Table 2.
Histone lysine methyltransferases (KMTs) and their selective inhibitors
| Enzyme | Alias | Structure | Inhibitor | Reference | ||
|---|---|---|---|---|---|---|
| H3K4 | MLL1 | KMT2A | TRX1 | SET/PHD/FYRC/BD | MM102* MM-401* WDR5-0103* |
[66–68] |
| 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** |
[96–99, 101–104] | |
| 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 |
[129–133] | |
| H4K20 | PR-Set7 | KMT5A | SETD8 | SET | ||
| SUV420H1 | KMT5B | CGI85 | SET | A-196 | [142] | |
| SUV420H2 | KMT5C | SET | ||||
| NSD1 | KMT3B | STO | SET/PHD |
*These compounds target MLL-WDR5 interaction
**This compound blocks EED, another component of PRC2 to inhibit H3K27 methylation