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CD3254 is a selective agonist of the retinoid X receptors (RXRs; EC50 = ~10 nM for human RXRβ) that is without effect on retinoic acid receptors (RARs).1,2 It stimulates the recruitment of the nuclear receptor interaction domain of the TRAP220 coactivator to RXRα/RARβ heterodimers in vitro.3 CD3254 also enhances the recruitment of the PPARγ coactivator 1α, PGC-1α, to RXRα/PPARγ heterodimers.4
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1. Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function. Proc. Natl. Acad. Sci. USA 104(44), 17323-17328 (2007).
2. Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR) selective agonists: Novel analogues of 4-
3. Characterization of the interaction between retinoic acid receptor/retinoid X receptor (RAR/RXR) heterodimers and transcriptional coactivators through structural and fluorescence anisotropy studies. The Journal of Biological Chemisty 280(2), 1625-1633 (2005).
4. Activation of RXR-