Table 1.
Negative 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 |
| DNA methyltransferases | 5-azacytidine (Vidaza)1 | Early Phase I to phase II[63,64] | No OR[63,65] | ||
| 5-aza-2’-désoxycytidine (Decitabine)1 | Phase I to phase II[66-68] | No OR[66]; beneficial with Panitumumab[68] | |||
| EGCG (Green tea extract) | Preclinical spheroid-derived cancer stem cell xenograft models[69] | Sensitization to chemotherapy | |||
| Zebularine | Preclinical xenografts[70] | Anticancer activity | |||
| RG108, Procainamide2 | |||||
| DNMT3A, DNMT3B, DNMT3L | -2.788/-4.848/-4.321 | < 0.005 | |||
| Activating Lysine methyltransferases | |||||
| SETD6 | vp22-RelA302-3163[71] | -4.641 | 3.47E-06 | ||
| SETD1A | -4.375 | 1.212E-05 | |||
| Repressive Lysine methyltransferases | |||||
| SMYD5 | - | -4.514 | 6.371E-06 | ||
| EHMT2 | UNC02243, UNC06423, BIX-012943 | -4.322 | 1.545E-05 | ||
| SETDB2 | - | -3.6 | 0.0003176 | ||
| PRDM13 | - | -3.442 | < 0.005 | ||
| SUV39H1, SUV39H2 | Chaetocin3 | -3.422/-2.934 | 0.0006216 | ||
| PRDM12 | - | -3.089 | 0.00201 | ||
| EZH1 | UNC19993 | -2.787 | 0.005314 | ||
| EZH2 | CPI-12052,4, EPZ-6438 (Tazemetostat)2, DZNep2, UNC19993 | -2.495 | 0.01259 | ||
| Arginine methyltransferases | |||||
| CARM1 | MS0493, SGC20853, TP-0643[72] | -3.812 | 0.0001381 | ||
| PRMT1 | MS0233[72] | -3.659 | 0.0002534 | ||
| PRMT6 | MS0233, MS049c, EPZ0204113[72], 6′-methyleneamine sinefungin3[73] | -3.521 | 0.0004301 | ||
| Histone acetylation | |||||
| KAT2A | CPTH23[74], γ-butyrolactone3 (MB-3)[75] | -4.683 | 2.823E-06 | ||
| NAA10, NAA16, NAA20, NAA38, NAA40 | - | -4.335/-3.255/-3.786/-3.801/-2.665 | < 0.01 | ||
| NAT8, NAT9 | - | -2.573/-3.995 | < 0.01 | ||
| NCOA5, NCOA6 | - | -3.238/-3.112 | < 0.002 | ||
| Histone phosphorylation | |||||
| BAZ1B | - | -2.374 | 0.01758 | ||
| Histone glycosylation | |||||
| OGT | - | -3.172 | 0.001512 | ||
1
Approved for the treatment of other diseases;
2
Used in clinical trials for other diseases;
3
Not yet used in clinical trials;
4
Activator. CRC: Colorectal cancer; OR: Objective response.