The interaction of 1,25-dihydroxyvitamin D3 with its intestinal mucosa receptor: Kinetic parameters and structural requirements |
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Authors: | John A Putkey Wayne R Wecksler Anthony W Norman |
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Affiliation: | (1) Department of Biochemistry, University of California, 92521 Riverside, California |
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Abstract: | Vitamin D3 and its metabolites comprise an endocrine system which plays a critical role in calcium homeostasis. The active form of vitamin
D3 is 1,25-dihydroxyvitamin D3 1,25(OH)2D3]. Chromatin localization of 1,25(OH)2D3 and sucrose density gradient centrifutation have demonstrated the presence of an intestinal mucosa cytosol receptor which
specifically binds 1,25(OH)2D3. The kinetic parameters of 1,25(OH)2D3 binding to its receptor have been determined by hydroxylapatite and reconstituted chromatin cytosol assays. Utilization of
these assays has also permitted a determination of the precise structural requirements of the vitamin D ligand for the intestinal
receptor. Furthermore, it has been possible to propose two receptor-ligand models which are capable of accommodating the conformationaly
modile A ring of the vitamin D seco-steroids. |
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