ビタミンD受容体の核移行シグナルおよびアンタゴニストの同定

概要

論文の詳細を見る
The localization of vitamin D receptor (VDR) in the absence of its ligand 1α,25-dihydroxyvitamin D_3 [1α,25(OH)_2D_3] was investigated using chimera proteins fused to green fluorescent protein (GFP) The obtained results indicate that VDR is located predominantly in nuclei with a significant presence in cytoplasm in the absence of the ligand and that a NLS consisting of 20 amino acids in the hinge region facilitates the transfer of VDR to the nucleus. Next, we showed that 10^-7 M TEI-9647, the novel 1α,25(OH)_2D_3 analogue, inhibited the transactivation effect of 10^-8 1α, 25(OH)_2D_3, while TEI-9647 alone did not activate the reporter activity driven by SV40 promoter containing two vitamin D response elements in Saos-2 cells. The results demonstrate that TEI-9647 is the first synthetic ligand for the VDR which efficiently antagonizes the action of 1α,25(OH)_2D_3, although the extent of its antagonism depends on cell-type.
日本ビタミン学会の論文
2002-04-25