Abstract
Isolated rat epidermis possesses a cytosolic 3.5 S receptor-like protein for 1,25-dihydroxyvitamin D3. This 3.5S binder has a high affinity (Kd = 1.4 X 10(-10) M) for 1,25-dihydroxyvitamin D3 and is present in low concentrations (31 fmol of binding sites per mg of cytosol protein). Analog competition for receptor binding revealed the following potency order: 1,25-dihydroxyvitamin D3 > 25-hydroxyvitamin D3 > 1 alpha-hydroxyvitamin D3 > 24 (R),25-dihydroxyvitamin D3 > vitamin D3. The receptor has a molecular weight of 60,000, has affinity for DNA-cellulose, and aggregates in the presence of low potassium concentrations. The 1,25-dihydroxyvitamin D3 binder is stabilized by sodium molybdate (10 mM). Addition of phenylmethylsulfonyl fluoride (3 mM) was found to yield more reproducible receptor preparations. The presence of a 1,25-dihydroxyvitamin D3 binding macromolecule with properties similar to those of the bone and intestinal receptor suggests that skin is an additional target organ for this hormone.
MeSH Terms
Animals
Calcitriol
Cytosol/metabolism
Dihydroxycholecalciferols/metabolism
Epidermis/metabolism
Hydroxycholecalciferols/metabolism
Ligands
Molecular Weight
Protein Binding
Rats
Receptors, Calcitriol
Receptors, Steroid/metabolism
Skin/metabolism
Structure-Activity Relationship
Chemicals
Dihydroxycholecalciferols
Hydroxycholecalciferols
Ligands
Receptors, Calcitriol
Receptors, Steroid
Calcitriol
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Simpson R U
DeLuca H F
References (24)
24 references, click to expand
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