Retinoic acid receptor-
related nuclear receptor γ (RORγ) plays a central role in T cell differentiation, particularly in the development of T
H17 cells, which are implicated in autoimmune diseases like multiple sclerosis and rheumatoid arthritis.
1,2 SR 1555 is a selective ligand of RORγ (IC
50 = 1 μM).
3 It does not bind RORα, LXR, or FXR. SR 1555 acts as an inverse agonist of RORγ, inhibiting endogenous IL-
17A gene expression in mouse splenocytes and suppressing differentiation of T
H17 cells when cultured under T
H17 polarizing conditions.
3 Moreover, SR 1555 stimulates T regulatory development when cultured under T regulatory polarizing conditions, unlike digoxin and ursolic acid.
3