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Abstract
More than 3000 synthetic analogues of the biologically active form of vitamin D, 1α,25-dihydroxyvitamin D3 (1α,25-(OH)2-D3), are presently known. All analogues interact with the molecular switch controlling nuclear 1α,25-(OH)2-D3 signalling, which is the complex of the vitamin D receptor (VDR), the retinoid X receptor (RXR) and a 1α,25-(OH)2-D3 response element (VDRE). The central element of this molecular switch is the ligand-binding domain (LBD) of the VDR, which can be stabilised by a 1α,25-(OH)2-D3 analogue in either its agonistic or antagonistic conformation. In this article, the patent literature on 1α,25-(OH)2-D3 analogues described in the last 4 years will be reviewed, and several new VDR ligands with promising selective profiles discussed. Although most of these ligands are agonists of the VDR, a few antagonists have been reported. Non-steroidal VDR ligands will be highlighted, as well as 1α,25-(OH)2-D3 analogues with two side chains.
