Recently, the FDA approved drug Bexarotene (Targretin) to treat cutaneous T cell lymphoma has been found to be effective in reducing the plaque lesions in mouse models of Alzheimer's disease.  It has been hypothesized that the drug works by promoting ABCA1 and Apo-E4 gene expression that may be regulated by a Retinoid-X-Receptor (RXR) / Liver-X-Receptor (LXR) heterodimer.  Herein, we explore the synthesis, modeling, and biological evaluation of several novel Bexarotene analogs for their ability to serve as selective RXR agonists and their effects in cell culture and Alzheimer's disease models. 

Modeling, synthesis and biological evaluation of Retinoid-X-Receptor (RXR) selective agonists with potential to treat Alzheimer's disease

243rd National Meeting (2012)

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