. Author manuscript; available in PMC: 2013 Oct 1.

Published in final edited form as: Drug Discov Today Ther Strateg. 2011 Sep 20;9(2-3):e75–e81. doi: 10.1016/j.ddstr.2011.08.002

Table 2.

Common sites of histone methylation in humans and a subset of KMTs published to utilize these sites as substrates. Diseases associated with specific KMTs or general deregulation of the histone methyl mark are indicated. Chemical inhibitors of specific enzymes are shown.

Methyl mark	KMTs	Diseases	Inhibitors
H3K4	hSET1/MLL family, SET7/SET9	Leukemia (AML, ALL, MLL), hepatocellular, colorectal and breast carcinoma	none
H3K9	SUV39H1/2, G9a, Eu-HMT1, SETDB1, PRDM2/RIZ1	B-cell lymphoma, breast, colorectal, hepatocellular carcinoma, neuroblastoma, melanoma, Huntington’s disease	Chaetocin (Dm Su-(var)3-9)[27] BIX-01294 (G9a)[28]
H3K27	EZH2, EZH1, G9a	Breast, bladder, colorectal and prostate cancer, lymphoma, melanoma	DZnep (EZH2)[20]
H3K36	SETD2/HYPB, NSD1, NSD2, NSD3	Acute myeloid leukemia, multiple myeloma, Wolf-Hirschhorn and Sotos syndromes, glioblastoma multiform, breast, lung and prostrate cancer	none
H3K79	DOT1L	Leukemia (AML, ALL), T-cell acute lymphoblastic leukemia	EPZ00477 [47]
H4K20	Pr-SET7/8, SUV4-20H	Lung cancer, Hutchinson-Gilford Progeria Syndrome (HGPS)	none