Skip to main content

Table 1 Principal writers and erasers of methyl lysines in histone 3 and 4 and their association with cancer

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].