The active metabolite of vitamin D modulates the expression of a wide variety of genes in a developmentally specific manner. This secosteroid hormone can up- or downregulate the expression of genes involved in a diverse array of responses such as proliferation, differentiation and calcium homeostasis. 1,25-(OH)2-vitamin D3 exerts its effects through interaction with the vitamin D receptor (VDR), a member of the superfamily of hormone-activated nuclear receptors. In its ligand-bound state, the VDR forms heterodimers with the 9-cis retinoic acid receptor, RXR, and affects gene expression by binding specific DNA sequences known as hormone response elements, or HREs. In addition to regulating the above-mentioned cellular responses, 1,25-(OH)2-vitamin D3 exhibits antiproliferative properties in osteosarcoma, melanoma, colon carcinoma and breast carcinoma cells.
