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The vitamin D receptor (VDR also known as the calcitriol receptor) is a member of the nuclear receptor family of transcription factors. [5] Calcitriol (the active form of vitamin D , 1,25-(OH) 2 vitamin D 3 ) binds to VDR, which then forms a heterodimer with the retinoid-X receptor .
Vitamin D response element (VDRE) is a type of DNA sequence that is found in the promoter region of vitamin D regulated genes. This sequence binds the vitamin D receptor (VDR), when complexed with calcitriol (1,25(OH) 2 D), the active form of vitamin D, and so regulates the expression of many genes.
Calcitriol was identified as the active form of vitamin D in 1971 and the drug was approved for medical use in the United States in 1978. [7] It is available as a generic medication . [ 12 ] In 2022, it was the 254th most commonly prescribed medication in the United States, with more than 1 million prescriptions.
The natural, active form of vitamin D is calcitriol (1,25-dihydroxycholecalciferol). This molecule and other naturally occurring forms of vitamin D, including its precursors and metabolites, have been modified to synthesize pharmaceuticals with potentially greater, or selective, therapeutic actions. [1] [2] [3] [4]
The active vitamin D metabolite, calcitriol, exerts its biological effects by binding to the vitamin D receptor (VDR), which is primarily located in the nuclei of target cells. [ 1 ] [ 13 ] When calcitriol binds to the VDR, it enables the receptor to act as a transcription factor , modulating the gene expression of transport proteins involved ...
Calcipotriol, also known as calcipotriene, is a synthetic derivative of calcitriol, a form of vitamin D. It is used in the treatment of psoriasis. [1] It is safe for long-term application in psoriatic skin conditions. [medical citation needed] It was patented in 1985 and approved for medical use in 1991. [2]
calcidiol + 2 reduced adrenodoxin + 2 H + + O 2 ⇌ calcitriol + 2 oxidized adrenodoxin + H 2 O The enzyme is also able to oxidize ercalcidiol (25-OH D2) to ercalcitriol, secalciferol to calcitetrol, and 25-hydroxy-24-oxocalciol to (1S)-1,25-dihydroxy-24-oxocalciol.
Eldecalcitol is an orally administered drug to patients, which binds to vitamin D receptors and binding protein for the goal of achieving greater specificity to bind calcium for its absorption. This greater affinity is 2.7-fold that of the active vitamin D form of calcitriol.
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