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Calcitriol is a hormone and the active form of vitamin D, normally made in the kidney. [ 8 ] [ 9 ] [ 10 ] It is also known as 1,25-dihydroxycholecalciferol . It binds to and activates the vitamin D receptor in the nucleus of the cell, which then increases the expression of many genes. [ 11 ]
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]
Calcitriol plays a key role in regulating vitamin D levels through a negative feedback mechanism. [203] It strongly upregulates the expression of the enzyme CYP24A1 , which inactivates vitamin D. This activation happens through binding of the activated vitamin D receptor (VDR) to two vitamin D response elements (VDREs) in the in the CYP24A1 gene.
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 .
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]
1α-Hydroxyvitamin D 5 is a chemical derivative of vitamin D 5.The motive to study 1α-hydroxyvitamin D 5 as a potential pharmaceutical drug stemmed from the tendency of calcitriol, a natural metabolite produced in the kidney, to cause toxic hypercalcemia in patients when dosed at concentrations needed to interrupt prostate cancer cells' cycle and stimulate apoptosis.
Calcifediol is the precursor for calcitriol, the active form of vitamin D. [3] [4] It is synthesized in the liver, by hydroxylation of cholecalciferol (vitamin D 3) at the 25-position. [3] This enzymatic 25-hydroxylase reaction is mostly due to the actions of CYP2R1 , present in microsomes , although other enzymes such as mitochondrial CYP27A1 ...
Vitamin D3 24-hydroxylase (EC 1.14.15.16, CYP24A1) is an enzyme with systematic name calcitriol,NADPH:oxygen oxidoreductase (24-hydroxylating). [1] ...
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