pan-type 1 PRMT MS023 graphic file with name rstb20170080-i13.jpg peptide competitive [43]
PRMT3 SGC707 graphic file with name rstb20170080-i14.jpg allosteric inhibitor [44]
CARM1 (PRMT4) SGC2085 graphic file with name rstb20170080-i15.jpg peptide competitive [45]
PRMT5 EPZ015666 graphic file with name rstb20170080-i16.jpg peptide competitive [46]
PRMT6 EPZ020411 graphic file with name rstb20170080-i17.jpg peptide competitive [47]