From: Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy
 | H3K4 | H3K9 | H3K27 | H3K36 | H3K79 | H4K20 |
---|---|---|---|---|---|---|
Writers | MLL1 (KMT2A) MLL2 (KMT2B) MLL3 (KMT2C) MLL4 (KMT2D) MLL5 (KMT2E) SET1A (KMT2F) SET1B (KMT2G) ASH1 (KMT2H) SMYD1 (KMT3D) SMYD2 (KMT3C) SMYD3 (KMT3E) SET7/9 (KMT7) | SUV39H1 (KMT1A) SUV39H2 (KMT1B) G9a (KMT1C) GLP (KMT1D) SETDB1 (KMT1E) SETDB2 (KMT1F) RIZ1 (KMT8) | EZH2 (KMT6) | SET2 (KMT3A) SET3 NSD1 (KMT3B) NSD2 NSD3 SMYD2 (KMT3C) SETMAR | DOT1L (KMT4) | SET8 (KMT5A) SUV420H1(KMT5B) SUV420H2 (KMT5C) NSD1(KMT3B) |
Erasers | LSD1(KDM1A) LSD2 (KDM1B) JHDM1A (KDM2A) JHDM1B (KDM2B) JARID1A (KDM5A) JARID1B (KDM5B) JARID1C (KDM5C) JARID1D (KDM5D) NO66 | LSD1 (KDM1A) JHDM2A (KDM3A) JHDM2B (KDM3B) JHDM3A (KDM4A) JMJD2B (KDM4B) JMJD2C (KDM4C) JMJD2D (KDM4D) JHDM1D (KDM7) PHF8 | UTX (KDM6A) JMJD3 (KDM6B) | JHDM1A (KDM2A) JHDM1B (KDM2B) JMJD2A (KDM4A) JMJD2B (KDM4B) JMJD2C (KDM4C) | Not described | Not described |
Cancer association | MLL rearrangement in leukemias and in different solid tumors [172, 173]. SMYD3 overexpressed in colorectal and hepatocellular cancers [174]. JARID1B overexpressed in breast cancer [175]. LSD1 overexpressed in prostate cancer [176]. | G9a involved in suppressor gene silencing [177]. SUV39H1, increased mRNA in colon cancer [178]. SETDB1 amplified and overexpressed in melanoma [179]. Downregulation of LSD1 impairs androgen-dependent proliferation of prostate cancer cells [140]. | EZH2 amplified in multiple solid tumors [84, 180] and mutated in lymphomas [110] and myelodysplastic syndromes and myeloproliferative neoplasms [181]. H3K27 mutated in glioblastoma[182]. | Translocation and overexpression of NSD3 in AML and breast cancer [183, 184] and of NSD1 in prostate cancer [185] and in neuroblastoma [186]. | MLL-rearranged leukemias | Loss of H4K20me3 in non-small cell lung cancer [187] and in several cancer cell lines [27, 188]. |