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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.
For example, CYP11A1, an enzyme chiefly known for its role in steroidogenesis, has been found to hydroxylate vitamin D3 at several positions, including C-20, C-22, and C-23, without cleaving the side chain. The resulting metabolites, such as 20-hydroxyvitamin D3 and 20,23-dihydroxyvitamin D3, act as inverse agonists for RORα and RORγ2.
24,25-dihydroxyvitamin D 3 is formed from 25-hydroxyvitamin D 3 by the action of CYP24A1 (25-hydroxyvitamin D3-24-hydroxylase). CYP24A1 appears to be "a multicatalytic enzyme catalyzing most, if not all, of the reactions in the C-24/C-23 pathway of 25-OH-D 3 metabolism." [5]
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The name 25(OH)D refers to any combination of calcifediol (25-hydroxy-cholecalciferol), derived from vitamin D 3, and ercalcidiol (25-hydroxy-ergocalciferol), [1] derived from vitamin D 2. The first of these (also known as 25-hydroxy vitamin D3) is made by the body, or is sourced from certain animal foods or cholecalciferol supplements.
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The Institute of Medicine in 2010 recommended a maximum uptake of vitamin D of 4000 IU/d, finding that the dose for lowest observed adverse effect level is 40,000 IU daily for at least 12 weeks, [25] and that there was a single case of toxicity above 10 000 IU after more than seven years of daily intake; this case of toxicity occurred in ...
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