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.

Oppermann Arthritis Research & Therapy 2013 15:209   doi:10.1186/ar4186