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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

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]

  1. BET, bromodomain and extraterminal; HDAC, histone deacetylase; I-BET, bromodomain and extraterminal bromodomain inhibitor; RA, rheumatoid arthritis.
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Arthritis Research & Therapy

ISSN: 1478-6362

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