Vitamin D is a pro-hormone, which is metabolized in the liver and kidneys to 1,25-dihydroxyvitamin D3 (1,25-(OH)2D3) that in turn binds the transcription factor VDR (vitamin D receptor) with high affinity. Regulation of genes responsible for cell growth, cell differentiation, and calcium homeostasis is mediated by VDR in the presence or absence of 1,25-(OH)2D3 and is governed by interactions between VDR and coregulators. The development of biochemical assays to quantify molecule interactions with VDR and cell-based assays and in vivo studies to determine VDR localization and distribution have been complicated by the fact that the current labeled vitamin D analogs suffer from low affinities, instability and inaccessibility.Herein, we present the synthesis and characterization of new and fundamentally different fluorescent probes for VDR and their application in biochemical and cell-based assays.

Development of fluorescent probes for the vitamin D receptor and their application as screening tools and the biological probes

243rd National Meeting (2012)

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