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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 .
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.
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 VDR is widely distributed in tissues, and is not restricted to those tissues considered the classic targets of vitamin D. The VDR upon binding to 1,25(OH) 2 D heterodimerizes with other nuclear hormone receptors, in particular the family of retinoid X receptors. This VDR/RXR heterodimer complex binds to the specific VDRE in the promoters of ...
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]
25-Hydroxyvitamin D 1-alpha-hydroxylase (VD 1A hydroxylase) also known as calcidiol 1-monooxygenase [5] or cytochrome p450 27B1 (CYP27B1) or simply 1-alpha-hydroxylase is a cytochrome P450 enzyme that in humans is encoded by the CYP27B1 gene.
Drug-drug interactions can be of serious concern for patients who are undergoing multi-drug therapies. [5] Coadministration of chloroquine , an anti-malaria drug, and statins for treatment of cardiovascular diseases has been shown to cause inhibition of organic anion-transporting polypeptides (OATPs) and lead to systemic statin exposure.