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Review

Targeting the vitamin D receptor: advances in drug discovery

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Pages 1133-1145 | Published online: 02 Dec 2005
 

Abstract

The vitamin D receptor (VDR), a member of the nuclear receptor superfamily, mediates the biological action of 1α,25-dihydroxyvitamin D3 [1,25(OH)2D3], the active form of vitamin D. VDR regulates bone and calcium homeostasis, immunity, cellular differentiation and other physiological processes. Mutations in the VDR gene were identified in hereditary vitamin D-resistant rickets (HVDRR), and VDR-null mice exhibit the HVDRR phenotype, characterised by rickets and hypocalcaemia. In addition to the treatment of rickets, vitamin D analogues are important therapeutics in osteoporosis and psoriasis. Vitamin D analogues are effective drugs in experimental models of immune disorders and malignancies, such as breast cancer, prostate cancer and leukaemia. The development of functionally selective VDR-targeted drugs is leading to an enhanced understanding and novel therapies for these VDR-related diseases.

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