PRC2: an epigenetic multiprotein complex with a key role in the development of rhabdomyosarcoma carcinogenesis

Clinical Epigenetics

Table 1 PRC2 inhibitors

Inhibitors of EZH2 methyltransferase activity	SAH hydrolase inhibitor which globally inhibits histone methylation	3-deazaneplanocin A (DZNep) [53]
Inhibitors of EZH2 methyltransferase activity	SAM-competitive Inhibitors	GSK126, EPZ005687, EL1 [70], GSK343, GSK926, Tazemetostat, EPZ011989, CPI-1205, CPI-169, ZLD1039, PF-06821497; [65, 67, 69, 71,72,73]; UNC199, OR-S1/OR-S2, DS-3201b [74, 75]
Inhibitors that break PRC2’s structure	Disrupting the EZH2-EED interaction	SAH-EZH2, Astemizole, Wedelolactone, apomorphine hydrochloride, oxyphenbutazone, nifedipine, ergonovine maleate, AZD9291, MAK683 (EED226) [76, 77]
Inhibitors that break PRC2’s structure	Disrupting the EZH2-SUZ12 interaction	A769662 (an AMPK agonist) [76]
Suppressing EZH2 through triggering EZH2 degradation	GNA022, ANCR, FBW7, ZRAMB1 siRNA and other inhibitors [77]

ISSN: 1868-7083