A Nonsecosteroidal Vitamin D Receptor Modulator Ameliorates Experimental Autoimmune Encephalomyelitis without Causing Hypercalcemia
Figure 2
Compound A induces VDR-mediated gene expression. (a) Compound A is as potent as 1,25-(OH)2D3 in inducing VDR-LBD-dependent gene expression. Luciferase activity (±SE) of HeLa cells transfected with Gal4-VDR-LBD in a mammalian one-hybrid setting in the presence of vehicle or various concentrations of 1,25-(OH)2D3 or compound A is shown. Results are in arbitrary light units obtained from experiments performed in triplicate. (b) Compound A induces VDRE-dependent expression of the rat osteocalcin promoter in osteoblasts. ROS17/2.8 cells stably transfected with rat osteocalcin reporter (OCN-Luc) were treated with various concentrations of 1,25-(OH)2D3 or compound A. Results are shown in percentage of the luciferase activity obtained by treating the cells with 1 μM 1,25-(OH)2D3. All the transfections were performed in triplicate.
