Table 2.
Negative correlation between combined expression of cancer stem cell markers CD133, CD44 and CD166 and epigenetic erasers
| Family/gene symbol | Epidrug/chemical probe | Clinical trials for CRC | Results | Z-score | P value |
| Histone deacetylation (Zinc-dependent) | |||||
| Acide valproïque1 | I to II | In combination: OR in 64% patients or SD[76,77] | |||
| Belinostat2, Apicidin3 | |||||
| Entinostat | I to I/II | No OR[78] or SD[79] | |||
| Panobinostat | I | PR and SD in combination with Bevacizumab[80] | |||
| Vorinostat (SAHA) | I to II | No OR[81,82]; SD and PR with Bortezomib or 5FU and leucovorin or Doxorubicin[83-85] | |||
| Trichostatine A2 | |||||
| Mocetinostat2 | |||||
| Sodium phenylbutyrate2 | I | In combination with 5-FU: SD[86] | |||
| Class I | Romidepsin (Istodax)1 | II | Ineffective[86] | ||
| CI-994 | I | PR in combination with carboplatin and placlitaxel[87] | |||
| HDAC8 | TM-2-514, CUDC-1012, Pracinostat2, Ricolinostat2, Citarinostat2, Abexinostat2, Quisinostat3, PCI-340513 | -2.527 | 0.0115 | ||
| Class IIa (1 catalytic site, mainly cytoplasmic) | |||||
| HDAC5 | CUDC-1012, Pracinostat2, Domatinostat2, Quisinostat3, LMK-2353, TMP1953, TMP2693 | -4.133 | 3.581E-05 | ||
| Class IIb (2 catalytic sites, mainly cytoplasmic) | |||||
| HDAC10 | CUDC-1012, CUDC-9072, Pracinostat2, Domatinostat2, Abexinostat2, Tucidinostat2, Quisinostat3 | -3.17 | 0.001525 | ||
| Histone deacetylation NAD+ dependent (Class III) | |||||
| Resveratrol4 | I | Reduced cell proliferation[88] | |||
| Salermide3[89] | |||||
| SIRT6 | OSS_1281673 | -3.467 | 0.0005257 | ||
| SIRT7 | -2.582 | 0.009835 | |||
| Histone demethylation | |||||
| LSD family of demethylases | |||||
| ORY-10013, (±)-tranylcypromine3 | |||||
| KDM2B | - | -3.54 | 0.0004003 | ||
| KDM4D | - | -2.704 | 0.006848 | ||
| JmjC containing lysine demethylases | |||||
| JIB-043 | |||||
| JMJD6 | IOX13 | -2.59 | 0.00961 | ||
| JMJD5 | IOX13 | -2.588 | 0.009654 | ||
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; SD: Stable disease; PR: Partial response.