Table 4.
Improved TRAIL-induced apoptosis pathway using inhibitors targeting enzymes in histone modifications
| Target | Small molecule | Regulation mechanisms | Cancer type | Ref. |
|---|---|---|---|---|
| Euchromatic histone-lysine N-methyltransferase 2 (EHMT2, G9a) | BIX-01294 | Downregulation of Survivin and Upregulation of DR5 | Renal carcinoma | [108] |
| Upregulation of DR5 | Breast cancer | [109] | ||
| PRC2 | Retinoic acid (RA) or 3-deazaneplanocin A (DZNep) | Increased DR5 transcript level | Colon cancer | [110] |
| Class I HDAC | Entinostat
(MS-275) |
Restore expression of Coxsackie Adenovirus receptor | Prostate cancer | [111] |
| Upregulation of DR4, DR5, Bax, Bak | Breast cancer | [112] | ||
| Decrease degradation of endogenous TRAIL | Anaplastic thyroid carcinoma | [113] | ||
| Expression of endogenous TRAIL | Acute myeloid leukemia | [114] | ||
| HDAC3 | RGFP966 | Upregulation of DR4 | Colon cancer | [115] |
| HDAC8 | PCI34051 |