Figure 1. VDRM2 induces VDR target genes and reduces VCaP cell growth.

(A) Chemical structure of the active vitamin D metabolite 1α,25-dihydroxyvitamin D3 (1,25D(OH)₂D₃). (B) Chemical structure of non-secosteroidal VDR agonist, VDRM2 (LSN2148936). (C, D) VCaP cells were treated with the indicated doses of vehicle (EtOH), 1,25D(OH)₂D₃ (1,25D), or VDRM2 for 24 hours, harvested, and RNA was purified. VDR target genes CYP24A1 and TMPRSS2 were measured by RT-qPCR and normalized to 18S. (E) VCaP cells were treated with the indicated doses of vehicle (EtOH), 1,25D(OH)₂D₃, or VDRM2 for twelve days; medium and treatments were replenished every third day. Cells were counted using a Beckman-Coulter Counter. (F) Doubling time was calculated for vehicle (EtOH), 100 nM 1,25D(OH)₂D₃, or 3 μM VDRM2 treated cells from day 9 to day 12 from three independent experiments. *p < 0.05, **p < 0.01, ***p < 0.001, relative to vehicle control. n = 3, representative graph, mean ± SEM.