The interaction of 1,25‐dihydroxyvitamin D 3  with its intestinal mucosa receptor: Kinetic parameters and structural requirements | Zendy

Putkey John A. | Zendy; Wecksler Wayne R. | Zendy; Norman Anthony W. | Zendy

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The interaction of 1,25‐dihydroxyvitamin D 3 with its intestinal mucosa receptor: Kinetic parameters and structural requirements

Author(s) -

Putkey John A.,

Wecksler Wayne R.,

Norman Anthony W.

Publication year - 1978

Publication title -

lipids

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.601

H-Index - 120

eISSN - 1558-9307

pISSN - 0024-4201

DOI - 10.1007/bf02533752

Subject(s) - calcitriol receptor , cytosol , intestinal mucosa , vitamin d and neurology , receptor , ligand (biochemistry) , chemistry , vitamin , biochemistry , biophysics , biology , endocrinology , medicine , enzyme

Vitamin D 3 and its metabolites comprise an endocrine system which plays a critical role in calcium homeostasis. The active form of vitamin D 3 is 1,25‐dihydroxyvitamin D 3 [1,25(OH) 2 D 3 ]. Chromatin localization of 1,25(OH) 2 D 3 and sucrose density gradient centrifutation have demonstrated the presence of an intestinal mucosa cytosol receptor which specifically binds 1,25(OH) 2 D 3 . The kinetic parameters of 1,25(OH) 2 D 3 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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