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Table 2 Epigenetic drugs or inhibitors targeting mechanisms in musculoskeletal disease

From: Why is epigenetics important in understanding the pathogenesis of inflammatory musculoskeletal diseases?

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
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   [4447, 88]
  1. BET, bromodomain and extraterminal; HDAC, histone deacetylase; I-BET, bromodomain and extraterminal bromodomain inhibitor; RA, rheumatoid arthritis.