Colon cancer stemness as a reversible epigenetic state: Implications for anticancer therapies

Table 4 Positive correlation between combined expression of cancer stem cell markers CD133, CD44 and CD166 and epigenetic writers

Family/gene symbol	Epidrug/chemical probe	Clinical trials for CRC	Results/status	Z-score	P value
Histone acetyltransferases
EP300	Curcumin	Early phase I to III	Low bioavailability[91]	2.513	0.01198
	Garcinol3, C6463
NCOA1	Bufalin2[92]			5.45	5.04E-08
NCOA4	-			4.183	2.88E-05
NCOA7	-			5.788	7.14E-09
KAT2B	Ischemin3[93]			6.514	7.31E-11
Activating Lysine methyltransferases
ASH1L	-			2.591	0.009565
SMYD1	-			2.739	0.00616
SETD7	PFI-23			5.11	3.23E-07
Repressing Lysine methyltransferases
PRDM8	-			3.411	0.0006465
Putative Lysine methyltransferase
PRDM10	-			2.448	0.01438
Arginine methyltransferases
PRDM1	-			2.874	0.004056
PRMT2	-			2.901	0.003726
Histone ubiquitination
UBE2B	-			2.748	0.005991
UBE2H	-			5.809	6.30E-09
Histone phosphorylation
JAK1	Ruxolitinib	Phase I and II	No benefit over Regorafenib alone[94]	7.739	1.01E-14
	Baricitinib2, Momelotinib2, Filgotinib2, Decernotinib2, Cerdulatinib2, Solcitinib2, Oclacitinib maleate2
JAK2	Ruxolitinib	Phase I and II	No benefit over Regorafenib alone[94]	6.7	2.09E-11
	Gandotinib2, AZD14802, BMS-9115432, AT92832, XL0192, Baricitinib2, Momelotinib2, Filgotinib2, Decernotinib2, Cerdulatinib2, JAK2/HDAC Dual Inhibitors3[95]
Histone biotinylation
BTD	Biotinyl-methyl 4-(amidomethyl)benzoate3[96]			4.379	1.19E-05

¹Approved for the treatment of other diseases;

²Used in clinical trials for other diseases;

³Not yet used in clinical trials. CRC: Colorectal cancer.