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Gene Review

VDR  -  vitamin D (1,25- dihydroxyvitamin D3)...

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Disease relevance of VDR


High impact information on VDR

  • Furthermore, this compound interacted as efficiently as 1,25(OH)2D3 with the vitamin D receptor (VDR), retinoid X receptor (RXR), coactivators, and DNA, which illustrated its potent ability to activate the genomic signal transduction pathway [3].
  • The 2-ethylidene-19-nor compounds with a methyl group from the ethylidene moiety in a trans relationship to the C(6)-C(7) bond (E-isomers) were more potent than the corresponding Z-isomers and the natural hormone in binding to the vitamin D receptor [4].
  • In the studies described here, we compared the expression of calbindin D-28K and the vitamin D receptor (VDR) in four renal cell lines: Madin-Darby bovine kidney (MDBK) cells, Madin-Darby canine kidney (MDCK) cells, LLC-PK1 pig kidney cells and opossum kidney (OK) cells [5].
  • Transfection of the h24(OH)ase promoter construct [-5,500/-22 luciferase; vitamin D response elements at -294/-274 and -174/-151; AP-1 site at -1,167/-1,160] in vitamin D receptor (VDR)-transfected COS-7 cells resulted in strong activation by 1,25(OH)(2)D(3) [6].
  • The promoter activity was markedly suppressed by 1alpha,25-dihydroxyvitamin D3 and 25-hydroxyvitamin D3 in presence of vitamin D receptor (VDR) [7].

Biological context of VDR


Anatomical context of VDR

  • The involvement of polyamines in the activation of vitamin D receptor from porcine intestinal mucosa [10].
  • All the synthesized vitamins possessing a 25-hydroxylated saturated side chain were slightly less active (3-5X) than 1 alpha,25-dihydroxyvitamin D(3) in binding to the porcine intestinal vitamin D receptor and significantly more potent (12-150X) in causing differentiation of HL-60 cells [11].
  • Among the synthesized 19-norvitamin D3 analogs, 2alpha-(3-hydroxypropyl)-1alpha,25-dihydroxy-19-norvitamin D3 (8a) showed almost the same potency in binding to the bovine thymus vitamin D receptor (VDR) as the natural hormone (1), while its beta-isomer had only a 3% affinity [12].

Associations of VDR with chemical compounds


  1. New vitamin D receptor agonists with decreased metabolic stability. Werz, O., Wiesinger, H., Steinmeyer, A., Steinhilber, D. Biochem. Pharmacol. (2000) [Pubmed]
  2. Antagonistic activity of 24-oxa-analogs of vitamin D. Allewaert, K., Sarandeses, L.A., Mourino, A., Convents, R., Tan, B.K., Zhao, J., Bouillon, R. Steroids (1995) [Pubmed]
  3. Previtamin D3 with a trans-fused decalin CD-ring has pronounced genomic activity. Verlinden, L., Verstuyf, A., Verboven, C., Eelen, G., De Ranter, C., Gao, L.J., Chen, Y.J., Murad, I., Choi, M., Yamamoto, K., Yamada, S., Van Haver, D., Vandewalle, M., De Clercq, P.J., Bouillon, R. J. Biol. Chem. (2003) [Pubmed]
  4. 2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain. Sicinski, R.R., Rotkiewicz, P., Kolinski, A., Sicinska, W., Prahl, J.M., Smith, C.M., DeLuca, H.F. J. Med. Chem. (2002) [Pubmed]
  5. Induction of calbindin D-28K in Madin-Darby bovine kidney cells by 1,25(OH)2D3. Gagnon, A.M., Simboli-Campbell, M., Welsh, J.E. Kidney Int. (1994) [Pubmed]
  6. Integration of hormone signaling in the regulation of human 25(OH)D3 24-hydroxylase transcription. Barletta, F., Dhawan, P., Christakos, S. Am. J. Physiol. Endocrinol. Metab. (2004) [Pubmed]
  7. Isolation and properties of the CYP2D25 promoter: transcriptional regulation by vitamin D3 metabolites. Ellfolk, M., Norlin, M., Wikvall, K. Biochem. Biophys. Res. Commun. (2006) [Pubmed]
  8. Biological evaluation of epoxy analogs of 1 alpha,25-dihydroxyvitamin D3. Allewaert, K., Zhao, X.Y., Zhao, J., Glibert, F., Branisteanu, D., De Clercq, P., Vandewalle, M., Bouillon, R. Steroids (1995) [Pubmed]
  9. Vitamin D deficiency in guinea pigs: exacerbation of bone phenotype during pregnancy and disturbed fetal mineralization, with recovery by 1,25(OH)2D3 infusion or dietary calcium-phosphate supplementation. Rummens, K., van Bree, R., Van Herck, E., Zaman, Z., Bouillon, R., Van Assche, F.A., Verhaeghe, J. Calcif. Tissue Int. (2002) [Pubmed]
  10. The involvement of polyamines in the activation of vitamin D receptor from porcine intestinal mucosa. Morishima, Y., Inaba, M., Nishizawa, Y., Morii, H., Hasuma, T., Matsui-Yuasa, I., Otani, S. Eur. J. Biochem. (1994) [Pubmed]
  11. New highly calcemic 1 alpha,25-dihydroxy-19-norvitamin D(3) compounds with modified side chain: 26,27-dihomo- and 26,27-dimethylene analogs in 20S-series. Sicinski, R.R., Prahl, J.M., Smith, C.M., DeLuca, H.F. Steroids (2002) [Pubmed]
  12. Novel 2-alkyl-1alpha,25-dihydroxy-19-norvitamin D3: efficient synthesis with Julia olefination, evaluation of biological activity and development of new analyzing system for co-activator recruitment. Arai, M.A., Kittaka, A. Anticancer Res. (2006) [Pubmed]
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