Targeting Enhancer of Zeste Homolog 2 as a promising strategy for cancer treatment

Table 1 Enhancer of Zeste Homolog 2 inhibitors classified for Enhancer of Zeste Homolog 2 inhibition mechanism

Mechanism of inhibition	Drug	Level of development	Ref.
Regulators of EZH2 levels	DZNep		[83-85,87]
	EGCG		[86,87]
	PL3		[93]
	CDF		[94]
	TPA		[98]
	Sorafenib		[99]
SAM analogues	EPZ005687		[100]
	EI1		[101]
	GSK126		[102,109]
	GSK343		[103]
	GSK926		[103]
	EPZ-6438	Phase 2 (ClinicalTrials.gov Identifier: NCT01897571)	[104,110]
	UNC199		[105,109]
	Tanshindiols		[106]
	5-Methoxyquinoline Derivatives		[107]
	Tetramethylpiperidinyl Benzamides		[108]
Inhibition of the interaction between EZH2 with other PRC2 subunits	SAH-EZH2 Astemizole		[111] [112]
Unknown	CPI-1205	Phase1 (ClinicalTrials.gov Identifier: NCT02395601)
	GSK2816126	Phase 1 (ClinicalTrials.gov Identifier: NCT02082977

PRC2: Polycomb-repressive complex 2; EZH2: Enhancer of Zeste Homolog 2; PL3: 16-Hydroxycleroda-3,13-dien-15,16-olide; CDF: Diflourinated-curcumin; SAM: S-Adenosyl methionine; DZNep: 3-Deazaneplanocin A; EGCG: (-)-epigallocatechin-3-gallate; TPA: 12-O-tetradecanoylphorbol-13-acetate; SAH-EZH2: Stabillized alpha-helix of EZH2.