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Table 2 Histone lysine methyltransferases (KMTs) and their selective inhibitors

From: Tackling malignant melanoma epigenetically: histone lysine methylation

  Enzyme Alias   Structure Inhibitor Reference
H3K4 MLL1 KMT2A TRX1 SET/PHD/FYRC/BD MM102*
MM-401*
WDR5-0103*
[66,67,68]
MLL2 KMT2B MLL4 SET/PHD/FYRC/BD
MLL3 KMT2C HALR SET/PHD/FYRC
MLL4 KMT2D MLL2 SET/PHD/FYRC
MLL5 KMT2E   SET/PHD
SET1A KMT2F SETD1A SET/RRM
SET1B KMT2G SETD1B SET/RRM
ASH1L KMT2H ASH1 SET/PHD
SET7/SET9 KMT7 SETD7 SET
H3K9 G9A KMT1C EHMT2 SET/TAD/ANK BIX01294
UNC0321
[83, 85]
GLP KMT1D EHMT1 SET/TAD/ANK
SUV39H1 KMT1A H3-K9-HMTase 1 SET/CD Chaetocin [82]
SUV39H2 KMT1B H3-K9-HMTase 2 SET/CD
SETDB1 KMT1E H3-K9-HMTase 4 SET/Tudor/MBD
RIZ1 KMT8 PRDM2 PR/ZF
H3K27 EZH2 KMT6   SET/SANT EPZ-6438 (Tazemetostat)
EPZ011989
GSK126
GSK503
GSK343
EPZ005687
CPI-1205
CPI-169
EI1
EED226**
[96,97,98,99, 101,102,103,104]
H3K36 SET2 KMT3A SETD2 SET/SRI N-propyl sinefungin
(Pr-SNF)
[124]
NSD1 KMT3B STO SET/PHD BIX01294 [125]
SMYD2 KMT3C ZMYND14 SET/MYND
ASH1L KMT2H ASH1 SET/PHD/BD
H3K79 DOT1L KMT4   LRR EPZ5676 (Pinometostat)
EPZ004777
SGC 0946
[129,130,131,132,133]
H4K20 PR-Set7 KMT5A SETD8 SET   
SUV420H1 KMT5B CGI85 SET A-196 [142]
SUV420H2 KMT5C   SET
NSD1 KMT3B STO SET/PHD   
  1. *These compounds target MLL-WDR5 interaction
  2. **This compound blocks EED, another component of PRC2 to inhibit H3K27 methylation