Table 3.

Inhibitors of histone-methylation enzymes in treating experimental colorectal cancer.

Family	Enzyme	No. of potent ligands*	Inhibitors used in treating CRC	Structure of catalytic domain available	Reference
HMT	KMT2B	N/A	N/A	No	N/A
	KMT2C	N/A	N/A	Yes	N/A
	KMT2D	N/A	N/A	No	N/A
	SETD1A	N/A	N/A	No	N/A
	SUV39H1	1	Chaetocin	Yes	Yokoyama et al. [2013]
	EHMT2	36	UNC0638; BIX01294	Yes	Zhang et al. [2015b]
	PRDM2	N/A	N/A	Yes	N/A
	PRDM16	N/A	N/A	No	N/A
	SETDB1	N/A	N/A	Yes	N/A
	EZH2	20	GSK126;GSK343; DZNep	Yes	Benoit et al. [2013a, 2013b]; Ferraro et al. [2014]; Maryan et al. [2015]
	DOT1L	28	EPZ004777	Yes	Kryczek et al. [2014]
	SMYD3	N/A	BCI-121	Yes	Peserico et al. [2015]
	WHSC1	N/A	N/A	Yes	N/A
	PRDM5	N/A	N/A	No	N/A
	CARM1	17	N/A	Yes	N/A
	PRMT5	N/A	AMI-1	No	Zhang et al. [2015a]
HDM	KDM1A	56	Tranylcypromine	Yes	Ding et al. [2013]
	KDM5B	N/A	N/A	Yes	N/A
	KDM3A	5	N/A	No	N/A
	KDM3B	N/A	N/A	Yes	N/A
	PHF2	N/A	N/A	Yes	N/A
	KDM4B	N/A	N/A	Yes	N/A
	KDM4C	10	FLLL-32	Yes	Lin et al. [2010]
	KDM6B	1	N/A	Yes	N/A
	JARID2	N/A	N/A	No	N/A

CRC, colorectal cancer; N/A, not applicable; HMT, histone methyltransferases; HDM, histone demethylase.

^*Data acquired from CHEMBL database (version 20).