Ligand Affinity, Homodimerization, and Ligand-Induced Secondary Structural Change of the Human Vitamin D Receptor

Author： Falsone S.F.   Kurkela R.   Chiarandini G.   Vihko P.   Kungl A.J.  

Publisher： Elsevier

ISSN： 0006-291X

Source： Biochemical and Biophysical Research Communications, Vol.285, Iss.5, 2001-08, pp. : 1180-1185

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Abstract

The intrinsic tryptophan fluorescence signal of the full-length nuclear receptor hVDR was used to directly determine the dissociation constants, Kd, of two ligands yielding Kd = 32 nM for 1α,25(OH)2D3 and Kd = 322 nM for 25(OH)D3. Ligand binding was accompanied by a conformational change in the α-helical part of hVDR as revealed by CD spectroscopy. In addition, the presence of calcitriol was found to be a necessary prerequisite for the homodimerisation of hVDR which was monitored using fluorescence anisotropy. We conclude that the observed ligand-induced structural change of hVDR is conditional for dimerisation of the protein.

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