High-throughput system for analyzing ligand-induced cofactor recruitment by vitamin D receptor
High-throughput system for analyzing ligand-induced cofactor recruitment by vitamin D receptor
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DOI：
10.1021/bc0601121
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发表时间：
2007-05-01
影响因子：
4.7
通讯作者：
Kittaka, Atsushi
中科院分区：
文献类型：
--
作者：
Arai, Midori A.;Takeyama, Ken-ichi;Kittaka, Atsushi
建立了一种用于分析维生素D受体（VDR）募集小分子诱导CoA的高通量筛选系统。采用新的HCHO固定方法在微孔板上成功检测了VDR与荧光团（Cy3或Cy5）标记的TIF2或SRC-1之间维生素d诱导的蛋白-蛋白相互作用。从我们的合成维生素D类似物的筛选结果表明，coa招募活性在决定各种维生素D类似物的生物活性中起重要作用，并解释了VDR结合亲和力与其生物活性之间的差异。
A high-throughput screening system for analyzing small molecule-induced coactivator (CoA) recruitment by the vitamin D receptor (VDR) has been developed. The vitamin D-induced protein - protein interactions between VDR and fluorophore (Cy3 or Cy5)-labeled TIF2 or SRC-1 were successfully detected by using a new HCHO fixing method of the protein complex on microplates. The results obtained from this screening of our synthetic vitamin D analogues suggest that the CoA-recruiting activities play an important role in determining the biological activity of various vitamin D analogues and explain the discrepancies between the VDR binding affinity and their biological activity.