2000
DOI: 10.1016/s0960-0760(99)00148-x
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The 3-epi- and 24-oxo-derivatives of 1α,25 dihydroxyvitamin D3 stimulate transcription through the vitamin D receptor

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Cited by 16 publications
(8 citation statements)
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“…Albeit not clearly understood, alternative metabolism of vitamin D via epimerisation to 3-epi-25(OH)D3 results in the formation of 3-epi-1,25(OH) 2 D3, which binds to VDR to activate target gene transcription. Importantly, 3-epi-1,25(OH) 2 D3 appears a less potent VDR agonist than 1,25(OH) 2 D3, which may have physiological consequences ( 48 ). In normal pregnancy, 3-epi-25(OH) 2 D3 appears directly linked to 25(OH)D3 concentrations ( 43 ); however, in the SCOPE cohort this relationship was lost only in those women who developed PET.…”
Section: Discussionmentioning
confidence: 99%
“…Albeit not clearly understood, alternative metabolism of vitamin D via epimerisation to 3-epi-25(OH)D3 results in the formation of 3-epi-1,25(OH) 2 D3, which binds to VDR to activate target gene transcription. Importantly, 3-epi-1,25(OH) 2 D3 appears a less potent VDR agonist than 1,25(OH) 2 D3, which may have physiological consequences ( 48 ). In normal pregnancy, 3-epi-25(OH) 2 D3 appears directly linked to 25(OH)D3 concentrations ( 43 ); however, in the SCOPE cohort this relationship was lost only in those women who developed PET.…”
Section: Discussionmentioning
confidence: 99%
“…Alternative metabolism of vitamin D may also occur via epimerisation of 25(OH)D3. The resulting 3- epi -25(OH)D3 can be converted to 3- epi -1,25(OH) 2 D3, and then bind to VDR to activate target gene transcription [36]. However, 3- epi -1,25(OH) 2 D3 is a much less potent VDR agonist than 1,25(OH) 2 D3, suggesting that epimerisation of 25(OH)D3 acts to dial-down VDR activity by generating a less effective ligand for the receptor [37].…”
Section: Discussionmentioning
confidence: 99%
“…The issue of the bioactivity of 1,25-OHD vs. that of 3-epi-1,25-OHD is more complex. 3-Epi-1,25-OHD can stimulate gene transcription through the vitamin D receptor (VDR) despite the fact that it appears to have weaker binding affinity to the VDR than 1,25-OHD (32,33). The lower receptor binding affinity does not translate into universally reduced biological effects of 3-epi-1,25-OHD in all vitamin-D-respon-sive tissues.…”
Section: Discussionmentioning
confidence: 99%