lα,25-dihydroxyvitamin D3 receptor: competitive binding of vitamin D analogs

Peter F. Brumbaugh, Mark R. Haussler

Research output: Contribution to journalArticle

49 Scopus citations

Abstract

The intestinal nuclear receptor for lα,25-dihydroxyvitamin D3 has been utilized to determine the ability of vitamin D-active sterols to compete with this hormone at the molecular level. 25-Hydroxyvitamin D3 and lα-hydroxyvitamin D3 must be present in 150 and 450 times the concentration respectively of lα,25-dihydroxyvitamin D3, in vitro, to displace the physiologic hormone. These data indicate that: i) superphysiologic levels of 25-hydroxyvitamin D3 may simulate lα,25-dihydroxyvitamin D3 and act directly on isolated target organs and ii) the biologic potency observed for low doses of lα-hydroxyvitamin D3, in vivo, is probably the result of 25-hidroxylation of the lα-derivative to form lα,25-dihydroxyvitamin D3.

Original languageEnglish (US)
Pages (from-to)1737-1746
Number of pages10
JournalLife Sciences
Volume13
Issue number12
DOIs
StatePublished - Dec 16 1973

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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