TABLE 2.

Summary of potential therapeutic targets and the corresponding clinical approved/non-approved drugs.

Category	Therapeutic targets	PDB-ID	Function	Clinical/non clinical approved drugs	References
Writers	P300	5LKU	Acetylates histone lysines	C646, B026, A-485, B029-2, etc.	Lasko et al. (2017), Peng et al. (2019), Yang et al. (2020), Cai et al. (2021)
	ASH1	3MQM	Methylates histone H3K36 and H3K4	—	Perugorria et al. (2012)
	EZH2	4MI5	Methylates histone H3K27	Tazemetostat; Valemetostat, GSK126, CPI-0209, CPI-1205	Huang et al. (2019), Bates (2020)
	SETDB1	3DLM	Methylates histone H3K9	Mithramycin, DZNep	Rivière et al. (2015), Karanth et al. (2017)
	MLL4/KMT2D, SET1A	4Z4P, 4RIQ	Methylates histone H3K4	Methyltransferase inhibitor 5′-deoxy-5'-(methylthio)adenosine (MTA)	El Mansouri et al. (2011), Kim et al. (2016)
	SET7/9 (KMT7)	1N6A	Methylates histone lysines	MTA, Cyproheptadine, Sinefungin, etc.	Gu et al. (2018), Tamura et al. (2018); Sharma et al. (2020)
	PRMT1, PRMT5	1OR8, 6UXX	Methylates histone arginine	EPZ015666, GSK33265 95, GSK591, LLY-283, etc.	Zhang et al. (2017), Guccione and Richard (2019)
	RNF20/BRE1A	5TRB	Ubiquitination of H2B	—	Chen et al. (2021)
Erasers	HDAC	—	Deacetylase removes acetyl groups from histone lysines	Vorinostat, belinostat, panobinostat, romidepsin; Fimepinostat, KA2507, OKI-179, etc.	Rodríguez-Aguilera et al. (2018), Bates (2020)
	LSD 1	4XBF	Demethylates histone lysines	Iadademstat, CC-90011, INCB059872	Alarcon et al. (2016), Bates (2020)
	JMJD2B/KDM4D	4UC4	Demethylates histone lysines	JIB04, Curcuminoids	Kim et al. (2014), Kurozumi et al. (2019), Kim et al. (2020)
	Phf2	3PTR	Demethylates histone lysines	—	Bricambert et al. (2018)
	BAP1	—	Deubiquitination of H2B	—	He et al. (2019)
Readers	BRD4	5EI4/5EGU	Bromodomain proteins read acetyl groups on histone lysines	Molibresib, Birabresib, ZEN003694, PLX51107	Bates (2020), Gao et al. (2021)