Abstract
Biological activities of 2alpha-substituted 1alpha,25-dihydroxyvitamin D3 analogues were evaluated in vitro. Their binding affinity was examined with calf thymus cytosolic vitamin D receptor (VDR) and rat plasma vitamin D-binding protein (DBP). In addition, the transcriptional activity of the analogues was measured using a rat 25-hydroxyvitamin D3-24-hydroxylase gene promoter, a human osteocalcin gene promoter, and VDR-GAL4 system. This study investigated the biological activities of 2alpha-substituted analogues in comparison with 2beta-substitued analogues at the molecular level, with regard to the structural differences of alkyl, hydroxyalkyl, hydroxyalkoxy substituents at the 2-position of 1alpha,25-dihydroxyvitamin D3.
MeSH terms
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Animals
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CD11b Antigen / biosynthesis
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Calcitriol / analogs & derivatives
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Calcitriol / metabolism
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Calcitriol / pharmacology*
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Cattle
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Cell Cycle / drug effects
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Cell Differentiation / drug effects*
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Cell Line, Tumor
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Cell Proliferation / drug effects*
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Flow Cytometry
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HL-60 Cells
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Humans
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Lipopolysaccharide Receptors / biosynthesis
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Luciferases / genetics
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Luciferases / metabolism
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Molecular Structure
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Osteocalcin / pharmacology
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Protein Binding / drug effects
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Rats
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Receptors, Calcitriol / genetics
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Receptors, Calcitriol / metabolism
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Steroid Hydroxylases / genetics
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Steroid Hydroxylases / metabolism
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Structure-Activity Relationship
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Transcriptional Activation / drug effects*
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Transcriptional Activation / genetics
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Transfection
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Vitamin D-Binding Protein / genetics
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Vitamin D-Binding Protein / metabolism
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Vitamin D3 24-Hydroxylase
Substances
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CD11b Antigen
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Lipopolysaccharide Receptors
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Receptors, Calcitriol
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Vitamin D-Binding Protein
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Osteocalcin
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Luciferases
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Steroid Hydroxylases
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Vitamin D3 24-Hydroxylase
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Calcitriol