Table 2.
Potential clinical significance of histone posttranslational modifications in HNSCC
| PTMs | Inhibitor | Function | References | |
|---|---|---|---|---|
| Acetylation | HATs | CCS1477 | Phase I/II clinical studies for the treatment of hematologic malignancies, prostate cancer, breast cancer and non-small cell lung cancer have been initiated | [83] |
| EP31670 | Phase I clinical trial of safety and maximum tolerated dose in advanced solid tumors | |||
| HDACs | SAHA |
1. Treatment of cutaneous T-cell lymphoma, laryngeal squamous cell carcinoma 2. Inhibits cell proliferation, induces cell cycle arrest and apoptosis 3. The combination with pembrolizumab has stronger therapeutic activity against HNSCC |
[86] [88] [92] |
|
| Romidepsin |
1. Treatment of cutaneous T-cell lymphoma 2. Inhibits tumor-associated histone deacetylase |
[83] | ||
| Valproic acid |
1. Increase cell arrest and promote apoptosis 2. It has strong efficacy in combination with cisplatin |
[93] | ||
| TSA |
1. By regulating cell cycle mediators 2. Inhibits cell proliferation and induces G2/M phase arrest in tumor cells 3. TSA-induced H3K9ac can ameliorate the chemoresistance of HNSCC to cisplatin under active NF-κB signaling pathway |
[94] [95] |
||
| PBA |
1. Damage to the EMT process 2. It increased p21 and p27, decreased the levels of G1/S molecules CDK6, cyclin D1 and phosphorylated kinase, and inhibited the growth of oral squamous cell carcinoma |
[96] | ||
| [97] | ||||
| Methylation | HMTs | Chaetocin | It plays an important role in the combination of drugs in cancer treatment | [83] |
|
BIX-01294 CUDC-101 |
Inhibits H3K9me2 expression Phage I study on intermediate or high-risk HNSCC patients |
[103] [113] |
||
| GSK-343 |
1. The tumor growth of tongue squamous cell carcinoma was significantly inhibited after DZNeP administration 2. DZNeP is effective against a variety of cancers, including HNSCC, either alone or in combination 3. Associated with HPV status |
[104] [105] [106] |
||
| DZNeP | ||||
| EPZ-568 | ||||
| HNMTs | TCP | Most are associated with hematologic disorders | [83] | |
| ORY-1001 | ||||
| INCB059872 | ||||
| IMG-7289 | ||||
| TAK-418 | ||||
| GSK-LSD1 |
1. Blocks EGF-induced proliferation 2. Weakens genes involved in carcinogenic properties Inhibits the growth of oral squamous cell carcinoma |
[112] | ||