Table 2.
Epigenetic drugs or inhibitors targeting mechanisms in musculoskeletal disease
| Target class/target | Reagent (drug/chemical probe/antisense) | Disease area | Mechanism | References |
|---|---|---|---|---|
| Histone demethylase, KDM6 subfamily of demethylases | GSK-J4 | Inflammation, autoimmunity | Suppression of proinflammatory cytokine production, targeting of H3K27 demethylases | [31] |
| BET bromodomains | I-BET | Sepsis, inflammation | Inhibition of BET bromodomain interactions, suppression of cytokine production | [84] |
| BET bromodomains | JQ1 | Bone disease/multiple myeloma |
Inhibition of BET bromodomain interactions, MYC targeting | [85] |
| Histone deacetylase (class 1 and II HDACs) | HDAC inhibitors | Osteoarthritis, RA | [77,78,89,90] | |
| miRNA (for example, miR146a, miR155) | Antisense RNA technologies | Autoimmunity, RA | [44-47,88] |
BET, bromodomain and extraterminal; HDAC, histone deacetylase; I-BET, bromodomain and extraterminal bromodomain inhibitor; RA, rheumatoid arthritis.